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Mnemonics PHARMACOLOGY

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Mnemonics PHARMACOLOGY Powered By Docstoc
					PHARMACOLOGY
MNEMONICS
Pulmonary infiltrations inducing drugs "Go BAN Me!":
Gold
Bleomycin/ Busulphan/ BCNU
Amiodarone/ Acyclovir/ Azathioprine
Nitrofurantoin
Melphalan/ Methotrexate/ Methysergide

MPTP: mechanism, effect MPTP:
Mitochondrial Parkinson's-Type Poison.
· A mitochondrial poison that elicits a Parkinson's-type effect.

Antimuscarinics: members, action
"Inhibits Parasympathetic And Sweat":
Ipratropium Pirenzepine Atropine Scopolamine
· Muscarinic receptors at all parasympathetic endings sweat glands in
sympathetic.

Teratogenic drugs: major non-antibiotics TAP CAP:
Thalidomide Androgens Progestins Corticosteroids Aspirin &
indomethacin Phenytoin

Steroid side effects CUSHINGOID:
Cataracts
Ulcers
Skin: striae, thinning, bruising
Hypertension/ Hirsutism/ Hyperglycemia
Infections
Necrosis, avascular necrosis of the femoral head
Glycosuria
Osteoporosis, obesity
Immunosuppression
Diabetes


Beta blockers with CYP2D6 polymorphic metabolism
"I Met Tim Carver, the metabolic polymorph":
· The following beta blockers require dose adjustment due to CYP2D6
polymorphic metabolism:
Metoprolol Timolol Carvedilol (in patients with lower or higher than
normal CYP2D6 activity)

Beta blockers with intrinsic sympathomimetic activity
Picture diabetic and asthmatic kids riding away on a cart that rolls
on pinwheels. Pindolol and Carteolol have high and moderate ISA
respectively, making them acceptable for use in some diabetics or
asthmatics despite the fact that they are non-seletive beta blockers.

Muscarinic effects SLUG BAM:
Salivation/ Secretions/ Sweating
Lacrimation
Urination
Gastrointestinal upset
Bradycardia/ Bronchoconstriction/ Bowel movement
Abdominal cramps/ Anorexia
Miosis

Sulfonamide: major side effects
· Sulfonamide side effects:
Steven-Johnson syndrome
Skin rash
Solubility low (causes crystalluria)
Serum albumin displaced (causes newborn kernicterus and
potentiation of other serum albumin-binders like warfarin)

Epilepsy types, drugs of choice:
"Military General Attacked Weary Fighters Pronouncing 'Veni Vedi
Veci' After Crushing Enemies":
· Epilepsy types: Myoclonic Grand mal Atonic West syndrome Focal
Petit mal (absence)
· Respective drugs: Valproate Valproate Valproate ACTH
Carbamazepine Ethosuximide
Quinolones [and Fluoroquinolones]: mechanism
"Topple the Queen": Quinolone interferes with Topoisomerase II.

Beta blockers:
B1 selective vs. B1-B2 non-selective
A through N: B1 selective: Acebutalol, Atenolol, Esmolol,
Metoprolol.
O through Z: B1, B2 non-selective: Pindolol, Propanalol, Timolol.

Ribavirin: indications RIBAvirin:
RSV
Influenza B
Arenaviruses (Lassa, Bolivian, etc.)
Hypertension: treatment ABCD:
ACE inhibitors/ AngII antagonists (sometimes Alpha agonists also)
Beta blockers
Calcium antagonists
Diuretics

Narcotics: side effects "SCRAM if you see a drug dealer":
Synergistic CNS depression with other drugs
Constipation
Respiratory depression
Addiction
Miosis
Sex hormone drugs: male "Feminine Males Need Testosterone":
Fluoxymesterone
Methyltestosterone
Nandrolone
Testosterone

Ca++ channel blockers: uses CA++ MASH:
Cerebral vasospasm/ CHF
Angina
Migranes
Atrial flutter, fibrillation
Supraventricular tachycardia
Hypertension
· Alternatively: "CHASM":
Cererbral vasospasm / CHF
Hypertension
Angina
Suprventricular tachyarrhythmia
Migranes

Disulfiram-like reaction inducing drugs "PM PMT" as in Pre
Medical Test in the PM:
Procarbazine
Metronidazole
Cefo (Perazone, Mandole, Tetan).

Delerium-causing drugs ACUTE CHANGE IN MS:
Antibiotics (biaxin, penicillin, ciprofloxacin)
Cardiac drugs (digoxin, lidocaine)
Urinary incontinence drugs (anticholinergics)
Theophylline
Ethanol
Corticosteroids
H2 blockers
Antiparkinsonian drugs
Narcotics (esp. mepridine)
Geriatric psychiatric drugs
ENT drugs
Insomnia drugs
NSAIDs (eg indomethacin, naproxin)
Muscle relaxants
Seizure medicines

Morphine: side-effects MORPHINE:
Myosis
Out of it (sedation)
Respiratory depression
Pneumonia (aspiration)
Hypotension
Infrequency (constipation, urinary retention)
Nausea
Emesis

Therapeutic dosage: toxicity values for most commonly
monitored medications
"The magic 2s":
Digitalis (.5-1.5) Toxicity = 2.
Lithium (.6-1.2) Toxicity = 2.
Theophylline (10-20) Toxicity = 20.
Dilantin (10-20) Toxicity = 20.
APAP (1-30) Toxicity = 200.

Diuretics:
thiazides: indications "CHIC to use thiazides":
CHF
Hypertension
Insipidous
Calcium calculi

Migraine: prophylaxis drugs
"Very Volatile Pharmacotherapeutic Agents For Migraine
Prophylaxis":
Verpamil
Valproic acid
Pizotifen
Amitriptyline
Flunarizine
Methysergide
Propranolol

Adrenoceptors: vasomotor function of alpha vs. beta
ABCD:
Alpha = Constrict.
Beta = Dilate.

Antiarrhythmics: classification
I to IV MBA College
· In order of class I to IV:
Membrane stabilizers (class I)
Beta blockers
Action potential widening agents
Calcium channel blockers

Opiods: mu receptor effects "MD CARES":
Miosis
Dependency
Constipation
Analgesics
Respiratory depression
Euphoria
Sedation

Cancer drugs: time of action between DNA->mRNA ABCDEF:
Alkylating agents
Bleomycin
Cisplastin
Dactinomycin/ Doxorubicin
Etoposide
Flutamide and other steroids or their antagonists (eg tamoxifen,
leuprolide)

Busulfan: features ABCDEF:
Alkylating agent
Bone marrow suppression s/e
CML indication
Dark skin (hyperpigmentation) s/e
Endrocrine insufficiency (adrenal) s/e
Fibrosis (pulmonary) s/e

Tricyclic antidepressants: members worth knowing
"I have to hide, the CIA is after me":
Clomipramine Imipramine Amitrptyline
· If want the next 3 worth knowing, the DNDis also after me:
Desipramine Norrtriptyline Doxepin

Torsades de Pointes: drugs causing APACHE:
Amiodarone Procainamide Arsenium Cisapride Haloperidol
Eritromycin

Serotonin syndrome: components Causes HARM:
Hyperthermia Autonomic instability (delirium) Rigidity Myoclonus

Tetracycline: teratogenicity
TEtracycline is a TEratogen that causes staining of TEeth in the
newborn.

Patent ductus arteriosus: treatment
"Come In and Close the door": INdomethacin is used to Close PDA.

Physostigmine vs. neostigmine LMNOP:
Lipid soluble
Miotic
Natural
Orally absorbed well
Physostigmine
· Neostigmine, on the contrary, is:
Water soluble
Used in myesthenia gravis
Synthetic
Poor oral absorption

Beta 1 selective blockers
"BEAM ONE up, Scotty":
Beta 1 blockers:
Esmolol
Atenolol
Metropolol

Antirheumatic agents (disease modifying): members
CHAMP:
Cyclophosphamide
Hydroxycloroquine and choloroquinine
Auranofin and other gold compounds
Methotrexate
Penicillamine


Auranofin, aurothioglucose: category and indication
Aurum is latin for "gold" (gold's chemical symbol is Au).
Generic Aur- drugs (Auranofin, Aurothioglucose) are gold
compounds.
· If didn't learn yet that gold's indication is rheumatoid arthritis, AUR-
Acts Upon Rheumatoid.

Antiarrhythmics: class III members       BIAS:
Bretylium
Ibutilide
Amiodarone
Sotalol

MAOIs: indications MAOI'S:
Melancholic [classic name for atypical depression]
Anxiety
Obesity disorders [anorexia, bulemia]
Imagined illnesses [hypochondria]
Social phobias
· Listed in decreasing order of importance.
· Note MAOI is inside MelAnchOlIc.

SIADH-inducing drugs ABCD:
Analgesics: opioids, NSAIDs
Barbiturates
Cyclophosphamide/ Chlorpromazine/ Carbamazepine
Diuretic (thiazide)

K+ increasing agents K-BANK:
K-sparing diuretic
Beta blocker
ACEI
NSAID
K supplement


Reserpine action:
Reserpine depletes the Reserves of catecholamines [and serotonin].

Succinylcholine:
action, use Succinylcholine gets Stuck to Ach receptor, then Sucks
ions in through open pore. You Suck stuff in through a mouth-tube,
and drug is used for intubation.
Beta-blockers: side effects "BBC Loses Viewers In Rochedale":
Bradycardia
Bronchoconstriction
Claudication
Lipids
Vivid dreams & nightmares
-ve Inotropic action
Reduced sensitivity to hypoglycaemia
Cisplatin: major side effect, action "Ci-Splat-In":
Major side effect: Splat (vomiting sound)--vomiting so severe that
anti-nausea drug needed. Action: Goes Into the DNA strand.

Vir-named drugs: use"-vir at start, middle or end means for virus": ·
Drugs:
Abacavir,
Acyclovir,
Amprenavir,
Cidofovir,
Denavir,
Efavirenz,
Indavir,
Invirase,
Famvir,
Ganciclovir,
Norvir,
Oseltamivir,
Penciclovir,
Ritonavir,
Saquinavir,
Valacyclovir,
Viracept,
Viramune,
Zanamivir,
Zovirax.

Phenobarbitone: side effects
Children are annoying (hyperkinesia, irritability, insomnia,
aggression).
Adults are dosy (sedation, dizziness, drowsiness).

Prazocin: usage
Prazocin sounds like an acronym of "praszz zour urine".
Therefore Prazocin used for urinary retention in BPH.

Opioids: effects BAD AMERICANS:
Bradycardia & hypotension
Anorexia
Diminished pupilary size
Analgesics
Miosis
Euphoria
Respiratory depression
Increased smooth muscle activity (biliary tract constriction)
Constipation
Ameliorate cough reflex
Nausea and vomiting
Sedation

TB: antibiotics used
STRIPE:
STreptomycin Rifampicin Isoniazid Pyrizinamide Ethambutol
Phenytoin: adverse effects PHENYTOIN:
P-450 interactions
Hirsutism
Enlarged gums
Nystagmus
Yellow-browning of skin
Teratogenicity
Osteomalacia
Interference with B12 metabolism (hence anemia)
Neuropathies: vertigo, ataxia, and headache


Narcotic antagonists
The Narcotic Antagonists are NAloxone and NAltrexone. ·
Important clinically to treat narcotic overdose.

Thrombolytic agents USA:
Urokinase Streptokinase Alteplase (tPA)

Routes of entry: most rapid ways meds/toxins enter body
"Stick it, Sniff it, Suck it, Soak it":
Stick = Injection
Sniff = inhalation
Suck = ingestion
Soak = absorption

Asthma drugs: inhibitor action
zAfirlukast: Antagonist of LT
zIlueton: Inhibitor of 5-LO

Direct sympathomimetic catecholamines DINED:
Dopamine
Isoproterenol
Norepinephrine
Epinephrine
Dobutamine

Anticholinergic side effects
"Know the ABCD'S of anticholinergic side effects":
Anorexia
Blurry vision
Constipation/ Confusion
Dry Mouth
Sedation/ Stasis of urine

Atropine use: tachycardia or bradycardia
"A goes with B": Atropine used clinically to treat Bradycardia.

Bleomycin: action
"Bleo-Mycin Blows My DNA to bits": Bleomycin works by
fragmenting DNA (blowing it to bits). My DNA signals that its used
for cancer (targeting self cells).

Aspirin: side effects ASPIRIN:
Asthma
Salicyalism
Peptic ulcer disease/ Phosphorylation-oxidation uncoupling/ PPH/
Platelet disaggregation/ Premature closure of PDA
Intestinal blood loss
Reye's syndrome
Idiosyncracy
Noise (tinnitus)

Lupus: drugs inducing it HIP:
Hydralazine
INH
Procanimide

Vigabatrin: mechanism Vi-GABA-Tr-In:
Via GABA Transferase Inhibition
Morphine: effects at mu receptor PEAR:
Physical dependence
Euphoria
Analgesia
Respiratory depression

Enoxaprin (prototype low molecular weight heparin): action,
monitoring EnoXaprin only acts on factor Xa. Monitor Xa
concentration, rather than APTT.

Beta-1 vs Beta-2 receptor location "You have 1 heart and 2 lungs":
Beta-1 are therefore primarily on heart. Beta-2 primarily on lungs.

SSRIs: side effects SSRI:
Serotonin syndrome
Stimulate CNS
Reproductive disfunctions in male
Insomnia

Ipratropium: action Atropine is buried in the middle:
iprAtropium, so it behaves like Atropine.

Warfarin: action, monitoring WePT:
Warfarin works on the extrinsic pathway and is monitored by PT.

Propranolol and related '-olol' drugs: usage"olol" is just two
backwards lower case b's. Backward b's stand for "beta blocker". ·
Beta blockers include acebutolol, betaxolol, bisoprolol, oxprenolol,
propranolol.

Depression: 5 drugs causing it PROMS:
Propranolol
Reserpine
Oral contraceptives
Methyldopa
Steroids
Lead poisoning: presentation ABCDEFG:
Anemia
Basophilic stripping
Colicky pain
Diarrhea
Encephalopathy
Foot drop
Gum (lead line)


Myasthenia gravis: edrophonium vs. pyridostigmine
eDrophonium is for Diagnosis.
pyRIDostigmine is to get RID of symptoms.

Morphine: effects MORPHINES:
Miosis
Orthostatic hypotension
Respiratory depression
Pain supression
Histamine release/ Hormonal alterations
Increased ICT
Nausea
Euphoria
Sedation

Inhalation anesthetics SHINE:
Sevoflurane
Halothane
Isoflurane
Nitrous oxide
Enflurane
· If want the defunct Methoxyflurane too, make it MoonSHINE.

Cholinergics (eg organophosphates): effects
If you know these, you will be "LESS DUMB":
Lacrimation
Excitation of nicotinic synapses
Salivation
Sweating
Diarrhea
Urination
Micturition
Bronchoconstriction

Benzodiazapines: ones not metabolized by the liver (safe to use in
liver failure) LOT: Lorazepam Oxazepam Temazepam

Benzodiazepines: actions
"Ben SCAMs Pam into seduction not by brain but by muscle":
Sedation
anti-Convulsant
anti-Anxiety
Muscle relaxant
Not by brain: No antipsychotic activity.

Botulism toxin: action, related bungarotoxin
Action: "Botulism Bottles up the Ach so it can't be the released":
Related bungarotoxin: "Botulism is related to Beta Bungarotoxin
(beta-, not alpha-bungarotoxin--alpha has different mechanism).

Teratogenic drugs "W/ TERATOgenic":
Warfarin
Thalidomide
Epileptic drugs: phenytoin, valproate, carbamazepine
Retinoid
ACE inhibitor
Third element: lithium
OCP and other hormones (eg danazol)

Gynaecomastia-causing drugs DISCOS:
Digoxin
Isoniazid
Spironolactone
Cimetidine
Oestrogens
Stilboestrol

Benzodiazepenes: drugs which decrease their metabolism
"I'm Overly Calm":
Isoniazid
Oral contraceptive pills
Cimetidine
· These drugs increase calming effect of BZDs by retarding
metabolism.

Anesthesia: 4 stages "Anesthesiologists Enjoy S & M":
Analgesia
Excitement
Surgical anesthesia
Medullary paralysis

4-Aminopyradine (4-AP) use"4-AP is For AP":
For AP (action potential) propagation in Multiple Sclerosis.

Osmotic diuretics: members GUM:
Glycerol
Urea
Mannitol

Sodium valproate: side effects VALPROATE:
Vomiting
Alopecia
Liver toxicity
Pancreatitis/ Pancytopenia
Retention of fats (weight gain)
Oedema (peripheral oedema)
Appetite increase
Tremor
Enzyme inducer (liver)

Nitrofurantoin: major side effects NitroFurAntoin:
Neuropathy (peripheral neuropathy)
Fibrosis (pulmonary fibrosis)
Anemia (hemolytic anemia)
Zafirlukast, Montelukast, Cinalukast:
mechanism, usage"Zafir-luk-ast, Monte-luk-ast, Cina-luk-ast": ·
Anti-Lukotrienes for Asthma.
· Dazzle your oral examiner: Zafirlukast antagonizes leukotriene-4.
Zero order kinetics drugs (most common ones) "PEAZ (sounds
like pees) out a constant amount":
Phenytoin
Ethanol
Aspirin
Zero order
· Someone that pees out a constant amount describes zero order
kinetics (always the same amount out)

Hepatic necrosis: drugs causing focal to massive necrosis
"Very Angry Hepatocytes":
Valproic acid
Acetaminophen
Halothane

Steroids: side effects BECLOMETHASONE:
Buffalo hump
Easy bruising
Cataracts
Larger appetite
Obesity
Moonface
Euphoria
Thin arms & legs
Hypertension/ Hyperglycaemia
Avascular necrosis of femoral head
Skin thinning
Osteoporosis
Negative nitrogen balance
Emotional liability
Amiodarone: action, side effects 6 P's:
Prolongs action potential duration
Photosensitivity
Pigmentation of skin
Peripheral neuropathy
Pulmonary alveolitis and fibrosis
Peripheral conversion of T4 to T3 is inhibited -> hypothyroidism


Monoamine oxidase inhibitors:
Members "PIT of despair":
Phenelzine
Isocarboxazid
Tranylcypromine ·
A pit of despair, since MAOs treat depression

 Warfarin: metabolism SLOW:
· Has a slow onset of action.
· A quicK Vitamin K antagonist, though.
Small lipid-soluble molecule
Liver: site of action
Oral route of administration.
Warfarin


Propythiouracil (PTU):
Mechanism It inhibits PTU:
Peroxidase/ Peripheral deiodination
Tyrosine iodination Union (coupling)


Antibiotics contraindicated during pregnancy MCAT:
Metronidazole
Chloramphenicol
Aminoglycoside
Tetracycline
Beta-blockers:
nonselective beta-blockers"Tim Pinches His Nasal Problem"
(because he has a runny nose...):
Timolol
Pindolol
Hismolol
Naldolol
Propranolol

Methyldopa:
side effects METHYLDOPA:
Mental retardation
Electrolyte imbalance
Tolerance
Headache/ Hepatotoxicity psYcological upset
Lactation in female
Dry mouth
Oedema
Parkinsonism
Anaemia (haemolytic)

Lithium: side effects LITH:
Leukocytosis
Insipidus [diabetes insipidus, tied to polyuria]
Tremor/ Teratogenesis
Hypothyroidism

Respiratory depression inducing drugs "STOP breathing":
Sedatives and hypnotics
Trimethoprim
Opiates
Polymyxins


Benzodiazepenes: antidote "Ben is off with the flu":
Benzodiazepine effects off with Flumazenil.
PHARMACOLOGY Mechanisms A. Scopolamine • Anti-muscarinic • Motion Sickness;
preoperatively to reduce secretions • Anti-muscarinic toxicities (mydriasis & cycloplegia;
decreased secretions & sweating; flushing; bradycardia (low doses); tachycardia (high doses);
urinary retention; drowsiness, hallucinations, coma)

Typical Anti-psychotics (Chlorpromazine, Haloperidol, Thioridazine) • Dopamine
antagonists • Schizophrenia; psychosis • Lactation; Extrapyramidal effects (parkinsonism,
akathisia (motor restlessness), tardive dyskinesia (lip smacking, jaw movements, etc.)); anti-
cholinergic effects (antimuscarinic, alpha-antagonistic (orthostatic hypotension), and anti-
histamine (sedation)). Toxicities are a tradeoff—higher extrapyramidal effects coincide with
lower anticholinergic effects and vice-versa. The higher the extrapyramidal effects, the higher
the potency (haloperidol > chlorpromazine > thioridazine)

Atypical anti-psychotics (Clozapine) • Dopamine antagonist • Schizophrenia; psychosis • NO
extrapyramidal effects or lactation; agranulocytosis (fatal); Neuroleptic Malignant Syndrome
(catatonia, autonomic instability, stupor); anti-cholinergic effects as above

B. Opiate Agonists (Morphine, Meperidine, Codeine, Methadone, Heroin, Fentanyl) • Act at
mu, kappa, delta receptors in CNS • Analgesia; Antitussive (Codeine); opiate addiction
(Methadone); antidiarrheal (loperamide) • CNS depression; nausea; respiratory depression;
constipation; urinary retention; dependence

Opiate Mixed Agonists-Antagonists (Pentazocine) • Same as agonists but will cause
withdrawal in those dependent on agonists

Opiate Antagonists (Naloxone, Naltrexone) • Block opiate receptors • Narcotic overdose (no
effect if used alone)

Erythropoietin • Increases RBC production in marrow • Anemia associated with renal failure

RU486 (Mifepristone) • Progestin antagonist • Early-term abortion • Uterine bleeding,
possible incomplete abortion

C. Acarbose • Alpha-glucosidase inhibitor—decreases absorption of glucose • NIDDM;
adjunct to insulin in IDDM • Flatulence; diarrhea; abdominal cramping

D. Losartan • Angiotensin II antagonist • Hypertension • Similar to ACE inhibitors but no
cough (decreased bradykinin activation)

E. Myasthenia Gravis Drugs • Inhibit cholinesterase • Diagnosis (edrophonium); long-term
treatment (Neostigmine, Pyridostigmine); open-angle glaucoma; reversal of non-depolarizing
nm blockade • Fasciculations & weakness

desensitization of pituitaryF. Leuprolide • GnRH analog decreased FSH, LH secretion •
Prostate Cancer •receptor Transient excess testosterone production (prevent by combining
with flutamide); impotence, hot flashes, tumor flare
G. Flutamide • Blocks inhibitory effects of testosterone on GnRH release • Combo with
leuprolide

pregneneloneH. Aminoglutethimide • Inhibits Cholesterol conversion (like metyrapone) •
Metastatic breast cancer (decreased estrogen) • Induces P450; transient CNS depression; rash

I. Metformin • Decreases gluconeogenesis; improves lipid profile (HDL rises, LDL falls) •
NIDDM – lower risk of hypoglycemia • GI side effects; lactic acidosis (rare); long-term
interference w B12 absorption

J. Stool Softeners (psyllium, methylcellulose) • Absorbs peristalsis • Constipation bulk
water and softens stool Mechanism, clinical use, and toxicity of dermatologic agents:
CORTICOSTEROIDS: Synthesized in the zona fascilculata of the adrenal cortex. Cortisol
and Cortisone produced. 1) Glucocorticoids are catabolic. They influence carbohydrate and
fat metabolism to insure adequate delivery of glucose to brain and tissues. 2) Decrease
intestinal uptake of calcium; increase renal excretion of calcium (contribute to osteoporosis).
3) Supress the inflammatory response – Decrease edema, fibrin deposition, capillary
dilatation, leukocyte migration and phagocytic activity. Inhibit prostaglandin and leukotriene
production by inhibiting phospholipase A2. 4) Include: Cortisone (short acting), Prednisone
(intermediate acting), Prednisolone (similar to prednisone but no hepatic metabolism for
activity), Methylprednisolone (similar to prednisolone but better anti-inflamatory and less
mineralocorticoid effects), Triamcinolone (5x more potent than cortisol), Dexamethasone
(long acting) & Beclomethasone (long acting available as aerosol). 5) Toxicity: a) Skin:
hirsutism, skin thinning, poor wound healing, striae, acne and purpura. b) Other:
hyperglycemia, hypertension, cataracts, glaucoma, peptic ulcer disease, osteoporosis, and
increased susceptibility to infection.

RETINOIDS: 1) Used to treat the following dermatologic diseases: Acne, psoriasis, icthyosis
and has a potential benefit in early skin cancers (actinic keratosis) 2) Toxicity: in skin it can
cause desquamation, dry skin and pruritus, erythema.

ANTIFUNGALS: 1) Polyene antibiotics are fungicidal against both filamentous and yeastlike
fungi including Histoplasma, Blastomyces, Coccidioides, Cryptococcus, Candida,
Aspergillus and Sporothrix. Polyenes interact with sterols in the cytoplasmic membrane of
fungi leading to rapid leakage of small molecules and death. Sensitive fungi have ergosterol
in their membranes. a) Amphotercin B: Broad spectrum to treat systemic fungal infections.
Side effects: Fever, chills, impaired renal function, anemia, thrombocytopenia. b) Nystatin
(Mycostatin): Similar to A but used primarily in topical preparations. Use in Candida
infections and prophylaxis. 2) Imidazoles: Block the synthesis of fungal cell membrane
ergosterols. a) Miconazole & Clomitrazole: Miconazole is the only imidazole that can be
administered IV; clotrimazole is only used topically. i) Intravenous miconazole is rarely used
due to toxicity. Treats ringworm, vulvovaginal candidiasis b) Ketoconazole: Oral
administration only. Causes gynecomastia. 3) Miscellaneous: a) Flucytosine: Administer with
amphotercin B in the treatment of cryptococcal meningitis and other systemic infections
(synergistic). b) Griseofulvin: Binds to keratin, treat Tineas (capitis, corporis etc),

Other new pharmacologic agents: 1) Erythopoietin (EPO): RBC growth factor. Produced in
kindneys. Recombinant form available (epoietin alpha). a) Use for tx of Anemia 2nd to renal
failure or zidovudine (AZT) use HIV patients. b) Use for tx of Anemia 2nd to chemo, or to
stimulate rbc production prior to surgery or to facilitate autologous donation. c) Side effects:
Clotting of dialysis tubing and hypertension. 2) RU486 (Mifrepristone): Abortificen. Blocks
progesterone receptors and thereby progesterone support of pregnancy. 80% effective, 95% if
used with prostaglandins. a) Complications include incomplete abortion (2%), ongoing
pregnancy (1%), hemorrhage during D&C (<1%). Know About......

1) Complications of empiric antibiotic use: a) Resistance: Must take into account
susceptibility patterns of local settings. Must distinguish between community vs. nosocomial
infection, and must take into account the patient’s immune status. b) Fungal Infections: Due
to destruction of normal flora. (candidiasis). c) Other complications: C. Diff ototoxicity
(must monitorPseudomembranous colitis. Gentamicin allergic reactions. 2)levels),
Sulfonamides and Penicillin osteoporosis withSecondary effects of other drugs: a) Heparin
chronic use. Thombocytopenia – usually transient and mild. b) Hyperlipidemia, hypokalemia.
3) Drugs thatThiazides block/increase hepatic drug metabolism: a) Cimetidine: Histamine
analog that cab reduce hepatic blood flow and slow clearance of other drugs and also reduces
activity of cytochrome p-450 b) Ethanol: Chronic use induces hepatic microsomal enzymes
and may enhance metabolism of other drugs. c) Phenobarbital: Increased phenobarbital levels
in patients that have ethanol, chloramphenicol or valproic acid on board, since it has
microsomal enzyme metabolism. d) Phenytoin (Dilantin): same as Metabolized by
microsomal enzymes. e)Phenobarb and ETOH Rifampin: Causes jaundice and
hepatotoxicity, also interacts with C p-450 system. 4) Fundamental Pharmacodinamics: a)
Partial agonists/agonist: Drugs that bind to receptors and stimulate them. b) Antagonists: are
drugs that bind to receptors and decrease or block the effect of an agonist. They do not
stimulate the receptors. i) Competitive antagonist: Reversibly binds to the receptor and
prevents binding of the agonist. ii) Non competitive antagonist: Usually binds to the receptor
irreversibly and prevents any agonist action. c) Efficacy: Maximal effect produced by a drug.
d) Potency: Activity of a drug compared to a reference standard; depends on the drug’s
ability to reach the receptors and its affinity to the receptor. 5) Drug efficacy and potency as
demonstrated on dose-response curves: a) ED50 (effect dose)- Dose which produces half-
maximal response (ie., observed effect seen in 50% of patients); used as a measure of potency
(the lower the ED50, the more potent the drug). b) TD50 (toxic dose)- Minimum dose which
produces a specific toxic effect in 50% of individual (or animals). c) LD50 (lethal dose)-
Minimum dose which kills 50% of animals. d) Therapeutic index- Ratio of dose required to
produce a toxic effect to the dose needed for a therapeutic effect. Used as an indication of
drug safety. Expressed as :

TI= TD50 or TI= LD50 You want drugs with a high therapeutic index (low ED 50 ED50 side
effects at usual doses).

6) Pharmacogenetics: drugs whose metabolism is affected by inheritance: a) Isoniazid: Most
commonly used drug for the treatment of TB. i) Inhibits biosynthesis of mycolic acids. ii)
Metabolized in the liver (acetylated); speed of acetylation and consequently isoniazid’s half
life is genetically determined (fast vs. slow acetylators). 7. Treatment of Anemia A. Anemia
is due to increased destruction or decreased production. B. Microcytic anemia 1. Iron –
absorbed in the duodenum and proximal jejunum. Iron deficiency seen in premature infants,
pregnant and lactating women. Ferrous oral salts can be given; give for 3-6 months to
replenish iron stores. IV iron can also be given. 2. Iron toxicity a. N/V, cramps, constipation,
diarrhea – dose-related so decrease the dose b. Acute toxicity – seen in kids, necrotizing
gastroenteritis followed by shock, lethargy, dyspnea c. Chronic iron toxicity -
hemochromatosis C. Megaloblastic anemia – lack of vitamins needed for normal DNA
synthesis, so the RBC gets biggger (macrocytic) 1. Vitamin B12 (normally obtained in
meats), requires intrinsic factor for absorption (pernicious anemia decreases absorption),
gastrectomy also decreases absorption. B12 is stored in the body (years supply) a. B12
deficiency also shows nervous defects b. B12 shots can be given if oral absorption is a
problem c. Folate will NOT correct neurological features, but WILL help with the anemia 2.
Folic Acid – from green leafy veggies, body stores of folate are lower (1-6 months) a.
Deficiency doesn’t have neurological deficits b. Folic acid is well absorbed orally D.
Decreased production 1. Erythropoietin – used for renal failure, bone diseases, chemotherapy
a. Toxicity – too rapid increase in hematocrit can lead to HTN, thrombotic complications 2.
Colony stimulating factors (G-CSF, GM-CSF) a. Increase recovery after myelosuppressive
chemotherapy or BMT 8. Prevention/treatment of cerebrovascular disease K. Aspirin 1.
Irreversibly blocks cyclooxygenase, = inhibits thromboxane (TxA2) formation from platelets
2. Only requires a small daily dose L. Ticlopidine 1. Inhibits platelet aggregation (inhibits
ADP pathway) 2. Decreases TIAs, completed strokes, unstable angina pectoris 3. Diarrhea in
20%, leukopenia in 1% (must monitor white count) M. Thrombolytics – catalyze formation
of plasmin, a generalized lytic state in body is produced 1. Streptokinase – cheap, allergic
reactions possible 2. Urokinase 3. Tissue plasminogen activators (t-PA) – expensive, from
recombinant DNA 9. Treatment of rheumatoid arthritis A. Drugs that alter Pain 1. Aspirin –
1st line drug, GI problems 2. NSAIDS - 3. COX-2 inhibitors – less GI problems B. Drugs
that Decrease Progression 1. Methotrexate and immunosuppressives – more toxic side effects
2. Gold – dermatitis is common side effect 10. Vaccines: indications, potential side effects A.
Indications 1. Active immunization – antigen is given so host develops antibodies (long
protection) a. Give to children 2. Passive – immunoglobins are given (short term protection)
a. Give to those recently exposed (Tetanus, Botulinum, HBV, Rabies) or to travelers (Polio,
tetanus, Measles, diphtheria) B. Side Effects 1. Giving live attenuated vaccines may cause the
disease (eg. Polio vaccine) 2. Killed vaccine will not cause the disease 3. Allergic reactions
are possible 11. Chemotherapeutic agents: risk of possible secondary cancer

				
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