Exam 1 Structures Flashcards
nicotine s enantiomer
effects ganglia and skeletal muscle, metabolized to cotinine and nicotine n-oxide
Bethanechol
relieves urinary retention, stimulates GI, systemic
carbachol
constricts pupil in glaucoma, alternative to pilocarpine for ocular surgery
carbaryl
insecticide, indirect reversible cholinergic
cevimeline
direct agoinst; selective M1, M3
-treatment of dry mouth
cotinine
-metabolite of nicotine
methacholine
- direct agonist
- diagnostic for asthma
muscarine
- postganglionic parasympathetic effects
- insensitive to AchE
- no clinical use
neostigmine
- methyl on carbamate increases stability
- quaternary ammounium makes polar: does not cross BBB
- topical applicaiton
- myasthenia gravis 150mg/day
nicotine n oxide
-metabolite of nicotine
nicotine s enantiomer
-effects ganglia and skeletal muscle
ach alpha
- nicotinic activity
- no muscarinic activity
physostigmine
- reversible indirect agonist
- glaucoma treatment
pilocarpine
- direct agonist, muscarinic
- glaucoma, pupil constriction, reduce ciliary muscle spasm
propoxur
- reversible indirect agonist
- insecticide
tacrine
- reversible agonist, Alzheimers
- Inhibits K1
- Liver toxicity
donepezil
- reversible indirect agonist, Alzheimers
- free base crosses BBB
- occupies active site of enzyme
- no hepatoxicity
rivastigmine
- reversible indirect agonist, Alzheimers
- cross BBB, carbamate limits regeneration of AchE
BID, 10 hr duration
-diarrhea
galantamine
-treats dementia
limits formation of complex w/ enzyme
isofluorophate
- irreversible inhibitor
- glaucoma
- discontinued: absroption into the skin and persistant miosis
echothiophate
- irreversible inhibitor
- does not cross BBB or skin
- treatment of glaucoma
- discontinued
parathion
- irreversible inh ACHE
- insecticide
- humans may convert to paraoxon, banned in US
malathion
- irreversible, organophosphate
- replaced parathion as insecticide
- can be eliminated through carboxyesterases
- converted to the very powerful malaoxon
pralidoxime
2-PAM
- reverses phosphorylation by an organophosphate
- must be used quickly
sarin
-nerve gas (phosphonate)
no regeneration by 2-PAM
soman
- nerve gas (phosphonate)
- more stable and toxic than sarin
- AchE cannot be regenerated by 2-PAM
