Cholinergic Agonists and Acetylcholinesterase Inhibitors
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Questions and Answers

What are cholinergic agonists also known as?

  • Parasympathomimetics or muscarinic agonists (correct)
  • Acetylcholinesterase inhibitors
  • Ganglionic stimulants
  • Adrenergic agonists

    • How can the effects of cholinergic agonists be achieved?

  • Only by preventing the breakdown of ACh by acetylcholinesterase (AChE)
  • By either direct agonist effect or by preventing the breakdown of ACh by AChE (correct)
  • Only by direct agonist effect
  • By both direct agonist effect and by preventing the breakdown of ACh by AChE

    • What is the main difference between the desired drug action and the adverse drug reactions (ADRs) of cholinergic agonists?

  • There is no difference between the desired drug action and ADRs
  • The desired drug action and ADRs are the same across all organs
  • The desired drug action targets a specific organ, while the ADRs affect other organs (correct)
  • The desired drug action and ADRs are organ-specific

    • Which category of cholinergic agonists includes nicotine as the prototypical drug?

    <p>Ganglionic stimulants</p> Signup and view all the answers

    Where are muscarinic receptors located?

    <p>In the eye, heart, blood vessels, lung, GI tract, urinary bladder, and sweat glands</p> Signup and view all the answers

    How do muscarinic agonists modify organ function?

    <p>By both activating muscarinic receptors on target organs and inhibiting the release of neurotransmitters from nerve terminals</p> Signup and view all the answers

    Which of the following is a characteristic of bethanechol?

    <p>It increases the tone of the detrusor urinae muscle.</p> Signup and view all the answers

    Which of the following is a reason bethanechol is contraindicated in patients with peptic ulcer disease?

    <p>It can cause excessive secretion of gastric acid.</p> Signup and view all the answers

    Which of the following is a characteristic of ACh (Miochol)?

    <p>It is highly susceptible to cholinesterase.</p> Signup and view all the answers

    Which of the following is a use of pilocarpine?

    <p>Treating glaucoma.</p> Signup and view all the answers

    Which of the following is a characteristic of the pharmacokinetics of bethanechol?

    <p>Its effects peak in 60 minutes for the oral dose.</p> Signup and view all the answers

    Which of the following is a reason bethanechol is contraindicated in patients with urinary tract obstruction?

    <p>It can increase pressure within the urinary tract.</p> Signup and view all the answers

    Which of the following is a characteristic of carbachol?

    <p>It acts at both muscarinic and nicotinic receptors.</p> Signup and view all the answers

    Which of the following is a characteristic of the pharmacokinetics of bethanechol?

    <p>Its effects are more prolonged than those of ACh.</p> Signup and view all the answers

    Which of the following is a reason bethanechol is contraindicated in patients with bronchospastic disorders?

    <p>It can stimulate muscarinic receptors in the lungs, resulting in bronchoconstriction.</p> Signup and view all the answers

    Which of the following is a characteristic of methacholine (Provocholine)?

    <p>It is active at muscarinic receptors only.</p> Signup and view all the answers

    What is the primary contraindication for bethanechol?

    <p>Cardiovascular disease</p> Signup and view all the answers

    How does bethanechol affect heart rate and blood pressure in patients with hyperthyroidism?

    <p>It causes increased heart rate due to increased NE release.</p> Signup and view all the answers

    What is the recommended route of administration for atropine as an antidote for bethanechol toxicity?

    <p>Subcutaneous</p> Signup and view all the answers

    Which of the following drugs should not be taken concurrently with bethanechol?

    <p>All of the above</p> Signup and view all the answers

    What is the recommended initial oral dose of bethanechol for urinary retention?

    <p>10-50 mg</p> Signup and view all the answers

    What is the recommended initial subcutaneous dose of bethanechol for urinary retention?

    <p>2.5 mg</p> Signup and view all the answers

    How should the patient take bethanechol to avoid nausea and vomiting?

    <p>Take 1 hour before or 2 hours after meals</p> Signup and view all the answers

    What is the maximum single dose of atropine recommended for children under 12 years old for bethanechol toxicity?

    <p>0.4 mg</p> Signup and view all the answers

    What adverse reactions may occur with bethanechol administration?

    <p>All of the above</p> Signup and view all the answers

    What is the primary use of bethanechol in primary care?

    <p>Treatment of urinary retention due to neurogenic atony of the bladder</p> Signup and view all the answers

    What percentage of the population has a genetic variation that leads to reduced levels of activity of CYP 2D6?

    <p>7%</p> Signup and view all the answers

    What percentage of the dose of galantamine is excreted unchanged in the urine?

    <p>20%</p> Signup and view all the answers

    What is the total renal elimination percentage for galantamine?

    <p>95%</p> Signup and view all the answers

    What is the recommended maximum daily dose of galantamine for patients with moderate hepatic impairment or moderate renal impairment?

    <p>16 mg/day</p> Signup and view all the answers

    What is the mechanism of metabolism for rivastigmine?

    <p>Primarily by cholinesterase-mediated hydrolysis</p> Signup and view all the answers

    How does moderate renal impairment affect the clearance of rivastigmine?

    <p>Decreases clearance by 64%</p> Signup and view all the answers

    What is the primary route of elimination for memantine?

    <p>Renal excretion</p> Signup and view all the answers

    What is the Pregnancy Category for donepezil?

    <p>Category C</p> Signup and view all the answers

    What is the Pregnancy Category for rivastigmine and galantamine?

    <p>Category B</p> Signup and view all the answers

    What is the Pregnancy Category for memantine?

    <p>Category B</p> Signup and view all the answers

    In patients with hepatic impairment, how should donepezil be dosed?

    <p>Donepezil should be titrated to response and tolerability</p> Signup and view all the answers

    What is the recommended dosage of memantine for patients with CrCl between 5 and 29 mL/min?

    <p>The dosage should not exceed 14 mg</p> Signup and view all the answers

    Which of the following adverse reactions is commonly associated with the use of cholinergic agonists and cholinesterase inhibitors?

    <p>All of the above</p> Signup and view all the answers

    Which of the following is true regarding the adverse reactions associated with donepezil, galantamine, and rivastigmine?

    <p>They are well tolerated, with few adverse reactions</p> Signup and view all the answers

    What is the recommended treatment for cholinergic-associated adverse reactions?

    <p>Temporarily reducing the dose or taking the drug with meals</p> Signup and view all the answers

    What is the main reason why cholinergic agonists and cholinesterase inhibitors should be used with caution in patients with a history of bronchospastic disorders?

    <p>They can exacerbate bronchospastic symptoms</p> Signup and view all the answers

    Which of the following drug interactions is considered unacceptable for cholinergic agonists and cholinesterase inhibitors?

    <p>Suppression of warning symptoms of overdose with atropine and belladonna derivatives</p> Signup and view all the answers

    Why are cholinergic agonists thought to have some potential to cause generalized seizures?

    <p>They can increase cholinergic activity in the brain</p> Signup and view all the answers

    Which of the following is true regarding the metabolism of donepezil and galantamine?

    <p>They undergo significant metabolism by the CYP enzyme systems of the liver</p> Signup and view all the answers

    In patients with renal impairment, what is the recommended dosing for donepezil?

    <p>No dosage adjustments are recommended</p> Signup and view all the answers

    What effect does erythromycin have on the bioavailability of galantamine?

    <p>Increases it due to inhibition of CYP 3A4</p> Signup and view all the answers

    Which enzyme inhibition causes an increase in the AUC of galantamine when taken with paroxetine?

    <p>CYP 2D6</p> Signup and view all the answers

    What effect do drugs that make urine alkaline have on the renal clearance of memantine?

    <p>Decrease renal clearance</p> Signup and view all the answers

    Which drugs interact with memantine due to shared renal cation exchange system for clearance?

    <p>Loop diuretics</p> Signup and view all the answers

    What is the mainstay treatment for myasthenia gravis?

    <p>Neostigmine and pyridostigmine</p> Signup and view all the answers

    How is the optimal dose for neostigmine and pyridostigmine in myasthenia gravis typically established?

    <p>By administering small initial doses followed by titration to an optimal dose</p> Signup and view all the answers

    What is the primary mechanism of action for cholinesterase inhibitors?

    <p>They prevent the degradation of ACh by acetylcholinesterase (AChE)</p> Signup and view all the answers

    Which of the following is NOT a reversible cholinesterase inhibitor?

    <p>Organophosphate cholinesterase inhibitors</p> Signup and view all the answers

    Which of the following statements about memantine (Namenda) is correct?

    <p>It is a cholinesterase inhibitor used to treat Alzheimer's disease</p> Signup and view all the answers

    What is the primary mechanism by which reversible cholinesterase inhibitors increase acetylcholine levels?

    <p>They bind to the active center of AChE, preventing the breakdown of ACh</p> Signup and view all the answers

    Which of the following statements about donepezil (Aricept) is correct?

    <p>It is a piperidine-type AChE inhibitor with increased affinity for the CNS</p> Signup and view all the answers

    What is the primary mechanism by which cholinesterase inhibitors can increase the risk of adverse effects?

    <p>They can intensify ACh activity at all cholinergic junctions (muscarinic, ganglionic, and nicotinic)</p> Signup and view all the answers

    Which of the following statements about rivastigmine (Exelon) is correct?

    <p>It is a potent selective inhibitor of AChE in the cortex and hippocampus</p> Signup and view all the answers

    Which of the following is NOT a potential adverse effect of cholinesterase inhibitors?

    <p>Increased production of AChE</p> Signup and view all the answers

    Which of the following statements about irreversible cholinesterase inhibitors is correct?

    <p>They are found in pesticides and chemical weapons</p> Signup and view all the answers

    What is the primary reason for using cholinesterase inhibitors in the treatment of Alzheimer's disease?

    <p>Alzheimer's disease is associated with profound cholinergic depletion</p> Signup and view all the answers

    What accounts for the decreased number of peripheral cholinergic ADRs of the drug, like donepezil?

    <p>The drug's selectivity for the brain</p> Signup and view all the answers

    How does the drug's carbamate structure affect its binding to AChE?

    <p>It results in slower dissociation from AChE compared to ACh</p> Signup and view all the answers

    What type of inhibitor of AChE is this drug considered to be?

    <p>Pseudo-irreversible</p> Signup and view all the answers

    How does the drug's plasma half-life compare to the duration of AChE inhibition?

    <p>The plasma half-life is shorter than the duration of AChE inhibition</p> Signup and view all the answers

    What additional mechanism of action does galantamine have besides AChE inhibition?

    <p>Enhancing the effect of ACh on nicotinic receptors</p> Signup and view all the answers

    How does the progression of Alzheimer's disease affect the efficacy of these cholinergic drugs?

    <p>The drugs become less effective as the disease progresses</p> Signup and view all the answers

    What is the primary mechanism of action of memantine in the treatment of Alzheimer's disease?

    <p>Noncompetitive antagonism of NMDA receptors</p> Signup and view all the answers

    How does the bioavailability of rivastigmine compare to donepezil and galantamine?

    <p>Rivastigmine has lower bioavailability due to a significant first-pass effect</p> Signup and view all the answers

    How are neostigmine and pyridostigmine primarily eliminated from the body?

    <p>Primarily as unchanged drug in the urine</p> Signup and view all the answers

    How is donepezil primarily metabolized?

    <p>Primarily by CYP 2D6 and 3A4 isoenzymes in the liver</p> Signup and view all the answers

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