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Flashcards in Pharm 7.2 Deck (46)
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1

M1 and M3 receptors

Gq - inc PLC

2

M2 receptors

Gi - dec cAMP

3

N(n) and N(m) receptors

open Na/K channels

4

Acetylcholine is hydrolyzed by

cholinesterase

5

two types of cholinesterase

acetylcholinesterase, butyrylcholinesterase

6

Acetylcholinesterase is present at

all cholinergic sites (Nm junction)

7

butyryl cholinesterase is present in

plasma, liver, intestine

8

cholinergic direct agonists

choline esters, cholinomimetic alkaloids

9

choline esters (direct agonists)

acetylcholine, methacholine, carbachol, bethanechol

10

cholinomimetic alkaloids (direct agonists)

pilocarpine, arecholine

11

cholinergic indirect agonsits

anticholinesterases

12

reversible anticholinesterase

neostigmine, physostigmine, pyridostigmine, edrophonium, donepezil

13

irreversible anticholinesterase

organophosphates, carbamates

14

therapeutic implication of Ach

none bc too diffuse action and rapid hydrolysis within seconds

15

M3 in CVS

on blood vessel endothelium - production of NO/EDRF --> PKG in SM-->hyperpolarization and SM relaxation by inc cGMP --> vasodialation

16

M2 in CVS

at SA and AV nodes

17

cholinergic effect on BP

dec BP by causing vasodialation - only by direct Ach administration bc there is no innervation ot blood vessels so indirect agonists has no use

18

cholinergic effect on the heart

dec HR, CO, and contraction (esp atrial but not on ventricles and purkinje system)

19

cholinergic effect on GIT

M3 - inc tone, peristalsis, secretions, causing contractions leading to diarrhea and involuntary defecation

20

cholinergic effect on Respiratory tract

M3 - bronchospasm and inc secretions

21

cholinergic effect on eye

M3 - contraction of spincter mucle (miosis), inc outflow of aqueous humor reducing IOT, contraction of ciliary muscle causing accomodation

22

acute angle glaucoma

block anble btw cornea and iris

23

muscuranic antagonsit on eye

mydriasis and paralysis of accomodation

24

cholinergic effect on bladder

M3 - contraction of detrusor and relaxation of trigone/sphincter, causes voiding of urine and urinary incontinence

25

cholinergic effect on glands

M3 - inc secreation of sweat (thermoregulatory, saliva, and lacrimation

26

Nn on autonomic ganglia

stimulation (at higher dose) both PNS and SNS --effect depends on dominant system

27

Nn on adrenal medulla

secretion of epinephrine and NE

28

high does Ach on heart after atropine causes

tachycardia and rise in BP due to nicotinic actions - only get the sympathetic effect bc muscuranics are blocked by atropine

29

Nm stimulation by Ach at muscle

contraction of skeletal muscle - twitch/hyperactivity

30

Choline esters

acetylcholine, mthacholine, bethanechol, carbachol