Cholinergic Pharmacology II Flashcards
Types of cholinoceptor-blocking drugs (3)
- Muscarinic Receptor antagonists
- Nicotinic receptor antagonists (NN and NM)
- Neuromuscular blocking drugs (NM only)
Muscarinic Receptor antagonists (3)
- Atropine
- Ipratropium
- Benztropine
Pharmacologic effects of atropine Secretory Vision Temperature Cardiovascular Behavioral GU Vascular effects BP effects
- decreased secretions (salivary, bronchiolar, sweat)
mydriasis, and cycloplegia
hyperthermia
tachycardia
sedation
urinary retention & constipation
behavioral excitation & hallucinations - Completely counteracts peripheral vasodilation caused by choline esters
- Does not affect blood pressure when given alone
Clinical uses of atropine
- Management of AChE inhibitor overdose
- Antispasmodic in GI tract
- Prevention of vagal reaction
Antidote for atropine overdose
Physostigmine
Ipratropium properties (2)
- Non-selective muscarinic antagonist
2. Acts on M3
Ipratropium effects and clinical uses
- Decreases bronchoconstriction and bronchosecretion
2. Used in COPD and asthma
Benztropine (Cogentin) uses (2)
- Re-establish dopaminergic-cholinergic balance in patients with Parkinson’s Disease
- Decrease GI/GU secretions, decrease motility, INCREASE heart rate
Nicotinic Receptor Antagonists (2)
Hemamethonium and Mecamylamine
Effects of nicotinic receptor antagonists
Reduces the predominant autonomic tone
Non-depolarizing NM blocker? Depolarizing NM blocker?
D-Tubocurarine
Succinylcholine
Why do the NM blockers not enter the CNS?
Because they are quaternary amines and highly ionized
3 mechanisms by which D-Tubocurarine blocks the NMJ?
- Binds to receptor (competes with ACh in low doses)
- Blocks channel (higher doses)
- Blocks pre-junctional Na+ channels which decreases ACh relsease
Prototype drug for depolarizing NM blocker?
Succinylcholine
Phase 1 blockade for succinylcholine
Binds to the NM causing strong, persistent depolarization. This leads to paralysis due to chronic activation