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Pharm Autonomic

USCSOM: Pharm: Autonomic Lecture Drugs

QuestionAnswer
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
Created by: jlellerm
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