Autonomic: Parasympathtic Cholinomimetic Drugs Flashcards
Cholinomimetics are
acetylcholine receptor agonists
Nicotinic acetylcholine receptors are found on
- Autonomic ganglia
- Skeletal muscle end plates
- Adrenal glands
Muscarinic acetylcholine receptors
are M1. M2, and M3
Nicotinic receptors act as
ion channels
M1 and M3 are coupled to
Gq
M2 is coupled to
Gi
M1 and M3 are coupled to Gq proteins which activate
the IP3-DAG cascade
M2 is coupled to a Gi protein which decreases
cAMP
M1 receptors are found in
nerves and the CNS
M2 receptors are found in the
atria, the SA and AV node
M3 receptors are found on
glands
Smooth muscle contains
M3 Receptors
M3 receptor activation
M3 receptor activation → nitric oxide release in vascular smooth muscle cells → increased cGMP and vasodilation
Atherosclerosis causes
atherosclerosis → vascular epithelial damage → direct muscarinic receptor activation → vasoconstriction
Bethanechol is a
- cholinomimetic
2. muscarinic agonist
Muscarinic agonists
- increase secretion and motor activity of the gut
2. cause accommodation of the lens
Bethanechol is used to treat
- Non-obstructive gastrointestinal dysmotility (e.g post-op ileus, neurogenic ileus)
- urinary retention
Pilocarpine increases
salivation
Pilocarpine causes
accommodation of the lens
Pilocarpine is a
- Cholinomimetic
2. Muscarinic agonist
Bethanechol increases
increase secretion and motor activity of the gut
Pilocarpine for glaucoma
pilocarpine contracts the ciliary muscle, increasing aqueous humor outflow (useful to treat glaucoma)
Pilocarpine for acute angle closure glaucoma
pilocarpine activates the sphincter pupillae muscle to cause pupillary constriction (useful in acute angle-closure glaucoma)
Carbachol for acute angle closure glaucoma
carbachol causes pupillary constriction (useful in acute angle-closure glaucoma)
Carbachol is both a
muscarinic and nicotinic agonist
Methacholine challenge
instigates asthma for pulmonary testing
Cholinomimetics (e.g. methacholine)
contract bronchial smooth muscle which may exacerbate asthma or COPD
Varenicline is a
nicotinic receptor partial agonist
Varenicline is used for
smoking cessation