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Pharm Autonomic
USCSOM: Pharm: Autonomic Lecture Drugs
Question | Answer |
---|---|
What adrenergic receptors are stimulated by NE? | alpha-1, beta-1, alpha-2 |
What adrenergic receptors are stimulated by Epi? | alpha-1, beta-1, beta-2, alpha-2 |
What adrenergic receptors are stimulated by low doses of Dopamine? | D1 |
What adrenergic receptors are stimulated by moderate doses of Dopamine? | D1, Beta-1 |
What adrenergic receptors are stimulated by high doses of Dopamine? | alpha1, beta-1 |
What does Beta-1 activation do? | increases all cardiac functions |
What does alpha 1 activation do? | contracts smooth muscle |
What does Beta-2 activation do? | relaxes smooth muscle |
Botulinus toxin (botox) | inhibits ACh release |
Latrotoxin | increase ACh release; black widow |
Acetylcholinesterase (AChE) | neuromuscular junction, autonomic ganglia, post para-synapses |
Psedocholinesterase | plasma, liver, glial cells |
Acetylcholine | muscarinic agonist; not clinically useful; hydrolized too rapidly |
Bethanechol | muscarinic agonist; long duration, no nicotinic, contract GI and bladder, no CNS |
Pilocarpine | muscarinic agonist; treat glaucoma, CNS effects, not for systemic use (too many secretions) |
Muscarine | muscarinic agonist; Amanita fungi; mushroom tox, no nicotinic |
Edrophonium | reversible AChE inhibitor; brief action, rapidly eliminated |
Neostigmine | AChE ihibitor; slowly reversible, NO CNS effects |
Physostigmine | AChE inhibitor; slowly reversible, CNS effects; treats muscarinic antagonist tox |
Carbaryl | "Seven Dust" insecticide; slowly reversible AChE inhibitor |
Donepezil | slowly reversible AChE inhibitor; Alzheimers; CNS effects |
Echothiophate | irreversible AChE inhibitor; treat glaucoma |
Nerve Gases | irreversible AChE inhibitor; Sarin, VX series |
Parathion | irreversible AChE inhibitor; insecticide converted to active state by Cyt P450 |
Malathion | irreversible AChE inhibitor; degraded in plasma, a "safer" insecticide; treat head lice |
Pralidoxime (2-PAM) | cholinesterase reactivator; must be given in a timely manner after irreversible AChE inhibition |
SLUDGE-BAM | muscarinic activity: salivation, lacrimation, urination, defecation, GI cramps, Emesis, Bronchoconstriction/Bradycardia, Accomidation, Miosis |
6 therapeutic uses of AChE inhibitors | Glaucoma, GI Atony, Myasthenia gravis, reverse NM blockade, muscarinic antagonist intoxication, Alzheimers |
Atropine | natural muscarinic antagonist; belladonna; treat AChE inhibitors |
Scopolamine | muscarinic antagonist; CNS effects; sedative; motion sicknesses |
Ipratropium Bromide | synthetic muscarinic antagonist; inhalent used from asthma |
Glycopyrrolate | synthetic muscarinic antagonists; antispasmodics for treating irritable bowel |
Nicotine | nicotinic receptor agonists; depolarization block at autonomic ganglia |
Hexamethonium | ganglionic nicotinic antagonists; postural hypotension |
Decamethonium | neuromuscular nicotinic antagonists |
d-Tubocurarine | competitive neuromuscular blocker; long acting, no CNS; histamine release |
Atracurium | intermediate nondepolarizing neuromuscular blocker; safe for renal; can cause seizures |
Vecuronium | intermediate nondepolarizing neuromuscular blocker; |
Succinylcholine | depolarizing neuromuscular blocker; rapid onset, brief duration; pseudocholinesterase sensitive; tracheal intubation |
Dantrolene | control malignant hyperthermia; inhibits calcium release |
Metyrosine | inhibits tyrosine hydroxylase; block NE synthesis |
Reserpine | block NE synthesis; decrease symp function; cause major depression |
Amphetamine | increase NE release; also increase Ser and DA release in CNS; CNS stimulant |
Tyramine | increase NE release; found in fermented foods, "cheese" effect; metabolized by MAO-A |
Guanethidine | decrease release of NE; reuptake, block and release NE stores; antihypertensive, pheochromocytoma sensitive |
Tricyclic Antidepressants | blocks reuptake at adrenergic receptors |
Cocaine | blocks reuptake at adrenergic; indirect acting sympathomimetic amine; CNS stimulant |
Pheneizine | MAO inhibitor; antidepressant; avoid Tyramine |
Tranylcypromine | MAO inhibitor; antidepressant; avoid Tyramine |
Tolcapone | COMT inhibitor; increase DA and NE |
Phenylephrine | alpha 1 agonists; increase BP, mydriasis, increase outflow in eye |
Clonidine/Methyldopa | alpha 2 agonists; decrease NE release, decrease BP, antihypertensives |
Brimonidine | alpha 2 agonist; treat glaucoma without mydriasis |
Isoproterenol | non-selective beta agonists; increase all cardiac, bronchodilation, relax uterine smooth mm |
Dobutamine | beta 1 agonist; increase all cardiac, use for congestive heart failure |
Albuterol | beta 2 agonist; short acting, used in asthma |
Salmeterol | long acting beta 2 agonist; used in combination with other drugs |
Ritodrine | beta 2 agonist; terminate preterm labor, falling out of favor |
Norepinephrine | Alpha 1/2, Beta 1 agonist; cardiogenic shock; ischemia with subcut. injections |
Epinephrine | alpha 1/2, beta 1/2 agonist; low doses beta 1/2; high doses alpha 1 beta-1; |
Dipivefrin | prodrug for epinephrine; mydriasis and open angle glaucoma |
Dopamine (low dose) | D1 stimulation; vasodilation in renal and mesenteric vascular beds |
Dopamine (moderate dose) | D1 and beta-1 |
Dopamine (high doses) | alpha 1 and beta-1 |
Selegiline | MAO-B inhibitor; increased Dopa in CNS; treat Parkinsons |
Phentolamine | competitive alpha 1/2 antagonist; used in pheocromocytoma |
Phenoxybenzamine | long acting alpha 1/2 antagonist; used in pheocromocytoma |
Prazosin | alpha-1 receptor antagonist; "sin" drugs; antihypertensive, benign prostatic hyperplasia |
Propranolol | beta blocker; decrease heart output, block renin release; antihypertensive |
Timolol | decrease production of aq humor; glaucoma |
Pindolol | beta blocker with partial beta agonist; less efects on receptor up-regulation and plasma lipids |
Carvedilol | blocks beta and alpha-1; decrease BP and increase heart efficiency; CHF, antihypertensive |
Metoprolol/Atenolol | Beta-1 antagonist; renal excretion; antihypertensive |