41 Questions
Which step in cholinergic transmission is the rate-limiting step?
ACh Synthesis
Where are the subtypes of nicotinic receptors found?
Brain, ganglia, adrenal medulla, neuromuscular junction
What is the general effect of muscarinic antagonists?
Compete with ACh for binding at muscarinic receptors
Which type of cholinesterase inhibitor is irreversible and interacts only with the esteratic site?
Irreversible inhibitors
What is the primary role of cholinesterase inhibitors in clinical applications?
Treatment of Alzheimer's disease
Which type of cholinesterase inhibitor is a peripheral and CNS inhibitor of AChE?
Physostigmine
What is the mechanism of action of Botulinum toxin (BoTox)?
It blocks the release of acetylcholine
Which autoimmune disorder involves a loss of voltage-sensitive calcium channels on the presynaptic motor nerve terminal?
Lambert-Eaton
Which autoimmune disease is characterized by fatigable weakness of skeletal muscles?
Myasthenia Gravis
What are the major pharmacodynamic properties of competitive NMJ blockers?
Highly polar, quaternary compounds with poor oral bioavailability
What is the difference in pharmacokinetics between nondepolarizing and depolarizing NMJ blockers?
Nondepolarizing blockers are metabolized at the synapse, while depolarizing blockers are metabolized in the liver and/or eliminated by the kidney
Which step in cholinergic transmission is Ca2+-dependent?
ACh release
Where are the subtypes of muscarinic receptors found?
Parasympathetic postganglionic endings
What is the primary role of muscarinic agonists?
Activate muscarinic receptors
Which type of receptors are controlled by ligand gating?
Nicotinic receptors
Which type of receptors occur in the CNS, autonomic ganglia, medulla, and neuromuscular junction?
Nicotinic receptors
What is the rate-limiting step in cholinergic transmission?
ACh synthesis
Which type of cholinesterase inhibitor interacts only with the esteratic site and is irreversible?
Irreversible cholinesterase inhibitor
What is the general effect of muscarinic antagonists?
Reduce the effects of ACh
Where are the subtypes of nicotinic receptors found?
Central nervous system
What drives the transport of ACh into vesicles?
Exchange with H+
Which type of cholinesterase inhibitor is a slowly reversible inhibitor of AChE?
Reversible inhibitors
What is the primary role of cholinesterase inhibitors in clinical applications?
Reversal of paralysis from neuromuscular drugs
What is the mechanism of action of pralidoxime in treating organophosphate toxicity?
It displaces the dialkylphosphate residue from the phosphorylated enzyme
What is the target tissue of Botulinum toxin (BoTox)?
Both smooth and skeletal muscle synapses
What is the effect of Botulinum toxin (BoTox) on ACh release?
It decreases ACh release
Which autoimmune disease is associated with dysfunction at the neuromuscular junction?
Myasthenia Gravis
What is the pharmacologic treatment for Myasthenia Gravis?
Cholinesterase inhibitors
Which type of cholinesterase is primarily responsible for the metabolism of ACh at cholinergic synapses?
Acetylcholinesterase
Which type of cholinesterase is found in plasma, liver, and glia?
Pseudocholinesterase
Which type of cholinesterase inhibitor is irreversible and interacts only with the esteratic site?
Irreversible inhibitors
Which autoimmune disorder involves a loss of voltage-sensitive calcium channels on the presynaptic motor nerve terminal?
Lambert-Eaton
Which autoimmune disease affects the postsynaptic neuromuscular junction and is characterized by fatigable weakness of skeletal muscles?
Myasthenia Gravis
What is the primary pharmacodynamic property of competitive NMJ blockers?
Highly polar, quaternary compounds with poor oral bioavailability
What is the primary pharmacokinetic difference between nondepolarizing and depolarizing NMJ blockers?
Metabolism at the synapse
What drug class is used to reverse the effects of NMJ blockers by increasing the concentration of ACh at NMJ synapses?
Acetylcholinesterase inhibitors
How does sugammadex reverse the effects of NMJ blockers?
By sequestering NMJ antagonist in blood
What are the consequences of genetic variation on succinylcholine metabolism?
Prolonged post-succinylcholine neuromuscular blockade
What is the duration of action of succinylcholine?
2-6 minutes
What is the primary mechanism of action of competitive NMJ blockers?
Blockade of ACh neurotransmission at NMJ
What is the effect of competitive NMJ blockers on sensation?
Sensation is unaffected
Test your knowledge of the major processes in cholinergic transmission, including ACh synthesis, storage, release, and elimination. Learn about the rate-limiting step in ACh synthesis, the concentration of ACh in vesicles, and the role of presynaptic autoreceptors.
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