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12 Cards in this Set
- Front
- Back
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MOA of M1 and M3 muscarinic receptors?
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receptor activates phospholipase C --> release DAG (modulates PKC for secretion) and IP3 (releases Ca from storage which contracts smooth muscle)
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MOA of M2 muscarinic receptors?
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1. receptor coupled to adenylyl cyclase through inhibitory Gi coupling protein
2. receptor linked to potassium channels by G protein in heart and elsewhere, receptor activation facilitates opening of channels |
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MOA of nicotinic receptors?
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activation of receptor --> opening of Na+/K+ channel --> depolarization of cell --> EPSP
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muscarinic agonists cause parasympathomimetic effects except for what?
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vasodilation and decreased BP
(d/t release of endothelium derived relaxing factor - i.e. NO) tachycardia (d/t reflex stimulation of heart after vasodilatory effect) sweating |
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what is the only clinical use of direct-acting nicotinic agonists?
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skeletal muscle paralysis (succinylcholine)
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types of cholinesterase inhibitors?
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carbamates (intermediate long-acting)
organophosphates (very long acting) edrophonium (short acting) |
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ChEI used for rapid reversal of non-depolarizing neuromuscular blockade and in diagnosing myasthenia?
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edrophonium
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administering edrophonium will _____ in myasthenic crisis, but will ______ in cholinergic crisis.
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improve muscle strength
weaken muscle strength |
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DOCs for tx of myasthenia?
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neostigmine, physostigmine, ambenonium, pyridostigmine
(carbamates) |
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two organophosphates used in medicine?
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malathion (scabicide), metrifonate (antihelminthic)
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toxic exposure to pesticides made with this cholinesterase inhibitor can be rapidly fatal
antidote? |
parathion
atropine |
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S/S of toxic exposure to ChEIs?
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diarrhea, urination, miosis, bronchoconstriction, bradycardia, excitation of skeletal muscle and CNS, lacrimation, salivation, sweating
(DUMBBELSS) |
