Cholinergic Drugs Flashcards
M1
Location:
R type:
Mechanism:
Location: nerves
R type: Gq
Mechanism: IP3, DAG
M2
Location:
R type:
Mechanism:
Location: heart, nerves, SM
R type: Gi
Mechanism: - AC/cAMP
M3
Location:
R type:
Mechanism:
Location: glands, SM, endothelium
R type: Gq
Mechanism: IP3, DAG
M4
Location:
R type:
Mechanism:
Location: CNS
R type: Gi
Mechanism: - AC/cAMP
NN
Location:
R type:
Mechanism:
Location: postganglionic cell body, dendrites, CNS
R type: alpha and beta only
Mechanism: depolarize Na/K channel
In most organs, what mAChR dominates?
M3
What mAChR dominates in the heart?
M2
What mAChRs are found in SM?
M2
M3
What are the 4 choline esters?
ACh
Methacholine
Carbachol
Bethanechol
MOA of choline esters
Agonists at cholinergic receptors
How are choline esters charged?
Where is the absorption/distribution subpar?
They are permanently charged.
There is poor absorption and distribution to the CNS.
Which 2 choline esters are negligably affected by cholinesterase?
Carbachol
Bethanechol
Which 2 choline esters have nicotinic actions?
ACh
Carbachol
MOA of alkaloids
Agonists at cholinergic receptors
What 4 major alkaloids and which Rs do they bind?
mAChR: muscarine, pilocarpine
nAChR: nicotine, lobeline
What is the structure of alkaloids?
What is the exception?
They are uncharged tertiary amines, which allows them to be easily absorbed (nicotine patch).
Muscarine, which can cross the BBB and is highly toxic (mushrooms). This is unusual.