cholinergic drugs

Question 1

Methacholine

Answer 1

M»N

slower metabolism with methyl on B carbon

Question 2

Carbachol

Answer 2

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

Question 3

Bethanechol

Answer 3

longer half life

due to presence of the carbamate and methyl on B carbon

Question 4

pilocarpine

Answer 4

plant derived
M agonist
lactone ring with ester = selective

Question 5

Cevimeline

Answer 5

muscarinic agonist

Question 6

post op or postpartum non obstructive urinary retention

Answer 6

bethanechol

Question 7

disabling anticholinergic side effects from medications such as tricyclic antidepressants

Answer 7

bethanechol

Question 8

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

Answer 8

methacholine

Question 9

miosis induction after ophthalmoscopic examination

Answer 9

pilocarpine

Question 10

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

Answer 10

pilocarpine

Question 11

atropine

Answer 11

muscarinic antagonists

ophthalmic = causing midrasis and relaxation of ciliary muscle

Question 12

tropicamide

Answer 12

muscarinic antagonists

ophthalmic = causing midrasis and relaxation of ciliary muscle

Question 13

cyclopentolate

Answer 13

muscarinic antagonists

ophthalmic = causing midrasis and relaxation of ciliary muscle

Question 14

Tiotropium

Answer 14

muscarinic antagonists

COPD

Question 15

Ipratropium

Answer 15

muscarinic antagonists

COPD

Question 16

Glycopyrrolate

Answer 16

muscarinic antagonists

COPD

Question 17

Aclidinium

Answer 17

muscarinic antagonists

COPD

Question 18

Umeclidinium

Answer 18

muscarinic antagonists

COPD

Question 19

Benztropine

Answer 19

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

Question 20

Trihexyphenydil

Answer 20

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

Question 21

Dicyclomine

Answer 21

muscarinic antagonists

IBS - d

Question 22

Scopolamine

Answer 22

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

Question 23

Oxybutynin IR / XL / patch

Answer 23

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

Question 24

Detrol LA / Tolterodine

Answer 24

muscarinic antagonists

OAB

Question 25

Vesicare / solifenacin

Answer 25

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

Question 26

Enablex / darifenacin

Answer 26

``` 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 ```

Question 27

Sanctura / Trospium

Answer 27

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

Question 28

Toviaz / Fesoterodine

Answer 28

muscarinic antagonist | OAB

Question 29

tolterodine

Answer 29

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

Question 30

Fesoterodine

Answer 30

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

Question 31

neostigmine

Answer 31

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

Question 32

physostigmine

Answer 32

AChE inhibitor

Question 33

pyridostigmine

Answer 33

AChE inhibitor | charged = less CNS effects

Question 34

Rivastigmine

Answer 34

AChE inhibitor

Question 35

carbamate esters

Answer 35

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

Question 36

Edrophenium

Answer 36

reversible AChE inhibitor

Question 37

Galantamine

Answer 37

reversible AChE inhibitor

Question 38

donepezil

Answer 38

reversible AChE inhibitor

Question 39

organophosphates

Answer 39

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