ANS: Anticholinergic Flashcards
Cholinergic receptor subtypes
Nicotinic
Pentameric, 5 subunits. Ligand gated ion channels
Cholinergic receptor subtypes
Muscarinic
G protein coupled. M1, M3, M5 inositol phosphate pathway. M2, M4 inhibit adenylyl cyclase and reduce cAMP
M1
CNS, stomach
M2
Cardiac muscle, CNS, a/w smooth muscle
M3
A/w smooth muscle, glandular tissues
M4, M5
CNS
NM
Skeletal muscle at NMJ
Nn
Autonomic ganglia, adrenal medulla, CNS
Antimuscarinic drugs: MOA
Competitively antagonize Ach at muscarinic receptors. Cation pt fits into Ach’s place, inhibits binding. Allows SNS to dominate. Only reversed if Ach conc increases.
Antimuscarinics
Two diff structure types
Natural (atropine and scop) are tertiary amines. Alkaloids of belladonna plant. Crosses BBB and resp epithelium
Semi-synthetic (glyco and robinal) quaternary ammonion deriv
Atropine Effect on: sedation/mydriasis/nausea, inc HR, relaxing smooth muscle, anti-sialogogue
Sed +
Hr +++(Give if hr in 20s, kicks in fast)
Smooth musc ++
Anti sial +
Scopolamine Sedation/nausea/mydriasis Inc hr Relax smooth musc Anti sialogogue
Sed +++
Hr +
Relax +
Anti +++
Glycopyrrolate Sedation, nausea, mydriasis Inc hr Relax smooth muscle Anti sialogogue
Sed 0
Inc hr ++
Smooth muscl ++
Anti ++ (less SE than other drugs)
IV atropine
Onset
Duration
E 1/2t
1 min
30-60 min
2.3 hrs
IV atropine
Metab/excretion
18% unchanged in urine, rest undergoes hydrolysis
IV glycopyrrolate
Onset
Duration
E 1/2 t
2-3 min
30-60 hrs
1.25 hrs