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Block 2 - vcomdo.com vcomdo by cuiliqing

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									Drug Name                        Class                   Mode of Action                                   Toxicity                                            Notes
Penicillin G                     Penicillin              •Cell wall synthesis inhibitor; binding of PBP   •Hypersensitivity                                   •To Tx susceptible organisms
                                                         (transpeptidase) inhibs syn of peptidoglycan                                                         •Narrow spectrum
                                                         •Porins tspt Abx inside cell                                                                         •Penicillium notatum (lab mold)
                                                         •β-lactam ring                                                                                       •Bacteriocidal

Penicillin V                     Penicillin              •Cell wall synthesis inhibitor; binding of PBP   •Hypersensitivity                                   •To Tx susceptible organisms
                                                         (transpeptidase) inhibs syn of peptidoglycan                                                         •Narrow spectrum
                                                         •Porins tspt Abx inside cell                                                                         •Natural source
Nefacillin                       Penicillin              •Cell wall ring
                                                         •β-lactamsynthesis inhibitor; binding of PBP     •Hypersensitivity                                   •Penicillinase resistant
                                                         (transpeptidase) inhibs syn of peptidoglycan                                                         •Natural source
                                                         •Porins tspt Abx inside cell
Ampicillin                       Penicillin              •β-lactam ring
                                                         •Cell wall synthesis inhibitor; binding of PBP   •Hypersensitivity                                   •Usually in combo w/ clavulanate
                                                         (transpeptidase) inhibs syn of peptidoglycan                                                         •Extended spectrum
                                                         •Porins tspt Abx inside cell                                                                         •Semi-synthetic source
                                                         •β-lactam ring

Amoxicillin                      Penicillin              •Cell wall synthesis inhibitor; binding of PBP   •Hypersensitivity                                   •Usually in combo w/ clavulanate
                                                         (transpeptidase) inhibs syn of peptidoglycan                                                         •Extended spectrum
                                                         •Porins tspt Abx inside cell                                                                         •Semi-synthetic source
                                                         •β-lactam ring

Clavulante, sulbactam            β-lactamase inhibitor   •Cell wall synthesis inhibitor                                                                       •β-lactamse competitive inhibitor



Cephalosporins                                           •Cell wall synthesis inhibitor; binding of PBP   •Cross sensitivity; Hypersensitivity (less severe   •4 generations
                                                         (transpeptidase) inhibs syn of peptidoglycan     than penicillins)                                   •Cephalosporium acremonium (fungus)
                                                         •Porins tspt Abx inside cell                     •Platelet dysfunction & bleeding                    •More stable than penicillins
                                                         •β-lactam ring                                                                                       •Useful when strains resistant to penicillins



Vancomycin                                               •Cell wall synthesis inhibitor; binding of PBP   •Nephrotoxic                                        •Streptomyces orientalis (soil)
                                                         (transpeptidase) inhibs syn of peptidoglycan     •Ototoxic                                           •Useful for some penicillin resistant strains
                                                         •Porins tspt Abx inside cell                     •Red man syndrome when infused rapidly
                                                         •β-lactam ring

Gentamicin                       Aminoglycoside          •Protein synthesis inhibitor: blocks aa-tRNA •Nephrotoxic                                            •Poor absorption; use topical for gastroenteritis
                                                         from binding to A site of ribo               •Ototoxic                                               •Not metabolized; renal excretion by filtration
                                                                                                      •Dose dependent & reversible                            •Micromonospora (soil Actinomyces )

Neomycin, Tobramycin, Amikacin   Aminoglycoside          •Protein synthesis inhibitor: blocks aa-tRNA •Nephrotoxic                                            •Poor absorption; use topical for gastroenteritis
                                                         from binding to A site of ribo               •Ototoxic                                               •Not metabolized; renal excretion by filtration
                                                                                                      •Dose dependent & reversible

Streptomycin                     Aminoglycoside          •Protein synthesis inhibitor: blocks aa-tRNA •Nephrotoxic                                            •Poor absorption; use topical for gastroenteritis
                                                         from binding to A site of ribo               •Ototoxic                                               •Not metabolized; renal excretion by filtration
                                                                                                      •Dose dependent & reversible                            •Streptomyces griseus (soil)
Doxycycline, Tetracycline          Tetracycline       •Protein synthesis inhibitor: blocks aa-tRNA •Teeth discoloration                             •Bacteriostatic
                                                      from binding to A site of ribo               •Nephrotoxicity (potentiates)                    •Semi-synthetic
                                                                                                   •Hepatotoxicity (pregnant women)                 •Broad spectrum
Erythromycin, Clarithromycin       Macrolides         •Protein synthesis inhibitor: blocks         •Some ototoxicity                                •Streptomyces erythreus (soil; Erythromycin)
                                                      formation of peptide bond & tsfr frm A to P
                                                      site

Chloramphenicol                                       •Protein synthesis inhibitor: blocks        •Aplastic anemia                                  •Well absorbed
                                                      formation of peptide bond                                                                     •Crosses BBB
                                                                                                                                                    •Only use if benefit outweighs tox
Sulfamethoxazole, sulfisoxazole,   Sulfonamides       •Folate synthesis inhibitors                •Crystalluria                                     •Dvlpd from pigments
sulfasalazine                                                                                     •Skin rash, gastroenteritis, hepatitis & anemia   •Synthetic
                                                                                                                                                    •Consume ample amounts of water



Trimethoprim                                          •Folate synthesis inhibitors                •Variety                                          •Usually in combo w/ sulfamethoxazole: synergistic
                                                                                                                                                    •Concentrated in weakly acidic organs (weakly basic
                                                                                                                                                    drug)



Ciprofloxacin, Levofloxacin        Fluoroquinolones   •DNA replication inhibitor: binds to DNA    •Joint Ds in young                              •PostAbx effect
(Quinolones)                                          gyrase                                                                                      •Bacteriocidal
                                                                                                                                                  •* + dependent killing
                                                                                                                                                  •Give high dose to prevent resistance
Zidovudine (AZT), Lamivudine,      NRTI               •Pyrimidine anti-metabolite                  •Lactic acidosis: inhib of human mito DNA pol- •Activation to NTP by host cell kinase
Abacavir                                              •Target=retroviral pol gene product (reverse gamma (liver); peripheral neuropathy,          •Most excreted in urine
                                                      txtase)                                      myopathy, cardiomyopathy, lipoatrophy          •Zid: Chemoprophylaxis in pregnancy
                                                      •Incorporation of drug into vDNA causes      •CNS: headache, insomnia                       •Lam has less side effects
                                                      inhib of DNA syn                             •GI: N/V/D                                     •Combivir=Zidovudine+Lamivudine
                                                                                                                                                  •Trizivir=Zidovudine+Lamivudine+Abacavir
Emtricitabine                      NRTI               •Cytosine analog incorporates into vDNA      •Extremely well tolerated                      •Activation to NTP by host cell kinase
                                                      inhibiting syn of RT                         •Lower that avg bone marrow toxicity
Tenofovir                          NRTI               •Nucleotide triphosphate incorporates into •Extremely well tolerated                        •Activation to NTP by host cell kinase
                                                      vDNA inhibiting syn of RT                    •Lower that avg bone marrow toxicity

Nevirapine                         NNRTI              •Allosteric inhibitor of RT                 •Skin rash                                      •No metabolic activation in host cell
                                                      •Pvts vDNA syn                              •P450 drug interactions w/ psychotropics, ergot •Preffered chemophylaxis in pregnancy
                                                                                                  alks, oral contraceptives, methadone, anti-     •Does not resemble nucleosides (NRTI)
                                                                                                  epileptics

Efavirenz                          NNRTI              •Allosteric inhibitor of RT                 •CNS: confusion, halucinations, nightmares        •No metabolic activation in host cell
                                                      •Pvts vDNA syn                              (better when taken @ night)                       •Active agst HIV-2
                                                                                                  •P450 inducer (Clairithromycin intrctns)          •Most potent in class for raising CD4+ T cell counts
                                                                                                  •Skin rash                                        •ATRIPLA=Tenofovir+Emtricitabine+Efavirenze; 1x/d
Saquinavir, Nelfinavir,             PI                      •Targets HIV-1 protease                         •N/V/D, paresthesias, TII diabetes,             •Pvts maturation of viral RT, viral integrase & viral
Ritonavir+Lopinavir, Indinavir                              •Binds to active site of protease and           hypercholersteremia, hypertriglycemia, "buffalo protease; Decreases release of new virons frm infected
                                                            competitively inhibit the cleavage of viral     hump"                                           cells
                                                            substrate (gag-pol gene product)                                                                •Pleiotropic effect=hit one target to take out many
                                                            •Combo w/ NRTI has synergistic anti-HIV                                                         proteins
                                                            activity                                                                                        •Peptidomimetics: fools protease into thinking drug is
                                                                                                                                                            S for E
Raltegravir                         Integrase inhibitor     •Incorporate viral DNA into host DNA
Enfuvirtide                         Entry inhibitor         •Pvt entry of virus into host cell
Filgrastim                          G-CSF                   •Lineage spc endogenous-like GF                 •Allergic rxn (E. coli ): skin, respiratory,     •Recombinant DNA produced protein from E. coli
                                    Antineutorpenic         •Stimulate Nu functions/count                   cardiovascular                                   •Differs from the natural cytokine; has 1 extra N-
                                    (myelopoietic) Agents   •Acts on pluriptnt hematopoietic→myeloid        •Spleenic rupture, bone pain                     terminal methionine and is not glycosylated
                                                            sc; CFU-G/M→CFU-Granulocyte                     •ARDS
                                                                                                            •AML cancer risk
Pegfilgrastin                       G-CSF                   •Lineage spc endogenous-like GF                                                                  •Pegylated form of Filgrastin
                                    Antineutorpenic         •Stimulate Nu functions/count                                                                    •More efficacious for the collection of peripheral blood
                                    (myelopoietic) Agents   •Acts on pluriptnt hematopoietic→myeloid                                                         cells in bone marrow replacement therapy
                                                            sc; CFU-G/M→CFU-Granulocyte                                                                      •Stimulation of CD34+ cells

Lenograstim                         G-CSF                   •Lineage spc endogenous-like GF                                                                  •Produced in mammalian cell culture
                                    Antineutorpenic         •Stimulate Nu functions/count                                                                    •Glycosylated
                                    (myelopoietic) Agents   •Acts on pluriptnt hematopoietic→myeloid
                                                            sc; CFU-S→CFU-G/M→CFU-G or M

Sargramostim                        GM-CSF                  •Multi-lineage endogenous-like GF               •Fever, arthralgia, edema, pleural & pericardial •Recombinant DNA produced protein from yeast
                                    Antineutorpenic         (granulocytes & Ma)                             effusion                                         •Leucine at amino acid 23 in the drug which is not in
                                    (myelopoietic) Agents   •Acts @ all stgs of diffn from pluriptnt→CFU-                                                    the natural human cytokine
                                                            M/G
                                                            •Enhance microbicidal actvty
Chlorpeniramine, Dimenhydrinate,    •1st generation         •H1 receptor antagonist; competitive            •Acute poisoning-central excitatory effects;     •High-medium sedative effects
Diphenhydramine, Hydroxyzine,       antihistimine           inhibitors                                      Hallucinations, ataxia, convulsions, fever       •Chl: no antiemetic effects
Meclizine, Doxylamine,                                      •Antag constcn action of histamine in resp      •Tachycardia; Dry mouth; Coma                    •Strong-medium anticholinergic effects (dry mouth,
Promethazine                                                sm; inhibs vasodil of endo cells; blocks vasc   •MUST HAVE A LOT TO REACH TOXIC LEVELS!!         dry nose, urinary retention)
                                                            perm, wheal & flare resps                                                                        •Crosses BBB
                                                            •DOES NOT PVT HIST RELEASE OR BIND TO
                                                            ALREADY RELEASED HIST
Cetirizine, Fexofenadine, Loratadine •2nd generation        •H1 receptor antagonist; competitive            •Same as 1st generation                          •Low sedative effects
                                     antihistimine          inhibitors                                                                                       •No antiemetic effects
                                                            •Same as 1st generation                                                                          •Very low anticholinergic effects
                                                                                                                                                             •Cet: Active metabolite of hydroxyzine
                                                                                                                                                             •Ionized at phys pH>do not cross membs
                                                                                                                                                             •High albumin binding>less F
Desloratidine, Levocetirizine       •3rd generation         •H1 receptor antagonist; competitive            •Same as 1st generation                          •Low sedative effects
                                    antihistimine           inhibitors                                                                                       •No antiemetic effects
                                                            •Same as 1st generation                                                                          •Very low anticholinergic effects
                                                                                                                                                             •Lev: Levoisomer of cetirizine
                                                                                                                                                             •Metabolites of 2nd gens
Azelastine                            Intranasal                  •H1 receptor antagonist; competitive             •Minimal side effects b/c locally distributed        •Low sedative effects
                                                                  inhibitors                                                                                            •No antiemetic effects
                                                                  •Same as 1st generation                                                                               •Very low anticholinergic effects
Sympathomimetics                                                  •Action at alpha and beta andrenergic                                                                 •Induce mass activation of sympathetic nervous system
                                                                  receptors                                                                                             •Beta(skeletal musc)-epi, albuterol, isoproterenol
                                                                  •Alpha1: vasc sm contrcn; inc HR                                                                      relaxes
                                                                  •Alpha2: vasc sm contrcn                                                                              •Alpha(periph, cutaneous)-epi constricts
                                                                  •Beta1: inc HR & force of contrcn; inc                                                                •Selectively activate different processes
                                                                  conduction velocity
                                                                  •Beta2: bronchial sm relaxation
Dopamine                              Vasopressor                 •Activates beta1 receptors in heart                                                                   •Inc HR and force of contrctns
Hydrocortisone (cortisol), Cortisone, Glucocorticoids             •Binding to Glucocorticoid/Mineralocorticoid •Cushing's Syndrome, cataracts, glaucoma,                •Short acting
Fludrocortisone                                                   receptors and either activating or inhibiting infection, diabetes, growth retardation (kids),         •Hyd: least potent
                                                                  txn of certain genes                          osteoporosis (inhib VitD), muscle weakness,             •Flu: MinAct=200; GluAct=10
                                                                                                                mood effects                                            •Cortisol (hyd) can exert glucocorticoid &
                                                                                                                •Route of delivery key to controlling side effects      mineralocorticoid effects; aldosterone cannot

Methylprednisolone, Prednisone,       Glucocorticoids             •Binding to Glucocorticoid/Mineralocorticoid •Cushing's Syndrome, cataracts, glaucoma,                •Intermediate acting
Triamcinolone                         (Adrenocorticosteroids)     receptors and either activating or inhibiting infection, diabetes, growth retardation (kids),         •Tri: MinAct=0; GluAct=5
                                                                  txn of certain genes                          osteoporosis (inhib VitD), muscle weakness,             •Prednisone is a prodrug converted in the liver to
                                                                                                                mood effects                                            prednisolone
                                                                                                                •Route of delivery key to controlling side effects

Betamethasone, Dexamethasone,        Glucocorticoids              •Binding to Glucocorticoid receptors and         •Cushing's Syndrome, cataracts, glaucoma,            •Long acting
Fluticasone, Flunisolide, Budesonide                              either activating or inhibiting txn of certain   infection, diabetes, growth retardation (kids),      •All: MinAct=0; Flut: GluAct=40
                                                                  genes                                            osteoporosis (inhib VitD), muscle                    •Higher specificity for Glu receptors; no
                                                                                                                   weakness,mood effects                                mineralocorticoid receptor action
                                                                                                                   •Inhaled: Oral candidiasis                           •Bet, Dex: Promotes fetal lung maturation
                                                                                                                   •Route of delivery key to controlling side effects

Desonide, Fluocinonide,               Glucocorticoids             •Binding to Glucocorticoid receptors and                                                              •Minimizes side effects and allows higher doses to
Desoximetasone, Clobetasol                                        either activating or inhibiting txn of certain                                                        target areas
                                                                  genes                                                                                                 •Low: thin skin; Low-med: ears, trunk, arms, scalp,
                                                                                                                                                                        legs
                                                                                                                                                                        •Med-high: thick skin
                                                                                                                                                                        =Ointment: dry, cracked skin; Lotion/cream: moist
                                                                                                                                                                        lesions, hairy areas
Methylprednisolone, Prednisone        Adrenocorticosteroids       •Suppress B & T cell responses by binding to •Adrenal suppression, high BP,                           •Most efficacious
                                      (Glucocorticoids)           glucocorticoid receptors                     hypercholesterolemia, mood chgs, metabolic
                                                                                                               syndromes
Cyclosporin A, Tacrolimus             Calcineurin (phosphatase)   •Suppress T cell response by blocking        •Tac: lower incidence of nephrotoxicity, hi BP,          •Tac: More efficacious
                                      Inhibitors                  intracellular signaling for txn of IL-2      hyperchole.                                              •Used in combo w/ adrenocorts & anti-prolifs
                                                                  •Binds immunophilins                         •Both have dose-limiting nephrotoxicity
                                                                  -CA binds cyclophilin                        •Diabetes, tremors, gingival hyperpl (CA),
                                                                  -Tac binds FKBP                              anaphylaxis
Sirolimus                             mTOR Inhibitor              •Binds FKBP to inhibit mammalian target      •NOT NEPHROTOXIC                                         •Used in combo w/ calcineurin inhibitor-allows red in
                                                                  rapamycin                                    •Hyperlipidemia, N/D, leukopenia,                        dose of CA or Tac
                                                                  •Pvts Cdk-2 stim of cell cycle               thrombocytopenia                                         •T cell spc
Antithymocute globulin,                 Ab Therapies                  •Suppress T cell response                        •Bas, Dac have no sig adv effs               •Bas, Dac used prior to tsplt to pvt T cell actvn
Muromonab, Daclizumab,                                                •Bas(more pot), Dac(longer t1/2) bind IL-2       •Profile is mild compared to otr agents      •Antithymocyte preferred for pre-surgical depletion of
Basiliximab                                                           receptor                                         •Anti-T, Mur (mouse): Anaphyl, Cyt inf rxn   bm
                                                                                                                                                                    •IS selective
Methotrexate, Azathioprine,             Anti-metabolite/anti-         •Inhibit DNA syn of B & T cells                  •Bone marrow toxicity                        •Not IS selective
Cyclophosphamide, Mycophenolate         proliferatives                                                                 •Cyc: Very toxic                             •Aza(targets hypoxanthine), MM(targets inosine MD):
Mofetil                                                                                                                                                             Purine biosyn inhibitor; prodrugs
                                                                                                                                                                    •Met: anti-folate; inhibs purine & pyrim syn
                                                                                                                                                                    Cyc: DNA alkylator

Cyclophosphamide(NM),                   Alkylating Agents (Directly •Bind DNA covalently: (1) DNA x-link (2) mut •Increased toxicity                                •N mustards, nitroureas
mechlorethamine, carmustine(NU),        alter DNA structure)        & mis-pr (3) sugar-P backbone breaks         •Car, lom: Hepatotox                               •Cytotoxic
lomustine, streptozocin,                                                                                         •Cis(less bm tox; antidote: diuretic), carb:       •Non-cell cycle spc
cisplatin(metal), carboplatin                                                                                    ototox, nephrotox, neurologic
                                                                                                                 •Cyc: hemorrhagic cystis, renal; antidote:
                                                                                                                 Mesna
                                                                                                                 •Busulfan: pulm fibrosis
Bleomycin, dactinomycin,                Topoisomerase II Inhibitors •Intercalating (increased toxicity) Abx;     •Dox: CHF (free radical damage; risk               •Ble, dau, & dox prod ROS tht cause DNA bks
doxorubicin, daunorubicin                                           inhibits Topo II; causes unrepairable DNA    factors=chest irradiation, tx w/                   •Non-cell cycle spc except Ble
                                                                    strand bks                                   cyclophosphamide, prev ht failure/MI, cumul        •Often cause accum of tumor cells in G2 phase
                                                                    •Dac inhibits DNA/RNA syn                    dose of 500-1000mg/m2)                             •Ble: G2 phase spc
                                                                                                                 •Ble has little bm tox; pulm fibrosis              •Pvt dox tox w/ vitE, ascorbic acid, probucol,
                                                                                                                 •Dau: Cardiomyopathy                               dexrazoxane
                                                                                                                 •Dox, dau (anthracyclines) andidote: anit-oxs

Topotecan, irinotecan                   Topoisomerase I Inhibitors    •Non-intercalating camptothecans                 •Less toxicity (non-intercalating)
                                                                      •Bind Topo I:DNA cmplx & inhibit
                                                                      resealing=DNA breakage
Etoposide, teniposide, irinotecan,        Topoisomerase II Inhibitors •Non-intercalating podophyllotoxins              •Less toxicity (non-intercalating)           •G2 phase spc
topotecan                                                             •Bind Topo II:DNA cmplx & inhibit
                                                                      resealing=DNA breakage
Vinca alkaloids(vincristine, vinblastine) Mitotic Inhibitors          •VA: blk tubulin polymzn & pvt fmn of            •Vinc, pac: neurotox, periph neuropathy      •Bind cells @ G1 and arrest @ M phase
Taxanes(paclitaxel, docetaxel)                                        mitotic spindle apparatus                        •Vinc: Less bm tox                           •Cytotoxic
                                                                      •T: bind tubulin and pvt depolymzn of
                                                                      spindle
Methotrexate                              DNA synthesis Inhibitors    •Inhibits dihydrofolate reductase; anti-folate   •Renal                                       •S phase spc
                                                                      (can't make thymine)                             •Antidote: Leucovorin                        •Thymine-less cell death
                                                                      •Depletion of FH4 pools                                                                       •Folate antag(Met)+Pyrimidine antag(5-FU)=common
                                                                      •Anti-metabolite                                                                              combo therapy
5-Flurouracil                             DNA synthesis Inhibitors    •dUMP inhibits thymidylate synthase;                                                          •S phase spc
                                                                      pyrimidine anti-metabolite (can't make                                                        •Pro-drug met to dUMP
                                                                      thymine)                                                                                      •Thymine-less cell death
                                                                      •Depletion of dTMP pools                                                                      •Anti-metabolite
Thioguanine/6-mercaptopurine              DNA synthesis Inhibitors    •Inhibits Inosine monophosphate DH &             •Hepatotox                                   •S phase spc
                                                                      glutamine phosphoribosyl pyrophosphate                                                        •Blocks Purine synthesis
                                                                      amidotransferase                                                                              •Anti-metabolite
Cytarabine, gemcitabine, cladribine, DNA synthesis Inhibitors         •Incorporation into DNA causing breakage                                                      •S phase spc
fludarabine phosphate                                                 and blockage of DNA pol; inhibits                                                             •Anti-metabolite
                                                                      ribonucleotide reductase
Rituximab, trastuzumab, bevacizumab Antibodies                        •Monoclonal Abs against lymphoid cell          •Less toxicity
                                                                      surface markers or growth factor receptors

Imatinib, erlotinib                      Tyrosine Kinase Inhibitors

Tamoxifen, raloxifene                    Estrogen receptor blockers •Binds estrogen receptors in ER breast           •Not cytotoxic; less toxicity                     •Hormonal therapy; prevents circulating estrogen from
                                         (SERMS)                    tumors                                           •Hormonal side effects                            stimulating tumor cell growth
                                                                                                                     •Tam: Hot-flash, N, vag bleeding,
                                                                                                                     thromboembolism, hepatotox, endometrial ca

Anastrozole, letrozole                   Aromatase Inhibitors         •Inhibits P450 enzyme (aromatase) that         •Hot-flash, N/H, vag bleeding, back pain          •Hormonal therapy; elimination of estrogens from
                                                                      converts androgens to estrogens                •Less toxicity                                    circulation; inhib biosyn
                                                                                                                     •Not cytotoxic                                    •More efficacious than ER blockers
Flutamide, leuprolide                                                 •Hormonal therapy

Coumarins (Warfarin)                     Delayed Acting Anti-coag     •Blocks reduction of VitK                      •Narrow therapeutic index                         •Inhibs formation of Vit K dependent CFs
                                                                      •Met to inactive form by P450                  •Sulfonamides displace from albumin               (prothrombin)
                                                                                                                     •Bleeding, Purple toe synd, Fetal warfarin synd   •No direct effect on prev syn factors
                                                                                                                     •Antidote: VitK(phytonadione), plasma, FIX        •Delay before effects (2d); 100% F
                                                                                                                                                                       •Inhibs syn of anti-coag proteins C & S that promote
                                                                                                                                                                       fibrinolysis(transient procoag effect)

Heparin                                  Immediate Acting Anti-coag •Binds ATIII (pwrfl anti-coag) and accelerates   •Bleeding, heparin induced thrombocytopenia       •Unfractionated: 5-30kDa
                                                                    intcn w/ Xa & Thrombin                           (HIT), hypersensitivity, thrombosis,              •LMWeight: 2-9kDa (enoxaparin, dalteparin,
                                                                    •LMW, Fondaparinux are more selective for        hyperkalemia                                      tinzaparin)
                                                                    Xa inhib(higher affinity); more predictable      •Antidote: Protamine Sulfate                      •Fondaparinux: synthetic

Hirudin Analogues (Argatroban)           Direct Inhibitors of         •Does not require ATIII to inhibit thrombin    •Do not cause thrombocytopenia                    •More predictable effecte than heparin
                                         Thrombin                                                                    •Bleeding                                         •Lepirudin=recombinant; Bivalirudin=synthetic
                                                                                                                     •Caution in pts w/ liver dysfunction              •Prod by salivary glands of H. medicinalis (leech)
                                                                                                                     •Used in pts w/ renal dysfunction

Aspirin                                  Anti-Platelet Agents       •Irreversibly inhibits COX by acetylatine        •GI ulceration, hypersensitivity, Reyes synd      •Activity not permanent in ECs; permanent in platelets
                                         Cyclooxygenase inhib (COX) serine near active site                          (children)                                        •IbP & indomethacin inhibit competatively
                                                                    •Blocks syn of TxA2
Dipyridamole                             Anti-Platelet Agents       •Inhibits platelet PDE>less cAMP                 •Angina in pts w/ coronary ht ds                  •Some vasodilation
                                         PDE Inhibitor              degraded>decrease in aggregation                                                                   •Aggrenox=combo of aspirin+dipyridamole
Ticlopidine, clopidogrel                 Anti-Platelet Agents       •Irrev inhib ADP-dep pwy of platelet agg         •Tic: Neutropenia, agranulocytosis,               •Clo: Prodrug met to active compound w/ t1/2=8h
                                         ADP Recep pwy inhib        •Covalently modify P2Y recep on                  thrombocytopenic purpura, aplastic anemia;        •Do not prevent aggragation, just reduces
                                                                    platelets>inhib of adenyl cyclase>inc cAMP       Black Box FDA warning
                                                                                                                     •Clo: Well tolerated, GI bleeding

Abciximab, Eptifibitide, Tirofiban (in   Anti-Platelet Agents         •Blocks binding of fibrinogen and vWF>pvt      •Bleeding, thrombocytopenia, hypotension,         •Abc: Chimeric monoclonal Ab
order of efficacy)                       Glycoprotein IIb/IIIa        agg                                            bradycardia                                       •In combo w/ aspirin & heparin
                                         Antagonist                   •Competitive & reversible inhibitors
Alteplase, reteplase, tenecteplase    Immediate Actyin            •Recombinant human t-PA                         •Inc local thrombi as clot dissolves>enhanced   •Clot dissolution better w/ early admin (must use w/n
                                      Fibrinolytic Agents         •Rapid proteolytic activation of                platelet agg>thrombosis(pvt w/ aspirin or       3h)
                                                                  plasmin>dissolve fibrin clot                    heparin)                                        •Serine protease
                                                                  •Serine protease                                •Hemorrhage(FFP, aprotinin, tranexemic acid)    •Fibrin selective; low affinity for plasminogen in plasma
                                                                                                                                                                  •First line agent

Streptokinase                         Immediate Actyin            •Complexes w/ free plasminogen to activate •Highly immunogenic                                  •From Gp C beta-hemolytic strep
                                      Fibrinolytic Agents         to plasmin & induce general fibrolytic state •Hemorrhage                                        •NOT fibrin selective
                                                                                                                                                                  •Must use in 3h window



Anistreplase                                                      •Plasminogen associated w/ streptokinase is •Inc local thrombi as clot dissolves>enhanced       •Complex of streptokinase and plasminogen
                                                                  activated                                   platelet agg>thrombosis                             •Prodrug
                                                                                                              •Hemorrhage
                                                                                                              •Immunogenic

Aminocaproic acid, tranexamic acid    Synthetic Antagonist        Synthetic inhibitor of plasminogen actvn        •Intravascular thrombosis

Protamine sulfate                     Synthetic Heparin           •(+) chgd protamine interacts w/ (-) chgd       •Dyspnea, flushing, bradycardia, hypotension    •Derived frm sperm or testes of fish
                                      Antagonist                  heparin forming inactive, stable complex

Phytonadione                          Vitamin K                   •Interferes w/ oral anticoags (warfarin)                                                        •Slow response; use FFP if pt needs immediate resps

Aprotinin                             Serine protease inhibitor   •Stops bleeding by blocking plasmin             •Renal dysfunct, anaphylactic rxns              •Inhibits streptokinase
                                                                                                                                                                  •Prophylactic use in cardiopulm bypass surgery

Ferrous sulfate, ferrous gluconate,   Iron                        •Abspn in SI; renews Fe stores                  •Epigastric pain, N/V/D, constipation           •Amt of Fe absbd inc w/ lgr dose; % absbd dec w/ lgr
ferrous fumarate                                                                                                  •Black stools, stain teeth, ROS(Fenton rxn),    dose
                                                                                                                  hemochormatosis(lethal)                         •Abspn inc w/ VitC

Iron Dextran                          FerricOH+Dextran            Complex removed by reticuloendothelial          •Fatal anaphylaxis
                                                                  sys>tsfrd to plasma>dist to bm & tissues        •Rxns @ injection site

Folic Acid                            Folic Acid                  •Supplement body's levels; role in prolif and                                                   •Rule out B12 deficiency b4 Tx; may mask
                                                                  erythropoiesis

Cyanocobalamin, hydroxocobalamin      VitB12                      •Supplement body's levels; role in prolif and                                                   •IF & Ca2+ must be present for abspn
                                                                  erythropoiesis                                                                                  •Rule out folate deficiency b4 Tx

Recombinant Human EPO,                Erythropoietic Agents       •Stimulate erythropoiesis @ EPO receptor                                                     •Increases use of Fe stores>should take Fe
Darbepoetin                                                                                                                                                    supplements
5-Azacytidine, hydroxyurea,           HbF inducing Agents         •A: DNA methylator; reverses Me of gamma- •A, H: Does not prevent end organ damage           •Hydroxyurea eff in 60% pts; slower induction of HbF
butyrates (arginine butyrate,                                     globin gene                                  •5-Az & butyrates may have long term risk of Ca •Inc HbF to ovr 20% Hb
phenylbutyrate)                                                   •H: Ribonucleotide reductase inhibitor; blk                                                  •Butyrates not effective in pts w/ HbF<1%; infants &
                                                                  div of HbS precursors                                                                        children
                                                                  •B: Sht chain FA inhib histone deacetylases;
                                                                  pvt switch frm HbF to HbS
rhTPO, PEG-rhMGDF, rhIL-1(only drug Thrombopoietin Analogs   •Inc platelet prod in dose dep manner   •Thrombosis   •1-3wk delay for activity
appvd thus far for                                                                                                 •In clinical trials
thrombocytopenia)
Resistance                                     Contraindications              Duration/Dose             Route of Admin        Uses
•β-lactamase production by bact destroys Abx   •Allergic rxn                  •Most use std 10d         •Oral                 •G(+) cocci: Enterococcus, Staphaureus, S. pyogenes,
•Decrease entry by modification in porins                                     •Dpds on severity of Ds   •Parenteral in some   Viridans, S. pneumoniae
•Reduced affinity to PBPs                                                                               circumstances         •G(-) cocci: Neisseria meningitides
                                                                                                                              •G(-) bacilli

•β-lactamase production by bact destroys Abx   •Allergic rxn                  •Most use std 10d         •Oral                 •G(+) cocci: S. pyogenes
•Decrease entry by modification in porins                                     •Dpds on severity of Ds   •Parenteral in some
•Reduced affinity to PBPs                                                                               circumstances
•β-lactamase production by bact destroys Abx   •Allergic rxn                  •Most use std 10d         •Oral                 • Staphaureus (MRSA)
•Decrease entry by modification in porins                                     •Dpds on severity of Ds   •Parenteral in some
•Reduced affinity to PBPs                                                                               circumstances
•β-lactamase production by bact destroys Abx   •Allergic rxn                  •Most use std 10d         •Oral                 •G(-) bacilli
•Decrease entry by modification in porins                                     •Dpds on severity of Ds   •Parenteral in some   •G(+) cocci: Enterococcus
•Reduced affinity to PBPs                                                                               circumstances



•β-lactamase production by bact destroys Abx   •Allergic rxn                  •Most use std 10d         •Oral                 •G(+) cocci: S. pneumoniae
•Decrease entry by modification in porins                                     •Dpds on severity of Ds   •Parenteral in some   •G(-) bacilli
•Reduced affinity to PBPs                                                                               circumstances



•Decrease entry by modification in porins                                     •Most use std 10d         •Oral                 •G(-) bacilli
•Reduced affinity to PBPs                                                     •Dpds on severity of Ds   •Parenteral in some
                                                                                                        circumstances
•β-lactamase production by bact destroys Abx   •Allergic rxn                  •Most use std 10d         •Oral                 1st = G(+) mainly
•Decrease entry by modification in porins      •Cross-allergy w/ penicillin   •Dpds on severity of Ds   •Parenteral in some   2nd, 3rd, 4th=
•Reduced affinity to PBPs                                                                               circumstances            •G(-) cocci: Neisseria meningitides
                                                                                                                                 •G(+) cocci: S. pyogenes, Viridans, S. pneumoniae
                                                                                                                                •G(-) bacilli

                                                                              •Most use std 10d         •Oral                 •G(+)
                                                                              •Dpds on severity of Ds   •Parenteral in some   •G(+) cocci: Enterococcus, Staphaureus, Viridans
                                                                                                        circumstances         •MRSA



•Formation of enzymes that inactivatedrugs     •Allergic rxn                  •Most use std 10d         •Oral                 •G(-) aerobes
                                               •Pregnancy                     •Dpds on severity of Ds   •Parenteral in some   •G(+) cocci: Enterococcus, Viridans
                                               •Nursing mothers                                         circumstances
                                               •Renal failure
•Formation of enzymes that inactivatedrugs     •Allergic rxn                  •Most use std 10d         •Oral                 •G(-) aerobes
                                               •Pregnancy                     •Dpds on severity of Ds   •Parenteral in some
                                               •Nursing mothers                                         circumstances
                                               •Renal failure
•Formation of enzymes that inactivatedrugs     •Allergic rxn                  •Most use std 10d         •Oral                 •G(-) aerobes
                                               •Pregnancy                     •Dpds on severity of Ds   •Parenteral in some
                                               •Nursing mothers                                         circumstances
                                               •Renal failure
•Efflux pumps                                         •Pregnancy, nursing                  •Most use std 10d         •Oral                 •Ehrlichia, reckettsiae, spirochetes, mycoplasma &
                                                      •<8yo                                •Dpds on severity of Ds   •Parenteral in some   chlamydiae
                                                                                                                     circumstances
•Increase efflux (pumping out) of Abx                 •Allergic rxn                        •Most use std 10d         •Oral                 •G(-) bacilli
•Formation of methyltranserases that alter drug       •Pregnancy                           •Dpds on severity of Ds   •Parenteral in some   •Resp tract pathogens
binding on ribos                                      •Concurrently taking other spc                                 circumstances
                                                      drugs
•Formation of inactivating acetyltransferases                                              •Most use std 10d         •Oral                 •G(-) cocci: Neisseria meningitides
                                                                                           •Dpds on severity of Ds   •Parenteral in some
                                                                                                                     circumstances
•Resistance-limited use to spc types of infection     •Allergic rxn                        •Most use std 10d         •Oral
•Change in sensitivity inhibition of target enzymes   •Pregnancy, nursing                  •Dpds on severity of Ds   •Parenteral in some
                                                      •Infants <2mo                                                  circumstances
                                                      •Megaloblastic anemia due to
                                                      folate deficiency
                                                      •Allergic rxn                        •Most use std 10d         •Oral                 •Prostatitis & vaginitis
                                                      •Pregnancy, nursing                  •Dpds on severity of Ds   •Parenteral in some   •G(-) bacilli, actinomycetes
                                                      •Infants <2mo                                                  circumstances
                                                      •Megaloblastic anemia due to
                                                      folate deficiency
•Modification of target                               •Allergic rxn                        •Admin once or 2x's       •Oral
•Efflux                                               •Pregnancy, nursing                  daily                     •Parenteral in some
•Decrease porin xprsn                                 •<18yo (usually)                     •Not given <18yo          circumstances

•Error prone pol gene (RT) syn leads to mutations     •Zid: Pregnancy (cat C)              •2x/d                     •Oral                 •Active agst HIV-1 & HIV-2




•Error prone pol gene (RT) syn leads to mutations                                          •Long half-life=once a    •Oral                 •Active agst HIV-1, HIV-2, HBV
                                                                                           day dosing
•Error prone pol gene (RT) syn leads to mutations                                          •2x's daily dosing        •Orally active & 1%   •Active agst HIV-1, HIV-2, HBV
                                                                                                                     vaginal gel prep

•Arises due to mutations in RT                                                                                       •Oral                 •Active agst HIV-1




•Arises due to mutations in RT                        •Pregnancy (teratogenic)             •1x/d                     •Oral
                                                      •P450 drug interactions w/
                                                      psychotropics, ergot alks, oral
                                                      contraceptives (inc clearance;
                                                      fails), methadone, anti-epileptics
•Mutations in protease gene           •Rifamycin, statins, psychotropics, •Combo of PI+NRTI has   •Oral admin, poor   •Active agst HIV-1
•Multi-drug resistance pump (MDR-1)   Fentanyl, Ergot alks, St. John's    synergistic anti-HIV    absorption
                                      Wort, Indinavir, Ritonavir, oral    actvty
                                      contraceptives




                                      •Pregnancy                        •Daily for several wks    •Parenteral         •Neutropenia
                                                                                                                      •Decrease infection rate
                                                                                                                      •Stimulate maturation of blood cells
                                                                                                                      •Harvesting peripheral blood precursor cells

                                      •Sickle cell (in some cases)      •Several days>dec need                        •Neutropenia
                                      •Pregnancy                        for daily dosing                              •Decrease infection rate
                                                                                                                      •Stimulate maturation of blood cells
                                                                                                                      •Harvesting peripheral blood precursor cells

                                                                                                                      •Neutropenia
                                                                                                                      •Decrease infection rate
                                                                                                                      •Harvesting peripheral blood precursor cells



                                                                                                                      •Replenish granulocytes & Ma
                                                                                                                      •Harvesting peripheral blood precursor cells
                                                                                                                      •Neutropenia



                                      •Hypersensitivity                 •Chl, Hyp: 6h             •Oral               •Chl, Hyd, Dim: Allergic rhinitis, urticaria(Doxepin), atopic
                                      •Newborn, nursing                 •Dim, Dip: 8h                                 allergy
                                      •Glaucoma                         •Mec, Dox, Pro: 12h                           •Dim, Pro, Mec: Nausea, motion sickness (Scopolamine)
                                      •Stenoding peptic ulcer                                                         •Dip, Dox: OTC sleep aid
                                      •Prostatic hypertrophy                                                          •Anaphylaxis (diphenhydramine, ranitidine), angioedema,
                                      •Asthma in LRT                                                                  nasal congestion
                                      •MAO's
                                      •Hypersensitivity                 •Cet, Lor: 24h            •Oral               •Allergic rhinitis, urticaria, atopic allergy
                                                                        •Fex: 12h                                     •Anaphylaxis (diphenhydramine, ranitidine), angioedema,
                                                                                                                      nasal congestion




                                      •Hypersensitivity                 24h                       •Oral               •Allergic rhinitis, urticaria, atopic allergy
                                                                                                                      •Anaphylaxis (diphenhydramine, ranitidine), angioedema,
                                                                                                                      nasal congestion
•Hypersensitivity                                       •Oral                     •Allergic rhinitis



                                                                                  •Anaphylactic shock




                                                                                  •Anaphylactic shock
•Pregnancy                    •8-12h                    •All: Oral                •Hyd, Cor: Low potency OTC topicals, congenital adrenal
                                                        •Hyd, Cor: Parenteral     hyperplasia
                                                        •Hyd, Cor: Topical        •Acute/chronic adrenal indufficiency
                                                                                  •Flu: Addison's Ds when hyperkalemia persists after Hyd,
                                                                                  mineralocorticoid deficiency

•Pregnancy except predisone   •12-36h                   •All: Oral                •Systemic inflammatory Tx
                                                        •Met, Tri: Parenteral     •Tri: Medium potency dermatological
                                                        •Met, Tri: Topical        •Met, Pre: Immunosuppression




•Pregnancy                    •Bet, Dex: 24-72h        •All: Topical              •Bet: Systemic/topical psoriasis, dermatitis,
                              •Flut, Flun, Bud: 12-36h •Bet, Dex, Bud: Oral,      neurodermatitis
                                                       topical                    •Dex: Neoplasias, inflammatory disorders, low potency
                                                       •Flun, Flut: Intranasal,   dermatological
                                                       inhaled                    •Flut (med pot derm), Flun, Bud: Asthma, allergic rhinitis
                                                                                  •Bet, Dex: Resp distress synd in pre-me's

                                                        •Topical                  •Deson:Low potency dermatological
                                                                                  •Flu, Desox: High potency dermatological
                                                                                  •Clo: Very high potency dermatological




                                                        •All: Oral                •Acute and chronic immunosuppression
                                                        •Met: Parenteral          •Phase 1, 2 tsplt therapy
                                                                                  •Pre: ALL, CLL, Hodgkin's, non-Hodgkin's
                                                        •Oral                     •Long-term immunesuppression for kidney, liver, cardiac
                                                        •IV                       tsplt
                                                                                  •Phase 2 tsplt therapy (not kidney)



                                                        •Oral                     •Phase 2 tsplt therapy
                                           •Anti-T, Mur: Epilepsy   •3-9d                    •Parenteral   •Phase 1 tsplt therapy
                                                                    •Dac: longer t1/2
                                                                    •Bas: more potent

                                                                                                           •Phase 2 tsplt therapy




•Innate, mutation, P-glycoprotein (MDR),                                                                   •Car, lom: brain ca
amplification                                                                                              •Cis, carb: head, neck, lung, testicular, cervical, thyroid,
                                                                                                           ovarian
                                                                                                           •Cyc: leukemia/lymphoma




•Innate, mutation, P-glycoprotein (MDR),                            •Children can tolerate                 •Testicular, ovarian, cervical, thyroid, acute leukemia,
amplification                                                       higher doses of dox                    Hodgkin's, breast, lung cancers




•Innate, mutation, P-glycoprotein (MDR),
amplification

•Innate, mutation, P-glycoprotein (MDR),
amplification

•RESIS TO ONE ALLOWS RESIS TO OTR                                                                          •T: Breast, ovarian cancer
•Innate, mutation, P-glycoprotein (MDR),                                                                   •V: Lymphomas, ALL
amplification

•Innate, mutation, P-glycoprotein (MDR),                                                                   •Breast, choriocarcinoma
amplification



•Innate, mutation, P-glycoprotein (MDR),                                                                   •Colon, stomach, liver, prostate, breast cancer
amplification



•Innate, mutation, P-glycoprotein (MDR),                                                                   • Blood cancers
amplification                                                                                              •Cyt: leukemias

•Innate, mutation, P-glycoprotein (MDR),                                                                   •Breast, bladder, pancreas
amplification
•Innate, mutation, P-glycoprotein (MDR),                                                                            •Bladder cancer
amplification

•Innate, mutation, P-glycoprotein (MDR),
amplification
•Innate, mutation, P-glycoprotein (MDR),                                                                            •Breast cancer
amplification




•Innate, mutation, P-glycoprotein (MDR),                                                                            •Breast cancer
amplification

•Innate, mutation, P-glycoprotein (MDR),                                                                            •Prostate cancer
amplification
                                           •Pregnancy, hemorrhagic          •Based of PT              •Oral         •DVT, A-fib, Heart valve replacement, MI, CVA
                                           tendencies, eye surgery, brain   •5mg/day (2mg in                        •In conjunction w/ Heparin
                                           bleed                            elderly); titrate to                    •Before some surgery
                                                                            approp INR                              •Inhibit embolization




                                                                            •Based of aPPT            •Parenteral   •Acute thromboembolic disorders, surgery, transfusions, A-
                                                                            •Max effect 3-5 hr post   •SubQ         fib, anti-coag in pregnancy, DVT, dialysis, pulmonary
                                                                            inj                                     embolism



                                           •Liver impairment                                          •Parenteral   •Pts who have experienced HIT




                                                                            •Persists up to 2d                      •Arterial thrombosis, CVA, TIA
                                                                            •Low dose=81mg

                                                                            •Usually w/ warfarin or                 •Ischemic stroke, TIA
                                                                            aspirin
                                                                                                                    •Tic: prevention of TIA in pts w/ prior thrombotic event
                                                                                                                    •Pts who are aspirin intolerant or unresponsive




                                                                            •24-48h                   •IV           •Percutaneous coronary interventions (angioplasty, stents)
                                                                                                                    •Acute coronary syndromes
•Pts w/ healing wounds,                                        •IV                          •Restore catheter/ shunt funct, clot lysis, coronary
pregnancy, Hx of CVA, metastatic                                                            thromboses, pulm embolism, acute ischemic stroke(w/n
ca                                                                                          3h)
•GI bleeding w/n 3mo, acute
pericarditis, Hx hypertension

•Pts w/ healing wounds,                                        •IV                          •Restore catheter/ shunt funct, clot lysis, coronary
pregnancy, Hx of CVA, metastatic                                                            thromboses, pulm embolism, acute ischemic stroke
ca
•GI bleeding w/n 3mo, acute
pericarditis, Hx hypertension
•Pts w/ healing wounds,                                        •IV                          •Restore catheter/ shunt funct, clot lysis, coronary
pregnancy, Hx of CVA, metastatic                                                            thromboses, pulm embolism, acute ischemic stroke
ca
•GI bleeding w/n 3mo, acute
pericarditis, Hx hypertension
                                                               •Oral                        •Tx adverse effects of plasminogen activators

                                                                                            •Tx heparin induced bleeding



                                                                                            •Tx warfarin OD; bleeding

•Pts who have recd the drug w/n                                                             •Reduction in perioperative blood loss, cardiopulm bypass
prev 12 mo (anaphylaxis)

                                   •100-200mg/d TID            •Oral                        •Fe deficiency anemia
                                   •4-6mo Tx                   •Sustained release prep



                                                               •IM                          •Fe deficient pts who cannot tolerate or fail w/ oral
                                                               •IV                          therapy

                                                                                            •Megaloblastic anemia, pragnancy
                                                                                            •Pvt neural tube defects during pregnancy
                                                                                            •Protection for coronary artery Ds
                                   •daily, 5-                  •IM, IV (cannot give         •Pernicious anemia, megaloblastic anemia
                                   10d>maintenance             orally due to lack of IF);   •Oral admin for dietary deficiency
                                                               dietary=oral
                                   •Dar has xtra sialic acid                                •Anemias assoc w/ chronic renal failure, Ca, toxicity,
                                   tht inc t1/2 3x's                                        Zidovudine therapy, CHF
                                                                                            •Sickle cell
                                                                                            •Beta-Thalassemia
•Thromboembolic disorders
Drug Interactions   Key
                    Abx




                    HIV/AIDS



                    Leukocytes



                    Antihistimines




                    Steroids




                    Immunosuppreso
                    rs

                    Anti-cancer




                    Anti-coagulants




                    Coagulants




                    Hematopoietics
•Interferes w/ metabolism of caffeine




•Not metabolized by P450
•AZT bone marrow toxicity inc w/ acetaminophen or
cimetidine (b/c slower glucuronidation in liver)




•Not metabolized by P450=infrequent drug interactions

•Not metabolized by P450=infrequent drug interactions
•Extensive P450 metabolism; inhibitor=many drug
interactions




•May induce P450




•May induce P451




•May induce P452
•May induce P453
•Inc eff: amodiarone, macrolides, sulfonamides(displace
frm albumin), quinolones, azole, antifungals, fluoxetine,
gemfibrozil, seraline, ginko, VitE, NSAIDs; P450 inhibitors
•Dec eff:Cabarnazepine, rifampin, cholestryamine, VitK, St.
John's Wort, ginseng, CoQ; P450 inducers



•Inc bleeding when used w/ otr anticoags




•Inc bleeding when used w/ otr anticoags




•Inc bleeding when used w/ otr anticoags



•Inc bleeding when used w/ otr anticoags

•Inc bleeding when used w/ phenytoin, tolbutamide,
warfarin, fluvastatin, tamoxifen
•Clo: P450 inhibitor
•Food retards abspn; ascorbic acid inc abspn
•Red abspn of tetracycline, fluoroquinolones,
levothyroxine, VitE
Drug Name                  Class                Mode of Action                         Notes                                              Toxicity                             Uses                                  Dose, Duration Route of
                                                                                                                                                                                                                                      Admin
ACh, Bethanechol &         Cholinergic Agonist Direct: acts at receptor level          Parasympathomimetic                         Cardiac (M2): Slow HR,                      ACh: cataract surgery, Dxtic          ACh: sm or lg    ACh: IV,
Carbachol, Cevimeline      (Choline esters-    Ach: reflex tachycardia, dec BP         Poor abspn, lack specificity                conduction; dec cntctlty                    angiography                           dose             Ocular
                           except Cev)         Bet(stim bladder, GI sm musc w/o aff    Ocular effects: lacrimal sec, miosis        GI & Urinary (M3): Inc scns,                Bet: urinary retention,               B&C: short (hrs) Bet: SubQ, oral
                                               HR), Cev: muscarinic spc                B&C resis to AChE                           motility, diarrhea; sm musc                 postop/partum                                          (NEVER IV)
                                                                                                                                   ctcn
                                                                                       Contraind: asthma, cardiac arr/insuff, peptic                                           Cev: xerostomia, dry eyes,                             Car: Ocular,
                                                                                       ulcer, hyperthyroidism                      CNS arousal                                 Sjogren's Synd                                         topical
                                                                                                                                   *Atropine for OD                                                                                   Cev: Oral
                                                                                                                                   Cev: Least side eff
                                                                                                                                   DUMBBELSS
Muscarine, Nicotine,       Cholinergic Agonist Direct: acts at receptor level          Parasympathomimetic                         DUMBBELSS                                   Pil: chr open angle glaucoma, Pil: less potent Pil: Oral,
Pilocarpine                (Plant alkaloids)   Pil: Muscarinic>nicotinic (ganglia)     Mycetism: mushroom poisoning(muscarinic) *Atropine, Epi for OD                          xerostomia                    than ACh         ocular, topical
                                               receptors                               due to xs cholinergic agonism (NOT Amantia)                                             Nic: smoking cessation                         (well absbd)

Neostimnine,               Cholinergic Agonist Indirect, REVERSIBLE: Binds, inhibits   Parasympathomimetic                                Cholinergic crisis: prolonged        Myasthenia gravis                     Small             Don: oral
Physostigmine (cross                           AChE                                    Eye: miosis, dec intraoc P                         musc depol>>depol                    Postop urinary ret, abd dist,         Edr: 10m, renal   Edr: IV
BBB), Pyridostigmine,                          Edr: blocks ACh hyrdolysis              GI: Inc ctcn/secretion                             blkade>>paralysis                    glaucoma                              extn              Neo: oral,
Edrophonium, Donepezil                                                                 NM junct: ctcn, inc [Ach] @ synapse                DUMBBELSS                            Edr: dDx M. gravis,                   Don: 24hrs        subQ, IM
                                                                                       Rev eff of non-depol NM blkng agents               *Atropine for OD                     Myasthenic crisis                     Neo: 2-4hr        Phy: topical,
                                                                                       Don, mPhy: cross BBB                                                                    Don: Alzheimer's                      Phy: 1-5hr        ocu, IM, IV
                                                                                                                                                                               Neo, Pyr: Curare tox                  Pyr: 3-6hr        Pyr: oral, IM,
                                                                                                                                                                               Atropine OD                                             IV
Echothiophate,             Cholinergic Agonist Indirect, IRREVERSIBLE: covalently      Parasympathomimetic                                lots of DUMBBELSS                    Little clinical use                   1 wk              Ech, Iso:
Isoflurophate, Malathion   (OrganoPO4)         bound to AChE; "aging" further stblzs   Highly lipid sol (lipid partitioning); absbd frm   Depol blockade, seizure, resp        Chr glaucoma                                            ocular, topical
(Organophosphates)                                                                     skin, eyes, gut, muc membs                         dep, coma                            Strabismus(esotropia)                                   Mal: topical
                                                                                       Pesticides, chem warfare                           *Atropine, 2-PAM,                    Mal: head lice
                                                                                       Effects of musc & nico actvn                       Butyrlcholinesterase = OD
                                                                                       Route of exposure imptnt                           Intermediate Syn (sm xpsr)
                                                                                                                                          Death usually from resp failure



Atropine, Scopolamine,     Cholinergic          Inhibit effects of parasymp nerve      Well absbd                                         Inc HR, AV conduction V; no chg      Mydriasis, iritis, cyclitis, opthal   Dose dpdt     Oral,
Hyoscyamine                Antagonist           stimulation (parasympatholytic)        Inhib of secretions, mydriasis, cycloplegia        in BP/CO; Bronchodilation;           exam, bradycard, asthma, red          effects       transdermal,
                           (Belladonna          Sco: blocks st memory, dec REM; actn   Ocular: t1/2 longer; binds to pigments             Reflulx, relaxation, red motility;   secretions, IBD, urinary              Tx OD w/      ocular
                           Alkaloids)           in CNS                                 Hyperthermia                                       Sedation, xctmt                      spasm, motion sickness,               repeated AChE
                                                Hyo: spasmolytic                       Ped suscep                                         Anti-DUMBBELSS                       Parkinson's                           agents
                                                                                                                                          *Anticholinesterase agents           Sco: sedation, anesthesia



Ipratropium, Tiotropium    Cholinergic          Inhibit effects of parasymp nerve      Bronchodilators                                    Dry mouth                            COPD, asthma                                            Inhalation
                           Antagonist           stimulation                            Some selectivity for M1, M3                        Localized due to inhalation
Darifenacin(M2, M3),       Cholinergic           Inhibit effects of parasymp nerve           Warning to those susceptible to Alzheimer's Dry mouth                          Overactive Bladder
Solifenacin, Oxybutynin,   Antagonist            stimulation                                 Some bladder spcfty                         Dry eyes
Tolterodine, Flavoxate                           Similar to Atropine



Dicyclomine,               Cholinergic          Inhibit effects of parasymp nerve Gly:       Dic: reduction in abd cramping; relieves       anti-DUMBBELSS                  Dic: IBD                                         Gly: oral,
Glycopyrrolate,            Antagonist           inhib of GI motility (oral); blocks eff of   urgency, pain                                  Dic, Pir: less systemic se      Pir: peptic ulcer Ds (not appvd                  parenteral
Pirenzepine                                     vagal stim during anesthesia&surgery         Pir: M1>M2, M3                                                                 in US)
                                                (parenteral)                                                                                                                Surgery
Mecamylamine               Nicotinic Antagonist Comptv ganglionic blocker                                                                                                   Emergency BP lowering, aortic Short acting       IV
                                                                                                                                                                            aneurysm
Epinephrine                Adrenergic Agonist    Direct Acting Catecholamine: bind to        Sympathomimetic; cardiac stim                  Xsv vasoconstcn, arrhythmias,   Bronchodilation, anaphylaxis                     IV, subQ
                                                 receptor & activate                         Vasc: redist of BF; diff vasc beds rspd diff   hyperglycemia secondary to
                                                 Stim all α & β receptors                    based of affinity and recep type               glycogenolysis, cerebral
                                                 Diastolic P usually falls, periph resis     Metabolic, sm musc, resp & CNS eff             hemorrhage
                                                 dec, mod inc in systolic P; mean BP
                                                 unchgd
Norepinephrine             Adrenergic Agonist    Direct Acting Catecholamine                 Less pot than Epi @ α                          Necrosis & sloughting of tissue Shock
                                                 Postganglionic symp nerves                  =Epi @ β1                                      @injection site if extravasated Severe hypotension
                                                 No actn @ β2(> elev in BP than Epi)         Inc syst, diast, pules P; CO unchgd; TPR inc   Similr to Epi
                                                                                             Poor abspn

Dopamine                   β Adrenergic          1: eff in CNS                               Periph andrenergic actvty                                                      Cardiogenic shock
                           Agonist (non-sel)     Direct Acting Catecholamine                 D1> β1> α                                                                      Cmplt ht blk
                                                                                             Renal vasodil, cardiac stim, inc BP                                            Cardiac surgery
                                                                                                                                                                            CHF, MI
Isoproterenol              β Adrenergic          Direct Acting Catecholamine                 Non-sel; low aff for α recep (almst no actn)   Met by COMT                     Inhibs rel of inflamm           Potent           Parenteral,
                           Agonist (non-sel)     Relaxes almst all sm musc when tone         Dec PVR, DP, MAP                               Palpitations, tachycard, HA,    mediators                       Brief but longer aerosol
                                                 high (bronchial/GI)                         Inc CO                                         flushing; cardiac ischemia,     Bradycardia, V-fib, asthma,     than Epi
                                                                                                                                            arrhythmia                      shock
Dobutamine                 β Adrenergic           α & β receptors                            Racemic mix                                    Complex                         Post cardiac surgery, CHF, MI   t1/2=2m
                           Agonist (non-sel)                                                 Inc CO, ctctlty, HR(slight)                    Inc BP, HR, A-fib, infarct
Metaproterenol,            β2 Andrenergic        Actvty @ β2 andrenergic receptors           Xtsv use-receptor down regulation              Caused by overstim of β1:                                                        Oral,
Terbutaline, Albuterol,    Agonist               promote sympathetic nervous resps                                                          tremor, anxiety, tachycard                                                       inhalation
Pibuterol, Salmeterol                                                                                                                       Pts w/ Coronary art Ds, MAOIs
                                                                                                                                            > eff
                                                                                                                                            Min by inhalation route
Phenylephrine,           α1 Adrenergic           Actvt α1 @ vasc sm musc                     Inc PR, BP                                                                     Decongestant
Oxymetazoline, Midodrine Agonist                                                                                                                                            Mid: autonomic insuff,
                                                                                                                                                                            hypotension
Clonidine                  α2 Andrenergic        Hypotensive resps due to dec symp           Dec symp outflow                               Dry mouth, sedation,            Systemic Hypertension,                           IV, oral,
                           Agonist               outflow frm CNS                                                                            bradycard, w/d Sx, hpotn        autonomic neuropathy, w/d                        transdermal
                                                                                                                                                                            prep, spasticity
Apraclonidine              α2 Andrenergic        Does not cross BBB                          Red intraoc P via red in aqueous humor prod Dry mouth, sedation,               Short term therapy for
                           Agonist                                                           Min-no systemic cardio eff                  bradycard, w/d Sx                  glaucoma
Guanfacine, Guanabenz   α2 Andrenergic      Selective α2                              Dec BP                                           W/d synd
                        Agonist             Suppresses symp actvty                    Central actg (brain stem)
Amphetamine             Andrenergic Agonist Indirect acting: inc [NE] @               Reverse NE tspt bk into synapse                                                 Narcolepsy, ADHD
                                            synapse>displaces storage of NE           CNS stimulant
Cocaine                 Andrenergic Agonist Indirect acting: inhibs catecholamine     Inhib NE reuptake
                                            tsptr in synaptic memb                    Inc [NE] @ synapse

Tyramine                Andrenergic Agonist Indirect acting: enters nerve terminal, Found in fermented foods                           Toxic in persons on MAOIs      Not clinically useful
                                            displaces stored NE                     Oxidized by MAO
Ephedrine,              Andrenergic Agonist Mixed acting agonist: actvts α & β      Resis to MAO, COMT (dangerous in BP)               Tachycardia ( β1 stim), inc BP, Eph: bronchodilator
Pseudoephedrine                             receps by direct & indirect mechs                                                          urinary ret, insomnia, CNS stim Pse: nasal decong
(stereoisomer)                              Vasoconst @ α1

Phenoxybenzamine        α Andrenergic        Inhib reuptk of catecholamines           CV sys mst impt for eff                          Postural hypotension, reflex   Acute hypertensive crisis in   3-4d
                        Antagonist           Actn in CNS, periph                      Non-selective, irreversible, delayed actn        tachycard, arrhythmias         pheochromocytoma
                                             Noncompetitive                           Major eff: blkade α2 in sm musc

Phentolamine            α Andrenergic        Competitive                                                                               Postural hypotension, reflex   Acute hypertensive crisis in   10-15m         IV
                        Antagonist                                                                                                     tachycard, arrhythmias,        pheochromocytoma or w/d
                                                                                                                                       ischemia, cardiac events       synd
                                                                                                                                                                      Dermal necrosis, ischemia

Prazosin, Terazosin,    α 1 Andrenergic      Inhibits cyclic nucleotide               Dec PR, venous return                            1st dose syncope               Essential hypertension, CHF    Longer; Dox:
Doxazosin               Antagonist           phosphodiesterase                        Favorable blood lipid profile, glc metabolism;   Orthostatic hypotension        BPH                            longest
                                             Depress barorecp rsps                    gtr F                                            Dizziness                                                     1x/d
                                                                                      Na+ & H2O retention
Propranolol, Nadolol,   β Adrenergic         Non-spc, competitive; slows HR, dec      Blkd of β recep has little actn in normal pt     Hypertension, angina           Hypertension, CHF, Ischemic                   Tim: ocular
Timolol,Pindolol        Antagonist           cntctlty/BP                              Antiox actvty; ISA                                                              HD, arrhythmia
                                             Blkd of Ca2+ channs, prod NO             Aff β1=β2; no α actvty                                                          Tim: glaucoma

Metoprolol, Atenolol,   β1 Andrenergic       Cardioselective β1 recep blockers        no ISA, MSA (Ace has some)                       PMs>eff                        Hypertension, MI, CHF,        1x/d            Low F
Esmolol, Acebutolol,    Antagonist           Bis: in combo w/ ACE inhibs, diuretics   Less bronchoconstcn (β2)                         Contraind: acute/sev HF        angina, premature ventricular IV for sht
Bisoprolol                                                                            Contraind: asthma                                                               beats                         duration
                                                                                      Genetic variability
Carvediol, Labetolol    3rd gen β            Cardioselective β blockers               Inc prd NO; antiox actvty                        Liver injury                   Hypertension
(racemic mixture)       Andrenergic          Blkd of α1 enhances vasodil              β2 agonist props(less bronchocstn)                                              Car: CHF
                        Antagonist           K+ chann actvtrs                         Car: MSA, no ISA; antiprolif eff
                                             Comptv antag @ α1 & β
                                             Inhib of neuronal NE uptake
Somatrem, Somatropin    Gwth Hormone         Stim nat rise in GH w/ sleep onset       Prod by recomb DNA tech                          Generally non-Tx                                              3x/wk @ bed    IM, subQ
                                                                                                                                       May inc TII diab, ped tumor
                                                                                                                                       gwth, GH Abs
Doxercalciferol (pro-drug), Vit D                Stim intest abspn of Ca2+                Vit D3 cnvtd to actv fm (calcitriol) by liver   Hypercalcemia/calciuria/phosp Osteoporosis, Rickets,               1200 IU/d       Oral
Paricalcitol, Calcipotriene,                     Red urinary xctn of Ca2+                 Recomm use in combo w/ Ca2+                     hatemia                       Osteomalacia, Osteopenia,
Fish oil                                         Aid in bone mineralization & Ca2+                                                                                      Hypoparathyroidism,
                                                 deposition                                                                                                             PseudoHPT

Ca2+ Supplements                                 Inc body's Ca2+ levs                     Recomm use in combo w/ Vit D                                                     Inc bone den, red loss of         1500mg/d        Oral
                                                                                          Post-menopausal women                                                            cortical bone
Alendronate,                Bisphosphonates      Incorp into bone matrix and inhib        Can inc BMD; take on empty stmch                Esophagitis                      Paget's, Osteoporosis,            5-10 mg/d     Oral
Pamidronate,                                     osteoclast actvty                        Red vert, hip Fx                                Contraind: Barrett's Eso         hypercalcimia due to malig        40 mg/wk      Pam: IV to
Risedronate, Tiludronate                                                                  Ris: btr oral F; more potent                                                                                       3-6 mo crs    bypass GI tox
                                                                                                                                                                                                             Pam: 30mg ovr
                                                                                                                                                                                                             3hr/3mo
Prempro (w/ progestin), Estrogen                 Inc estrogen levs in body                E-sulfate: 1/10th binding aff for ER than       CV effs                          Endometrial ca, post-                           Oral
Premarin, Estrone sulfate, Replacement                                                    Estradiol                                       E-diol: lwr adv eff profile      hysterectomy, Osteoporosis                      E-diol: tns
Estradiol                  Therapy                                                        F, <45yo w/ premat menopause                                                                                                     derm, cream,
                                                                                                                                                                                                                           oral
Raloxifene                  Selective Estrogen                                            Shws inc in BMD                                                                  Osteoporosis in post-             60-120mg/d    Oral
                            Receptor Modulator                                            Dec risk vert Fx                                                                 menopausal women



Teriperatide                PTH analog           Stim frmtn of Vit D3 by kidney>inc     More efficacious in bldng BMD in L-spine          Chr use causes net bone loss,    Osteoporosis                      Intermittent    Parenteral
                                                 intest abspn of Ca2+                                                                     hypercalcemia,                                                     admin
                                                 Calcimimetics (Cinacalcet) mimic the                                                     hyperphosphatemia
                                                 actn of Ca2+ and inhib PTH sec frm PTG

Calcimar, Osteocalcin       Calcitonin Analog    Red serum Ca2+ levs>inhib osteoclast     Salmon calcitonin btr thn human                 Nausea, swollen hands,           Acute hypercalcemia,              Intermittent    SubQ, IM,
                                                 actvty & inc Ca2+ dep in bone                                                            urticaria                        Osteoporosis, Paget's             admin           nasal spray

Aspirin                     NSAID (salicylate)   Acetylates and inactvts COX (irrev)>dec Inc alveolar vent; dec inc of colorectal ca;     GI ulceration, epig distress,    Anti-inflamm, analgesic,          Low: 60-80mg/d Oral, topical
                                                 prostgldns                              topical applcns                                  hemorrhage, renal                antipyretic, respiratory, anti-
                                                 (-)TxA2 in plts                         Contra: peds w/ fvr due to virus (Reye's         dysfnct>water, salt retn         coag, gout
                                                                                         Synd)
Ibuprofen, Naproxen,        NSAID (Propionic     Rev & non-sel inhib COX                 Nap: 20x more ptnt than Aspirin                  Less svr GI eff                   Pain, inflamm                    Oxa: 1x/d dose Flu: oral,
Ketoprofen, Flubiprofen,    acid der)                                                    Ket: inhib lipoxygenase                          Peptic ulcer, liver/kidney injury Oxa: gout                                       topical (eye)
Oxaprozin

Indomethacin, Sulindac,     NSAID (Acetic acid   Rev & non-sel inhib COX                  Dic: Mst ptnt; res for svr inflam condish                                        Ind: patent ductus arteriosis,                    Oral, topical
Etodolac, Diclofenac,       der)                                                          Severe inflamm disorders                                                         gout                                              Ker: parenteral
Kerorolac                                                                                                                                                                  Sul: familial adenomatous
                                                                                                                                                                           polyposis
                                                                                                                                                                           Arthritis, pain
Acetaminophen               NSAID                Little eff on COX                        Anti-inflamm aff insig                          Renal                            Mild pain, fever
                                                                                          Safe for pts w/ fvr caused by viral infctn      OD=liver injury (antidote-N-
                                                                                                                                          acetylcysteine)
Celecoxib               COX-2 inhibitor    Sel for COX-2                              Red GI adv eff                                 CV risk (thrombogenicity)         Inflamm, fever, pain, arthritis,
                                           No anti-plt actns                                                                                                           primary dysmenorrhea

Etanercept, Infliximab, DMARDs (cytokine   Interrupt the inflamm process by                                                          Infctn due to imm supp            Arthritis, RA, Crohn's                             SubQ
Adalimumab (TNF-alpha); Inhibitors)        neutralizing cytokines                                                                    Inc risk of lymphoma
Anakinra (IL-1)

Abatacept               DMARDs (T-cell     Costim modulator that inhibs T cell        Contra: w/ TNF-alpha inhibs                    Infctn, hypersensitivity          RA that is refractory to                           IV
                        Inhibitor)         actvn>apoptosis                                                                                                             methotrexate or TNF-alpha
                                                                                                                                                                       inhibs
Rituximab               DMARDs (B cell     Depletes circulating B cells                                                              Infusion related rxns             RA refractory to TNF-alpha                         IV
                        inhibitor)                                                                                                                                     inhibs
Glucocorticoids                            Indctn of annexin 1> (-) fmn PGs           Contra: ht ds, diabetes, infctn, osteoporosis, Cushing's, htn, h-glycemia,       Inflamm, adrenal insuff,     Low
                                           Inhib of cytokine txn                      psychoses                                      infctn, peptic ulcer,             Cushing's, autoimm, Ca, Resp
                                           Inhib of COX-1 gene xpsn                                                                  osteoporosis, cataracts,          distress, dermatologic, gout
                                           Dec stblty mRNA                                                                           glaucoma, acute ad insuff
Methotrexate,           DMARDs             Met: dihydrofolate red inhib               Contra: pregnancy                              GI, hematologic, hepatic,         RA                                 Low
Leflunomide,                               Lef:inhib dihydroorotate dehyd             Sal: 2nd line                                  pulmonary, alopecia
Hydroxychloroquine,                                                                   Combo therapy                                  Hyd: best tolerated (lst eff)
Salfasalazine
Colchicine                                 Inhibits recruitment of inflamm cells to                                                  GI, bone marrow tox, diarrhea     Gout pts who don't tolerate        Low
                                           jts                                                                                                                         NSAIDs
Allopurinol             Uric acid syn      Inhibs xanthine oxidase>dec fmn of uric    DO NOT admin during acute attk              Drug intctn w/ anticancer            Chr gout
                        inhibitor          acid                                       Often in combo w/ colchicine/NSAID          agents
Probenecid,                                Inc exctn of uric acid                     May take in combo w/ oral Ca2+citrate or Na Urate stones in kidney, ureter       Hyperuricemia in pts w/ gout
Sulfinpyrazone                             Inhib basolat anion xchgr of prox          bicarb
                                           tubules
Pancuronium,           Non-depolarizing    Paralytic eff on sk mu                Mu b/cms instv to motor nerve impulse,              Hist rel, dec HR/BP               Muscle relaxation during           Miv: 16min      IV
Cistracurium,          (antagonists)       Actn @ mtr endplt                     Ach>mu retains sens to K+                           *Sympathomimetic, atropine,       anesthesia                         Cis: 90min
Tubocurarine,                              Binds nicotinic AChR>blks             not cross membs (consciousness mntd),               antihist, airway                                                     Roc onset: 1min
Mivacurium, Rocuronium                                                           exrtd in urine, bile
                                                                                 Ca2+ blkrs enhance eff
                                                                                 Contra: Aminoglycoside Abx
Succinylcholine         Depolarizing       Binds to AChR and opens chann>initial Mu remains depol in flaccid paralysis               Dibucaine #: tst for alt plasma   Muscle relaxation during           10-30mg: 5-     IV
                        (agonist)          ctn followd by rlxn                   Phase I: mu depol>some twitch                       cholinest                         anesthesia                         10min
                                           Rapid recovery due to cholinesterase  Phase II: prolongd admin sycc>mu repolarize         Apnea, pain, malignant
                                           met                                   (desensitizing)                                     hyperthermia, hyperkalemia
                                                                                 Contra: burn, trauma, fluid imbal, MD, sp cd        *Dantrolene
                                                                                 inj, <8yo, CHF, Anti-AChE (MG pt)

Botox                   Muscle blkr        Blkd of pre-syn Ach rel                    Toxin prod by Clostridium botulinum            Flaccid paralysis                 Spasmodic torticollis,                             Parenteral
                                           Chem denervation>mu atrophy                                                                                                 strabismus, brain injury,
                                                                                                                                                                       blepharospasm, stroke
Baclofen, Dantrolene     True Spasmolytic     Bac: Hyprpolzn thru GABA agonism           CNS depress actvty                           Sedation, resp, CV, seizure w/   Cerebral palsy, MS, Stroke,   Bac: 5mg/d @     Oral,
                                              (inhib NT)>red excitability of alpha-mns   Liver fnct test                              abrupt w/d                       Paralysis                     night            intrathecal,
                                              Dan: acts dir on mu>inhib Ca2+ seq in      *Mu rlxnts used in combo w/ NSAIDs,          Weakness                         Dan: malig hyperthermia       Dan: 25mg/d      pump
                                              SR (exctn-ctn coup)                        Acetaminophen, Codeine, Steroids

Tizanidine               Alpha2 andrenergic Inhib rel of excitatory aas in sp           Inc presyn inhib                              Hpotn, hepatotox, sedation,     Spasticity in sp cd & MS
                         agonist            cd>facilitates actn of glycine              Contra: renal dz                              hallucination, dry mouth, dizzy CNS ds
                                                                                        Intctns: oral contracep, alc, antihtn
Diazepam                 Benzodiazepine       GABA recep in CNS: hyprpol neurons        Mu rlxn by sedative effs                      Sedation, cognitibe              Spasticity                    2mg bid or 5mg
                                              (inc CI curr; inhib)                      Met to actv cmpd by liver                     impairment, possibility for                                    @ bed
                                                                                        Abrupt cessation>w/d Sx>seizure               dpdnc
Gabapentin               Antiepileptic        GABAergic actvty>bind recep in            Not metabolized>dec drug inctns (add-on                                        Seizures, chr low bk pain     3600mg/d
                                              neocortex & hippocampus                   drug)
Carosoprodol,            Centrally actng Mu   Does not dir act dir on sk mu             Adjunct to rest & PT                          Sedation, vertigo, orthostatic   Musculosk inj, pain           Sht trm
Chlorzoxazone (Parafon   Rlxnt                Chl: inhib multisyn rflx arcs>sp cd areas Sedative props pvd mu rlxn                    hpotn, tachycard, GI
forte)                                                                                                                                Chl: mild

Cyclobenzaprine,         Centrally actng Mu   Cyc: Rel to tricyclic antideps             Adjunct to rest & PT                         Sedation, vertigo                Musculosk inj, pain           Sht trm
Methocarbamol            Rlxnt                Gen CNS dep                                Cyc: Ineff in mu spsm CNS ds; may intract w/ Anticholinergic eff
                                              Not act at nm jctn or dir on sk mu         MAOIs

								
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