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31 Cards in this Set

  • Front
  • Back
choline transporter (CHT) can be inhibited by
hemicholiniums
vesicle-associated transporter (VAT) can be inhibited by
vesamicol
VAMPs and SNAPs can be blocked by
(especially the VAMP synaptogamin)
botulinum toxin
Acetylcholine (Ach) receptors and effects at moderate dose
M3 - vasodilation, decreased TPR, reflex tachycardia
Acetylcholine (Ach) receptors and effects at high doses
M2 - bradycardia, decreased AV conduction, negative inotrope
M3 - bronchial constriction, secretion, salivating, sweat, urine, tears
Methacholine characteristics and uses
- longer half life
-diagnose bronchiolar hypersensitivity
- dx belladonna alkaloid poisoning
Carbachol effects, uses, adverse effects
nicotinic effects - autonomic ganglia, adrenal medulla, skeletal muscle
uses - topically in glaucoma
adverse - high doses - muscarinic effects on the heart -- cardiac arrest
Bethanechol charac, uses
-not susceptible to AchE, predominately M3, no nicotinic action
uses - reduce reflux (increase LES tone), urinary retention (detrusor contraction, decrease outlet resist of internal spincter)
muscarinic choline esters
-acetylcholine
-methacholine
-carbachol
-bethanechol
muscarinic alkaloids
-muscarine
-pilocarpine
muscarine characteristics and symptoms
activates muscarinic receptors with 100-fold potency of Ach
not destroyed by AchE, longer half life
no nicotinic activity
sx - salivation, sweating, tear flow; large doses - abd pn, nausea, diarrhea, blurred vision, dyspnea
pilocarpine effects
muscarinic - opthalmic effects predominate
- contracts spincter - miosis
-frees canal of Schlemm (narrow angle)
-enhances tone of trabecular network (wide angle)
-contracts ciliary - accommodation
nicotinic alkaloids
nicotine
succinylcholine
(nicotinic receptor agonists)
nicotine effects and use and
Nm - skeletal m contraction, depolarizing blockade
Nn - increased HR, vasoconstriction,gut motility and secretion, incresed resp rate, nausea and vomiting
--for smoking cessation
contraindications of cholinoceptor agonists
- peptic ulcers, GI disorders, asthma
Drugs that block effects of muscarinic agonists
- quinidine
- procainamide
- tricyclic antidepressants
indirect acting cholinomimetics
reversible - edrophonium, physostigmine, neostigmine, donepezil, tacrine
irreversible - echothiphosphate, malathion, parathion, sarin
erdophonium charac and uses
short acting
dx - differentiate MG from cholinergic crisis
physostigmine charac and use
-tertiary amine, enters CNS
- glaucoma, antidote in atropine od
neostigmine, pyridostigmine charac and use
quternary amine, doesnt enter CNS
- ileus, urinary retention, MG, reversal of non-depolarizing NM blockers
Donepezil and Tacrine charac and use
-lipid soluble (CNS)
-Alzheimer's
Organophosphates charac and use
-lipid soluble, long-acting AchE irriversible inhibitors
- glaucoma (echothiophosphate)
insecticides - malathion, parathion
nerve gas - sarin
sx of AchE inhibitor intoxication
Diarrhea
Urination
Miosis
Bronchiolar constriction
Bradycardia
Excitement
Lacrimation
Sweating
Salivation
muscarinic receptor antagonists
-atropine
-ipratropium
-benzotropine
nicotinic receptor antagonists(Nn and Nm)
hexamethonium
mecamylamine
neuromuscular blocking drugs
non-depolarizing - D-turbocurarine
depolarizing - succinylcholine
ipratropium prop, effects, uses
-M3 in bronchial SMCs and glands when inhaled, no CNS absorption
-decreases bronchoconstriction and secretions
-chronic obstructive lung disease and asthma
benztropine prop, effects, uses
-CNS absoption, muscarinic in brain
-dopaminergic-cholinergic balance, decrease GI/GU secretions, decrease motility, increase HR
-parkinson's
ganglionic blocking agents
hexamethonium and mecamylamine
D-turbourarine charac
-non-depolarizing neuromuscular blockers
-small doses prevent opening of Na channel
succinylcholine charac
-persistent depolarization, augmented by AchE inhibitors
-repolarization but desensitized