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30 Cards in this Set
- Front
- Back
ganglion blockers and NMJ blockers make up
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antinicotinic drugs
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M1 subtype
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CNS, sympathetic postganglionic cell bodies and many presynaptic sites
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M2 subtype
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myocardium, smooth muscle organs, and some neuronal sites
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M3 subtype
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effector cell membranes, especially glandular and smooth muscle cells
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M4 subtype and M5
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greater role in CNS than periphery
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Atropine
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prototype of antimuscarinics
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tertiary antimuscarinic common use
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eye or CNS effects
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quanternary amine antimuscarinic common use
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peripheral effects with reduced CNS effects
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atropine excretion
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50% urine unchanged; remaining hydrolysis and conjugation products
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how long do atropine effects last
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>72 hours in eye; rapidly declines elsewhere
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atropine MOA
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reversible blockade of cholinomimetic actions at muscarinic receptors (M1, M2, and M3)
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muscarinic drugs that are inverse agonists
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atropine, pirenzepine, trihexyphenidyl, AF-DX 116, 4-DAMP, and a methyl derivative of scopolamine
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tissues most sensitive to antimuscarinics (atropine)
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salivary, bronchial, and sweat glands
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antimuscarinics and the eye
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mydriasis (dilation) and cycloplegia (weaken contraction of ciliary muscle)
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cardiovascular and antimuscarinics
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tachycardia=blockade of vagal slowing
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atropine in presence of high vagal tone
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significantly reduce PR interval by blocking muscarinic receptors in AV node
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parasympathetic innervation of vessels
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stimulation dilates coronaries; constricts skeletal muscle vascular bed
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atropine on lungs
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bronchodilation and decreased secretions
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atropine and GI tract
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reduces motility and secretion for basal secretion
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atropine and GU
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relaxes smooth muscle of ureters and bladder wall slowing voiding
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antimuscarinic used in motion sickness
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scopolamine
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mydriasis for funduscopic exam
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alpha-adrenoceptor stimulant drugs; antimuscarinics work, but are only used if prolonged action required or cycloplegia
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inhalation antimuscarinic used in asthma
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ipratropium; recently tiotropium in COPD
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antimuscarnic somewhat selective for M3 and used to relieve bladder spasm
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oxybutynin
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pralidoxime
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cholinesterase regenerator cmpd-doesn't reverse CNS effects
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pyridostigmine use
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pretreatment-reversible enzyme inhibitor of irreversible organophosphate inhibitor
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rapid-onset mushroom poisoning symptoms
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muscarinic excess=nausea, vomiting, diarrhea, urinary urgency, vasodilation, reflex tachycardia, sweating, salivation, sometimes bronchoconstriction
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atropine OD treatment
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mostly symptomatic treatment
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cardiovascular and ganglionic blockers
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marked decrease in arteriolar and venomotor tone (sympathetic vasoconstrictor fibers); BP falls, marked in upright position (postural reflexes blocked)
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trimethaphan
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ganglion blocking drug; hypertensive emergencies and dissecting aortic aneurysm to produce hypotension
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