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pharm sci > cholinergic drugs > Flashcards

cholinergic drugs Flashcards

1
Q

Methacholine

A

M»N

slower metabolism with methyl on B carbon

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2
Q

Carbachol

A

non selective M = N
decreases hydrolysis due to presence of the carbamate
less likely to be broken down with AChE
longer circulation time

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3
Q

Bethanechol

A

longer half life

due to presence of the carbamate and methyl on B carbon

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4
Q

pilocarpine

A

plant derived
M agonist
lactone ring with ester = selective

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5
Q

Cevimeline

A

muscarinic agonist

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6
Q

post op or postpartum non obstructive urinary retention

A

bethanechol

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7
Q

disabling anticholinergic side effects from medications such as tricyclic antidepressants

A

bethanechol

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8
Q

diagonsis of bronchial airway hyper reactivity in subjects that do not have asthma

A

methacholine

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9
Q

miosis induction after ophthalmoscopic examination

A

pilocarpine

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10
Q

treatment of dry mouth (xerostomia) caused by radiation from cancer treatments / or Sjogren’s syndrome

A

pilocarpine

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11
Q

atropine

A

muscarinic antagonists

ophthalmic = causing midrasis and relaxation of ciliary muscle

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12
Q

tropicamide

A

muscarinic antagonists

ophthalmic = causing midrasis and relaxation of ciliary muscle

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13
Q

cyclopentolate

A

muscarinic antagonists

ophthalmic = causing midrasis and relaxation of ciliary muscle

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14
Q

Tiotropium

A

muscarinic antagonists

COPD

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15
Q

Ipratropium

A

muscarinic antagonists

COPD

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16
Q

Glycopyrrolate

A

muscarinic antagonists

COPD

17
Q

Aclidinium

A

muscarinic antagonists

COPD

18
Q

Umeclidinium

A

muscarinic antagonists

COPD

19
Q

Benztropine

A

muscarinic antagonists
Parkinsons disease
tertiary amine = increases ability to reach the CNS

20
Q

Trihexyphenydil

A

muscarinic antagonists
Parkinsons disease
tertiary amine = increases ability to reach the CNS

21
Q

Dicyclomine

A

muscarinic antagonists

IBS - d

22
Q

Scopolamine

A

patch given to help with motion sickness
muscarinic antagonist
blocks M1 effects which causes vestibular nausea and vomiting

23
Q

Oxybutynin IR / XL / patch

A 
OAB
muscarinic antagonists
Cmax is related to adverse effects
adverse effects decrease as dosing interval becomes smaller
lipophilic
active metabolite = desethyloxybutynin
tert amine = easily gets into CNS
most likely to cause ADR
do not use IR in elderly patients
most likely metabolized by CYP enzymes - remove an ethyl group and replace with a H
24
Q

Detrol LA / Tolterodine

A

muscarinic antagonists

OAB

25
Q

Vesicare / solifenacin

A

muscarinic antagonists
OAB
functional tissue selectivity for bladder M3
lower ADE such as dry mouth

26
Q

Enablex / darifenacin

A 
muscarinic antagonists
OAB
pharmacologically selective for M3 
causes dry mouth
metabolized by 3A4 and 2D6
check for genetic polymorphisms and watch if they are on another drug that inhibits these enzymes
27
Q

Sanctura / Trospium

A

muscarinic antagonists
OAB
has a quat ammonium = limit CNS effects
has an ester = can be metabolized by plasma esterases with CYP450

28
Q

Toviaz / Fesoterodine

A

muscarinic antagonist

OAB

29
Q

tolterodine

A

muscarinic antagonist
active metabolite = 5-hydroxymethyltolterodine
both are pharmacologically active
in a patient that is a poor metabolizer or rapid metabolizer = same pharmacological effect

30
Q

Fesoterodine

A 
muscarinic antagonist
prodrug of 5-HMT
ester prodrug
abundance of esterases in plasma
has a higher affinity for muscarinic
31
Q

neostigmine

A

AChE inhibitor
carbamate / 2 methyl groups
looks similar enough to get into AChE binding site
takes significantly longer to regenerate charge regulation at all cholinergic synapses
drug must be metabolized in order to be activated
plasma conc would be decreased
charged = less CNS effects

32
Q

physostigmine

A

AChE inhibitor

33
Q

pyridostigmine

A

AChE inhibitor

charged = less CNS effects

34
Q

Rivastigmine

A

AChE inhibitor

35
Q

carbamate esters

A

very long processes
plasma conc of these drugs would decrease as AChE is breaking it down
work through temporary covalent modification of enzyme active site

36
Q

Edrophenium

A

reversible AChE inhibitor

37
Q

Galantamine

A

reversible AChE inhibitor

38
Q

donepezil

A

reversible AChE inhibitor

39
Q

organophosphates

A

extremely toxic phosphorylated enzyme is extremely resistant to hydrolysis
delay or even prevention of a functional enzyme

pharm sci (12 decks)

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