cholinergic drugs Flashcards
Methacholine
M»N
slower metabolism with methyl on B carbon
Carbachol
non selective M = N
decreases hydrolysis due to presence of the carbamate
less likely to be broken down with AChE
longer circulation time
Bethanechol
longer half life
due to presence of the carbamate and methyl on B carbon
pilocarpine
plant derived
M agonist
lactone ring with ester = selective
Cevimeline
muscarinic agonist
post op or postpartum non obstructive urinary retention
bethanechol
disabling anticholinergic side effects from medications such as tricyclic antidepressants
bethanechol
diagonsis of bronchial airway hyper reactivity in subjects that do not have asthma
methacholine
miosis induction after ophthalmoscopic examination
pilocarpine
treatment of dry mouth (xerostomia) caused by radiation from cancer treatments / or Sjogren’s syndrome
pilocarpine
atropine
muscarinic antagonists
ophthalmic = causing midrasis and relaxation of ciliary muscle
tropicamide
muscarinic antagonists
ophthalmic = causing midrasis and relaxation of ciliary muscle
cyclopentolate
muscarinic antagonists
ophthalmic = causing midrasis and relaxation of ciliary muscle
Tiotropium
muscarinic antagonists
COPD
Ipratropium
muscarinic antagonists
COPD
Glycopyrrolate
muscarinic antagonists
COPD
Aclidinium
muscarinic antagonists
COPD
Umeclidinium
muscarinic antagonists
COPD
Benztropine
muscarinic antagonists
Parkinsons disease
tertiary amine = increases ability to reach the CNS
Trihexyphenydil
muscarinic antagonists
Parkinsons disease
tertiary amine = increases ability to reach the CNS
Dicyclomine
muscarinic antagonists
IBS - d
Scopolamine
patch given to help with motion sickness
muscarinic antagonist
blocks M1 effects which causes vestibular nausea and vomiting
Oxybutynin IR / XL / patch
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
Detrol LA / Tolterodine
muscarinic antagonists
OAB
Vesicare / solifenacin
muscarinic antagonists
OAB
functional tissue selectivity for bladder M3
lower ADE such as dry mouth
Enablex / darifenacin
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
Sanctura / Trospium
muscarinic antagonists
OAB
has a quat ammonium = limit CNS effects
has an ester = can be metabolized by plasma esterases with CYP450
Toviaz / Fesoterodine
muscarinic antagonist
OAB
tolterodine
muscarinic antagonist
active metabolite = 5-hydroxymethyltolterodine
both are pharmacologically active
in a patient that is a poor metabolizer or rapid metabolizer = same pharmacological effect
Fesoterodine
muscarinic antagonist prodrug of 5-HMT ester prodrug abundance of esterases in plasma has a higher affinity for muscarinic
neostigmine
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
physostigmine
AChE inhibitor
pyridostigmine
AChE inhibitor
charged = less CNS effects
Rivastigmine
AChE inhibitor
carbamate esters
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
Edrophenium
reversible AChE inhibitor
Galantamine
reversible AChE inhibitor
donepezil
reversible AChE inhibitor
organophosphates
extremely toxic phosphorylated enzyme is extremely resistant to hydrolysis
delay or even prevention of a functional enzyme
