Nicotine Flashcards
Absorption of nicotine if swallowed.
Weak base: Absorption in the INTESTINE if swallowed.
half-life
2hours
Metabolised by
CYP2A6
Pharmacodynamic of nicotine
Nicotinic acetylcholine Receptor (nAChRs)
Classic agonist of mAChRs
MUSCARINE
Classic agonist of nAChRs
Nicotine
nAChR-nicotinic cholinergic receptor is (witch type of receptor)
Classic Ion channel
mAChR-muscarinic cholinergic receptor is (witch type of receptor)
G-protein couple receptor
Structure of nAChRs
PENTAMERIC: 5 subunits
4 domains
For the activation of the receptor nAChRs we need
2x alpha4 and 3x beta2
TWO BINDING SITES for stimultaneous binding (between each a2 and b2)
The defect of CYP2A6 decrease carcinogenicity and a smaller risk of comorbidity from cigarette-related to:
CYP2A6 is resposible to activate procarcinogen into carcinogen and convert nicotine into cotinine (nicotine’s metabolite)
nAChRs can be blocked by:
Curare
mAChRs can be blocked by:
Atropine
alpha 7 is a (type of channel)
Calcium channel ONLY.
alpha 4 beta 2 is (type of channel)
Mainly sodium channel (but also calcium channel)