ALL THE DRUGS Flashcards
muscarinic agonist
increase SLUDGE, decrease HR, miosis, dec dopamine. bronchoconstriction
acetylcholine
muscarinic agonist, quat, all synapses
methacholine
muscarinic agonist, B carbon methyl, quat, induces asthma attack
carbachol
muscarinic agonist, quat, carbamate, glaucoma
bethanechol
muscarinic agonist, carbamate and methyl on b carbon, treats urinary retention (non-obstructive) and dec symptoms of depression
muscarine
muscarinic agonist, quat,
pilocarpine
muscarinic agonist,, tert, glaucoma, miosis after eye exam
cevimeline
muscarinic agonist, tert, salivary gland issue
muscarinic antagonist
decreases slud, mydriasis, increases HR, bronchodilation
muscarinic agonist SAR
- N capable of being + , no huge groups dec methyls for H on N terminal = dec potency / increased carbons on N antagonist
- ethylene bridge (2C)
- alcoxyl group (ketone, ester, ether)/ Ing’s rule of 5/
SAR muscarinic antagonist
- N tertiary or quat
- R1 and R2 heterocyclic (can’t be naphthelene)
- R3 -H, -OH part of ring
- X=ester, ether
atropine
muscarinic antagonist, ophthalmic, tert
tropicamide
muscarinic antagonist, opthalmic, tert
cyclopentolate
muscarinic antagonist,, opthalmic, tert
iptratropium
COPD, muscarinic antagonist,, quat
tiotropium
COPD, tert, muscarinic antagonist,
umeclidinium
COPD, tert, muscarinic antagonist,
glycopyrrolate
COPD, tert, muscarinic antagonist,
acidinium
COPD, tert, muscarinic antagonist,
benztopine
parkinsons, tert, muscarinic antagonist,
trihexylphenydil
parkinsons, tert, muscarinic antagonist,
dicycloamine
IBS-D, tert, muscarinic antagonist,
scopolamine
motion sickness, tert, muscarinic antagonist,
oxybutynin
tert, OAB/urinary retention, muscurinic antagonist, cmax related to ADE/lipophillic/P450
tolterodine
tert, OAB/urinary retention, muscurinic antagonist, prodrug 2D6
solifenacin
tert, OAB/urinary retention, muscurinic antagonist, functional selectivity for M3 bladder/ 3A4
darifenacin
tert, OAB/urinary retention, muscurinic antagonist, , pharmacologically selective M3, cause dry mouth, 3A4 and 2D6
trospium
tert, OAB/urinary retention, muscurinic antagonist, P450/esterase/hydroxylation
fesoterodine
tert, OAB/urinary retention, muscurinic antagonist, prodrug 5-HMT
AChE inhibitors
increases the ACh, increase SLUDGE, decreases HR and miosis of the eye
neostigmine
AChE inhibitor, quat, carbamate ester, myasthenia gravis
phyostigmine
AChE inhibitor, tert, carbamate ester
pyridostigmine
AChE inhibitor, quat, carbamate ester, myasthenia gravis
rivastigmine
alzheimers, carbamate ester, tert
carbamate ester
“stigmine” temporary covalent modification, work through being metabolized
edrophenium
reversible inhibitor of AChE, quat
galantamine
reversible inhibitor of AChE, tert, alzheimers
doneprexil
reversible inhibitor of AChE, tert, alzheimers
echothiophate
irreversible inhibitor of AChE, quat, glaucoma
organophosphates
toxic/dephosphroylate = resistant to hydrolysis = too much ACh build up / use 2-PAM if hasn’t aged
neuromusuclar blocking agent MOA
immobilize patients for surgery, procedures = work by causing paralysis
depolarizing agents
opens the cel membrane and becomes refractory and the muscle becomes resistant to further stimulation, fasciculations and then flaccid paralysis
succinylcholine
more ach wouldnt do anything because you are blocking to the binding site to cause muscle activation