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					       Name                                 MOA                               Therapeutic Uses                     Adverse Effects                           Other
Sulfonamides            Bacteriostatic; competes w/ PABA which          UTI (E. coli); any gram (+)      In acid urine = crystaluria;         Triple Sulfonamide = sulfadiazine,
                        is necessary for folic acid; no purines,        (-), cocci or bacilli            hypersensitivity; acute hemo.        sulfamerazine, sulfamethazine: less
                        thymine, amino acids; poorly soluble in                                          anemia if lack G6PDH; shock like     crystaluria; Resist. via 1) dec.
                        H2O; rapidly absorbed by duodenum; peak                                          symptoms; GI, hepatitis; CNS;        permeability, 2) dec. affinity for
                        3-4 hrs., DOA 2-3 days; acetylated deriv.                                        long term can greatly reduce bact.   sulfonamide, 3) PABA production
                        protein bound; 90% excreted by kidneys                                           pop. of bowel = Vit. K deficiency,   inc. to out compete; long acting 
                                                                                                         neonates = kernicterus;              StevenJohnson Syndrome
                                                                                                         hypoglycemia; easier to
                                                                                                         anesthetize; inc. phenytoin t1/2;
                                                                                                         teratogenic
Prontosil
Sulfanilamide
Sulfadiazine            Short Acting; liquid suspension                 widely used; oral
Sulfisoxazole           Short Acting                                    UTI; topical eye, nose, ear,
                                                                        vagina
Mefenide                Topical; differ in that they are a-amino-p-     chronic burn lesions                                                  Topical normally bad b/c blocked
                        toluensulfonamides                                                                                                    by pus & risk allergic sensitization
Succinylsulfathiazole   Decrease gut flora                              ulcerative colitis; bacilliary
                                                                        dysentary
                                                                        bowel sterilization
Salicylazosufa-         Decrease gut flora                              Ditto
pyridine
Sulfamethoxazole        Intermediate Acting                                                              Crystaluria more likely              Like sulfisoxazole
Folic Acid Antag.       XXXXXXXXXXXXXXXXXXXXXXX                         XXXXXXXXXXXXXXX                  XXXXXXXXXXXXXXXXXXX                  XXXXXXXXXXXXXXXXXXX
Trimethoprim            Inhibits dihydrofolate reductase; psedo-                                         Excess = N/V                         Resist. by inc. folate reductase
                        irreversible
Trimethoprim –          Well absorbed orally; long t1/2; excreted       UTI, otitis media, chronic       Combination of the two               Synergistic Effects
sulfamethoxazole        in urine; sulfa. clr. inc. in alkalinization,   bronchitis, Shigella,
(Septra or Bactrim)     trimeth. inc. clr. in acid                      Pneumo.
DNA Syn. Inhib.         XXXXXXXXXXXXXXXXXXXXXXX                         XXXXXXXXXXXXXXX                  XXXXXXXXXXXXXXXXXXX                  XXXXXXXXXXXXXXXXXXX
Quinolones              Inhibit Gyrase DNA supercoiling; oral;                                           Nausea, abdominal discomfort,
                        wide distrib.; most excreted in urin                                             headache, dizziness;
                        unchanged, hepatic metabolisim                                                   Contraindicted in pregnant and
                                                                                                         children
Norfloxacin                                                             UTI & bact. infect.
Ciprofloxacin                                                           UTI & prostatitis, bone &
                                                                        soft tissue infect by Staph. +
                                                                        Gram (-)
Nalidixic Acid                                                          UTI
Cinoxacin                                                               UTI
Ofloxacin                                                               Same As Cipro.
Levofloxacin                                                            Same As Cipro.
Nitrofuratoin                                                           Prevent & treat UTI              A/N/V, neuropathy, hemolytic
                                                                                                         anemia
Gen. Anesthetics        XXXXXXXXXXXXXXXXXXXXXXX                         XXXXXXXXXXXXXXX                  XXXXXXXXXXXXXXXXXXX                  XXXXXXXXXXXXXXXXXXX
Nitrous Oxide           Inhalation (gaseous); low sol.; low pot.;       Dental Procedures; very          Little Cardio.; slight resp.
                                                                        good analgesic                   depression; diffusion hypoxia



                                                             Pharmacology / Block III / Duc H. Vu / p. 1
Halothane           Inhalation (volatile); more potent & sol.,    Poor analgesic & muscle       Depresses ht. rate, vasc. tone, CO,
                    fluorinated compds. inc. stability; potency   relax.                        BP, cerbrovasc. resist, vebtilation,
                    inc. with more halogens                                                     saliva; liver toxicity
Desflurane          Inhalation (volatile); analog of isoflurane                                 Modest Cardio. and Resp.
                    w/one more fluorinelow sol.; pot.                                          depression
                    decreased
Thiopental          IV; Barbituate; very lipophilicvery                                        Cardio & Resp. depression
                    potent
Etomidate           IV; ultrashort onset & duration                                             Modest Cardio.; N/V
Midazolam           IV; Benzidiazepines; H2O soluble; lipid       Achieve anesthesia, &
                    sol. @ blood pH, poor analgesia; t1/2 2-4     induction, premed.,
                    hrs.                                          intraoperative sedation
Fentanyl            IV, Opioids                                   Sole or analgesic             Resp. depression, dec. BP; long        Releives anxiety & suppress cough
                                                                  supplement                    emergence time, N/V
Ketamine            IV                                            Dissociative anesthetic,      Inc. BP, CO, intraocular pressure;
                                                                  Rapid Induc.; marked          nightmare & hallucinations in
                                                                  amalgesic                     adults, children less side effects
Diazepam            Preanesthetic; not H2O sol., Antianxiety      Same As Midazolam
Hydroxyzine         Preanesthetic; Antihistamine; sedation,       Antianxiety
                    bronchodil., anti-emetic, anti-muscarenic
Meperidine          Preanesthetic, Opioid                         Releive anxiety; inhibit
                                                                  cough reflex
Morphine            Preanesthetic; Less halothane = less                                        Resp. depression
                    cadiac depression, opioid
Atropine            Preanesthetic; stop secretions, dec.
                    bradycardia; antmuscarinic
Succinycholine      Adjunctive; neuromuscular blocker             skeletal muscle blocker
d-tubocurarine      Adjunctive; neuromuscular blocker             skeletal muscle blocker
Trimethaphan        Adjunctive; ganglionic blocker                reduces bleeding              hypotension
Local Anesthetics   Block nerve conduction; bind to                                             Numbness of tongue, oral, light        lipohilic, intermediate, ionizable
                    intracellular Na pore; time & voltage dep.                                  head, tinnitus, nystagmus, dizzy,      group, intermediate = ester or
                    fashion; higher affintiy for in/activated;                                  convulsion; higher doses CNS           amide; ester metabolized by
                    weak bases, uncharged enters cell; smaller                                  depression; ester allergies b/c        plasma butrycholinesterase, liver
                    more lipophilic faster interaction; B>C>A                                   PABA derivatives from metab.           esterase, short t1/2; amide cleared
                    delta>A gamma; pain then sensory                                                                                   by hepatic metab.; vasoconstrictors
                                                                                                                                       prolong


Procaine            Short; prototype ester, plasma esterase;      infiltration & nerve block;   hypersensitivity                       PABA allergic rxn.  don’t put on
                    poorly absobed via mucous mem. must           spinal anesthesia                                                    skin
                    inject
Chloroprocaine      Short t1/2; least toxic; ester                no systemic absorption        contraindicated for IV block           Can cause thrombosis
Tetracaine          Long t1/2; ester                              topical (eye, skin, mucous)
                                                                  or spinal
Cocaine             CNS stimulant; ester                          Surface anesthesia of Resp.   tonic clonic seizure; tachy., HTN,     Sympathomimetic; only one to
                                                                  tract, no eye                 arrythmias, cardiac failure, pyrexia   block catecholamine uptake =
                                                                                                                                       tachy & vasoconst.
Benzocaine          Ester                                         topical in creams &
                                                                  ointment; burns

                                                      Pharmacology / Block III / Duc H. Vu / p. 2
Lidocaine        Amidepromt, intense, long acting,             All routes except eyes
                 extensive anesthesia; absobded form
                 mucous; Metab. = liver enzymes; good for
                 IV b/c no thrombosis; Intermediate
Bupivacaine      Long duration of action                        infiltration, nerve block,
                                                                spinal, epidural; More toxic,
                                                                but binds to mom’s protein
                                                                 no baby
Epinephrine      Vasoconstrictors
Norepinephrine   Vasoconstrictors
Phenylephrine    Vasoconstrictors
Vasopressin      Vasoconstrictors
Acute Headache   XXXXXXXXXXXXXXXXXXXXXXX                        XXXXXXXXXXXXXXX                 XXXXXXXXXXXXXXXXXXX                   XXXXXXXXXXXXXXXXXXX
Ergotamine       Sublingually; 5-HT1, 5-HT2,  1 & 2,           Migrane & Clusters              N/V, paresthesis of extremities,      Absorption in GI slow &
                 &D2 receptor agonist; anti-migrane effect                                      myalgia, angina like; chronic =       incomplete; caffiene inc. rate of
                 @ 5-HT1B & 1D; vasconstrictor of ateries                                       endarteritis, thrombosis, ischemia,   abs.; 97% 1st pass; sequestered in
                 and veins; restores blood to brain                                             gangrene; dependency; contra. –       various tissue
                 parenchyma, blocks release of                                                  pregnant, vasc. disease, ulcer
                 proinflammatory neurotrans.
Sumatriptan      5-HT1 agonist; subcutaneous or oral, 5-HT      Migrane & Clusters              pain @ inject. site; rebound
                 1B & 1D, restores blood to brain                                               headache; no IV b/c vasospasms
                 parenchyma, blocks release of
                 proinflammatory neurotrans.
Isometheptene    Sympathomimetic vasoconstrictor, better                                        Sleepy, dizzy, palpitations, contra
                 tolerated than ergotamine                                                      – HTN, ht. & vascular disease
Acetominophen                                                   All Headaches
Naproxen                                                        All Headaches

Prophylactic     XXXXXXXXXXXXXXXXXXXXXXX                        XXXXXXXXXXXXXXX                 XXXXXXXXXXXXXXXXXXX                   XXXXXXXXXXXXXXXXXXX
Methysergide     Taken several times daily for effect; 5-HT     Migrane & Clusters              fibrosis in pleropulmonary and
                 antagonist & vasodilator                                                       cardiac, angina, peripheral vasc.
                                                                                                insufficiency, CNS, GI effects
Propanalol       Prevents catecholamine induced lypolysis       Migrane                         Na intake inc. serum conc. and
                 = dec. prostaglandin synthesis                                                 toxicity
Lithium          Efficacy restored after 2 wk. holiday          Drug of choice for chronic
                                                                cluster
Amitriptylene    Inhibit Reuptake of NE & Serotonin             Migrane & Tension
Penicillin       Competitively inhibits transpeptidatin rxn;                                    Penicillamine – cooper chealator      -lactam attaches to Penicillin BP,
                 resembles D-alany-D-alanine; also effect                                       (Wilson’s disease); Peniloic acid     cell wall synthesis inhib. by
                 penicillin BP, cause loss of an inhibitor of                                   becomes a haptene; if too much in     blocking transpeptidase, autolytic
                 autolysin; poorly penetrates BBB unless                                        CNS can cause epilepsy; 10-15%        enzymes are activated;
                 meninegies are inflammed                                                       hypersensitive (Immediate,            w/chlorotetracycline antagonoize
                                                                                                accelerated, delayed)                 bactericidal
Amoxicillin                                                                                                                           Amoxicllin-clavulanic – orla
                                                                                                                                      treatment of ottitis, sinusitis, lower
                                                                                                                                      RT, UTI; DOC for human or
                                                                                                                                      animal bite
Ampicillin       DOC for L. Monocytogenes; inactivated by       Gram (+); & some gram (-)       Skin rash, GI, Monilial overgrowth    w/clavulinic; don’t use w/ oral
                 penicilinase; renal excretion                  = Hemophilus, Salmonella                                              contraceptive
Azlocillin                                                      10X more active than
                                                    Pharmacology / Block III / Duc H. Vu / p. 3
                                                                Carbenicillin
Carbenicillin   @ high dose, bactericidal against P.            UTI, bacteremias caused by     w/Gentamicin = bilogically           Combo w/gentamicin  resist.;
                aerginosa; less active against gram (+)         P. aerginosa                   incative amides                      Carb indanyl acid stable  oral
Cloxacillin
Methicillin     Renal excretion blocked by probenecid;          Gram (+) only                  Hematuria, neutropenia; higer        Resistance carried on plasmid
                diffuses poorly into brain                                                     incidence of nephrotoxicity
Mezlocillin                                                     Klebisella and Psedomonas
Nafcillin       Similar to Methicillin
Oxaxillin       Similar to Methicillin
Penicilin G     Short t1/2 b/c cleared by both glomerular                                                                           Acid labile, destroyed by lactaase,
                and tubular filtration (weak acid); cleared                                                                         narrow spect., rapidly excreted,
                in 1 pass                                                                                                           poor tissue penetration
Pencillin V                                                                                                                         Oxygen added to side chain to
                                                                                                                                    increase acid stability
Piperacilin                                                     Klebisella and Psedomonas
Ticarcillin     Similar to carbenicillin                        2 – 4X more active aginst P.                                        w/clavulanic
                                                                aerginosa
Carbapenem      Broad spectrum; include Pseudomonas,
                Acinetobacter, anerobic bact.
Monobactams     Monocycli beta lactam rings, resist beta                                       Superinfections w/ staph. and
                lactamase, active agianst gram (-) rods                                        enterococci may occur
Cycloserine     Inhibits the racemase that cinverts L-
                alanine to D-alanine
Vancomycin      Bactericidal; inhibits cell wall synthesis by   Severe Satph. aureus infect.   Ototoxicity, phlebitis, pain @       Renal excretion
                inhibiting peptidoglycan synthesis                                             inject site
Bacitracin      Polypeptide inhibits cell wall syn. by          Topical admin. of staph        Nephrotoxicity, eosinophilia         Intrathecal or intrapleural for
                interfering w/peptide-polysacharide form.;      infect., gram (+) rods                                              staph. meningitis or empymea
                not absorbed from gut
Polymyxin B     disorients protein & lipid components;          topical for gram (-); 1       Paresthesia, hyperesthesia, ataxia
                does not pass BBB; not absorbed well            pseudomonas
                form gut; excreted via kidneys
Colistin        Similar to polymixin B; rapid renal             Gram (-)                       Circumoral paresthesias, slurred
                excretion;                                                                     speech, visual, nephrotoxicity
Cephalosporin   Stops cell wall form. (Blocks                   Gram (+), Gram (-)             nephrotoxic; hypersen.; can cross    relatively resist. to lactamase;
                trtanspeptidase (cross linking)); Oral;                                        react w/ penicillin                  probenecid slows excretion
                crosses placenta, some BBB; renal
                excretion
First Gen.      Can’t cross BBB
Cefadroxil      Oral                                                                                                                Most lactamase resist.
Cefazolin       Gram (-)                                        Surgical prophylaxis
Cephalexin      Oral
Cephalothin                                                     Endocarditis                   Nephrotoxic
Second Gen.     Cross BBB                                                                                                           Better against Gram (-)
Cefaclor        Oral
Cefamandole                                                     Gram +, gram -, anaerobes      Inhibits Vit. K; disulfram like
Cefoxitin       Anaerobes
Cefluroxime                                                     Meningitis
Third Gen.      Cross BBB                                                                                                           Great gram (-); bad gram (+)
Cefixime        Oral
Cefoperazone                                                                                   Inhibits Vit. K; Disulfram like      No longer used
                                                    Pharmacology / Block III / Duc H. Vu / p. 4
Cefotaxime                                                          Gram (-)
Fourth Gen.           Can Cross BBB
Cefepime              Excelent pentration into CSF                                                                                         Stble to plasmid encoded
                                                                                                                                           lactamase, but not to extended-
                                                                                                                                           spectrum lactamase
Protein Syn. Inhib.   XXXXXXXXXXXXXXXXXXXXXXXX                      XXXXXXXXXXXXXXXX                XXXXXXXXXXXXXXXXXXX                    XXXXXXXXXXXXXXXXXXX
                      XXXXXXXXXXXXXXXXXXXXXXXX                      XXXXXXXXXXXXXX                  XXXXXXXXXXXXXXXXXXX                    XXXXXXXXXXXXXXXXXXX
Erythromycin          Macrolide; binds 50S, blocks                  Gram (+), & N.                  Hypersensitivity, liver obstruction;   Gram (-) org. do not admit erythro.
                      translocation; bacteriostatic; adsorbed GI,   menengitidis, ghonerrhoeae,     hepatic tox.                           into cell wall; inc. pH can treat E.
                      inactivated by acid; excreted in feces        H. influenza, pertusis;                                                coli UTI; Resist. = alter ribosome,
                                                                    syphilis, prophalactic                                                  permeability, induced resist.;
                                                                    rheumatic                                                              antag. w/Clindamycin
Clarithromycin        Macrolide                                     H. influenzae;
                                                                    mycobacterium, H. pylori
Azithromycin          Macrolide                                     Mycobac., Chlamydia                                                    toxoplasmosi enceph. in AIDS
Clindamycin           Lincosamides; binds 50S; inhibits peptidy     Gram (+), particularly strep.   Persistent diarrhea                    Erythromycin can reverse
                      transferase; passes readily into tissue,                                                                             lincosamides effects
                      poor;y CSF; liver metab.
Clindamycin                                                         DOC for anaerobes
phosphate
Tetracycline          Bacteriostatic; inhibit protein synthesis,    Gram (+) & (-); rickettsiae,    Chelating abilities = adverse          Resist. via R factors, primarily seen
                      bind to 30S, prevent attchment at A site;     some fungal & parasitic         effects; hyper, photosensitive,        in gram (-); gram (-) cross resist to
                      glomerular filtrationl; feces                                                 liver, renal damage, vestib.,          chloramphenicol, not (+)
                                                                                                    discolor teeth, depression of bone
                                                                                                    growth
Minocycline           2X a day
Doxycycline           2X a day                                      Extrarenal infect.
Chloramphenicol       Broad spectrum bacteriostatic; binds to       DOC only for Salmonella         Bone marrow toxicity, aplastic         Resist. via acetylation
                      50S, depresses peptidytransferase; oral,      typhosa                         anemia, GI, superinfection, gray
                      hepatic metab. rapid; good NS                                                 baby – die of acute vasc. collapse
Streptomycin          Aminoglycosides; inhibit protein              Miliary Tb, pylonepritis,       8th cranial nerve, especially          Rapid resist.
                      synthesis, block energy production @ kreb     peritonitis, osteomylistis,     vestibular; may cause clinical
                      cycle; more basci 10-80 fold inc.; inhibits   plague,tuleremia,               menengitis; neuromuscualr blocker
                      bindng of f-met; incorporates of wrong        brucellosis                     (curare like effects); skin rashes,
                      amno acids; high conc. bactcidal, low                                         renal damage
                      static; binds irreversibly to P10 on 30S,
                      IM, no CSF
Neomycin              Aminoglycosides; orally for GI or topical     Shigella, Klebsiella; bowel     Disturbs normal flora; nephrotox,
                                                                    sterilization; gram (+) (-)     ototox.; Ulcer; curare like effect
Gentamycin            Aminoglycosides; renal excretion, more        Klebsiella, proteus, pseudo.    Nephro., oto. (vestibular), rapid
                      active basic pH                                                               resist.
Tobramycin            Aminoglycosides                               Gram (-) bacilli
Amikacin              Aminoglycosides                               those resist. to Gentamycin
                                                                    & tobramycin
Viomycin              Aminoglycosides; weak Tbstatic                2nd line drug for Tb.
Spectinomycin         Aminoglycosides; inhibits protein syn,        Acute gonococal urthrits,       fever, skin rash
                      binds to 30S; IM inject.                      procitis, cervicits from N.
                                                                    gonorrhoea
Netilmicin            Aminoglycosides                               Gram (-) bacilli                Some ototox., and nephrotox.           Resist. to aminoglycoside
                                                                                                                                           inactivating enzyme
Antifungal
                                                         Pharmacology / Block III / Duc H. Vu / p. 5
Nystatin            Punches holes iby reorientation of sterol;      Candida infect of skin,          Can affect amalian RBS &
                    Topical; poor GI                                mucous mem., intestinal          lysosomal membranes; systemic =
                                                                    tract                            hemolytica nemia, kideny damage
Amphotericin B      IV; similar to Nystatin, poor GI absorbtion     Deep fungal disease (bone        Mamalian cells are effected;
                                                                    infect., meningitis, pneumo.,    headache, anemia, hepatic failure
                                                                    disseminated)
Ketoconazole        Oral; broad spectrum                            Systemic fungal; DOC for         Nauseas prurits, gynecomastoia,
                                                                    chronic mucocutaneous            hepatittis
                                                                    candidiasis
Flucytosine         Must be deaminated to 5-flurouracil;            C. albicans                      Tox. low, may cause bone marrow     Resist. high; potetntiation w/
                    incorporate dinto mRNA in place of uracil;                                       depression                          amphotericin B
                    demaination by fungis
Griseofulvin        Org. must be growing; uptake of drug id         Microsporum, Trichophyton        headache
                    energy dependent; adsorbtion inc. w/fatty       Epidermophyton; athelet’s
                    meal; grud bound to keratin; relies on          foot
                    turnover; only stops growth, doesn’t kill
Miconazole                                                          Tinea pedis, cruris,                                                 Vulvovaginal cndidiasis
                                                                    vesicolor
Fluconazole                                                         Oral & esophageal                                                    May have effect on cryptococal
                                                                    candidiasis in AIDS                                                  meningitis
Undecylenic Acid    Fatty acid possesing antifungal activity        Tinea pedis
Tolnaftate                                                          Wider spectrum of                                                    Ideal for Tricophyton rubrum
                                                                    dermatophytic infect.
Terbinafine         Inhibitor of squalene epoxidase; blocks         Trichophyton,                    Diarrhea, headache, dyspepsia;
                    necessary copmponent of ergosterol; oral        Epidermophyton,                  changes in taste patterns
                    or topically; t1/2 16 days; liver metab. &      Microsproum
                    real excretion
Anitiviral Agents
Amantadine HCL      Prevents viral uncaoting; completely            Prophalaxis of influenza         Nervousness, insomnia, dizzy;
                    adsorbed in GI; excreted by kidneys                                              bascially CNS, some GI
Idoxuridine         Inhibit DNA synthesis (DNA Polymerase);         Herpetic keratitis, herpes       Iritation, itching, photophobia,    Prodrug, No effect against RNA
                    rapidly inactivated by liver; IV or topical     virus; only approved for         marrow aplasia, hepatic             viruses
                                                                    infect. of eyelid, conjuntiva,   degradation
                                                                    cornea
Vidarabine          Inhibits DNA Polymerase; topical or IV          Topical opthalmic; herpes        CNS, teratogenic, opthamology
                    (causes deamination to lesser ptoent);          simplex 1 & 2; keratitis         problems
                    kidney excretion                                caused by herpes
Interferon          Endogenous glycoproteins                        Cytomegalovirus, herpes,         Headaches, weakness, fatigue,
                                                                    hep. B, C, genital warts         anemia, GI
Acyclovir           Inhibits replication of herpes 1,2, varicella   Topica use fo herpes             Headache, vomiting, renal           Safe
                    zoster, epstein barr; after triphosphate        simplex; herpes simplex          dysfunction
                    conversion – interferes w/ DNA                  encephalitis
                    polymerase; kidney excretion
Ganciclovir         Inhibits viral DNA polymerase                   Cytomegalovirus                  Leukopenis, neutropenia, seizures
Ribavirin           Inhibits viral MRNA & viral polymerase;         Infabts & children w/ severe     Death, decreased pul. & cardio.
                    administered as aerosol                         lower RTI                        function
Trifluridine        Inhibits viral DNA synthesis; topical only      Epitheleal keratitis             Palpebral edema
Zidovuldine         AZT inhibits RNA dependent DNA                                                   granulocytopenia, anemia,
                    polymerase, causing chain termination                                            headache, nausea
Didanosine                                                          Adult pts. w/ advanced HIV       Pancreatitis & peripheral neurop.
Foscarnet           Inhibits Rna polymerase & Reerse                CMV retinitis (IV)               Hypocalcemia, hypomagnesemia
                                                        Pharmacology / Block III / Duc H. Vu / p. 6
                      transcriptase; deposited in bone; renal
                      excretion
Anti – Tb.            XXXXXXXXXXXXXXXXXXXXXXXX                      XXXXXXXXXXXXXXX               XXXXXXXXXXXXXXXXXXX                   XXXXXXXXXXXXXXXXXXX
Isoniazid             Bactericidal; Inhibits carbohydrate           Antituberculosis              Resist. quick; pyridoxine def. In     Resist. - Mutants lack catalases &
                      metabolisim; inhibit glycolysis; specefic                                   slow acetylators; uses can lead to    peroxidases, break hydrazide, inc.
                      for myobact.; oral; acetylation in liver by                                 anticonvulsant tox.; peripheral       syn. of mycolic acids
                      N-acetyltransferase; exreted in urine                                       neuropathy, hep. tox.
Ethambutol            Interfere w/ RNA syn.; GI; urine excretion,   1 anti-Tb. drug              Reversible optic neuritis, allergic
                      partially oxidized                                                          rxns.
Streptomycin 2nd      Secondary antibiotics                                                       More toxic
Rifampin              Inhibits DNA-dep. RNA syn. (interfer.         Tb. & gram (+); may inhibit   Very low; Contra. W/ oral             Produced by Strep. Mediterranei;
                      w/RNA polymerase); effects core enzyme        certain viruses               contraceptives                        urine excretion; 1 eleminated in
                      B                                                                                                                 bile; liver deacylates but still active
Pyrazinamide          Oral                                          Tb.                           Liver damage; uric acid retention
Antileprosy           XXXXXXXXXXXXXXXXXXXXXXXX                      XXXXXXXXXXXXXXX               XXXXXXXXXXXXXXXXXXX                   XXXXXXXXXXXXXXXXXXX
Dapsone               GI; enterohepatic circ. delays excretion      Longe term leprosy            GI; blood dyscarisis
Clofazimine           Substitue for sulfones
Amithiozone           Substitue for sulfones                        > effect on tb. form                                                Resist. after 2nd year
Thalidomide                                                         Leprosy                       teratogenic
Ethionamide
Antiviral             XXXXXXXXXXXXXXXXXXXXXXXX                      XXXXXXXXXXXXXXX               XXXXXXXXXXXXXXXXXXX                   XXXXXXXXXXXXXXXXXXX
Rev. Trans. Inhib     XXXXXXXXXXXXXXXXXXXXXXXX                      XXXXXXXXXXXXXXX               XXXXXXXXXXXXXXXXXXX                   XXXXXXXXXXXXXXXXXXX
Nucleoside analog     Prodrug; Oral; 2-3 doses; kidney                                            Early resist.; cross resist.
                      excretion; comp. inhib. of enzyme
Abacavir              Liver metab.; renal excretion; CNS pen.       Combo. w/ AZT                 hypersensitivity
                      good
Didanosine (ddI)      Renal elim.; poor CNS                         Combo AZT or d4T              Pancreatitis, peripheral neuro        Gastric acidity slows adsorption
Lamivudine            Renal elim.; poor CNS                         Combo AZT or d4T              Pancreatitis in children
Stavudine (d4T)       okay CNS                                      DO Not combo w/ AZT           Peripheral neuro.
                                                                    (b/c slows activation)
Zalcitabine           Renal elim.; poor CNS                         Peripheral neuro.
azidodeoxythymidine   Meatb. liver; renal elim.; good CNS (60%)                                   Marrow suppression, myopathy,
                                                                                                  hepatitis
Non-nucleoside        Oral; already active; renal elim.; poor                                     Inhib. P450
                      CNS; non-comp. inhib.
Delaviridine          Liver; renal; CNS 0%                          Combo Nucleoside RTI          Rashe, headache                       Inhibits P450
Nevirapine            CNS 45%                                       Ditto                         Ditto                                 Ditto
Efavirenz             QD                                            Ditto                         Dizziness                             Ditto
Nucleotide Analo.     XXXXXXXXXXXXXXXXXXXXXXXX                      XXXXXXXXXXXXXXX               XXXXXXXXXXXXXXXXXXX                   XXXXXXXXXXXXXXXXXXX
Hydroxyurea           Integrase Inhib.                              Use w/ ddI                    Bone marrow supp.; renal failure      Salvage Therapy
Protease              CNS poor; Inhibits final enzymatic step       combo w/ RTI                  Lipididistrophy; Inhib. P450
Inhibibitors
Saquinavir            Poor CNS; tid                                 Combo w/ RTI                  GI intolerance; transaminase inc.     Contra. w/ Cisapride
Nelfinavir            tid; moderate CNS                                                           Diarrhea
Ritonavir             poor CNS                                                                    GI; paresthesia                       dec. AZT levels
Indinavir             Taken w/ low fat meal; biliary metabolism;    Combo w/ RTI                  Diabetes, lipidostrophy, nephrotox.
                      moderate CNS
Malaria
Chloroquine           Erythrocytic Forms; inhib. necleic acid       Blood schizonticide           Ocular toxicity                       Does not prevent relapse of P.
                      syn. in dividing cells; paracitized eryth.                                                                        vivax, malariae, ovale
                                                         Pharmacology / Block III / Duc H. Vu / p. 7
                     concentrate drug
Mefloquine           Erythrocytic Forms;                                                                                                 Contra. epilepsy, psyc., cardiac
Hydroxchloroquine    Erythrocytic Forms;                             Used instead of chloroquine
Quinine              Erythrocytic Forms; binds to DNA;                                             Cinchonism – efeects 8th nerve =
                     inhib. plasmoial parasites; suppress                                          disurb vission, deafness, vertigo;
                     oxidative process                                                             black water fever
Primaquine           Exo-erythrocytic forms; binds to DNA            P. vivax & faciform           GI, headache, prurtis, lekopenia;
                                                                                                   anemia
Chloroquinide        Erythro & exo-erythro.; Inhib.                  P. falciform & sporozoites    Macrocytic normochromic anemia
                     dyhdrofolate (interfere w/ folic acid); slow                                  w/ megaloblastic bone marrow
                     acting;
Pyrimethamine        Ditto                                                                         Ditto
Trimethoprim         Ditto                                                                         Ditto
DDS                  Analogs of PABA  comp. inhib. folic a.                                       GI, dermatologic, hemolytic effects
                                                                                                   w/ G-6-P-D deficiency
Sulfa Drugs          Ditto                                                                         Ditto
Bactrim              combo of trimeth & sulfa
Amebicides           XXXXXXXXXXXXXXXXXXXXXXXX                        XXXXXXXXXXXXXXX               XXXXXXXXXXXXXXXXXXX                   XXXXXXXXXXXXXXXXXXX
Metronidazole                                                        DOC for amebiasis; trich.;    disulfuram effects;l metallic taste
                                                                     leish.; giardiasis
Iodoquinol           Direct Luminal amebicide; minimal gut           DOC asymptomatic of mild      GI, malaise, thyroid enalrgement      Contra. renal, thyroid disease
                     asorbtion                                       intestinal amebiasis
Diloxanide           Direct Amebicide                                Combo w/ metronidazole
Emetine              Tissue Amebicide; combo w/ chloroquine;         Bowel & liver parasites       B/c slowly excreted, myocardium       Used only if flagyl no good
                     emetine - inhibit protein syn. @                                              effects, neuromuscular
                     trophozoite stage
Dehydroemetine       Ditto                                           Ditto                         Less toxic effects
Chloroquine HCL                                                      Hepatic amebiasis             GI, renal ischemiam cardiac
Suramin sodium                                                       Onchocerca volvulus           Anemia; GI
Pentamidine                                                          DOC in combo w/Bactrim        Rapid hypotension
                                                                     for P. carinii in AIDS pts.
Quinacrine           Intercalates w/ DNA                             Giardiasis                    GI, exfoliative derm., dyscraciasis
Antihelmintics       XXXXXXXXXXXXXXXXXXXXXXXX                        XXXXXXXXXXXXXXX               XXXXXXXXXXXXXXXXXXX                   XXXXXXXXXXXXXXXXXXX
Piperazine citrate   Blocks chloinergic myyoneural junc. =           Ascariasis, enterobiasis      Exascerbation of seizures
                     paralysis = expulsion
Thiabendazole        Effects uncapsulated form                       Strongylodies stercoralis     drowsiness, headache                  Pork Worm
Mebendazole          Gut; liver metab.; kidney elim.; impairs        Trichuris trichuria           GI
                     glucose uptake
Albendazole          Oral                                            Pinworm, ascariasis, trich.   GI, N/V/D
Pyrantel Pamoate                                                     Broad spectrum                GI; hepatic dysfunction
Praziquantal                                                         Trematodes                    Carcinogenicity, mutation, contra.    Ocular cysticercosis – destroy
                                                                                                   preg. & brast feeding                 parasite my impair eye
Bithionol                                                            Liver fluke worms             photosensitivity
Niclosamide          Kills scolex (causes release from gut); poor    Cestodes                      N/V/D
                     gut adsorb.
Quinacrine           Causes worm detachment                          Large tapeworms
Antineoblastic       XXXXXXXXXXXXXXXXXXXXXXXX                        XXXXXXXXXXXXXXX               XXXXXXXXXXXXXXXXXXX                   XXXXXXXXXXXXXXXXXXX
Alkylating agents    Akylate nucleic acids & proteins; lipid sol.;                                 Resist. = dec. drug uptake; E.coli
                     Immonium ion intemediate is highyly                                           can excise cross link
                     reactive on both side chains
                                                        Pharmacology / Block III / Duc H. Vu / p. 8
Mechlorethamine        Nitrogen Mustard; form carbonium ions                                          N/V; severe vesicant
                       which form covalent linkages; IV; rapid
Chlorambucil           Distributed to site before activated; oral                                                                          Slow conversion to carbonium ion
Cyclophosphamide       Nitrogen Mustard; form carbonium ions                                          N/V; alopecia; hemoragic cystitis
                       wqhich form covalent linkages; prodrug
Ifosfamide
Melphalan              Distributed to site before activated, oral
Trethylene
thiophosphoramide
Busulfan               Sulfate strippers, oral; selectively           Chronic granulocytic anemia     Inc. pigmentation; pul. fibrosis
                       myelosuppressive
BCNU                   Nitrosurea; cross BBB; IV                                                      Hematopoitec, liver, kidney tox.
Procarbazine                                                          Hodgkin’s Disease
Cisplatin              Modify cancer cells; platinum ions             Testicular, ovarian, bladder,   Kidney damage                        Give w/ diuretic
                       combine w/ compds. in bact. culture to         head and neck
                       form cordination complexes that prevent
                       cell division, allows cell growth
Carboplatin            Similar to Cisplatin; large dose required




Antmetabolites         XXXXXXXXXXXXXXXXXXXXXXXX                       XXXXXXXXXXXXXXX                 XXXXXXXXXXXXXXXXXXX                  XXXXXXXXXXXXXXXXXXX
6-Mercaptopurine       Prodrug; converted intracellularly;            Antileukemic therapy            Hematoplogical - Lekopenia,          Allopurionol results in inc. purines
                       suppression of purine bosynthesis via                                          thrombocytopenia, anemia;            = gout
                       pseudofeedback inhib.; inhibits conversion                                     Anorexia; hepatic
                       of inosinic acid to adenylic & guanylic
                       acid; oral, some CNS
Azathioprine                                                          Prevention of transplant        <6-MP
                                                                      reject.; treat rhematoid and
                                                                      lupus
Fluorouracil           Prodrug; prevents dUMP to dTMP;                GI tract; female genetalia,     GI; leukopenia, thrombocytopenia     Too toxic for leukemia
                       depresses RNA syn.                             breast
Cytosine Arabinoside   Prodrug; inhibits DNA syn.; slows chain        Remission induction of          Hematological, GI
                       elongation; IV                                 acute granulocytic
                                                                      leukemias
Methotrexate           Folic acid reductase inhib.; oral              Choriocacinoma in women;        Annorexia, leukopenia, depression;   hemoragic desquamating enteritis;
                                                                      ALL                             severe psoriasis                     if OD give folinic acid
Natural Products       XXXXXXXXXXXXXXXXXXXXXXXX                       XXXXXXXXXXXXXXX                 XXXXXXXXXXXXXXXXXXX                  XXXXXXXXXXXXXXXXXXX
Vinblastine            Bind microtubular proteins; prevent            Hodgkin’s                       Bone marrow suppression
                       spindle form.
Vincristine                                                           remisison of acute leukemia     CNS TOX.
Etoposide              Block S-G2 phase; affect topoisomerase II      testicular, non-hodgkin’s;      Hematologic; alopecia; N/V/D
                                                                      ALL; breast; kaposi’s
Teniposide             Ditto                                          refractory acute                Ditto
                                                                      lympyphoblastic leukemia
Taxol                  Binds to tubulin dimers & microtubulin         Breast, ovary, lung             Mylosuppression, peripheral
                       filaments = disrupt mitosis                                                    neuropathies; cardio.
Daunorubicin           Intercalates btwn. DNA = prevent               Acute leukemia                  Bone marrow sup.; arrhytmias
                       replication; inhibits top. II
                                                              Pharmacology / Block III / Duc H. Vu / p. 9
Doxorubicin          Ditto                                          Lung, breast, bladder           Bone Marrow; CHF
Plicamycin           Binds DNA, inhibits RNA syn.                   Testicular; Padgets                                                  Lowers serum Ca
Dactinomycin         Binds DNA = no syn.                            Wilm’s; Ewing’’s sarcoma        bone marrow; lekopenina; anemia
Bleomycin            Inhi. mitosis and DNA syn.                     Ski, testicual                  Pul. fibrosis
Mitomycin            Prodrug; palative
Hormones             XXXXXXXXXXXXXXXXXXXXXXXX                       XXXXXXXXXXXXXXX                 XXXXXXXXXXXXXXXXXXX                  XXXXXXXXXXXXXXXXXXX
Progesterone                                                        Palliative metastatic
                                                                    endometrial carcinoma
Flutamide            Pharamlogical castration                       Prostatic carcinoma
Estramustine         Estrogen + alkylating agent                    Prostatic carcinoma
Leuprolide           GNRH Analog; down regulates cell-              Prostatic carcinoma
                     surface receptors of GNRH; dec. LH, FSH
                     = castration
Testosterone         Any age                                        Breaat Carcinoma
Diethylstilbestrol   DOC for estorgen therapy; post menopause       Breaat Carcinoma
Tamoxifen                                                           Breaat Carcinoma
Aminoglutethimide    Inhibits. cholesterol to pregnenolone          Breaat Carcinoma
Misc.                XXXXXXXXXXXXXXXXXXXXXXXX                       XXXXXXXXXXXXXXX                 XXXXXXXXXXXXXXXXXXX                  XXXXXXXXXXXXXXXXXXX
L-Asparaginase       Dec. L-asparg. = slowed growth                 ALL                             Liver dysfunction
Gold-198                                                            Pleral effusion, ascites, 2nd
                                                                    to cancer
Mitotane             Palliative treatment                           adrenocortical carcinoma
Sodium phosphate                                                    Polycythemia vera;
                                                                    palliative chronic
                                                                    myelocytic leukemia
Hydroxyurea          Inhibits ribonucleoside diphosphate            Chronic granulocytic            Bone marrow depression
                     reductase                                      leukemia
Procarbazine         Methylating agent                              Hodgkin’s
Herceptin            Antibody; Binds to HER2 (cell growth           Breast Cancer                   CHF; lekopenia, anemia;
                     regulator); metatstatic breast produce                                         exacerbaes infect.
                     excess HER2 receptors
Nonnarcotic          XXXXXXXXXXXXXXXXXXXXXXXX                       XXXXXXXXXXXXXXXX                XXXXXXXXXXXXXXXXXXX                  XXXXXXXXXXXXXXXXXXX
Analgesics.          XXXXXXXXXXXXXXXXXXXXXXXX                       XXXXXXXXXXXXXX                  XXXXXXXXXXXXXXXXXXX                  XXXXXXXXXXXXXXXXXXX
Aspirin              Inhibits syn. of prostaglandins &              Headache, myalgia,              resp. stimulation, high doses        Does NOT inhibit form. of
                     thromboxane; inhibit COX-1 & 2, platlet        arthralgia, antipyretic;        depression; posioning = alkalosis;   leukotrienes via lipoxegenase
                     action is irreversible; they uncople           antiinflame (COX-2);            w/ depressed resp. = acidosis;       pathway; OD w/ gastric lavage,
                     oxidative phosphorylation which inhibits       antiplatlet; dec. colorectal    dehydartion by H2O loss during       emesis; don’t use w/ warfin, MTX,
                     ATP dependent rxns. = pyrexia; CNS             cancer                          hyperventialtion; hypokalemia;      thyroid hormone; Causes reye’s
                     stimulant followed by depression; rapid                                        prostaglandin =  renal flow;        syndrome in children
                     adsorb in small intestine; highly protein                                      convulsions, hyperthermia;
                     bound; metab liver, high doses zero order,                                     hypersensitivity
                     low first order; alkalization inc. clearance
Acetamionophen       Metab. in liver; metabolites normally          Analgesic, antipyretic; NOT     Hepatic necrosis; may appear to
                     inactivated by glutathione                     antiinflamatory                 improve, but rebound
N-acetylcysteine     Inactivates toxic metabolites                  Acetaminophen tox. w/in 24
                                                                    hrs.
Nonsteroidal         XXXXXXXXXXXXXXXXXXXXXXXX                       XXXXXXXXXXXXXXXX                XXXXXXXXXXXXXXXXXXX                  XXXXXXXXXXXXXXXXXXX
Antiinflamatory      XXXXXXXXXXXXXXXXXXXXXXXX                       XXXXXXXXXXXXXX                  XXXXXXXXXXXXXXXXXXX                  XXXXXXXXXXXXXXXXXXX
Ibuprofen            Inhibits COX 1 & 2                                                             Renal impairment in elderly; blood   Contra nasal polyps, angiodema,
                                                                                                    dyscarias                            bronchospastic

                                                       Pharmacology / Block III / Duc H. Vu / p. 10
Naproxen             Long t1/2; protein bound; OTC                  Arthritis, spondylitius;       Ditto
                                                                    migrane
Piroxicam            Longest t1/2, inhibits activation of           Rheumatoid, osteo., spond.     GI, drug displacement
                     neutrophils; COX 1> COX 2
Ketorolac            Parenteral NSAID; strong analgesic; can                                                                            Don’t use obstetrical b/c inhibits
                     be oral; kidney elim.; salicylates displace                                                                        uterine contractions, closes ductus
                     drug from protein                                                                                                  arteriosis
Ketoprofen           Inhibits COX & lipoxygenase                    Rheumatoid & osteo.            GI & CNS                             Doesn’t affect warfin or digoxin
Sulindac             Prodrug; converted by liver; enterohepatic     Rheumatoid, gouty arthritis    GI; Steven Johnson,
                     cycling; COX 1 > COX 2                                                        thrombocytopenia; renal
Indomethacin         Potent prostaglandin syn. inhib; COX 1>        Arthritis, spondylitis,        Depression, memory loss;
                     COX 2; dec. leukotriene syn.                   osteoarthritis; Bartter’s      thrombocytopenia, aplastic anemia
                                                                    syndrome
Phenybutazone        Oldest most toxic NSAID; potent anti-          Acute gouty arthritis,         Agranulocytosis; aplastic anemia,    Poor rhematoid arthritis
                     inflamatory; short term                        superficial thrombophlebitis   nephrotic syndrome, deaf, kidney
                                                                                                   & liver necrosis
Gold Compds.         Retards or prevents progression of bone        Rheumatoid                     Stomatitis, rash, proteinuria,       Contra w/ penicllamine b/c will
                     and articular erosion; IM; protein bound                                      anemia, nephrotic                    remove gold
Penicillamine        Can retard bone & articular destruction        Rheumatoid                     Ditto; teratogenic
Methotrexate         Antimetabolite; kidney elim.                   Rheumatoid                     Hepatic fibosis, pneumonitis; bone   Contra renal insufficiency,
                                                                                                   marrow                               pregnancy
Narcotic Analgesia   XXXXXXXXXXXXXXXXXXXXXXXX                       XXXXXXXXXXXXXXXX               XXXXXXXXXXXXXXXXXXX                  XXXXXXXXXXXXXXXXXXX
                     XXXXXXXXXXXXXXXXXXXXXXXX                       XXXXXXXXXXXXXX                 XXXXXXXXXXXXXXXXXXX                  XXXXXXXXXXXXXXXXXXX
Pure Agonist         Opiods reduce rxn. to pain; dull better than                                  Sedation, euphoria, N/Vl; resp.      Triad = pin-point pupils,
(Opiods)             sharp; analgesia w/o impairment; dec.                                         depression; miosis; dec. cardio;     unconcious, dep. resp.;
                     response to CO2; and depression of                                            depression of vasometer; inc. CSF    mu – supraspinal, spinal
                     pontine & medualry centers; Histamine                                         pressure & inc. pCO2; slows GI;      anesthesia, euphoria; kappa –
                     release; suppresses cough reflex; ADH                                         constipation; contraction of biel    spinal, disphoria; delta – analgesia;
                     release; dec. edema; parenteral                                               duct and sphincter oddi; depressed   sigma – hallucinations
                                                                                                   renal
Morphine             Mu receptor; parenteral; no motor or                                                                               Avoid if asthmatic
                     smpathetic nerve block; little into brain;
                     liver metab; high 1st pass
Heroin               More potent than morphine; mu; cross
                     BBB > morphine
Codeine              Oral, lesspotent than morphine                 Antitusive                     Excititory in children
Meperidine           Rapid onset; short duration; mu; oral                                         Excitement causing convulsions;      Contra w/ MAO; cautin w/
                                                                                                   tachy w/ IV; useful w/ labor         astmatics
Methadone            Oral; can pass via breast milk; long DOA;      Chronic pain; treat narcotic
                     mu                                             dependence
Fentanyl             Short DOA; mu; potent                          Anesthesia                     Resp. depression                     Doesn’t release histamine
Propoxphene          Mu; oral                                                                      Excitement causing convulsions;      No antitusive effect
                                                                                                   resp, circ. collapse

Mixed An/agonist                                                                                   Psychotomimetic                      Reduced abuse; les resp.
                                                                                                                                        depression
Pentazocine          Agonist @ kappa; antag. @ mu                                                  Anxiety, hallucinations; inc.        Won’t improve narc withdrawal
                                                                                                   cardiac workload
Butorphanol          Anytag. mu, agonist kappa; parenterally                                       Resp. depression; Inc. cardiac       Low abuse potential
                                                                                                   workload
                                                        Pharmacology / Block III / Duc H. Vu / p. 11
Buprenorphine      Partial Ag.; mu agonist, kappa antag.                                          Less resp. depression;             Less resp. depression
                                                                                                  Psychotomimetic
Pure Antag.                                                       Treat narcotic posioning;
                                                                  abuse; neonatal resp.
                                                                  depression
Naloxone           Mu & kappa; short DOA; liver metab.            DOC = opiod over dose
Naltrexone         More effective orally                          Block opioid analgesic          Hepatic toxicity
                                                                  effect
Dextromethorphan   Antitussive                                    Cough suppression w/o
                                                                  analgesia; neiro protective
                                                                  properties
Gout               XXXXXXXXXXXXXXXXXXXXXXXX                       XXXXXXXXXXXXXXX                 XXXXXXXXXXXXXXXXXXX                XXXXXXXXXXXXXXXXXXX
Colchicine         Anti-inflam.; rapid releif of acute attacks;   Gouty arthritis; prophalaxis;   Bone Marrow; N/V/D
                   binds to tubuin = depolymerization =           good for acute attacks
                   inhibit. of migration of phagocytic granules
                   = stops infam. mediators; oral, IV
Allopurinol        Long term; inhibit xanthine oxidase; low       Gouty arthritis                 Hyupersensitive, rash; dyscarias   Enhances probenecid;
                   copetitive, high noncompetitive; casues                                                                           mercaptopurine toxicity; interfere
                   excretion of xanthine and uric acid; dec.                                                                         w/ metab. of oral anticoagulants
                   plasma urate which promotes dissolution of
                   tophi and prevents gouty arthritis; intitial
                   inc. in attcks
Probenecid         Oral; protein bound; inhibits readsorb. of     treat w/ colchcine              GI, hypersen., rash
                   urate = inc. excretion; long term &
                   prevention
Indomethacin                                                      Gouty arthritis, prophylaxis                                       Salicylcates interfere w/ drug
Sulfinpyrazone     Like probenecid                                Gouty arthritis
Naproxen                                                          Gouty arthritis, prophylaxis




Drug Dependence    XXXXXXXXXXXXXXXXXXXXXXXX                       XXXXXXXXXXXXXXX                 XXXXXXXXXXXXXXXXXXX                XXXXXXXXXXXXXXXXXXX
Clonidine          Hyperpolarization of locus cereleus via
                   alpha-2; dec. signs and symptoms but not
                   craving.
Naltrexone         Opiod antagonist
1-alpha-acetyl-    Longer acting than methadone; suppresses
methadol           for 72 hrs.
Methadone          Pt. stabalized on high doses methadone;
                   releives craving & produces cross
                   tolerance to other opiids
Meperidine
Pentobarbital
Phenobarbital      Produces mild intoxication, used for
                   barbituate dependence

                                                     Pharmacology / Block III / Duc H. Vu / p. 12
Diazepam          Substituted for short acting
                  benzodiazepines and then slowly
                  withdrawn
Buprenorphine     Partial agonist; substitue for opiates;
                  blocks euphoria prodeuced by full agonist
Hypnotic Agents   XXXXXXXXXXXXXXXXXXXXXXXX                     XXXXXXXXXXXXXXX                 XXXXXXXXXXXXXXXXXXX                    XXXXXXXXXXXXXXXXXXX
Barbituates       Well absorbed, hepatic metab.; hich conc.    Sedation, hypnosis, anagesia    Induce Liver enzymes;
                  – raise neuronal threshold for excitation                                    laryngospasm; Contra. acute
                  and dec. reptitive activity; prolong GABA                                    intermitent porphiria; Resp. failure
                  mediated Cl channels; GABA Mimetic
Phenobarbital     Long-acting; renal excertion, 25-50%
                  unchanged, excertion inc. by alkanization
Pentobarbital     Short-intermediate
Benzodiazepines   Inc. sleep time; dec. Stages 3,4, Rem                                        Sedation, CNS depression, ataxia,      High TI; contra sleep apnea, preg.,
                  unaffected                                                                   vertigo, physical dependence           does not induce liver enz.
Flurazepam        Effective for at least 4 weeks; no rebound                                   “hangover”
                  effect, short
Temazepam         intermediate
Triazolam         ultrashort acting; tolerence quickly;                                        Abterograde amnesia; rebound
                  rebound inc. in REM                                                          insomnia
Diazepam
Flumazenil        Benz. Antagonist; reversal of sedative and
                  depressant; competitively antagonizes
                  binding; quick action
Zolpidem          NonBenz. hypnotic; weak muscle relax.        Little effect on sleep stages
                  and anticonvulsant; acts on GABA
                  receptor, more selective for alpha-1




                                                  Pharmacology / Block III / Duc H. Vu / p. 13
Anti-anxiety
Chlordiazepoxide      t 1/2 inc. w/ alcoholic cirrhosis               Children
Diazepam                                                              Status epelepticus; amnestic
Alprazolam                                                            Elderly; antidepressant,
                                                                      panic disorder; dependence;
                                                                      delerium during withdraw
Oxazepam              Safer for elderly b/c short half life           Elderly
Lorazepam                                                             Elderly
Clonazepam                                                            Panic disorder
Buspirone             Non benz, nonbar.; less sedation &                                              Dizziness, headache, nausea; Don’t    Mimics serotonin to suppress
                      psy.motor impair.; lacks anticonvulsant,                                        use w/MAO                             neuronal activity in dorsal raphe &
                      hypnotic, muscle relax Acts on 5-HT1A                                                                                 hippo.
                      and DA-2
Baclofen              para-chlorophenyl GABA; spasmolytic             Reduces flexor extensor         Drowsiness
                      effects; dec. Ca influx = dec. trans. release   assoc. w/ spinal injury; dec.
                                                                      spacstoicity
CNS Stimulants                                                        Inc. wake, attentiveness,
                                                                      euphoria, inc. confidence,
                                                                      motor, speech, dec. fatigue
d-amphetamine         Inhibit reuptake of NE, DA                      Narc.; petit mal;               Excessive CNS stim., toxic
                                                                      antidepressant                  psychosis, HTN, tachy,
                                                                                                      hyperthermia
Methamphetamine                                                       Narc.                           Lesion Brain
Magnesium pemoline                                                                                    Hepatic failure                       Contra. – hypersensitive,
                                                                                                                                            Tourette’s
Phenylpropanolamine   Tolerence quickly                               Obesity                         Psychosis, HTN, stroke, renal
                                                                                                      failure, arrythmias
Fenfluramine          Affetcs 5-HT turnover, & glucose                Obesity; Lacks stim. effects    Hyperpyrexia, tremors, agitation,
                      utilization                                     of amphetamine; GI,             confusion, convulsion
                                                                      withdarwl = depression
Cocaine               Inhibits reuptake of catecholamines;                                            Tachy., HTN, hyperpyrexia,            Crosses placenta = Ht. abnorm.;
                      sympathomimetic; CNS stimulant; short                                           Stroke, paranoid, dementia            retards growth, in breast milk;
                      acting; vasoconstriction                                                                                              tricyclics dec. craving
Caffeine              Anatg. of adenosine receptor, inhibits          CNS & Ht. stim.; reduces        Restless, ringing in ears, anxiety
                      phosphodiesterase                               drowsiness, inc. motor,         neurosis
                                                                      appetite suppresion
Theophyline           Vasodilation                                    Asthma
Theobromine           No CNS
LSD                   No withdrawl; no cross tole. w/mescaline;       Myadriasis,                     Flashbacks, paninc, depression        Treat w/ Diazepam
                      activates 5-HT = dec. raphe = dec. filtering    sympathomimetic,
                                                                      hyperreflexia, paranoid
Mescaline
MDMA                  “Ecstacy”; degen. of serotonergic cell
                      bodies & axons
MDA
PCP                   Dissociative amnestetic; ataxia, rigidity       Tx.: Give quiet time            Toxic psychosis                       Violent & amnesia
Marijuana             Euphoria, difficulty attention, thinking                                        Dizzy, hot-cold, blurry vision;
                                                                                                      Tachy. & conj. reddening
Dronabinol                                                            Prevent nausea & vomiting;      Highly protein bound; tachy.; otrho
                                                                      appetite stimulant              hypo.; endocrine

                                                          Pharmacology / Block III / Duc H. Vu / p. 14
Antipsychotic       XXXXXXXXXXXXXXXXXXXXXXXX                    XXXXXXXXXXXXXXX                 XXXXXXXXXXXXXXXXXXX                      XXXXXXXXXXXXXXXXXXX
Phenothiazines      Antagonist at D2>D1, which inhibits         dec. hallucinations, anxiety;   EPS: park., acute dystonia,              Alpha adrenergic & mescarionic
                    adenylate cyclase; not good for motion      sedation; lowered seizure       akathisia, tardive dyskinesia,           recep. blockade; potentiation of
                    sickness; anti-emetic; ES efffects caused   threshold                       perioral tremor; inc. T- wave,           CNS depressants & opiods; dec.
                    mostly b/c dop. blockade                                                    prolonged Q-T; inc. prolactin b/c        gonadotropin; hypoten; ortho.;
                                                                                                dop. blockade                            anticholinergic effects; toxic
                                                                                                                                         retinopathy
Chloropromazine     Aliphatic; low potency                                                      Sedation; ortho. hypo.;                  Less lilely to cause parkinson
Thioridazine        Piperidine; low potency
Fluphenazine        Piperazine; high potnecy                                                    Extrapyramidal effects                   Less sed. & ortho.
Haloperidol         High potency; potent D2 antagonist          Acute mania; bipolar,           EPS effects common                       Lacks anticholinergic effects
                                                                tourette’s, panic
Clozapine           Blocks Dop. in mesolimbic-mesocortical      Better response                 Agranulocytosis (cell <3000,
                    sys, less D2  less EPS; doesn’t                                            granulocyte <1500; seizures; rapid
                    anatgonize levodpoa; blocks 5-HT2                                           withdrawl = exacerbation of
                                                                                                psychosis
Risperidone         First line alternative to high potency;                                     Insomnia, agitation, anxiety,            Less EPS, no agranulocytosis
                    blocks D2, 5-HT2, alpha 1; (+ & -)                                          neuroleptic malignant syndrome
Olanzapine          Cloazapine analog; blocks D2, 5-HT2, and                                    Wgt. gain, somnolence, agitation,        Less EPS, but does have tardive
                    many more; selective for limbic/frontal                                     nervous, antichlinergic, oirtho., inc.   dyskinesia, akathisia
                    cortex dop.; (+ & -)                                                        liver enzymes
Quetiapine          Cloazapine analog; low potency; binds                                       Transient prolactin; drowsinbess,        Mild EPS
                    many recep. w/ low affinity                                                 tachy, wgt. gain, dry mouth
Sertindole          5-HT2, D2, alpha 1; Limbic D2>Striatal      Potent antianxiety effects      Mild prolactinl nasal congestion,        Mild EPS, no hemoragic
                    D2; (+ & -)                                                                 sex dysfunc.; abnormal EKG
Lithium Carbonate                                               Antimanic, bipolar manic-                                                NSAIDS reduce renal excretion
                                                                depressive; DOC – mild to
                                                                moderate mania;
                                                                depression, cluster




                                                    Pharmacology / Block III / Duc H. Vu / p. 15
Antidepressant        XXXXXXXXXXXXXXXXXXXXXXXX                       XXXXXXXXXXXXXXXX        XXXXXXXXXXXXXXXXXXX                   XXXXXXXXXXXXXXXXXXX
Drugs                 XXXXXXXXXXXXXXXXXXXXXXXX                       XXXXXXXXXXXXXX          XXXXXXXXXXXXXXXXXXX                   XXXXXXXXXXXXXXXXXXX
MAO Inhibitors        Non-selectively inhibit MAO A&B; long                                  Liver, brain, cardio.; hypertensive   Last Resort
                      duration; inc. NE, dop, serotonin                                      crisis
Phenelzine
Tranylcypromine
Tricyclic             Inhibits uptake pumps; effect develops                                 down regulation of beta-adrenergic    arrythmias from acute tox.
                      rapidly;                                                               & presyn. ser. receptors occurs;
                                                                                             presynatic subsensitivity result of
                                                                                             inc. synaptc conc.; sedation;
                                                                                             anticholenergic; tachy.; delerium,
                                                                                             lower seizure thresh.; inhit
                                                                                             microsomal
Imipramine            Tertiary - Inhibit amine reuptake pumps of
                      Serotonin & NE
Amitriptyline         Tertiary - Inhibit amine reuptake pumps of
                      Serotonin & NE
Desipramine           Sec. – greater effect on NE uptake
Nortryptiline         Sec. – greater effect on NE uptake
Third Genreation      XXXXXXXXXXXXXXXXXXXXXXXX                       XXXXXXXXXXXXXXX         XXXXXXXXXXXXXXXXXXX                   XXXXXXXXXXXXXXXXXXX
Maprotiline           Selectively inhibits NE reuptake; good for
                      pts. w/ defecit in noradrenergic sys.
Fluoxetine (prozac)   SSRI, little effect on central NE,DA, hist.,   DOC – mild depression   Nervousnees, anxiety, akathisia;      Less anticholinergic, cardiac, no
                      cholinergic; long t1/2                                                 headaches inc.; suicidal              ortho.; Don’t use w/MAO, no
                                                                                                                                   hypo.
Sertraline            SSRI; less anticholin., gfatigue, and          DOC – mild depression                                         Doesn’t inhibit P450; no hypo.
                      dizziness
Paroxetine            SSRI                                           DOC – mild depression   Nausea, tremmor, sweating;            In breast milk, don’t use w/MAO
                                                                                             inhibits P450
Rolipram              PDE inhibitor = inc. cAMP = PKA = gene
                      transcription
Venlafaxine           Inhibits NE & serotonin reuptake               Anti-depressant         Like fluoxetine; inc. BP
Lithium               Target level 1mM; Inhibits G protein           Bipolar                                                       Very small theraputic window
                      coupling to second mes. sys.; Na depletion
                      = Li retention
Carbamazepine         Anticonvulsant                                 Bipolar
Valproate             Anticonvulsant                                 Bipolar




                                                        Pharmacology / Block III / Duc H. Vu / p. 16
Extrapyramidal    XXXXXXXXXXXXXXXXXXXXXXXX                     XXXXXXXXXXXXXXXX               XXXXXXXXXXXXXXXXXXX                    XXXXXXXXXXXXXXXXXXX
Dysfunction       XXXXXXXXXXXXXXXXXXXXXXX                      XXXXXXXXXXXXXX                 XXXXXXXXXXXXXXXXXXX                    XXXXXXXXXXXXXXXXXXX
Levodopa          Crosses BBB; only anout 1% gets through;     Improves akinesia, rigidity,   Ortho. hypo, arrythmias, N/V,          Contra. narrow angel gluacoma,
                  absorbeded small intestine; decarboxylated   posture, mood changes,         anorexia; stimulates CTZ (give         acute psychosis; B6 reverses
                  in stomach, intestine, liver                 mental improved                domperidone); inhib prolatic           actiuon of levodpal w/MAO =
                                                                                              secretipon; dyskinesias; insomnia,     HTN crisis; contra. antipsychotic
                                                                                              vivid dreams
Carbidopa         Peripheral decarboxylase Inhibitor; dec.
                  levodopa by 75%; theraptutic more rapid
Levo/carbid       Sinemet; combo of the two
Trihexyphenidyl   Anticholinergic; Muscarinic recep.           Tremors, bradykinesia,         Dry mouth, memory, insomnia
                  antagonist in CNS which corrects balance     rigidity
                  btwn dopa & cholinergic effects in
                  striatum; facilitate DA transmission by
                  inhibiting presyn uptake
Benztropine       Ditto
Diphenhydramine   Ditto
Pramipexole       Direct DA receptor selective D3/D4;                                         Ortho hypo., nausea
                  Neuroprotective
Ropinirole        D2 receptor agonist                                                         Light headed; slowed Ht., drowsy,
                                                                                              hallucinations
Amantadine        Release dopamine from intrneuronal           DOC – mild park.               Tolerence in few weeks;                Renal excretion, watch kidneys
                  stores; dec. reuptake                                                       anticholinergic effects (thinking,
                                                                                              confusion, hallucinations, anxiety);
                                                                                              Livedo Reticularis, edema,
Bromocriptine     Used w/levodopa; works on D2                 dec. motor fluctuations        N/V, hypo., constipation,              If used, dec. levodopa; less
                                                                                              nightmares, hallucinations,            tendency to produce dyskinesia
                                                                                              paranoid
Selegiline        MAO B inhibitor                              Slows progression of           Hallucinations
                                                               disease
MPTP              Causes destruction of substanti nigra DA
                  neurons
Tolocapone        COMT inhibitor (COMT breaks levodopa)        Longer “on”, shorter “off”     Nausea, sleepy, confusion; urine       Check liver func., MAO’s are
                                                                                              discolor                               potentiated




                                                  Pharmacology / Block III / Duc H. Vu / p. 17

				
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