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ANS Pharmacology
Fill-in-the-blanks about adrenergic and cholinergic drugs
Drug | is used to treat... | because it is a(n)... | Major effect... |
---|---|---|---|
Methyldopa | Hypertension | alpha-2 agonist | decrease SNS effects on vasculature |
Prazosin | Hypertension AND urinary retention from BPH | alpha-1 antagonist | decrease SNS effects on vasculature and smooth muscle |
Terazosin | Hypertension AND urinary retention from BPH | alpha-1 antagonist | decrease SNS effects on vasculature and smooth muscle |
Doxazosin | Hypertension AND urinary retention from BPH | alpha-1 antagonist | decrease SNS effects on vasculature and smooth muscle |
Phenoxybenzamine | Hypertension in PTs with excess catecholamines | nonselective alpha antagonist | decrease SNS effects on vasculature |
Phentolamine | Hypertension in PTs with excess catecholamines | nonselective alpha antagonist | decrease SNS effects on vasculature |
Guanethidine | Hypertension | adrenergic neuron blocker | decrease SNS effects by promoting degradation of NE |
Amphetamine | ADHD, obesity, fatigue, narcolepsy | indirect sympathomimetic (blocks NE reuptake and potentiates its effects) | potentiate NE effect in synapse |
Reserpine | Hypertension (formerly) | indirect sympathoplegic (prevents NE entry into vesicles and promotes NE degradation) | promote NE degradation --> decrease SNS activity |
Dopamine | poor renal perfusion by increasing natriuresis; shock; CHF, hypotension | direct sympathomimetic AND activates D1 receptors | increase SNS activity, increase natriuresis |
Epinephrine | Brochospasm, anaphylactic shock, restoration of cardiac activity following MI | direct sympathomimetic | activate all adrenergic receptors |
Norepinephrine | Hypotension | direct sympathomimetic | increase SNS effect on vasculature |
Isoproterenol | Bradycardia or heart block in emergencies | nonselective beta agonist | increase SNS effect on heart and CO |
Dobutamine | CHF | (mainly) beta-1 agonist; also some alpha-1, beta-2 agonist effects | increase inotropy |
Phenylephrine | Hypotension, induce mydriasis | alpha-1 agonist | increase peripheral resistance, constrict pupillary dilator muscle |
Methoxamine | Hypotension, induce mydriasis | alpha-1 agonist | increase peripheral resistance, constrict pupillary dilator muscle |
Albuterol | Asthma, bronchospasm, emphysema, suppress premature labor | beta-2 agonist | bronchodilation, smooth muscle relaxation |
Metaproterenol | Asthma, bronchospasm, emphysema, suppress premature labor | beta-2 agonist | bronchodilation, smooth muscle relaxation |
Terbutaline | Asthma, bronchospasm, emphysema, suppress premature labor | beta-2 agonist | bronchodilation, smooth muscle relaxation |
Ritodrine | Relax uterine smooth muscle, suppress premature labor | beta-2 agonist | bronchodilation, smooth muscle relaxation |
Ephedrine | Nasal congestion, orthostatic hypotension, bronchiolar asthma, induce mydriasis | alpha-1 and beta-2 agonist, indirect sympathomimetic (stimulates NE release) | increase BP, decrease secretions, bronchodilation, CNS stimulant |
Yohimbin | erectile dysfunction (formerly) | alpha-2 antagonist | increase SNS tone - hypertension, some peripheral vasodilation |
Propranolol | heart disease, hypertension, arrythmias, angina | nonselective beta blocker | decr inotropy, decr heart rate, decr CO, decr myocardial O2 demand, may cause bronchospasm (B2) |
Pindolol | heart disease, hypertension, arrythmias | nonselective beta blocker; partial beta agonist | less likely than propranolol to cause bradycardia, also less likely to help w/angina, may cause bronchospasm |
Atenolol | heart disease, hypertension, arrythmias, angina | beta-1 antagonist (some relative B2 activity) | decr inotropy, decr heart rate, decr CO, decr myocardial O2 demand |
Metoprolol | heart disease, hypertension, arrythmias, angina | beta-1 antagonist (some relative B2 activity) | decr inotropy, decr heart rate, decr CO, decr myocardial O2 demand |
Labetalol | heart disease, hypertension, arrythmias, angina | beta-1 antagonist, partial alpha-1 antagonist + beta-2 agonist | decr inotropy, decr heart rate, decr CO, decr myocardial O2 demand, some peripheral vasodilatory effects |
Acetylcholine | direct cholinergic | PNS activation (muscarinic and nicotinic receptors) | |
Arecoline | Recreational drug | muscarinic agonist | Potentiate PNS effects |
Atropine | Bradycardia, organophosphate toxicity, mydriatic, noninfectious diarrhea | muscarinic antagonist (nonselective) | Incr HR; "red as a beet, blind as a bat, dry as a bone, hot as a hare, mad as a hatter" |
Botulinum Toxin | Muscle spasticity, wrinkles | spasmoloytic, anticholinergic | inhibits presynaptic vesicle fusion (+ ACh release) at NMJ |
Curare | (formerly) paralytic/muscle relaxant for surgery | antinicotinic, nondepolarizing NM blocker, nonselective for all ACh receptors, competitive antagonist | Muscle paralysis, considerable histamine release (edema, hypotension, tachycardia) |
Edrophonium | diagnose myasthenia gravis | noncarbamate AChE inhibitor | Tensilon test - transient incr ACh --> sudden, short-lasting improvement in MG Sx |
Glycopyrrolate | Preoperatively: reduce secretions | muscarinic antagonist (nonselective) | Blocks ACh @ PNS sites on smooth m., secretory glands |
Hexamethonium | (formerly) paralytic and treatment of hypertensive crises | Nn antagonist at PNS and SNS ganglia | Loss of ALL autonomic tone |
Neostigmine | Reverse nondepolarizing NM blockade from surgical anesthesia; myasthenia gravis | anticholinesterase | reverse nondepolarizing block; PNS stimulation of heart |
Muscarine | muscarinic agonist | bradycardia, vasodilation, miosis, PNS stimulation | |
Nicotine | smoking cessation | nicotinic agonist, relatively selective for Nn receptor | Crosses BBB: PNS + SNS activation: EPI release from adrenal medulla, incr HR, BP, vasoconstriction |
Parathion | insecticide | anticholinesterase, organophosphate | insects metabolize into active AChE inhibitors |
Physostigmine | glaucoma, atropine overdose, myasthenia gravis, Alzheimer's | anticholinesterase | crosses BBB, miosis |
Pilocarpine | glaucoma | muscarinic agonist (nonselective) | miosis, increased muscle tension in ciliary body --> decr intraocular pressure |
Pralidoxime (2-pam) | Organophosphate toxicity | cholinesterase regenerator | Remove phosphorylating group from AChE |
Rocuronium | surgical paralytic | antinicotinic, nondepolarizing NM blocker, Nm selective, competitive antagonist | Prevents depolarization at NMJ --> skeletal muscle paralysis |
Sarin | Organophosphate toxin (nerve gas) | anticholinesterase | ACh accumulates @ NMJ, ganglia: DUMBELS (diarrhea, urination, miosis + muscle weakness, bronchospasm, excitation, lacrimation, seizures, sweating, salivation), coma, death |
Scopolamine | motion sickness; preanesthetic for sedation, amnesia, drying of secretions | antimuscarinic | decrease GI tone, motility, secretions; more CNS FX than atropine |
Succinylcholine | Paralytic for emergency tracheal intubation | depolarizing blocker, Nm selective nicotinic agonist | Rapid onset of paralysis, Na+ channels inactivated until endplate repolarizes |
Varenclinine (Chantix) | smoking cessation | partial Nn receptor agonist | CNS, nausea, suicidal ideation (??) |
Clonidine | Hypertension | alpha-2 agonist | decrease SNS effects on vasculature |