exam 1 lecture 5 anticholinergics

Question 1

anticholinergics

Answer 1

binds to the cholinoreceptor and blocks acetylcholine binding
contain both amine + ester

Question 2

atropine

Answer 2

competitive antagonist for muscarinic receptors M1,M2,M3
eye - opens the eye, do not use for glaucoma
cardiovascular - increases HR
resipratory tract - bronchodilation

Question 3

antimuscarinics

Answer 3

antagonist by competitive + irreversible inhibition
antagonist are generally bigger
two classes tertiary (ocular + cns) + quaternary (gi tract + peripheral)

Question 4

tertiary amines

Answer 4

3 bond N, good CNS bc no charge

Question 5

belladonna alkaloids

Answer 5

longer lasting
atropine: CNS + ocular uses
scopolamine: better CNS due to increase lipophilicity of epoxide.

Question 6

tertiary amine derivatives

Answer 6

shorter acting for less sides
homotropine + tropicamide

Question 7

antiparkinsons tertiary amines

Answer 7

benztropine: sedative activity with LDOPA to balance cholinergic and dopaminergic neurotransmission

Question 8

quaternary amines

Answer 8

+ charge N
anisotropine: GI + peripheral application
ipratropium: antimuscarinic, M3 antagonist to block constriction to open airways (combo w/ albuteraol for COPD)
glycopyrrolate: GI spasms + peptic ulcers

Question 9

OAB

Answer 9

tolterodine (detrol): somewhat selective antimuscarinic for M3 receptor on bladder, can cause anticholinergic effects
“fenacin”: M3 selective antagonist used to treat OAB

Question 10

antimuscarinic poisoning

Answer 10

OTC medication contain drugs with antimuscarinic activity
diphenhydramine: H1 receptor antagonist. sides include drymouth + increase HR (anticholinergic activity)
treatment: AChE inhibitor (physostigmine), change medication or dose.

Question 11

nicotinic receptor antagonist

Answer 11

AChE degradation method
two main agents: succinylcholine + tubocurarine

Question 12

succinylcholine

Answer 12

depolarizing blockade
binds to nicotine receptor, activates it, and stays on. blocks due to continual stimulation
skeletal muscle relaxant for anesthesia

Question 13

depolarizing blockade

Answer 13

agonist binds to nicotine receptor (activates) –> stays on nicotine receptor –> nicotine receptor stays inactive state
nicotine receptor cannot reset to active form

Question 14

tubocurarine

Answer 14

nondepolarizing blockade
binds to nicotine receptor, blocks and does not allow depolarization
short-term muscle relaxant

Question 15

non-depolarizing blockade

Answer 15

binds receptor and blocks. does not allow depolarization. normal antagonist

Question 16

nicotine on muscle

Answer 16

ACh binds –> depolarization –> opens Na+ channels –> action potential
Na+ channels open, depolarize (inactive), ACh comes off and repolarizes (active)

Question 17

botulin toxin (Botox)

Answer 17

indirect acting: inhibits ACh release
use: muscle spasm, cerebral palsy, ocular muscle spasm
problem: spread from injection site

Question 18

hexamethonium

Answer 18

nicotinic antagonist at autonomic ganglia –> blocks all SNS + PSNS activity
no clinical use bc adverse sides
sides: hypotension (SNS), decreases perspiration (SNS), dry mouth (PSNS)