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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 |