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Pharm-Drugs (Exam 3)
| Question | Answer |
|---|---|
| Acetylcholine | NT, metabolized quickly so not therapeutically useful, nonspecific (activate N & M receptors), little CV effects, increase GI motility, stimulate bladder, miosis, bronchoconstriction, increase glandular secretions |
| Epinephrine | NT, increase HR, CX, CO, reflex bradycardia, bronchodilation, dec. GI motility, dec. intraocular pressure TX: asthma, anaphylaxis, cardiac arrest |
| Norepinephrine | NT, inc. HR, CX, CO, reflex bradycardia, inc. renin in kidney |
| Dopamine | NT, inc. HR, CX, CO, inc. renin in kidney TX: shock caused by dec. CO and dec. renal function, parkinson's, CHF |
| Seratonin | NT? |
| Amphetamine | indirect symphathomimetic (displace NE from vesicles), competitively inhibits NE reuptake, inhibits MAO activity -> NE lingers TX: narcolepsy |
| Tyramine | indirect symphathomimetic/sympathetic modulator (alpha-1, beta-1)- cheese, beer, wine; compete with NET contraind. in pts taking MAOI: incr. HR, CX, CO (reflex bradycardia), initial potentiates NE effects, then depletes NE, inc. renin release in kidney |
| Ephedrine | symp modulator-displaces NE from vesicles, compet. inhib NE reuptake, inhib MAO -> NE lingers (acts like amphetamine) USES: bronchial relax (beta-2) and mydriasis w/o cycloplegia (alpha-1), used as bronchodilator, eye exams, nasal decong., VASOSPASM |
| Reserpine | sympathetic modulator, binds VMAT-2 irreversibly inhibits vesicular conc. of NE and DA -> SNS depletion TX: HTN-gradual decline in BP and HR, long duration action |
| Guanethidine | sympathetic modulator, depletes NE in SNS (does not cross BBB), acts like reserpine, false NT TX: severe hypertension |
| Phenylephrine | alpha-1 selective (receptor agonist)-reflex bradycardia TX: nasal decongestant |
| Clonidine | alpha-2 selective (receptor agonist)- decrease SNS outflow, decrease BP TX: hypertension |
| Alpha Methyldopa | alpha-2 selective (receptor agonist)-competitive inhibitor of DOPA decarboxylase -> deplete terminals of DA and NE TX: HTN during pregnancy SEs: hepatotoxicity, autoimmune hemolytic anemia |
| Phentolamine | alpha antagonist (nonselective)-dec. BP progressively, hypotension, miosis, nasal congestion, inhibit ejacuation, acts similar to phenoxybenzamine TX: short-term control of BP and manage pheochromocytoma |
| Phenoxybenzamine | alpha antagonist (nonselective)-increase SNS outflow, reflex tachycardia, dec vasocx, biphasic: comp. blockade of alpha receptors followed by a non-comp. block that is irreversible TX: pheochromocytoma |
| Doxazosin | alpha-1 antagonist-highly selective a-1 blocker but non-selec. for alpha subtypes, long half-life and long duration of action TX: HTN and BPH |
| Prazosin | alpha-1 antagonist-reflex tachycardia, decrease vasocx, smooth muscle RX, binds alpha-1 glycoprotein, inc. dose slowly TX: HTN and BPH, CHF SEs: syncope |
| Alfuzosin | alpha-1 antagonist-selective for alpha-1A in urinary tract TX: BPH |
| Tamsulosin | alpha-1 antagonist (alpha-1A, 1D)-reflex tachycardia, dec. vasocx, lower incidence of orthostatic HTN TX: BPH SEs: weakness (muscle or psychogenic) |
| Terazosin | alpha-1 antagonist-little first pass metabolism, low tachycardia TX: HTN, CHF SEs: syncope |
| Yohimbine | alpha-2 antagonist-inc. HR and BP, no clinical uses |
| Isoproterenol | beta agonist (nonselective)-powerful bronchodilator but not drug of choice due to cardiac effects SEs: tachycardia, palpitations, headache, flushing TX: emergencies to stimualate HR in pts with bradycardia or heart block |
| Dobutamine | alpha-1 & beta-1 agonist (mostly beta-1)-increase cardiac efficiency, HR, CX, CO, incr. DBP and SBP, incr. renin secretion TX: decompensated heart failure SEs: tachycardia, arrythmias |
| Albuterol | beta 2 agonist-bronchodilation, short acting acute relief, nebulizer TX: bronchospasm |
| Metaproterenol | beta 2 agonist-bronchodilation, medium duration (oral administration) TX: bronchospasm, obstructive airway disease |
| Terbutaline | beta 2 agonist-bronchodilation, minimal tachycardia TX: obstructive airway disease |
| Salmeterol | beta 2 agonist (long-acting)-slow acting, bronchodilation, must be accompanied by steriod for nebulizer TX: bronchospasm |
| Formoterol | beta 2 agonist (long-acting)-fast acting, bronchodilation, highly lipophilic TX: bronchospasm |
| Propanolol | beta antagonist (nonselective)-dec. HR, CX, CO; dec. SBP, bronchocx, dec. renin secretion, lipid soluble, fast acting, short half life, first pass effect TX: HTN and migrane, stage anxiety (low dose) |
| Pindolol | beta antagonist (nonselective)-partial agonist (ISA) TX: HTN in pts with bradycardia or exercise intolerance |
| Carvedilol | beta antagonist (nonselective beta, alpha-1 blocker), short half-life, no ISA, extensively metabolized by P450 TX: CHF |
| Labetalol | beta antagonist (nonselective beta, alpha-1 blocker)-dec. HR, CX, CO; dec. SBP, bronchocx, dec. renin secretion, ISA at beta-2 receptor TX: HTN and HTN emergencies |
| Acebutolol | beta-1 antagonist (cardio selective), partial agonist (ISA), dec. HR, CX, CO TX: HTN, arrythmias, for pts with bradycardia and exercise intolerance |
| Metoprolol | beta-1 antagonist (cardio selective), moderate lipid solubility, first pass effect TX: HTN |
| Atenolol | beta-1 antagonist (cardio selective)-dec. HR, CX, CO; dec. SBP, long-lasting, specific, reduced CNS activity, no bronchocx, dec. renin secretion, long half-life TX: HTN w/o bronchocx |
| Bisoprolol | beta-1 antagonist (cardio selective)-well tolerated, no ISA activity, long half-life TX: std. when combined with ACE inhibitor and diuretic -> HTN SEs: bradycardia |
| Esmolol | beta-1 antagonist (cardio selective), very short half-life TX: admin. IV where immediate onset of blockade is required |
| Bethanechol | muscarinic agonist- TX: enhance intestinal activity and promote urination, reduced CV SEs compared to carbachol or methacholine, more selective (M3 in GI and bladder) |
| Pilocarpine | muscarinic agonist-similar to synthetic agents with similar SE and no receptor selectivity TX: first choice for open angle glaucoma (topical) SEs: impaired night vision, spasms of accommodation |
| Carbachol (Carbamylcholine) | muscarinic agonist TX: open angle glaucoma, useful alternative when resistance to pilocarpine or physostigmine |
| Atropine | muscarinic antagonist-brady (low), inc. HR (normal) vasocx, bronchodl, dec GI motiliy, urine retention, mydriasis TX: GI spasms, eye exams, CHEI toxicity, anethesic adjuvant, motion sickness, overactive bladder, ulcer, anti-parkinsonism |
| Scopolamine | muscarinic antagonist-brady (low), incr. HR (normal), vasocx, bronchodl, dec gastric motility, urine retention, mydriasis TX: GI spasms, eye exams, CHEI toxicity, anethesic adj, motion sickness, overactive bladder, ulcer, anti-parkinson SEs: CNS effec |
| Pirezepine | muscarinic antagonist (M1)- TX: used with H-2 blockers to reduce gastric acid secretions to produce gastric ulcer healing |
| Ipratropium | muscarinic antagonist, decreased bronchial secretions, bronchocx TX: COPD |
| Tiotropium | muscarinic antagonist-bronchial effects similar to tiptropium, administered as an inhalant, long duration of action (24h) TX: asthma, COPD |
| Tubocararine | competitive NMJ blocker-inc. HR, dec. BP, resp. paralysis, bronchocx DI: aminoglycosides and tetracyclines CONTRA: asthma, MG TX: procedures that require muscle paralysis |
| Atracurium | competitive NMJ blocker-? TX: procedures that require muscle paralysis |
| Mivacurium | competitive NMJ blocker-more bronchocx, inc. histamine release, short duration of action, dec. cardiac effects (less tachycardia) CONTRA: asthma, compromised pulmonary fx TX: procedures that require muscle paralysis |
| Vecuronium | competitive NMJ blocker-inc. cardiac effects (more tachycardia), dec. histamine release (less bronchocx) TX: procedures that require muscle paralysis |
| Succinylcholine | depolarizing NMJ blocker-dec. HR, inc. BP, resp. paralysis, slight histamine release DI: w/ halothane (abnormal ryanodine receptor) -> malignant hyperpyrexia |
| Botulinum toxin | ACh release inhibitor (irreversible)-cleaves synaptobrevin and SNAP to prevent vesicle fusion/release TX: dystonias, spasticity, stroke, chronic anal fissure, severe wrinkles, spasmodic dysphonia, hyperhydrosis |
| Neostigmine | AChE inhibitor (reversible)-reflex tachy, vasodilation, bronchocx, inc secretions, inc. GI motility, micturition, miosis, skeletal m. fasiculation, CNS depression TX: paralytic ileus, tx of MG, xerostomia |
| Physostigmine | AChE inhibitor (reversible)-reflex tachy, vasodilation, bronchocx, inc secretions, inc. GI motility, micturition, miosis, skeletal m. fasiculation, CNS depression TX: atropine toxicity (crosses BBB) |
| Edrophonium | AChE inhibitor (reversible)-very short acting TX: diagnosis of MG, PAT |
| Diisopropyl flurophosphate (DFP) | AChE inhibitor (irreversible, organophosphate)-reflex tachy, vasodilation, bronchocx, inc secretions, inc. GI motility, micturition, miosis, skeletal m. fasiculation, CNS depression, volatile, lipid soluble, cross BBB |
| Nerve Gases (Soman) | AChE inhibitor (irreversible, organophosphate)--reflex tachy, vasodilation, bronchocx, inc secretions, inc. GI motility, micturition, miosis, skeletal m. fasiculation, CNS depression |
| Echothiphate | AChE inhibitor (irreversible, organophosphate)--reflex tachy, vasodilation, bronchocx, inc secretions, inc. GI motility, micturition, miosis, skeletal m. fasiculation, CNS depression |
| 2-pralidoxime (2-PAM) | AchE reactivator-splits covalent bond, forms oxime-phosphonate -> leaves regenerated ChE TX: reverses CHEI toxicity |
| Dantrolene | skeletal muscle relaxant-binds ryanodine receptor -> prevent Ca2+ release TX: malignant hyperpyrexia caused by succinylcholine+halothane SEs: muscle weakness, sedation, hepatitis |
| Nicotine | nicotinic agent-Nm and Nn agonist, can produce depolarization blockade in toxic doses SEs: respiratory stim leading to arrest, convulsions, nausea |
| Varenicline | partial nicotine receptor agonist selective for alpha4beta2 nicotinic receptor, long half-life TX: nicotine addiction SEs: weight gain |
| Teriparatide acetate | synthetic PTH, diagnostic for pseudohypoparathyroidism MOA: inc extracell and circul. Ca2+ TX: daily intermittent injection for osteoporosis in men and postmen women at high risk of fracture SEs: may lead to hypercalcemia |
| Calcitonin | MOA: dec. osteoclast-mediated Ca2+ mobilization TX: severe hypercalcemia (SQ or IM every 12 hrs), osteoporosis (when HRT contraind), paget's disease SE: nausea, facial flushing, swelling (hands), inflamm rxn, urticaria |
| Calcitriol (Vit D), Dihydrotachysterol | MOA: inc. intestinal Ca2+ uptake, inc. osteoclast different, inc. osteocalcin express. TX: hypocalcemia, hypoparathyroidism, pseudoparathyroidism, osteoporosis (combo with ca2+), rickets and osteomalacia, impaired vit D synthesis SE: hypervitaminosis |
| Aledronate, Ibandronate, Zoledronic acid | bisphosphonates MOA: inhibit bone resorption, may produce gains in bone mass TX: osteoporosis (dec fracture risk-50%), paget's disease, hypercalcemia assoc with malignancy SE: hypocalcemia, hypophosphatemia, upper GI irritation |
| Allopurinol | inhibitor of uric acid synthesis-standard txt for chronic tophaceous gout MOA: comp. inhibitor of xanthine oxidase SE: maculopapular rash, GI, hepatotoxicity, fever, hypersens. -not useful for acute gout attacks -inhibit kidney reperfusion injury |
| Febuxostat | inhibitor of uric acid synthesis, selective inhibitor of xanthine oxidase -rapidly and extensively absorbed TX: chronic gout (prophylactic NSAIDs or colchicine used in beg to prevent gout attack) SE: GI intolerance, hepatic function alterations |
| Probenecid | uricosuric agent-inhibit proximal tubule resorption, oral admin, not used in acute gout attacks TX: hyperuricemia control DI: PCN, ASA, sulfa, allopurinol TOX: GI, dermatitis, nephrotic syndrome |
| Colchicine | gout pain and inflammation MOA: binds microtub tubulin -> dec. urate phagocytosis -admin oral TOX: GI, blood dyscrasias, CNS depression, shock TX: gouty arthritis attacks, pseudogout, fam. med fever |
| Indomethacin | gout pain and inflammation, anti-inflammatory TX: acute gouty attacks -not used for chronic gout or prophylaxis |
| Rasburicane | increases uric acid degradation-lowers uric acid levels better than allopurinol TX: initial management of pediatric pts with chemo-induced hyperuricemia SE: prod of antibodies, acute renal failure, anaphalaxis, GI abnormalities |
| Alprazolam | benzodiazepines-bind a1-gamma1 on GABA-A receptor, dec. neuron activity, short acting TX: anxiety, depression |
| Chlordiazepoxide | benzodiazepines-bind a1-gamma1 on GABA-A receptor, dec. neuron activity, rapidly absorbed, short acting TX: anxiety, alcohol withdrawal TOX: lots! |
| Clonazepam | benzodiazepines, anti-convulsant-bind a1-gamma1 on GABA-A receptor, dec. neuron activity, long acting TX: status elipticus TOX: lots! |
| Diazepam | benzodiazepines, anti-convulsant-rapidly absorbed, long acting TX: anxiety, status epilepiticus TOX: lots! |
| Flurazepam | benzodiazepines-bind a1-gamma1 on GABA-A receptor, dec. neuron activity, long acting TX: insomnia TOX: lots! |
| Triazolam | benzodiazepines-bind a1-gamma1 on GABA-A receptor, dec. neuron activity, rapidly absorbed, very short acting TX: insomnia TOX: lots! |
| Pentobarbital, Secobarbital | barbituate-act at GABA-A receptor -> prolong Cl channel opening -> inhibition, short-intermediate acting -drugs of abuse TOX: excess sed, confusion, lethargy, tolerance, phys/psyh dependence -> WD, respiratory arrest |
| Flumazenil | BZ-1 and BZ-2 receptor antagonist-reverse toxicity caused by benzos and non-benzos, not effective with other agents, short acting, must be given IV |
| Busopirone | alternative anxiolytic-slowly develop anti anx effect without sedation MOA: no GABA, maybe 5HT1A? TX: general anx disorder (not panic/PTSD) -no sedation, dependence, withdrawal, cross tolerance, no muscle relaxation |
| Anti-histamines | may produce some anxiety relief as consequence of sedative properties, useful in pts prone to abuse of benzos |
| Amitriptyline | TCA-inhibit NE and 5-HT reuptake TX: depression, eunuresis, pain, ADHD TOX: lots! SE: pronounced anti-ACh visual effects (mydriasis and dec. accomodation) |
| Nortriptyline | TCA-inhibit NE and 5-HT reptake TX: depression, eunuresis, pain, ADHD TOX: lots! |
| Imipramine | TCA-inhibit NE and 5-HT reuptake TX: depression, eunuresis, pain, ADHD TOX: lots! |
| Clomipramine | TCA TX: depression, eunuresis, pain, ADHD, OCD TOX: lots! |
| Desipramine | TCA-inhibit NE reuptake TOX: lots! sudden death in children TX: depression, eunuresis, pain, ADHD |
| Bupropion | cyclic antidepressant-inhibit DA reuptake TX: depression, nicotine withdrawal -dec. CV SEs, dec. sexual complications, dec. seizure threshold |
| Mirtazapine | cyclic antidepressant-enhance NE release |
| Trazodone | cyclic antidepressant-heavily promoted, rel. poor AD, few SEs, sedation, good hypnotic -produces priapism |
| Fluoxetine | SSRI-inhibit 5-HT reuptake -long acting, active metabolite, inhib p450 system TX: depression, OCD, bulimia TOX: lots!-inc risk of suicide DI: MAOI -> seratonin syndrome SE: weight loss |
| Sertraline | SSRI-like fluoxetine but less akathesia, no inhib of p450 system, shorter half-life |
| Paroxetine, Fluvoxamine | SSRI-similar to sertraline, some inhib of p450 system (P>F), short half-life |
| Citalopram | SSRI-similar to sertraline, most selective, widely used |
| Duloxetine | SNRI? |
| Venlafaxine | SNRI? |
| Phenelzine | MAOI TX: depression, narcolepsy, phobia anxiety D/O, OCD TOX: dec BP, headache, sexual dysfunction, hypertension/hypotension DI: tyramine->hypertensive crisis -mood elevation in depressed/normal indiv. |
| Selegiline | MAOI-relatively selective for MAO-B, used in PD, also approved for major depression |
| Midazolam | benzodiazepines-bind a1-gamma1 on GABA-A receptor, dec. neuron activity, sleep dose-response curve, short acting, water soluble |
| Zolpidem | non-benzo BZ1 agonist, short acting TX: insomnia TOX: bizarre nighttime behavior, less SEs than benzos/barbs (reversed by flumazenil) |
| Thiopental | barbituates-act at GABA-A receptor -> prolong Cl channel opening -> inhibition, ultra short acting TX: anesthesia adjunct TOX: excess sed, confusion, lethargy, tolerance, phys/psyh dependence -> WD, respiratory arrest |
| Ramelteon | melatonin-1 and 2 agonist -> decrease sleep onset TX: insomnia (sleep onset problems) |
| Lithium | anti-manic-Na+ or Mg2+ replacement -> dec. IP3/DAG, dec. cAMP, dec. NT release, oral absorp, narrow therapeutic window, only drug that dec. suicide TX: mania TOX: acute-fatigue, weakness, tremor, chronic-dec thyroid, diabetes insipidus, nephritis, edema |
| Valproate | anti-manic, anti-convulsant-block Na+, enhance GABA, used for early mania, used as lithium adjunct TX: mania TOX: sedation, GI, hepatotoxicity, birth defects |
| Carbamazepine | anti-manic, anti-convulsant-block Na+ and enhance GABA, use anti-convulsant dose, used if lithium inadequate TX: mania TOX: diplopia, ataxia, GI, aplastic anemia, birth defects, agraunlocytosis |
| Olanzapine | anti-manic-blocks 5HTA>D2>alpha TX: schizophrenia, schizoaffective disorder, bipolar diorder, mania, tourette's syndrome TOX: weight gain, metabolic syndrome -less SEs |
| Aripiprazole | anti-manic-partial agonist at D2 and 5HT2A TX: schizophrenia, schizoaffective disorder, bipolar diorder, mania, tourette's syndrome -less SEs, no weight gain |
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