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Cholinergic Agonists
Natural and Synthetic Cholinomimetic Drugs
19
Pharmacology
Professional
11/15/2010

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Cards

Term
CHOLINOMIMETIC agents/agonists
Definition
Drugs that mimic Acetylcholine
Direct Acting: Bind directly to ACh receptors
Indirect Acting: inhibit degradation of ACh
Term
Acetylcholine Agonist Sites
Definition
At all muscarinic receptors
At all ganglia: Nn receptors
At all somatic neuromuscular junctions:Nm
Term
MUSCARINIC receptor sites
Definition
Heart and smooth muscle
Glands and endothelium
Nerve
Term
NICOTINIC receptor sites
Definition
All autonomic ganglia
Neuromuscular end plate
Skeletal Muscle
Term
MIOSIS
Definition
Reduction in pupil size caused by the contraction of the pupillary constrictor muscle (muscarine receptor-mediated)
Term
NICOTINE
Definition
Used for smoking cessation therapy
Agonist at both Nm and Nn receptors
Can enter CNS
Term
LOBELINE
Definition
Plant Alkyloid similar to nicotine
Term
VARENICLINE
Definition
Selective partial agonist at nicotinic receptors; triggers partial dopamine release in CNS
Term
Nicotinic Systemic Pharmacological Effects
Definition
Think about activation of the nerve ganglia and skeletal muscle end plate
Term
Nicotinic CNS effects
Definition
Tremors,Convulsions,Respiratory stimulation or depression, Release ofantidiuretic hormone from the pituitary gland, NauseaEmesis
Term
ACETYLCHOLINE (DRUG)
Definition
MIOCHOL
quaternary ammonium group limits drug to local effects
opthalmic solution for pupil contraction
cardiac vasodilation
Term
METHACHOLINE
Definition
Less susceptible to AChesterase
All muscarinic action, no nicotinic stimulation
No skeletal muscle spasms
Diagnoses bronchial hyperactivity
Term
BETHANECHOL
Definition
Pure muscarinic agonist that spurs a parasympathetic response w/o skeletal spasms
NOT given IV
Used to increase GI movement and bladder contractions
Term
CARBACHOL
Definition
Muscarinic receptor agonist
Used to contract ciliary bodies to treat open angle glaucoma
- Used only in pt. non-responsive to pilocarpine
Term
Acetylcholine analogs
Definition
Choline esters of carbamic acid
Greater muscarinic selectivity
Longer half life
Term
PILOCARPINE
Definition
Pure muscarinic alkaloid agonist
Not degraded by ACHesterase
Causes miosis,salivation, used for wide angle glaucoma, ocular HTN
Dosed in ocular reservoir to avoid systemic affects (can cross membranes)
Term
CEVIMELINE
Definition
Synthetic Muscarinic Agonist
Major M3 and M1 action
Used to treat dry mouth (Sjogren's)
Term
Optical Side Effects of Para drugs
Definition
Engorged blood vessels
Inability to focus
Clouding of the lens
Term
M1
M2
M3
M4&M5
Definition
1:Nerves
2:Heart, nerves, smooth muscle
3:Glands, smooth muscle, epithelium
4&5: CNS
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