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Parasympathetic NS
PHAR340
22
Pharmacology
Undergraduate 3
12/06/2012

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Cards

Term
Hemicholinium
Definition
Blocks reuptake of choline into nerve terminal
Co-transport with Na+
Rate-limiting step
Term
Vesamicol
Definition
Inhibits Ach transport into vesicles
Antiporter with proton
Term
Botulinum toxin
Definition
Degrades proteins required for membrane-vesicle fusion and release of neurotransmitter
Term
Black widow toxin (ɑ-latrotoxin)
Definition
Uncontrolled release of neurotransmitter into the synaptic cleft
Muscle cramps, spasms and paralysis
Term
Acetylcholine
Activity? Degradation?
Definition
Muscarinic and nicotinic agonist
Degradation by cholinesterase
Term
Methacholine
Definition
Muscarinic >>> nicotinic agonist
Degradation by cholinesterase
Term
Carbachol
Definition
Nicotinic > muscarinic agonist
Term
Bethanechol
Definition
Muscarinic agonist only
Term
Edrophonium
Definition
Fast-acting (2-10 minutes)
Reversible binding to substrate binding site
Diagnosis for myasthenia gravis
Autoimmune disease, antibodies block Ach receptor
Term
Physostigmine, neostigmine
Definition
Medium (up to 6 hours)
Reversible, covalent binding to cholinesterase
Treatment for myasthenia gravis
Term
Organophosphates
Definition
Slow (many days)
Phosphorylates the substrate binding site and inactivates the enzyme (irreversible)
Treat poisoning with pralidoximine
Regenerates Ach at neuromuscular junction
Term
Atropine
Definition
Tertiary amine → CNS penetration
Use for cholinergic (organophosphate) poisoning at muscarinic receptor
Competitive antagonist
Term
Scopolamine
Definition
Tertiary amine → CNS penetration
Use for motion sickness
Decrease GI motility and increase sphincter tone
Term
Ipatropium
Definition

Anti-cholinergic

Synthetic, quaternary amine → poor CNS penetration Use for asthma Decrease bronchoconstriction and secretions

Term
Nicotine
Definition
Nicotinic receptor agonists (sodium channel)
Tertiary amines → CNS activity
Effect at sympathetic and parasympathetic ganglia
Increase/decrease in heart rate by stimulation of sympathetic/parasympathetic ganglia
Overall increase in heart rate and blood pressure by release of epinephrine
Transient stimulation followed by depression of peripheral NS and exocrine system
Increase GI motility and tone
Nausea, vomiting and diarrhea
Term
Lobeline
Definition
Nicotinic receptor agonists (sodium channel)
Tertiary amines → CNS activity
Effect at sympathetic and parasympathetic ganglia
Increase/decrease in heart rate by stimulation of sympathetic/parasympathetic ganglia
Overall increase in heart rate and blood pressure by release of epinephrine
Transient stimulation followed by depression of peripheral NS and exocrine system
Increase GI motility and tone
Nausea, vomiting and diarrhea
Term
Hexamethonium
Definition
Ganglionic blocking drug
Term
Decamethonium
Definition
Neuromuscular junction blocking drug
Depolarizing blocking agent
Term
Tubocurarine
Definition
Non-Depolarizing blocking agents
Occupy NM receptor without activation of sodium channel
Motor paralysis, skeletal muscle relaxation
Hypotension, tachycardia, bronchospasm
Term
Vecuronium
Definition
Non-Depolarizing blocking agents
Occupy NM receptor without activation of sodium channel
Motor paralysis, skeletal muscle relaxation
Hypotension, tachycardia, bronchospasm
Term
Pancuronium
Definition
Non-Depolarizing blocking agents
Occupy NM receptor without activation of sodium channel
Motor paralysis, skeletal muscle relaxation
Hypotension, tachycardia, bronchospasm
Term
Succinylcholine
Definition
Depolarizing blocking agent
Phase I: irreversible depolarization, brief excitation
Phase II: agonist continues to occupy receptor binding site, reversible with AChE
Rapid, complete, predictable paralysis
Susceptible to AChE
Blocking effects augmented by AChE inhibitors
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