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Cholinergic Agonists
Neuro 3 Pharm
24
Pharmacology
Graduate
06/06/2011

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Cards

Term
Hemicholinium
Definition
Blocks entry of choline into cell- so anticholinergic?
Term
Vesamicol
Definition
Blocks uptake of ACh into vesicles
Term
Botulism toxin
Definition
Blocks release of ACh vesicles
- removal of 2 AAs from synaptobrevin- prevents vesicle fusion
- Uses: strabismus, estropia, frown lines, stroke paralysis, migraines, stuttering, incontinence, club foot, etc
Term
M1
Definition
- neural
- only on parasympathetic postsynaptic
- increases IP3 and DAG, affecting Ca levels
Term
M2
Definition
- cardiac
- only on para post
- decreases HR, contractility, and conduction by decreasing cAMP and increasing K efflux
Term
M3
Definition
- glandular
- eye, GI, bladder, bronchoconstrition
- via IP3, DAG, Ca
Term
Bethanechol
Definition
- muscarinic agonist
- treats flaccid abdomen, urinary retention
- adverse effects: bronchospasms, increased exocrine secretions
Term
Pilocarpine
Definition
- muscarinic agonist
- treats glaucoma, dry mouth
- adverse effects: bronchospasms, increased exocrine secretions
Term
Nicotine
Definition
- At lose doses, simulates nicotinic receptors
- smoking cessation
- at high doses, it can inhibit NR and cause death
Term
Acethylcholinesterase
Definition
- acts only on ACh
- located on membrane
Term
Butyrylcholinesterase
Definition
- in plasma, intestine, skin, etc
- acts on ACh, benzylcholine, succinylcholine
- located in plasma
Term
Examples of organophosphates
Definition
- glaucoma drugs- isoflurophate, echothiophate
- nerve gas
- insecticides- parathion, malathion
Term
Area obstructed in chronic glaucoma
Definition
- schlemm's canal
Term
Edrophonium
Definition
- inhibits AChE (5-10 minutes)
- used to diagnose myasthenia gravis
- can cause cholinergic crisis
- short acting anticholinesterase drug
Term
Donepezil
Definition
- inhibits AChE
- treats Alzheimers
- Adverse effects: insomnia
Term
Pyridostgmine
Definition
- inhibits AChE
- treats myasthenia gravis
- can cause cholinergic crisis
Term
Echothiophate
Definition
- irreversible inhibitor of AChE
- treats glaucoma, estropia
- can cause cholinergic crisis
Term
Pralidoxime
Definition
- reactivates AChE
- treats cholinergic crisis (with atropine)
- can cause blurred vision, tachycardia, dizziness
Term
Carbachol
Definition
- resistant to cleavage by AChE
- direct ACh receptor agonist
Term
Methacholine
Definition
- muscarinic agonist
Term
medium - acting anticholinesterase drugs
Definition
neostigmine, physostimine
Treat myasthenia gravis
Same category as pyridostigmine
Neostigmine doesn't cross BBB, physostigmine does
Term
Carbachol
Definition
muscarinic agonist
use in glaucoma (like pilocarpine)
Term
Methacholine
Definition
- muscarinic agonist
- for treatment of asthma
Term
Contraindications of cholinergic agonists
Definition
PUD, CAD, asthma, hyperthyroidism
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