Pharm 7.2

Question 1

M1 and M3 receptors

Answer 1

Gq - inc PLC

Question 2

M2 receptors

Answer 2

Gi - dec cAMP

Question 3

N(n) and N(m) receptors

Answer 3

open Na/K channels

Question 4

Acetylcholine is hydrolyzed by

Answer 4

cholinesterase

Question 5

two types of cholinesterase

Answer 5

acetylcholinesterase, butyrylcholinesterase

Question 6

Acetylcholinesterase is present at

Answer 6

all cholinergic sites (Nm junction)

Question 7

butyryl cholinesterase is present in

Answer 7

plasma, liver, intestine

Question 8

cholinergic direct agonists

Answer 8

choline esters, cholinomimetic alkaloids

Question 9

choline esters (direct agonists)

Answer 9

acetylcholine, methacholine, carbachol, bethanechol

Question 10

cholinomimetic alkaloids (direct agonists)

Answer 10

pilocarpine, arecholine

Question 11

cholinergic indirect agonsits

Answer 11

anticholinesterases

Question 12

reversible anticholinesterase

Answer 12

neostigmine, physostigmine, pyridostigmine, edrophonium, donepezil

Question 13

irreversible anticholinesterase

Answer 13

organophosphates, carbamates

Question 14

therapeutic implication of Ach

Answer 14

none bc too diffuse action and rapid hydrolysis within seconds

Question 15

M3 in CVS

Answer 15

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

Question 16

M2 in CVS

Answer 16

at SA and AV nodes

Question 17

cholinergic effect on BP

Answer 17

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

Question 18

cholinergic effect on the heart

Answer 18

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

Question 19

cholinergic effect on GIT

Answer 19

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

Question 20

cholinergic effect on Respiratory tract

Answer 20

M3 - bronchospasm and inc secretions

Question 21

cholinergic effect on eye

Answer 21

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

Question 22

acute angle glaucoma

Answer 22

block anble btw cornea and iris

Question 23

muscuranic antagonsit on eye

Answer 23

mydriasis and paralysis of accomodation

Question 24

cholinergic effect on bladder

Answer 24

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

Question 25

cholinergic effect on glands

Answer 25

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

Question 26

Nn on autonomic ganglia

Answer 26

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

Question 27

Nn on adrenal medulla

Answer 27

secretion of epinephrine and NE

Question 28

high does Ach on heart after atropine causes

Answer 28

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

Question 29

Nm stimulation by Ach at muscle

Answer 29

contraction of skeletal muscle - twitch/hyperactivity

Question 30

Choline esters

Answer 30

acetylcholine, mthacholine, bethanechol, carbachol

Question 31

choline ester sturcture

Answer 31

charged water soluble - poor absorbtion form stomach, poor lipid solubility, poor BBB penetration

Question 32

Choline ester succeptible to cholinesterase

Answer 32

Ach > Methacholine

Question 33

Choline esters with muscuranic action

Answer 33

Methacholine > Ach, carbachol, bethanechol

Question 34

Choline esters with nicotinic action

Answer 34

Ach, Carbachol

Question 35

Choline esters with prominent CVS action

Answer 35

Methacholine and Carbachol

Question 36

Choline esters with GIT and bladder action

Answer 36

Carbachol and Bethanechol

Question 37

Choline ester causing release of Epi from adrenal medulla due to action on Nn

Answer 37

Carbachol

Question 38

Bethanechol use

Answer 38

postpartum/postoperative nonobstructive urinary retention, congenital megacolon, and paralytic ileus

Question 39

Bethanechol adverse effects

Answer 39

sweating, salivation, flushing, dec BP, nausea, abdominal pain, diarrhea, bronchospasm

Question 40

Carbachol adverse effects

Answer 40

quaternary amine so lack of systemicside effects since used topically for opthalmological use

Question 41

Methacholine use

Answer 41

short lived and used for diagnosis of bronchial hyperactivity (no effects in pt w/o asthma bc no hyperactivity)

Question 42

Pilocarpine structure

Answer 42

tertiary amine (penetrates BBB), alkaloid from Pilocarpus microphyllus, resistant to hydorlysis by AChE, less potent, stimulates only muscuranic rec

Question 43

Pilocarpine actions

Answer 43

topically on cornea produces myosis and spasm of accomodation, also causes sweating salivation, lacrimation, and other secretions

Question 44

drug of choice to reduce IOT

Answer 44

Pilocarbine - both for wide and narrow angle glaucoma

Question 45

Pilocarpine is used in

Answer 45

xerostomia - promotes salivation, Sjogen's syndrome

Question 46

adverse effects of pilocarpine

Answer 46

profuse sweating (diaphoresis) and salivation, can enter the brain and cause CNS disturbances (convulsion with high doses)