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25 Cards in this Set
- Front
- Back
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Acetylcholine (ACh) |
Muscarinic Agonist - Choline ester - quaternary - no CNS - sensitive to cholinesterase - M receptors and N receptors - topical on conjunctiva - local |
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Carbachol |
Muscarinic Agonist - Choline ester - quaternary - no CNS - not sensitive to cholinesterase - M3 > M1 > M1 - affect N receptors - topical on conjunctiva - local |
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Bethanecol |
Muscarinic Agonist - Choline ester - quaternary - no CNS - not sensitive to Cholinesterase - M3 > M1 > M2 - No N activity - PO, SC administer ** avoid IV/IM admin** - systemic effects |
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Pilocarpine |
Muscarinic agonist - natural alkaloid - tertiary amine - enter CNS - M receptors only - glaucoma treatment **drug of choice for emergency IOC reduction - xerostomia (dry mouth from radiation or Sjogren) - oral |
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Muscarine |
Muscarinic agonist - nature alkaloid (mushrooms) - quaternary amonium - still can enter CNS - M receptors only - no therapeutic uses |
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Nicotine (carbachol) |
Nicotinic agonist |
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Edrophonium |
Reversible cholinesterase inhibitor - short acting 10-20min - diagnose MG (diff MG from cholinergic crisis) - if muscle power improve = MG |
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Physostigmine |
reversible cholinesterase inhibitor - tert amine = CNS -> convulsion in high dose - glaucoma - bladder/intestinal atony **antidote in atropine poisioning** |
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Neostigmine |
reversible cholinesterase inhibitor - last 0.5-2hr - quat amine -> no CNS action - poor oral absorption - treat paralytic ileus, urinary retention, treat symptoms of MG |
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Donepezil |
reversible cholinesterase inhibitor - lipid soluble - treat Alzheimer's |
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Organophosphates (parathion, etc) |
irreversible cholinesterase inhibitor - bind covalently to AChE -OH in active site - need to make new - nerve gas agents - can be used for glaucoma **atropine is antidote |
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Pralidoxime |
AKA PAM = Cholinesterase reactivators - oxime -> ** give as soon as possible to -aging** |
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MOA of Cholinergic agonists |
all Choline esters and natural alkaloids activate M1, M2, M3 receptors - postsynaptic -> alter function of effector organ - presynaptic -> inhib release of NT |
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choline esters and effect on nicotinic receptors |
some choline esters -> activation -> - initial => depolarize postjunction mem -> AP -> response in effector organ - depolarization blockade = prolonged activation of N receptors -> no depol -> no further AP -> response of organ is blocked |
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Pharm effects of Cholinergic agonists |
effects = that of postganglionic parasymp nerve impulses |
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Pharmacodynamics of Choline esters on the CVS (heart/vessels) |
heart - SA node -> -HR (M2 open K+ channels) - atria -> -refractoriness, -contractility - AV node -> -conduction, -automaticity, +refractoriness - vent -> few recep -> few effects (-NE release) **low dose -> direct effect counter by relfex tachy from vasodilation, high dose -> direct effect > relfex** vessels - general vasodilation (M3 -> NO release) |
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Pharmacodynamics of Choline esters on the GI and endocrine |
GI - +tone, +contract (peristaltic), +secretions of GI - relax sphincters (N stim in ganglionic peptidergic neurons), pure M agonist -> -effect - contract lower esophageal sphincter Endocrine - mild insulin secretion |
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Pharmacodynamics of Choline esters on the GU system |
GU = Micturition - +uretal peristalsis - contract detrusor - relax trigone and internal sphincter (decr effect if pure M agonist) - erection (negligible on uterus) |
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Pharmacodynamics of Choline esters on the eye |
Eye - contr sphinter of iris - contract ciliary muscle -> - +lens curve -> near vision focus - +aq humor outflow schlem cannal - incr secretion of lacrimal glad |
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Pharmacodynamics of Choline esters on the respiratory system |
Repiratory - bronchial sm muscle contract - +tracheobronchial secretions skin - +sweat gland secretions |
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Pharmacokinetics of choline esters |
absorption - oral = low (hydrophilic, hydrolized in GI) Dist = in periph tissue only (quaternary amines dont cross BBB to CNS) biotransform - ACh by acetylcholinesterase excretion - kidney |
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choline esters - adverse effects when locally admin (eye) |
ACh and carbachol - vision problem (far and dim light) - reddening stinging of the conjunctiva - cataract - long term - retinal detachment - long term |
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choline esters - adverse effects when systemic admin |
bethanechol - nausea (GI activity) & vomit (CTZ M receptor) - abdominal pain, diarrhea - cough (bronchospasm and +secretions) - sweating, acrimation, salivation - flushing - urinary urgency - low BP |
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choline esters - contraindication |
local (eye) - iritis, cataract, previous retinal detachment systemic - asthma/COPD - cardiac arrhythmia, miocardial disease, CAD - peptic ulcer, GI obstruct, IBD - urinary tract obstruction - hyperthyroidism |
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natural alkaloids - MOA, Pharm effects, adverse effects, and contraindications |
effects similar to choline esters except: ** greater for sweating and salivation** - can enter CNS - mycetism = mushroom poisoning |
