Cholinergic Agonists and Antagonists Flashcards
Cholinergic Agonists will mimic the action of what neurotransmitter?
Acetylcholine
What are the 2 types of Cholinergic Agonists?
Direct = Receptor Stimulants Indirect = Cholinesterase (-)
What are the 2 types of Acetylcholine receptors?
Muscarinic
Nicotinic
M1 receptors are located where and have what GPCR?
Nerves
- Gq/11 = IP3/DAG cascade
M2 receptors are located where and have what GPCR?
Heart, nerves and smooth muscle
- Gi/o = (-) cAMP
M3 receptors are located where and have what GPCR?
Glands and smooth muscle
- Gq/11 = IP3/DAG cascade
M4 receptors are located where and have what GPCR?
CNS
- Gi/o = (-) cAMP
M5 receptors are located where and have what GPCR?
CNS
- Gq/11 = IP3/DAG cascade
Nicotinic type N receptors are found where and have what types/effects?
CNS
- Alpha and Beta types
= K+/Na+ depolarizing channel
What type of Muscarinic receptor predominates in most tissues?
M3
What are 3 charged and poorly absorbed Cholinergic Agonists?
- Carbachol
- Methacholine
- Bethanechol
Carbachol classification and what it treats?
Charged and poorly absorbed Cholinergic Agonist
= Glaucoma and decreases pupil size
What Acetylcholine receptor type do Methacholine and Bethanechol act on?
Muscarinic
Methacholine classification and what it treats?
Muscarinic charged and poorly absorbed Cholinergic Agonist
= Bronchospasm
Bethanechol classification and what it treats?
Muscarinic charged and poorly absorbed Cholinergic Agonist
= Treats urinary retention, heartburn and post-op Ileus
What are 3 Uncharged and Highly Absorbed Cholinergic Agonists?
- Cevimeline
- Pilocarpine
- Varenicline
Cevimeline classification and what it treats?
Uncharged and highly absorbed Cholinergic Agonist
= Treats Xerostomia (dry eye) in Sjogrens Syndrome
What metabolizes Cevimeline?
CYP450
Pilocarpine classification and what it treats?
Muscarinic Uncharged and Highly absorbed Cholinergic Agonist
= Treats Xerostomia (dry eye), Glaucoma and decreases pupil size
What Cholinergic Agonists that are Uncharged and Highly absorbed can treat Xerostomia?
Cevimeline
Pilocarpine
Varenicline classification and what specific receptor it is a Cholinergic Agonist for?
Uncharged and Highly absorbed
- Alpha4 Beta2 nAchR partial agonist