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107 Cards in this Set
- Front
- Back
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5-Hydroxytryptamine
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Serotonin
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Acetaminophen
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Mx: CNS COX-3 (weak peripheral COX1/2) inhibitor. Analgesic+antipyretic. No aspirin-like GI irritation (aspirin not specific to compartment). Choice for children (no risk of Reye's).
Kx: Rapid GI absorb, short HL, metab. P450, need glutathione for next step. Tox: Not enough glutathione. Give N-acetyl-cysteine. |
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Acetylcholine
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ACTH
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Mx: Hormone receptor agonist
Fx: ↑CE takeup, ↑steroid synthesis, ↑adrenal growth Dz: Too much: Cushing syndrome/dz (↑wt, ↓protein, osteoporosis, ↓growth, ↓glu tolerance, HTN), not enough: Addison (GI, ↓H2O, ↓Na, ↓K, weak, lethargy, ↓BP) |
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Alanine aminotransferase
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ALT
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Allopurinol
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Mx: purine analog, xanthine oxidase inhibitor.
Fx: Serum UA↓ Tx: Chronic gout (esp w/renal), 2ry hyperuricemia; don't correct underlying defect Kx: PO, active w/active metabs S/E: May precipitate acute gout attack - give w/colchicine or NSAIDs Tox: Hypersensitivity |
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Alpha-methyldopa hydrazine
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Syn: Carbidopa
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Alpha-methyltyrosine
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Syn: AMPT
Mx: Competitive inhibitor of tyrosine hydroxylase Fx: Blocks tyrosine→L-DOPA conversion: lowered catecholamine levels. Tx: Pheochromocytoma S/E: Sedation |
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Alprostadil
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PGE1. Mx: smooth muscle relaxation. Tx: Impotence.
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Aluminum
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Antidote: Deferroxamine
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Amantadine
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Mx: Unk
Tx: Parkinson's (less potent than L-DOPA) S/E: L-DOPA-like, but less; also every other CNS symptom |
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Ammonium chloride
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With lavage, urine acidifies to pH 4.5
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Amphetamine
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Mx: Catecholamine releaser/reuptake inhibitor
Fx: psychotic-like action, reversed by DA receptor blocker Tx: Producing schizophrenia Antidote: alkalinize urine w/ammonium chloride. |
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Apomorphine
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Emetic agent, CTZ-acting, reversible w/naloxone, rapid-acting. Risk of CNS/respiratory depression - counterindicated w/double-whammy.
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Arachidonic acid
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From ingested. Constituent of cell membranes. Released via PLA2 (c/s) (+bradykinin/angiotensin, -steroids) or PLC+DGL. Processed by 4 pathways, important ones are LOX, COX, and isoeicosanoid. COX: AA→PGG2→PGH2→PGI2/PGE2+PGF2a/TXA2. LOX: LT.
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Arsenic
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Antidote: BAL
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Aspartate aminotransferase
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AST
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Aspirin
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Mx: non-specific, non-competitive inhibitor of COX1/2
Fx: analgesic, antipyretic (↓temp, vasodil), anti-inflammatory, anti-platelet. Tx: slight to moderate pain, chronic > acute. Tox: emesis, tinnitus, vertigo, CNS, resp dep, resp failure, Reyes. Antidote: cold, lavage, cathartics, bicarb (alk. urine, reverse acidosis), rehydration, KCl, glu. C/I: Gout |
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Atropine
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Mx: Acetylcholine antagonist, anti-ACh.
Tx: Malathion poisoning |
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Benztropine
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Mx: Antimuscarinic
Fx: Improves tremor+rigidity, but no fx on bradykinesia; less effective than L-DOPA Tx: Adjunct w/L-DOPA (Parkinson symptom exacerbation if not tapered off) S/E: Atropine-like (dry mouth, mydriasis, tachy, nausea, blah blah) |
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Bromocryptine
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Mx: ergot, D2 agonist, D1 partial agonist
Tx: Parkinson (more than anticholinergics/amantadine, less than L-DOPA), lower doses of L-DOPA when used together S/E: Like L-DOPA - worse GI, better on-off. |
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Cadmium
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Tox: inhaled - irritation, edema, emphysema, renal dz, brittle bones. CA questionable.
Antidote: EDTA - poor. |
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Carbidopa
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DOPA decarboxylase inhibitor, can't cross BBB
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Catechol-O-methyl transferase
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Degrades catecholamines extracellularly. Inhibited by entacapone.
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Catecholamines
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E, NE, DA
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Celecoxib
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Mx: Selective COX-2 inhibitor
Fx: No platelet inhibition Kx: P450, 1/d C/I: NSAID allergy, standard NSAID: asthma, GI, hepatic, renal, pregnancy S/E: GI, less ulcers, kidney, elevation of b-blockers, antipsych, antidep. Tx: Arthritis (both kinds) |
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Chlorpromazine
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Mx: Classical antipsychotic
S/E: Sedation, seizures, galactorrhea, anti-emetic, flushing, sexual function, extrapyramidal...lots. |
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Colchicine
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Mx: microtubule polymerization inhibitor
Fx: ↓leukocyte migration, ↓LTB4 Kx: PO, IV (careful), fast absorb, tissue bind, v.long HL, exc feces Tx: Acute gout attack, give until pain stops or tox Tox: GI (PO worse), diarrhea, leukopenia, renal (IV worse) |
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Cyclooxygenase
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COX1/COX2. Catalyzes AA→PGG2→PGH2.
COX1: housekeeping, wide dist, minimal inducibility, imp: PGs in GI mucosa, vasodilating PGs in kidney, precursor PGs for TX production in platelets. COX2: Inflammatory/immune cells, induced. |
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Deferroxamine
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Mx: Chelating agent
Tx: PO gut, IV systemic; Fe, Al. S/E: Hypotension, tachycardia, fever. |
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Desipramine
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Mx: TCA - NE+5HT reuptake inhibitor, M+H+α(1>2) antagonist (S/E).
Fx: Depressed - mood↑, alert↑, phys act↑, morbid thought↓. Normal - sedation, diff. thinking, irritability, anxiety. 2wk fx onset, quick tolerance to anticholinergic s/e, slower adrenergic tolerance, dependence, no effectiveness loss, 1/3 won't respond. Tx: Depression, ADHD, panic, bed-wetting, chronic pain S/E: anti-Muscarinic, adrenergic, weight gain, sexual, heart block, cardiac overstim, orthostatic hypotension (a-adrenergic block), sedation, mania, narrow therapeutic index. D/I: ethanol, benzos - sedation. C/I: ANY USE OF MAOI IN LAST 3 WEEKS! Serotonin syndrome. |
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Dexamethasone
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Mx: Steroid, v.powerful gluco, no mineral, long-act.
Fx: ↑liver gluconeogenesis, ↑periph protein catab, ↑gly synthesis, ↓glu use in periph, sensitizes TG↔FFA, ↓Ca, anti-inflammatory (↓AA convert, ↓COX). Tx: steroid replenishment (Addison, CAH) |
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Diazepam
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Mx: Benzodiazepine, enhances GABA fx at GABA-A channel
Fx: Sed, hyp, anxiolysis, muscle relax, anterograde amnesia, anticonvulsant. Tx: Anxiety (prolonged tx), terminating grand mal/status epilepticus, muscle spasms (strains/MS/cerebral palsy), anasthesia adjunct (IV) Kx: Long-acting, lipid-soluble, active metabs, slow elim. S/E: Psych dep, active metabs, amnesiac, additive w/depressants Antidote: Flumazenil |
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Diclofenac
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Mx: NSAID
Fx: COX1/2 inhibitor (stronger than indomethacin or naproxen) Tx: Arthritis, spondylitis, post-op opthalmic S/E: Usual |
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Dinoprostone
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Mx: Synthetic PGE2.
Tx: Abortion (vag 2nd tr, IV 1st/2nd tr), labor induce (a la oxytocin), soften cervix for birth. |
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Disulfiram
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Tx for chronic ethanol abuse.
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DOPA-decarboxylase
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L-DOPA→DA, inhibited by carbidopa.
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Dopamine
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EDTA
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Mx: Chelating agent
Tx: IV - Pb, Zn, Fe, Cd (poor) S/E: Complexes Ca (Ca-deficient tetany) - give with Ca, proximal nephron damage. |
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Entacopone
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Mx: COMT inhibitor
Fx: Inhibits production of breakdown product which competes for CNS access with L-DOPA; ↓L-DOPA dosage, ↑HL Tx: L-DOPA adjunct (reduces "off" relative to L-DOPA+Carbidopa, reduces dyskinesias) |
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Ethanol
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Tx: Methanol poisoning, polyethylene glycol poisoning.
Tox: CNS depression, lack of coordination, hypoglycemia, lactic acidosis, convulsions, coma. Antidote: lavage, bicarb, glu, heat, hypertonic mannitol diuresis. |
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Flumazenil
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Benzodiazepine antagonist, v. short HL, so caution rebound.
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Fluoxetine
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Mx: SSRI
S/E: sexual, nausea, tremor, headache, insomnia, P450 inhibit. Tx: Depression, panic, OCD, bulimia/anorexia, social phobia, neuropathic pain, PMS |
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Flurazepam
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Mx: Benzodiazepine, enhances GABA fx at GABA-A channel
Fx: Sed, hyp, anxiolysis, muscle relax, anterograde amnesia, anticonvulsant. Tx: Anxiety (prolonged tx) Kx: Long-acting, active metabs, slow elim. S/E: Psych dep, active metabs, amnesiac, additive w/depressants Antidote: Flumazenil |
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GABA
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Main CNS inhibitory system (PNS is glycine). Main is GABA-A (Cl- channel), binds GABA, benos, barbs at different sites (all enhance channel activity). Opposing NT: Glutamate.
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Glucose
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Glutamate
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Excitatory NT system.
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Guanethidine
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Haloperidol
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Mx: Classical antipsychotic (strong)
Tx: Schizophrenia, Huntington's chorea, Tourette's, mania, chronic amphetamine psychosis S/E: Less main (ortho hypoten, sedation), more extrapyramidal |
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Histamine
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Ibuprofen
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Mx: NSAID
Fx: COX1/2 inhibitor - anti-inflammatory, analgesic, anti-pyretic Kx: P450+kidneys Tx: Usual S/E: Usual - GI, bleeding time, etc. |
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Imipramine
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Mx: TCA - NE+5HT reuptake inhibitor, M+H+α(1>2) antagonist (S/E).
Fx: Depressed - mood↑, alert↑, phys act↑, morbid thought↓. Normal - sedation, diff. thinking, irritability, anxiety. 2wk fx onset, quick tolerance to anticholinergic s/e, slower adrenergic tolerance, dependence, no effectiveness loss, 1/3 won't respond. Tx: Depression, ADHD, panic, bed-wetting, chronic pain. S/E: anti-Muscarinic, adrenergic, weight gain, sexual, heart block, cardiac overstim, orthostatic hypotension (a-adrenergic block), sedation, mania, narrow therapeutic index. D/I: ethanol, benzos - sedation. C/I: ANY USE OF MAOI IN LAST 3 WEEKS! Serotonin syndrome. |
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Indomethacin
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Mx: NSAID
Fx: STRONG anti-inflammatory (PLA/C inhibitor), analgesic 2nd. Tx: Arthritis, spondylitis, acute gout (preferred), uveitis, antipyretic (Hodgkin's), uterine contraction suppression S/E: STRONG! Standard NSAID, plus FRONTAL HEADACHE C/I: Pregnancy |
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Ipecac
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Emetic agent, PO, acts on gastric mucosa and CTZ, slow-acting. Chronic use (wt loss)→cardiomypathy, v.fib. Follow w/water, can interfere w/later tx. Prob: Ingestion of caustics, petroleum distillates, convulsants; no gag reflex (infants<6mo), CNS stimulants, cardiopulmonary pts (emetine, cardiotoxin).
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Isoprostane
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Synthesized from AA via non-COX/LOX pathway (free radical). Fx on thromboxane receptor.
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Ketamine
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Emergency antidepressant? "Don't worry about it."
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L-DOPA
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Mx: Crosses BBB, converted by DOPA decarboxylase to DA.
Fx: Increases DA in brain Kx: Decarboxylated in periphery (give carbidopa) with s/e: vomiting, hypoten, nausea, cardiac arrhythmia. With carbidopa, s/e reduced, but central remain. Tx: Parkinson (first few yrs of dz) S/E: dyskenesia, on-off phenomenon (decreasing fluctuation at receptors helps), psychosis Antidote: drug holiday; but no help to on-off D/I: MAOI - even more catecholamine production - HTN crisis C/I: Psychosis - exacerbates symptoms |
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Leukotriene B4
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Neutrophil chemoattractant, leukocyte adhesion promoter, ROS-synthesis promoter.
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Leukotriene
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Mx: AA→[LOX]→→LTs
LTC4+LTD4: Bronchoconstrictors (asthma, anaphylaxis), syn blocked by zileuton. |
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Levodopa
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Mx: Crosses BBB, converted by DOPA decarboxylase to DA.
Fx: Increases DA in brain Kx: Decarboxylated in periphery (give carbidopa) with s/e: vomiting, hypoten, nausea, cardiac arrhythmia. With carbidopa, s/e reduced, but central remain. Tx: Parkinson (first few yrs of dz) S/E: dyskenesia, on-off phenomenon (decreasing fluctuation at receptors helps), psychosis Antidote: drug holiday; but no help to on-off D/I: MAOI - even more catecholamine production - HTN crisis C/I: Psychosis - exacerbates symptoms |
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Lipoxygenase
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Makes LTs from AA. Inhibited by zileuton.
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Lithium
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Mx: Many exp, best defined PI turnover, depleting PIP2, downregulating IP3/DAG pathway (lots of metabotropic receptor fx).
Fx: "Mood-Stabilizing" in bipolar, no fx on normal people. Tx: Bipolar (mild: standalone, severe: combo w/ benzo|antipsych, maint combo w/ benzo) Kx: PO: PP in 30-120min, no metab, kidney excr. Intx: Diuretics (THIAZIDES) reduce renal clearance by 25%, some NSAIDS reduce renal clearance (not aspirin/acetamin), antipsychotics cause more severe extrapyramid S/E. S/E: TREMOR (block w/b-blocker), nephorgenic diabetes insipidus, motor fx, speech fx, confusion, weight gain. CARRIED IN BREAST MILK. D/I: Diuretics (reduce clearance), NSAIDs (reduce clearance - not aspirin/tylenol), antipsychotics (more extrapyramidal s/e). Tox: Low-salt diet, salt loss, diuretics, etc. Antidote: DIALYSIS. |
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Malathion
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Mx: ↑ACh
Tox: Muscarinic (SLUD: salivation, lacrimation, urination, defecation), Nicotinic (weakness/twitch/paralysis, pallor, anxiety, confusion, slurring, convulsions, coma) Antidote: Clothes off, wash, emesis, ventilate. Atropine! Pralidoxime! |
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Mercury
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Tox: Elemental (Inhaled) - shyness, irritability, depression. Organic - paresthesia, sensory constriction (visual, hearing, taste), laughter, crying, intellectual deterioration. Inorganic - kidney damage.
Antidote: Penicillamine. |
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Methanol
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S/S: Inebriation, vomiting, visual, acidosis.
Antidote: Ethanol! Keep drunk! Emesis, lavage, bicarb, dialysis. |
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Methylene blue
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Tx: nitrite poisoning, triggers reduction of MetHb→Hb
Tox: Makes MetHb! |
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Mineral oil
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Tx: lubricant laxative
Tox: dry cough long after exposure, dizziness, CNS depression Antidote: lavage - DO NOT INDUCE VOMITING |
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Misoprostol
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PGE1 derivative. Tx: peptic ulcer (cytoprotective), abortion.
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Monoamine oxidase
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Mitochondrial enzyme. Two forms: MAO-A metabolizes NE, 5HT, MAO-B metabolizes DA.
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N-acetyl-cysteine
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Acetaminophen antidote.
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NAD
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Naloxone
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Opioid antagonist.
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Naltrexone
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Opioid antagonist. Also ethanol craving reducer.
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Naproxen
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Tx: Acute gout, rest like Ibuprofen
Kx: LONG HALF-LIFE compared to Ibuprofen |
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Norepinephrine
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Penicillamine
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Mx: Chelating agent
Tx: PO: Cu, Hg, Zn, Pb S/E: Rare agranulocytosis, aplastic anemia. C/I: Penicillin allergy. |
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Phenelzine
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Mx: MAO inhibitor (irreversible)
Fx: Anti-depressant, amphetamine-like stimulant Tx: Strong anxiety, phobic states, low psychomotor, atypical depression (labile mood) S/E: Hypotension, vertigo, weakness, dry mouth, urination problem, ejaculation problem, insomnia. D/I: SEROTONIN SYNDROME (lots, esp. hyperpyrexia!) if mixed w/SSRIs, HYPERTENSIVE CRISIS if mixed with tyramine! Antidote: if HTN crisis, give PHENOXYBENZAMINE! (anti-adrenergic) |
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Phenobarbital
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Mx: barbiturate; GABA-A bind: Diff bind site than benzo, enhance bind of GABA and benzo to rec, incr open time, at high dose can open w/o GABA
Fx: CNS depression (sedation-hypnosis-anesthesia-coma-death), resp depression (like sleep but severe with pulm dz, CO2 response), P450 induce Kx: PO rapid absorb, low lipid soluble, cross placenta+BBB, liver elim, excr unch, metabs inactive, 2 day HL Tx: anticonvulsant long-term, grand mal/status epilepticus (see diazepam), anxiety (not much), hypnosis (not much, decr REM), hypnosedative withdrawal S/E: Physio+Psych dep, abrupt withdrawal fx, hypotension, CNS fx, P450 induce. |
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Phenoxybenzamine
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Phosphatidylinositol-4,5 biphosphate
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PIP2: precursor of IP3/DAG. Lithium depletes this, thus OVER TIME reducing activity of the IP3/DAG pathway.
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Piroxicam
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Mx: COX1/2 inhibitor
Kx: ONCE DAILY DOSAGE Tx: Arthritis, spondylitis S/E: Standard, plus ULCERS (10x!) D/I: LITHIUM (urine elim) |
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Platinum
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Polyethylene glycol
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Tx: bowel cleansing (cathartic)
Tox: renal damage if absorbed Antidote: Ethanol, dialysis. |
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Pralidoxime
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Mx: Reverses organophosphate damage to ACh esterase.
Tx: Malathion poisoning |
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Prednisone
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Mx: Steroid
Fx: ↑liver gluconeogenesis, ↑periph protein catab, ↑gly synthesis, ↓glu use in periph, sensitizes TG↔FFA, aldo fx, ↓Ca, anti-inflammatory (↓AA convert, ↓COX). Tx: steroid replenishment (Addison, CAH), anti-inflammatory, acute gout (into joint) |
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Probenecid
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Mx: organic acid, ↓UA reabsorption in tubule
Fx: Serum UA↓→Urine UA↑ Tx: Chronic gout (UA underproducers); don't correct underlying defect Kx: PO, start w/low dose S/E: May precipitate acute gout attack - give w/colchicine or NSAIDs, GI D/I: Aspirin (↓UA secretion) Tox: Hypersensitivity, renal stones (keep pH, volume up) |
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Procyclidine
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Mx: Antimuscarinic
Fx: Improves tremor+rigidity, but no fx on bradykinesia; less effective than L-DOPA Tx: Adjunct w/L-DOPA (Parkinson symptom exacerbation if not tapered off) S/E: Atropine-like (dry mouth, mydriasis, tachy, nausea, blah blah) |
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Propranolol
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Tx: anxiety (if tremor, sweat, tachy), lithium tremor
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Prostacyclin
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PGI2. Mx: Gs (↑cAMP).
Tx: Pulmonary HTN Vasc Fx: Vasodilator, ↓HTN, ↓Ca in vasc smooth musc. Blood Fx: Inhibit platelet agg (made by vasc endothelium). GI Fx: Increase GI activity (cont. circ), ↓acid. Lung Fx: N/A Renal Fx: Medulla+Cortex. ↑RPF, ↑H2O+Na excretion. Furosemide fx→stim COX. ♀ Fx: N/A CNS Fx: ↑Temp. Immune Fx: Suppress. |
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Prostaglandin E2
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Mx: GPCR metabotropic. Complex mechanism, 4 receptors (EP1-EP4).
Vasc Fx: Vasodilators/sphincter-dilators (↓HTN, ↓Ca in vascular smooth muscle). Blood Fx: Inhibit platelet agg (made by vasc. endothelium). GI Fx: Increases GI activity (contract long, relax circ), ↓acid, ↑mucus, tx NSAID/steroid s/e. Lung Fx: Powerful bronchodilator, but induce cough. Renal Fx: Medulla+Cortex. ↑RPF, ↑H2O+Na excretion. Furosemide fx→stim COX. ♀ Fx: Strong uterine contx. Dinoprostone tx abortion (vag 2nd tr, IV 1st/2nd tr), labor induce, soften cervix. CNS Fx: ↑Temp, ↑GH/prolac/TSH/FSH. Immune Fx: Suppress. |
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Prostaglandin F2
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Mx: Gq (IP3/DAG/Ca)
Vasc Fx: Vasoconstrictor. Blood Fx: N/A GI Fx: Increase GI activity (cont. long+circ). Lung Fx: Bronchoconstrictor, but no asthma involvement. Renal Fx: N/A ♀ Fx: Strong uterine contx. Can soften cervix, but no more drug. CNS Fx: N/A Immune Fx: N/A |
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Prostaglandin G2
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AA→PGG2→PGH2→[PGE2+PGF2+PGI2+TXA2]
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Prostaglandin H2
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AA→PGG2→PGH2→[PGE2+PGF2+PGI2+TXA2]
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Prostaglandin
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Reserpine
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Mx: depletes catecholamine stores
Tx: HTN, schizophrenia S/E: depression, Parkinson's? |
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Selegiline
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Mx: MAO-B inhibitor
Fx: Increases DA levels in brain (5HT, NE unchanged) Tx: Parkinsons (adjunct w/L-DOPA) S/E: Increased DA fx - nausea, hallucinations, dyskinesias, dizziness, confusion. Tox: High dose inhibits MAO-A - HTN |
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Serotonin
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Sodium bicarbonate
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IV, urine alkalinizes to pH 8
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Sodium carbonate
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Sodium nitrite
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Tx: Cyanide antidote, oxidized MetHb binds CN.
Tox: oxidizes Hb Fe, Hb→MetHb. Infants most. Antidote: Oxygen, if MetHb>30%, give methylene blue to activate reductase (1-2 mg/kg, 5+ makes MetHb). |
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Thromboxane
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Mx: Gq, made from PGH2. opposes PGI2.
Vasc Fx: Vasoconstrictor Blood Fx: Platelet agg, made by platelets. Released more during agg. GI Fx: N/A Lung Fx: Bronchoconstrictor, but no asthma connection. Renal Fx: N/A ♀ Fx: N/A CNS Fx: N/A Immune Fx: N/A |
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Tranylcypromine
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Mx: MAO inhibitor (reversible, long action)
Fx: Anti-depressant, amphetamine-like stimulant Tx: Strong anxiety, phobic states, low psychomotor, atypical depression (labile mood) S/E: Hypotension, vertigo, weakness, dry mouth, urination problem, ejaculation problem, insomnia. D/I: SEROTONIN SYNDROME (lots, esp. hyperpyrexia!) if mixed w/SSRIs, HYPERTENSIVE CRISIS if mixed with tyramine! Antidote: if HTN crisis, give PHENOXYBENZAMINE! (anti-adrenergic) |
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Triazolam
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Mx: Benzodiazepine, enhances GABA fx at GABA-A channel
Fx: Sed, hyp, anxiolysis, muscle relax, anterograde amnesia, anticonvulsant. Tx: Anxiety (panic attack, rapid) Kx: SHORT-acting, lipid soluble, active metabs, slow elim. S/E: Severe withdrawal, psych dep, active metabs, amnesiac, additive w/depressants Antidote: Flumazenil |
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Uric acid
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Vitamin C
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Tox: Releases Fe from hemosiderin, enhances bone turnover, acidosis in renal insufficiency.
Antidote: bicarbonate? |
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Zileuton
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Mx: Lipooxygenase inhibitor
Tx: Asthma |
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Extrapyramidal symptoms
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Drug-induced parkinsonism (give central anticholinergic), akathisia (give central cholinergic), tardive dyskinesia (give DA blocker)
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