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30 Cards in this Set

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