Autonomic Drugs Flashcards
Adrenal medulla and sweat gland innervation
Sympathetic nervous system innervated by cholinergic fibers
Nicotinic ACh receptors
ligand-gated Na/K channels
Nn in autoniomic ganglia
Nm in NMJ
H1 G-protein
Gq, increase mucus and permability
H2 G-protein
Gs, increases gastric secretion
V1 G-protein
Gq, increase vascular smooth muscle contraction
V2 G-protein
Gs, increase H2O permeability
Gq G protein receptors
H1, alpha1, V1, M1, M3
activates PLC and makes PIP2 into IP3/DAG
IP3 increases Ca
DAG protein kinase C
Gs Protein receptors
Beta-1 &2, D1, H2, V2
activates Adenylyl Cyclase
Gi protein receptors
M2, alpha2, D2
inactivates adenylyl cyclase
MoA Hemichoinium
Inhibits reuptake of choline
MoA Botulinum
inhibits release of ACh from presynaptic
MoA of Vesamicol
Inhibits ACh storage
MoA of Metyrosine
Inhibits Tyrosine becoming DOPA
MoA of Reserpine
Irreversibly inhibits VMAT whichnormally transports NE, Dopamine, and serotonin into intracellular vesicles
MoA of Bretylium and Guanethidine
inhibits NE release
Cocaine, TCAs, amphetamines
inhibits reuptake of NE
Bethanechol
Postoperative ileus, neurogenic ileus, and urinary retention
Carbachol
glaucoma, pupillary constriction, and relief of intraocular pressure
Pilocarpine
potent stimulator of sweat, tears, and saliva
open and closed-angled glaucoma
Methacholine
challenge test for diagnosis of asthma
Direct cholinomimetic agents
bethanechol, carbachol, pilocarpine, methacholine
Anticholinesterases
neostigmines, pyridostigmine, physostigmine, Donepezil, Rivastigmine, galantamine, edrophonium
Neostigmine
postoperative and neurogenic ileus and urinary retention, myasthenia gravis, reversal of NMJ blockade postop
AChE for myasthenia gravis (long acting); does not penetrate CNS
Pyridostigmine
AChE for anticholinergic toxicity (crosses BBB)
Physostigmine
Anticholinesterase for Alzheimer’s
Donepezil, rivastigmine, galantamine
Edrophonium
historically used for myasthenia gravis diagnosis
Cholinesterase inhibitor poisoning
DUMBBELSS
diarrhea, urination, miosis, bronchospasm, bradycardia, excitation of skeletal muscle and CNS, lacrimatino, sweating and salivation
Antidote for cholinesterase poisoning
Atropine(competitive inhibitor) + Pralidoxime (regenerates AChE)
Produce mydriasis and cycloplegia
Atropine, homatropine, tropicamide