Cholinergic Agents

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Questions and Answers

Which enzyme hydrolyzes acetylcholine?

Butyrylcholinesterase

AChE (correct)

Where are cholinergic terminals found?

Muscle Skeletal

Autonomic System

Central Nervous System

All of the above (correct)

Which receptor subtype is responsible for bronchoconstriction?

M3 (correct)

What is the effect of M2 receptors on the cardiovascular system?

Decrease heart rate Signup and view all the answers

Which receptor subtype is responsible for vasodilation?

M3 Signup and view all the answers

Which type of receptors do cholinergic neurons have?

Both mAChRs and nAChRs Signup and view all the answers

What are the subunits of mAChRs?

a, B, y Signup and view all the answers

What are the subunits of nAChRs?

a, B, y, E Signup and view all the answers

Which muscarinic agonist is used for the treatment of glaucoma and ocular surgery?

Miostat (carbachol chloride) Signup and view all the answers

Which muscarinic agonist is used for bronchial challenge test?

Provocholine (methacholine chloride) Signup and view all the answers

Which receptor does Methacholine primarily act on?

Muscarinic receptors Signup and view all the answers

What is the main therapeutic application of Methacholine?

Treatment of asthma and COPD Signup and view all the answers

Which of the following is a contraindication for Methacholine use?

Coronary insufficiency Signup and view all the answers

What is the effect of Methacholine on the cardiovascular system?

It causes bradycardia and hypotension Signup and view all the answers

What is the primary diagnostic use of Methacholine?

Diagnosis of asthma and COPD Signup and view all the answers

Which isomer of ACh hydrolyzes slower than acetylcholine by AChE?

S-(+)-P-ACh Signup and view all the answers

What is the SAR of Urecholine (bethanechol chloride)?

It has a metilo group and a carbamate group Signup and view all the answers

Which amine in pilocarpene reacts to form HCl salt?

Tertiary amine Signup and view all the answers

What metabolic/physicochemical vulnerabilities do you expect pilocarpene to have?

Epimerization Signup and view all the answers

What kind of relationship do the highlighted functional groups in Arecoline and Xanomeline have?

Bioisosteric (nonclassical) Signup and view all the answers

Which enzyme is responsible for breaking down Acetylcholine (ACh)?

Acetylcholinesterase (AChE) Signup and view all the answers

What is the role of autoreceptors in the cholinergic system?

To regulate the release of ACh Signup and view all the answers

Which neurotransmitter is released by the sympathetic system to decrease the release of ACh?

Norepinephrine (NE) Signup and view all the answers

What is the role of M4 receptors in the cholinergic system?

To regulate the release of ACh Signup and view all the answers

What happens when there is an excess of ACh in the synapse?

ACh escapes the synapse Signup and view all the answers

Which of the following is a reversible acetylcholinesterase inhibitor that forms a more stable inactive site of AChE or has a higher affinity for the active site than ACh but does not react as a substrate?

Antilirium Signup and view all the answers

Which of the following drugs is a synthetic compound that resembles physostigmine and is used for prophylaxis of abdominal distension and urinary retention, myasthenia gravis, and reversal of neuromuscular blockade?

Prostigmin Signup and view all the answers

Which of the following drugs is a synthetic compound closely related to neostigmine, has a longer duration of action, and a lower incidence of side effects?

Mestinon Signup and view all the answers

Which of the following drugs is a centrally-acting reversible and non-competitive inhibitor with a long elimination half-life of 70+ hours?

Aricept Signup and view all the answers

Which of the following drugs is a pseudo-irreversible inhibitor that inhibits plasma choline-E and crosses the blood-brain barrier?

Exelon Signup and view all the answers

What is the primary diagnostic use of Methacholine?

Bronchial challenge test Signup and view all the answers

Which muscarinic agonist is used for the treatment of glaucoma and ocular surgery?

Pilocarpine Signup and view all the answers

Which receptor does Methacholine primarily act on?

M3 Signup and view all the answers

Which type of receptors are coupled to G-proteins and produce effectors in cholinergic neurons?

mAChRs Signup and view all the answers

What is the main therapeutic application of Miostat (carbachol chloride)?

Treatment of glaucoma and ocular surgery Signup and view all the answers

Which muscarinic agonist is preferentially selective for mAChRs over nAChRs?

Xanomeline Signup and view all the answers

What is the main diagnostic use of Provocholine (methacholine chloride)?

Bronchial challenge test Signup and view all the answers

What makes carbachol chloride more stable to hydrolysis compared to ACh?

Carbamate ester Signup and view all the answers

Which of the following drugs is a reversible acetylcholinesterase inhibitor that forms a more stable inactive site of AChE or has a higher affinity for the active site than ACh but does not react as a substrate?

Antilirium Signup and view all the answers

What is the elimination half-life of Cognex (tacrine HCl)?

1.5-4 hrs Signup and view all the answers

Which of the following drugs is a centrally-acting reversible and non-competitive inhibitor with a long elimination half-life of 70+ hours?

Aricept Signup and view all the answers

Which of the following drugs crosses the blood-brain barrier and is not associated with hepatotoxicity?

Exelon Signup and view all the answers

Which of the following is an irreversible acetylcholinesterase inhibitor that generates an extremely stable phosphorylated-Serine residue in AChE?

Phospholine Iodide Signup and view all the answers

Which of the following statements about acetylcholine (ACh) is correct?

ACh is hydrolyzed by Acetylcholinesterase (AChE) Signup and view all the answers

Which receptor subtype is responsible for bronchoconstriction?

M3 Signup and view all the answers

Which of the following is a therapeutic application of Bethanechol?

Retaining urine in non-obstructive cases Signup and view all the answers

Which of the following statements about Muscarinic receptors is correct?

M2 and M4 receptors are acutely inhibited by Gi proteins Signup and view all the answers

Which of the following drugs is used for the treatment of open-angle glaucoma and xerostomia (dry-mouth)?

Salogen or Isopto Carpine (pilocarpene HCl) Signup and view all the answers

Which of the following drugs is a partial direct M1 agonist in the CNS and an M3 agonist in the epithelial tissue of lacrimal and salivary glands?

Evoxac (Cevimeline Hydrochloride) Signup and view all the answers

What is the main therapeutic application of Acetylcholinesterase (AChE) inhibitors?

All of the above Signup and view all the answers

What is the catalytic triad involved in the esteratic site of AChE?

Glutamate, histidine, serine Signup and view all the answers

If the AChE enzyme is acylated by an agent with a more stable functional group, what happens?

It becomes inactive for a longer period of time Signup and view all the answers

What is the main diagnostic use of Methacholine?

To diagnose asthma and COPD Signup and view all the answers

Which of the following is true about Methacholine's effect on the cardiovascular system?

Methacholine causes bradycardia and hypotension Signup and view all the answers

Which of the following is a therapeutic application of Methacholine?

Treatment of asthma and COPD Signup and view all the answers

Which receptor subtype is responsible for vasodilation?

M3 Signup and view all the answers

What is the effect of M2 receptors on the cardiovascular system?

Negative chronotropic effect Signup and view all the answers

What is the main therapeutic application of Acetylcholinesterase (AChE) inhibitors?

Treatment of myasthenia gravis Signup and view all the answers

True or false: Acetylcholine is a neurotransmitter for both the sympathetic and parasympathetic nervous systems.

False Signup and view all the answers

True or false: Muscarinic cholinergic agents interact with nicotinic receptors.

False Signup and view all the answers

True or false: Muscarinic acetylcholinergic receptors are metabotropic receptors.

True Signup and view all the answers

True or false: Pirenzepine acts as a muscarinic agonist without blocking the effect of muscarinic antagonists?

False Signup and view all the answers

True or false: Anticholinergic agents are used to treat glaucoma?

False Signup and view all the answers

True or false: Odd numbered mAChRs are coupled to Gq proteins?

True Signup and view all the answers

True or false: Nicotinic receptors are found in the neuromuscular junctions, adrenal medulla, and autonomic ganglia?

True Signup and view all the answers

True or false: ACh cannot be administered orally due to its physicochemical properties and inability to penetrate the Blood-Brain Barrier?

True Signup and view all the answers

True or false: Acetylcholine (ACh) is a poor therapeutic agent due to its promiscuity towards both muscarinic (mAChRs) and nicotinic (nAChRs) receptors?

True Signup and view all the answers

Which of the following drugs is a non-specific muscarinic agonist that acts as an agonist to both mAChRs and nAChRs?

Miostat (carbachol chloride) Signup and view all the answers

True or false: Muscarinic agonists with a longer chain length between the ethylene group and the N atom have increased activity?

False Signup and view all the answers

True or false: Muscarinic agonists with quaternary ammonium groups substituted with heteroatoms like S, Se, Ar, Ph are more active than those with nitrogen?

False Signup and view all the answers

Which of the following drugs is a specific muscarinic agonist that has a preference to act as an agonist to mAChRs over nAChRs?

Pilocarpine Signup and view all the answers

Which of the following drugs is a synthetic compound closely related to neostigmine, has a longer duration of action, and a lower incidence of side effects?

Neostigmine Signup and view all the answers

Which of the following drugs is used for the treatment of post-surgical and post-partum urinary retention?

Urecholine (bethanechol chloride) Signup and view all the answers

Which muscarinic agonist is used to treat open-angle glaucoma and xerostomia (dry-mouth)?

Salogen or Isopto Carpine (pilocarpene HCl) Signup and view all the answers

Which muscarinic agonist is a partial direct M1 agonist in the CNS and an M3 agonist in epithelial tissue of lacrimal and salivary glands?

Evoxac (Cevimeline Hydrochloride) Signup and view all the answers

Which muscarinic agonist has affinity for M3 subtype and is used as an ocular and oral treatment for open-angle glaucoma and xerostomia (dry-mouth)?

Salogen or Isopto Carpine (pilocarpene HCl) Signup and view all the answers

Which of the following drugs is an irreversible acetylcholinesterase inhibitor that generates an extremely stable phosphorylated-Serine residue in AChE?

Antilirium (Physostigmine) Signup and view all the answers

Which of the following drugs is a synthetic compound closely related to neostigmine, has a longer duration of action, and a lower incidence of side effects?

Mestinon (Pyridostigmine) Signup and view all the answers

Which of the following drugs is a reversible acetylcholinesterase inhibitor that forms a more stable inactive site of AChE or has a higher affinity for the active site than ACh but does not react as a substrate?

Antilirium (Physostigmine) Signup and view all the answers

Which of the following drugs is an alkaloid isolated from the calabar bean (Physostigma venenosum), carbamylates AChE at a slow rate but has high affinity, and can diffuse across the blood-brain barrier?

Antilirium (Physostigmine) Signup and view all the answers

Study Notes

Cholinergic System

Acetylcholine (ACh) is broken down by the enzyme acetylcholinesterase (AChE)
Cholinergic terminals are found in the neuromuscular junction, autonomic ganglia, and central nervous system

Receptors and Agonists

Muscarinic receptors are responsible for various physiological responses, including bronchoconstriction and vasodilation
M2 receptors are responsible for bronchoconstriction
M3 receptors are responsible for vasodilation
Methacholine is a muscarinic agonist used for bronchial challenge tests and has a primary diagnostic use for bronchial hyperreactivity
Methacholine primarily acts on M3 receptors
Pilocarpine is a muscarinic agonist used to treat glaucoma and ocular surgery

Enzymes and Inhibitors

Acetylcholinesterase (AChE) is the enzyme responsible for breaking down acetylcholine (ACh)
Reversible acetylcholinesterase inhibitors, such as Neostigmine, form a more stable inactive site of AChE or have a higher affinity for the active site than ACh
Physostigmine is a reversible acetylcholinesterase inhibitor that crosses the blood-brain barrier
Tacrine is a centrally-acting reversible and non-competitive inhibitor with a long elimination half-life of 70+ hours

Autoreceptors and Neurotransmitters

Autoreceptors in the cholinergic system decrease the release of ACh
The sympathetic system releases norepinephrine to decrease the release of ACh
M4 receptors play a role in the cholinergic system

Other

Excess ACh in the synapse leads to increased transmission
Arecoline and Xanomeline have a synergistic relationship between their functional groups

Studying That Suits You

Use AI to generate personalized quizzes and flashcards to suit your learning preferences.

Description

Test your knowledge on Agonistas Muscarínicos Directos and their role in the cholinergic system. This multiple-choice exam will assess your understanding of neurotransmission, the transformation of choline into acetylcholine, and the release of acetylcholine from vesicles. Put your knowledge to the test and see how well you know these structures.

Cholinergic Agents - Caro

Podcast

Questions and Answers

Which enzyme hydrolyzes acetylcholine?

Where are cholinergic terminals found?

Which receptor subtype is responsible for bronchoconstriction?

What is the effect of M2 receptors on the cardiovascular system?

Which receptor subtype is responsible for vasodilation?

Which type of receptors do cholinergic neurons have?

What are the subunits of mAChRs?

What are the subunits of nAChRs?

Which muscarinic agonist is used for the treatment of glaucoma and ocular surgery?

Which muscarinic agonist is used for bronchial challenge test?

Which receptor does Methacholine primarily act on?

What is the main therapeutic application of Methacholine?

Which of the following is a contraindication for Methacholine use?

What is the effect of Methacholine on the cardiovascular system?

What is the primary diagnostic use of Methacholine?

Which isomer of ACh hydrolyzes slower than acetylcholine by AChE?

What is the SAR of Urecholine (bethanechol chloride)?

Which amine in pilocarpene reacts to form HCl salt?

What metabolic/physicochemical vulnerabilities do you expect pilocarpene to have?

What kind of relationship do the highlighted functional groups in Arecoline and Xanomeline have?

Which enzyme is responsible for breaking down Acetylcholine (ACh)?

What is the role of autoreceptors in the cholinergic system?

Which neurotransmitter is released by the sympathetic system to decrease the release of ACh?

What is the role of M4 receptors in the cholinergic system?

What happens when there is an excess of ACh in the synapse?

Which of the following is a reversible acetylcholinesterase inhibitor that forms a more stable inactive site of AChE or has a higher affinity for the active site than ACh but does not react as a substrate?

Which of the following drugs is a synthetic compound that resembles physostigmine and is used for prophylaxis of abdominal distension and urinary retention, myasthenia gravis, and reversal of neuromuscular blockade?

Which of the following drugs is a synthetic compound closely related to neostigmine, has a longer duration of action, and a lower incidence of side effects?

Which of the following drugs is a centrally-acting reversible and non-competitive inhibitor with a long elimination half-life of 70+ hours?

Which of the following drugs is a pseudo-irreversible inhibitor that inhibits plasma choline-E and crosses the blood-brain barrier?

What is the primary diagnostic use of Methacholine?

Which muscarinic agonist is used for the treatment of glaucoma and ocular surgery?

Which receptor does Methacholine primarily act on?

Which type of receptors are coupled to G-proteins and produce effectors in cholinergic neurons?

What is the main therapeutic application of Miostat (carbachol chloride)?

Which muscarinic agonist is preferentially selective for mAChRs over nAChRs?

What is the main diagnostic use of Provocholine (methacholine chloride)?

What makes carbachol chloride more stable to hydrolysis compared to ACh?

Which of the following drugs is a reversible acetylcholinesterase inhibitor that forms a more stable inactive site of AChE or has a higher affinity for the active site than ACh but does not react as a substrate?

What is the elimination half-life of Cognex (tacrine HCl)?

Which of the following drugs is a centrally-acting reversible and non-competitive inhibitor with a long elimination half-life of 70+ hours?

Which of the following drugs crosses the blood-brain barrier and is not associated with hepatotoxicity?

Which of the following is an irreversible acetylcholinesterase inhibitor that generates an extremely stable phosphorylated-Serine residue in AChE?

Which of the following statements about acetylcholine (ACh) is correct?

Which receptor subtype is responsible for bronchoconstriction?

Which of the following is a therapeutic application of Bethanechol?

Which of the following statements about Muscarinic receptors is correct?

Which of the following drugs is used for the treatment of open-angle glaucoma and xerostomia (dry-mouth)?

Which of the following drugs is a partial direct M1 agonist in the CNS and an M3 agonist in the epithelial tissue of lacrimal and salivary glands?

What is the main therapeutic application of Acetylcholinesterase (AChE) inhibitors?

What is the catalytic triad involved in the esteratic site of AChE?

If the AChE enzyme is acylated by an agent with a more stable functional group, what happens?

What is the main diagnostic use of Methacholine?

Which of the following is true about Methacholine's effect on the cardiovascular system?

Which of the following is a therapeutic application of Methacholine?

Which receptor subtype is responsible for vasodilation?

What is the effect of M2 receptors on the cardiovascular system?

What is the main therapeutic application of Acetylcholinesterase (AChE) inhibitors?

True or false: Acetylcholine is a neurotransmitter for both the sympathetic and parasympathetic nervous systems.

True or false: Muscarinic cholinergic agents interact with nicotinic receptors.

True or false: Muscarinic acetylcholinergic receptors are metabotropic receptors.

True or false: Pirenzepine acts as a muscarinic agonist without blocking the effect of muscarinic antagonists?

True or false: Anticholinergic agents are used to treat glaucoma?

True or false: Odd numbered mAChRs are coupled to Gq proteins?

True or false: Nicotinic receptors are found in the neuromuscular junctions, adrenal medulla, and autonomic ganglia?

True or false: ACh cannot be administered orally due to its physicochemical properties and inability to penetrate the Blood-Brain Barrier?

True or false: Acetylcholine (ACh) is a poor therapeutic agent due to its promiscuity towards both muscarinic (mAChRs) and nicotinic (nAChRs) receptors?

Which of the following drugs is a non-specific muscarinic agonist that acts as an agonist to both mAChRs and nAChRs?

True or false: Muscarinic agonists with a longer chain length between the ethylene group and the N atom have increased activity?

True or false: Muscarinic agonists with quaternary ammonium groups substituted with heteroatoms like S, Se, Ar, Ph are more active than those with nitrogen?

Which of the following drugs is a specific muscarinic agonist that has a preference to act as an agonist to mAChRs over nAChRs?

Which of the following drugs is a synthetic compound closely related to neostigmine, has a longer duration of action, and a lower incidence of side effects?

Which of the following drugs is used for the treatment of post-surgical and post-partum urinary retention?

Which muscarinic agonist is used to treat open-angle glaucoma and xerostomia (dry-mouth)?

Which muscarinic agonist is a partial direct M1 agonist in the CNS and an M3 agonist in epithelial tissue of lacrimal and salivary glands?

Which muscarinic agonist has affinity for M3 subtype and is used as an ocular and oral treatment for open-angle glaucoma and xerostomia (dry-mouth)?

Which of the following drugs is an irreversible acetylcholinesterase inhibitor that generates an extremely stable phosphorylated-Serine residue in AChE?