Cholinergic Antagonist Flashcards
Exam 4
Nicotinic receptor antagonist
- ganglionic blocking agents
- neuromuscular blocking agents
Muscarinic receptor antagonist
- block muscarinic receptor of PSN
- blocking PSN allows SNS to go unopposed
- used to relax smooth muscle, decrease gland secretions, and stimulate heart
Ganglionic blocking agents
- mecamylamine
- prevents stimulation of postsynaptic receptors by ACh released from presynaptic nerve endings
Neuromuscular blocking agents
- bind to nicotinic receptor on skeletal muscle inhibiting neurotransmission leading to muscle weakness and paralysis
- nondepolarizing neuromuscular blocking agents
- depolarizing neuromuscular blocking agents
Nondepolarizing neuromuscular blocking agents
- competitive antagonists of ACh at nicotinic receptors
- Atracurium, cistracurium, pancuronium, rocuronium, vecuronium
Depoarlizing neuromuscular blocking agents
- binds to and continually stimulates nicotinic receptors, inhibiting neuron from further depolarization, preventing neuronal impuses
- Succinylcholine
Eye muscarinic receptor antagonist
- Atropine (mydriasis & bradycardia)
- Homatropine
- Tropicamide
CNS muscarinic receptor antagonist
- Bentropine
- Trihexyphenidyl
- Scopolamine
GI & respiratory muscarinic receptor antagonist
-Glycopyrrolate (decrease mucus production)
GI muscarinic receptor antagonist
- Hyoscyamine
- Dicyclomine
Respiratory muscarinic receptor antagonist
- Ipratopium (asthma and COPD)
- Tiotropium
GU muscarinic receptor antagonist
- Oxybutyinin
- Darifenacin
- Solifenacin
- Tolterodine
MOA of muscarinic antagonist
- compete with ACh for muscarinic receptors at parasympathetic junctions and inhibit nerve stimulation
- reversible antagonist which block M1, M2, or M3 receptors depending on selectivity of the agent
- because they are reversible blockers their effects can overcome by giving larger doses of agonist = more ACh
Anticholinergic effects on eye
- block M3 receptors
- pupillary constrictor muscles are inhibited (relax)
- mydriasis & cycloplegia: paralysis of the accommodation muscle for near vision causing blurred vision
- dry eyes (from decreased tearing)
- clinical use: eye exams to dilate pupils & paralyze lens
Anticholinergic effects on CNS
- agents block several muscarinic receptor subtypes
- sedation
- anti motion sickness action
- anti parkinson action
- amnesia
- delirium