Pharmacology of ANS Flashcards
cholinergic receptors
*receive Ach as neurotransmitter
*nicotinic and muscarinic receptors
adrenergic receptors
*receive norepinephrine as neurotransmitter
*alpha (1 + 2) and beta (1, 2, 3) receptors
cholinomimetics
drugs that mimic or augment the action of acetylcholine (parasympathetic agonists)
muscarinic receptors are found on
*organs innervated by PARASYMPATHETIC nerves
*sweat glands (innervated by ACh sympathetic nerves)
*CNS
M2 receptor - location
HEART, nerves, smooth muscle
M3 receptor - location
GLANDS, smooth muscle, endothelium
direct-acting cholinomimetics: MOA
bind and activate muscarinic and/or nicotinic receptors
indirect-acting cholinomimetics - MOA
*inhibits acetylcholinesterase
*result: amplification of endogenous ACh (keeps for ACh around at the receptor)
*note: affect both nicotinic and muscarinic receptors
important direct-acting cholinomimetics to know
1) bethanechol
2) pilocarpine
3) carbachol
4) muscarine-containing mushrooms
bethanechol
*muscarinic agonist (direct-acting cholinomimetic; results in parasympathetic responses)
pilocarpine
*muscarinic agonist, penetrates CNS
(direct-acting cholinomimetic; results in parasympathetic responses)
carbachol
*muscarinic AND nicotinic agonist (direct-acting cholinomimetic; results in parasympathetic responses)
*mostly used as eye drops for GLAUCOMA
important indirect-acting cholinomimetics to know
1) edrophonium (we don’t use this anymore)
2) neostigmine
3) pyridostigmine
4) physostigmine
*also, organophosphates (parathion, sarin)
neostigmine
*indirect acting cholinomimetic
(acetylcholinesterase inhibitor)
*quaternary: poor CNS penetration
pyridostigmine
*indirect acting cholinomimetic (acetylcholinesterase inhibitor)
*quaternary: poor CNS penetration
physostigmine
*indirect acting cholinomimetic
(acetylcholinesterase inhibitor)
*tertiary: better CNS penetration
main difference in effect of indirect-acting cholinomimetics (compared to direct-acting)
act like direct-acting agents, EXCEPT FOR THE VASCULATURE EFFECTS
what cholinomimetic do we use to treat dry mouth
pilocarpine (direct-acting cholinomimetic)
ACh toxicity (organophosphate poisoning) - SLUDGE
Salivation
Lacrimation
Urination
Defecation
GI symptoms
Emesis
(also, constricted pupil, slow heart rate, and bronchospasm)
ACh toxicity (organophosphate poisoning) - DUMBBELSS
Diarrhea
Urination
Miosis
Bronchoconstriction
Bradycardia
Emesis
Lacrimation
Salivation
Sweating
carbamates
*pesticide; reversible AChE inhibitors
what do you treat carbamate toxicity with
atropine (antimuscarinic) alone
what do you treat organophosphate poisoning with
atropine + pralidoxime
anticholinergics
*acetylcholine receptor-blocking drugs
*antimuscarinics are a subtype
*atropine is protype