autonomic drugs Flashcards
Nicotinic ACh receptors
ligand-gated Na/K channels. Nn= autonomic ganglia. Nm= neuromuscular junction.
muscarinic receptors
G-protein coupled. parasympathetic. 5 subtypes
alpha-1 receptor
Gq. sympathetic. vasoconstriction, pupil dilation (mydriasis), intestinal and bladder sphincter contraction.
alpha-2 receptor
Gi. sympathetic. negative feedback, decrease sympathetic outflow. decrease insulin release.
Beta-1 receptor
Gs. sympathetic. increase HR, contractility, renin release, lipolysis.
Beta-2 receptor
Gs. sympathetic. vasodilation, bronchodilation, increase insulin release, decrease uterine tone, increase aqueous humor.
M1 receptor
Gq. para-sympathetic. CNS, enteric nervous system.
M2 receptor
Gi. parasympathetic. decrease HR and contractility.
M3 receptor
Gq. parasympathetic. exocrine gland secretion, gut motility, bladder contraction, bronchoconstriction, miosis, accommodation.
D1 receptor
Gs. Dopamine. relaxes renal vascular smooth muscle.
D2 receptor
Gi. Dopamine. Modulates transmitter release, especially in brain (decrease in parkinsons, increase in psychosis).
H1-receptor
Gq. Histamine. nasa/bronchiole mucus secretion, increase vascular permeability, contraction of bronchioles, pruritis, pain. Allergic responce
H2 receptor
Gs. Histamine. increase gastric acid secretion.
V1 receptor
Gq. VAsopressin. vasoconstriction.
V2 receptor.
Gs. Vasopressin. water permeability and reabsorption in collecting tubules.
Gs
stimulate adenylyl cyclase to increase cAMP and stimulate PKA to increase [CA2+].
Gi
inhibit adenylyl cyclase to decrease cAMP and not stimulate PKA to increase [CA2+].
Gq
activate phospholipase C to cleave PIP2 to DAG and IP3. activate PKC and increase [Ca2+].
Cholinomimetic. direct agonist. treat ileus and urinary retention. activates bowel and bladder. resistant to AChE.
bethanechol
Cholinomimetic. direct agonist. causes pupillary constriction to treat glaucoma and relieve intraocular pressure.
carbachol
Cholinomimetic. direct agonist. stimulate sweat, tears, and saliva. treat wide and and closed-angle glaucoma. resistant to AChE.
pilocarpine