Term
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Definition
Blocks reuptake of choline into nerve terminal
Co-transport with Na+
Rate-limiting step |
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Term
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Definition
Inhibits Ach transport into vesicles
Antiporter with proton |
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Term
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Definition
| Degrades proteins required for membrane-vesicle fusion and release of neurotransmitter |
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Term
| Black widow toxin (ɑ-latrotoxin) |
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Definition
Uncontrolled release of neurotransmitter into the synaptic cleft
Muscle cramps, spasms and paralysis |
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Term
Acetylcholine
Activity? Degradation? |
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Definition
Muscarinic and nicotinic agonist
Degradation by cholinesterase |
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Term
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Definition
Muscarinic >>> nicotinic agonist
Degradation by cholinesterase |
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Term
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Definition
| Nicotinic > muscarinic agonist |
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Term
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Definition
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Term
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Definition
Fast-acting (2-10 minutes)
Reversible binding to substrate binding site
Diagnosis for myasthenia gravis
Autoimmune disease, antibodies block Ach receptor |
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Term
| Physostigmine, neostigmine |
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Definition
Medium (up to 6 hours)
Reversible, covalent binding to cholinesterase
Treatment for myasthenia gravis |
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Term
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Definition
Slow (many days)
Phosphorylates the substrate binding site and inactivates the enzyme (irreversible)
Treat poisoning with pralidoximine
Regenerates Ach at neuromuscular junction |
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Term
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Definition
Tertiary amine → CNS penetration
Use for cholinergic (organophosphate) poisoning at muscarinic receptor
Competitive antagonist |
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Term
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Definition
Tertiary amine → CNS penetration
Use for motion sickness
Decrease GI motility and increase sphincter tone |
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Term
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Definition
Anti-cholinergic
Synthetic, quaternary amine → poor CNS penetration Use for asthma Decrease bronchoconstriction and secretions |
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Term
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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 |
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Term
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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 |
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Term
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Definition
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Term
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Definition
Neuromuscular junction blocking drug
Depolarizing blocking agent |
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Term
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Definition
Non-Depolarizing blocking agents
Occupy NM receptor without activation of sodium channel
Motor paralysis, skeletal muscle relaxation
Hypotension, tachycardia, bronchospasm |
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Term
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Definition
Non-Depolarizing blocking agents
Occupy NM receptor without activation of sodium channel
Motor paralysis, skeletal muscle relaxation
Hypotension, tachycardia, bronchospasm |
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Term
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Definition
Non-Depolarizing blocking agents
Occupy NM receptor without activation of sodium channel
Motor paralysis, skeletal muscle relaxation
Hypotension, tachycardia, bronchospasm |
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Term
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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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