(9.1) Intro to Cholinergic drugs (Kruse) Flashcards
What system does the cholinergic system act on?
Parasympathetic
What are the neurotransmitters and receptors for the parasympathetic system?
Neurotransmitters: ACh
Receptors : nAChR, mAChR
Subtypes and characteristics of AChRs
Receptor type: M1
Location:
Structural features:
Mechanism:
Location: Nerves
Structural features: GPCR, Gq/11
Mechanism: IP3 , DAG cascade
Subtypes and characteristics of AChRs
Receptor type: M2
Location:
Structural features:
Mechanism:
Location: Heart, nerves, smooth muscle
Structural features: GPCR, Gi/o
Mechanism: Inhibition of cAMP production, activation of K+ channels
Subtypes and characteristics of AChRs
Receptor type: M3
Location:
Structural features:
Mechanism:
Location: Glands, smooth muscle, endothelium
Structural features: GPCR, Gq/11
Mechanism: IP3, DAG cascade
Subtypes and characteristics of AChRs
Receptor type: M4
Location:
Structural features:
Mechanism:
Location: CNS
Structural features: GPCR, Gi/o
Mechanism: Inhibition of cAMP production
Subtypes and characteristics of AChRs
Receptor type: M5
Location:
Structural features:
Mechanism:
Location: CNS
Structural features: GPCR, Gq/11
Mechanism: IP3 , DAG cascade
Subtypes and characteristics of AChRs
Receptor type: Nn
Location:
Structural features:
Mechanism:
Location: Postganglionic cell body, dendrites, CNS
Structural features: alpha and beta only
Mechanism: Na+, K+ depolarizing ion channel
General rules to follow with organs and mAChR receptors:
GENERALLY…
In most organs _____ is predominant
M3
General rules to follow with organs and mAChR receptors:
GENERALLY…
____ predominates in the heart
M2
General rules to follow with organs and mAChR receptors:
GENERALLY…
Smooth muscle is predominated by _____ and ______
M2, M3
Define:
Cholinergic agonist
Mimic the actions of ACh on nAChRs and mAChRs
They are classified based on their MOA
Direct acting cholinergic agonists:
Choline esters
MOA?
Examples?
MOA = agonists at cholinergic receptors
Acetylcholine, Methacholine, Carbachol, Bethanechol
What are the three groups of AChE inhibitors?
- Alcohols (reversible)
- Carbamic acid esters (reversible but longer lasting than alcohols)
- Organophosphates (irreversible)
General rule for actions of cholinergic agonists?
Rest and digest
Pupillary constriction (near vision), salivation, constriction/secretion of bronchi, slowing heart rate, gastric secretion, voiding of urine