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Pharmacology > Pharm 7.2 > Flashcards

Pharm 7.2 Flashcards

1
Q

M1 and M3 receptors

A

Gq - inc PLC

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2
Q

M2 receptors

A

Gi - dec cAMP

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3
Q

N(n) and N(m) receptors

A

open Na/K channels

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4
Q

Acetylcholine is hydrolyzed by

A

cholinesterase

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5
Q

two types of cholinesterase

A

acetylcholinesterase, butyrylcholinesterase

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6
Q

Acetylcholinesterase is present at

A

all cholinergic sites (Nm junction)

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7
Q

butyryl cholinesterase is present in

A

plasma, liver, intestine

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8
Q

cholinergic direct agonists

A

choline esters, cholinomimetic alkaloids

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9
Q

choline esters (direct agonists)

A

acetylcholine, methacholine, carbachol, bethanechol

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10
Q

cholinomimetic alkaloids (direct agonists)

A

pilocarpine, arecholine

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11
Q

cholinergic indirect agonsits

A

anticholinesterases

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12
Q

reversible anticholinesterase

A

neostigmine, physostigmine, pyridostigmine, edrophonium, donepezil

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13
Q

irreversible anticholinesterase

A

organophosphates, carbamates

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14
Q

therapeutic implication of Ach

A

none bc too diffuse action and rapid hydrolysis within seconds

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15
Q

M3 in CVS

A

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

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16
Q

M2 in CVS

A

at SA and AV nodes

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17
Q

cholinergic effect on BP

A

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

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18
Q

cholinergic effect on the heart

A

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

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19
Q

cholinergic effect on GIT

A

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

20
Q

cholinergic effect on Respiratory tract

A

M3 - bronchospasm and inc secretions

21
Q

cholinergic effect on eye

A

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

22
Q

acute angle glaucoma

A

block anble btw cornea and iris

23
Q

muscuranic antagonsit on eye

A

mydriasis and paralysis of accomodation

24
Q

cholinergic effect on bladder

A

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

25
Q

cholinergic effect on glands

A

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

26
Q

Nn on autonomic ganglia

A

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

27
Q

Nn on adrenal medulla

A

secretion of epinephrine and NE

28
Q

high does Ach on heart after atropine causes

A

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

29
Q

Nm stimulation by Ach at muscle

A

contraction of skeletal muscle - twitch/hyperactivity

30
Q

Choline esters

A

acetylcholine, mthacholine, bethanechol, carbachol

31
Q

choline ester sturcture

A

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

32
Q

Choline ester succeptible to cholinesterase

A

Ach > Methacholine

33
Q

Choline esters with muscuranic action

A

Methacholine > Ach, carbachol, bethanechol

34
Q

Choline esters with nicotinic action

A

Ach, Carbachol

35
Q

Choline esters with prominent CVS action

A

Methacholine and Carbachol

36
Q

Choline esters with GIT and bladder action

A

Carbachol and Bethanechol

37
Q

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

38
Q

Bethanechol use

A

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

39
Q

Bethanechol adverse effects

A

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

40
Q

Carbachol adverse effects

A

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

41
Q

Methacholine use

A

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

42
Q

Pilocarpine structure

A

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

43
Q

Pilocarpine actions

A

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

44
Q

drug of choice to reduce IOT

A

Pilocarbine - both for wide and narrow angle glaucoma

45
Q

Pilocarpine is used in

A

xerostomia - promotes salivation, Sjogen’s syndrome

46
Q

adverse effects of pilocarpine

A

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

Pharmacology (15 decks)

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