CNS drugs Flashcards
Alpha 2 receptor
Sympathetic
Gi
Decreased sympathetic outflow (also decreased insulin, decreased aqueous humor)
Beta 1 receptor
Sympathetic
Gs
Increased HR, contractility, renin, lipolysis
Beta 2 receptor
Sympathetics
Gs
Vasodilation, bronchodilation, lipolysis, ciliary muscle relaxation (pupil dilation), increased insulin, decreased uterine tone, increased aqueous humor prodn
M1 receptor
Parasympathetic
Gq
CNS, enteric NS
M2 receptor
Parasymp
Gi
In heart – decreased HR and contractility
M3 receptor
Parasympathetic
Gq
Everywhere that’s not heart or CNS - increased gland secretions, increased bladder contraction, bronchoconstriction, pupil constriction (contract pupillary sphincter) and ciliary muscle constriction (accommodation)
Dopamine receptor on renal vascular smooth muscle
D1 (Gs)
Vasopressin receptors
V1 (Gq) - increased vasc smooth muscle contraction
V2 (Gs) - increased H2O permeability and reabs in collecting tubules of kidney
Cholinomimetic agents
Direct:
Bethanechol - move bowel and bladder
Carbachol - constrict pupil and treat glaucoma
Methacholine - challenge test for asthma (causes bronchocon)
Pilocarpine - stimulate sweat, tears, saliva, treat glaucoma
Indirect:
Anticholinesterases (donepezil, galantamine, rivastigmine (AD), edrophonium (diagnose MG), neostigmine (treat MG, treat ileus and urinary retention, reverse NM blockade), physostigmine (reverse atropine overdose b/c crosses BBB), pyridostigmine (treat MG, doesn’t cross BBB)
Contraindications for cholinomimetics
COPD, asthma, peptic ulcers
Common cause of cholinesterase inhibitor poisoning + antidote
Organophosphates (eg parathion - insecticide)
antidote = atropine + pralidoxime (binds organophosphate-AChE complex and boots the organophosphate off, recovering AChE)
sx = parasympathetic activation everywhere
Muscarinic antagonists
Atropine (treats bradycardia and dilates pupil, decreases gut acid secretion and motility, decreases urgency in cystitis; tox: increased body temp b/c decreased sweating, tachycardia, dry/flushed skin, disorientation, cycloplegia, constipation)
Benztropine (treats PD)
glycopyrrolate (preop to reduce secretions, treat drooling and peptic ulcers - works on GI and resp tracts)
Hyoscyamine, dicyclomine (GI)
Ipratropium, tiotropium (resp - treats COPD, asthma)
oxybutynin, solifenacin, tolterodine (GU, reduce bladder spasms, urgency, incontinence)
Scopolamine (CNS - treat motion sickness)
Alpha 1 receptor
Sympathetic
Gq
Increased vasc smooth muscle contraction (increased PVR), mydriasis (pupil dilation from contraction of pupillary dilator), sphincter contraction
Tetrodotoxin
Prevents depol by binding Na channels in cardiac and nerve tissue
Pufferfish (Japanese)
–> n/d, weakness, dizziness, loss of reflexes
Ciguatoxin
Reef fish
Opens Na channels –> depol (lots of parasympathetic effects + temperature-related dysesthesia [cold feels hot, hot feels cold])