Cholinergics - 8/21/15 (Scrogin) Flashcards
Name 2 classes of cholinergic receptors
- Muscarinic (GPCR)
2. Nicotinic (ligand gated ion)
How many transmembrane polypeptides compose nicotinic receptors?
5
Nicotinic receptors are permeable to what ions?
K+ and Na+
Nicotinic receptors are located on what cell types?
Nn type: POST-ganglionic cells
Nm type: skeletal muscle
Which system, sympathetic or parasympathetic, is activated by nicotinic agonists?
Both, simultaneously
Nicotine stimulates what type of receptors, specifically
Nn in autonomic ganglia, and CNS
What’s nicotine used for
smoking cessation
What is the MOA of succinylcholine
Blocks Nm receptors in the NMJ, causing depolarization block
Succinylcholine - Rx?
relaxation for intubation or ECT
Succinylcholine - 2 contraindications?
familial hyperthermia
skeletal muscle myopathies
Name 4 quaternary nitrogen analogs
Acetylcholine
Methacholine
Carbachol
Bethanechol
Acetylcholine - what receptors?
Nicotinic and muscarinic
Acetylcholine - clearance?
BOTH acetyl and plasma-cholinesterase
Acetylcholine - Rx?
No therapeutic use - metabolized to fast
Methacholine - clearance?
acetylcholinesterase, slowed hydrolysis (longer t1/2 than acetylcholine)
Methacholine - receptors?
Muscarinic - smooth muscle, glands, heart
Methacholine - Rx?
Diagnose asthma
Methacholine - Tx?
Bronchiolar constriction
Methacholine - contraindication?
B-blockers
Carbachol - clearance?
More resistant to acetylcholinesterase
Carbachol - receptors?
Both muscarinic and nicotinic activity
Carbachol - Rx
miotic agent
Reduces intraocular pressure after cataract surgery
Carbachol - SE?
excessive muscarinic/nicotinic activation
Bethanochol - clearance
resistant to acetyl- and plasma cholinesterase
Bethanochol - receptor selectivity?
Muscarinic only (GI and urinary bladder)
Bethanochol - Rx?
Post-op urinary retention
Post-partum urinary retention
Neurogenic bladder atony
Can quaternary amine drugs cross the BBB
No they’re charged
Bethanochol - contra?
peptic ulcer
asthma
bradycardia
Muscarine poisoning causes profound
sympathetic activation
Muscarine poisoning - antidote?
Atropine - muscarinic antagonist
Pilocarpine - receptor selectivity?
pure muscarinic
Pilocarpine - BBB?
Yes, crosses (tertiary amine). Appreciable CNS effects