exam 1 lecture 3 cholinergics Flashcards
cholinergic agents
parasympathetic functions involving ACh receptor
neurotransmitter: ACh
nicotinic receptor Nm
skeletal muscle contraction
motor endplate depolarization –> ligand gated Na/K channel
nicotinic receptor Nn
neuronal post ganglionic depolarization –> ligand gated Na/K channel
adrenal medulla –> catecholamine secretion
muscarinic m1 receptor
postganglionic –> depolarizes (mainly CNS)
Gq increases –> PLC –> IP3 + DAG
muscarinic m2 receptor
heart –> inhibition to decrease HR, conduction, force
Gi inhibition of adenyl cyclase + activation of K channels
muscarinic m3 receptors
smooth muscles –> contraction
exocrine –> increase secretion: salivary, sweat, digestive
endothelium –> relaxation
Gq increases
direct receptor antagonist
ACh degrades fast, so functional group slows it down
B-substitutions reduce AChE activity making it harder to bind
pilocarpine
similar structure to ACh
no quaternery –> can cross BBB
m3 agonist –> facilitates outflow of aqueous humor for glaucoma treatment
antimuscarinics
contraindicated for glaucoma –> increase aqueous humor fluid
DUMBBELS
muscarinic receptor agonist sides
diarrhea, urination, miosis, bradycardia, bronchoconstriction, emesis, lacrimation, salivation + sweating
caution w/ asthma, bradycardia, GI defect
effects of nicotine
low dose: activating system (alert) + dopamine release (addictive)
high dose: CV (HTN, tachycardia)
toxic: seizures, neuromuscular blockade
varenicline (chantix)
nicotine receptor partial
low/moderate release of dopamine (reward)
block nicotine binding (positive reinforcement)
do not use with those who have suicide/depression
buproprion (wellbutrin)
not as effective as varenicline
weakly inhibits NET + DAT
