Pharmacology: Entacapone Metabolism Quiz
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Questions and Answers

Which enzyme do entacapone and tolcapone inhibit to block the conversion of dopamine?

  • Glucuronidation enzyme
  • Monoamine oxidase
  • Alkene isomerase
  • Catechol-O-methyltransferase (correct)

    • What is the main route of excretion for the metabolites of safinamide?

  • Pulmonary excretion
  • Biliary excretion
  • Renal excretion (correct)
  • Fecal excretion

    • Which metabolite of entacapone is found in human plasma as an inactive form?

  • (S)-entacapone
  • (Z)-entacapone (correct)
  • (E)-entacapone
  • (R)-entacapone

    • What are the most common adverse effects associated with safinamide?

    <p>Uncontrolled involuntary movements, nausea, insomnia, falls</p> Signup and view all the answers

    Individuals using which of the following medications should not use safinamide?

    <p>Monoamine oxidase inhibitors</p> Signup and view all the answers

    Which medication is significantly metabolized prior to excretion, with only 0.2% of the parent drug found unchanged in urine?

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

    What is the main metabolic pathway for the parent drug of entacapone?

    <p>Glucuronidation by UGT1A9</p> Signup and view all the answers

    Which enzyme is a selective and reversible inhibitor in the context of Parkinson's disease treatment?

    <p>Catechol-O-methyltransferase</p> Signup and view all the answers

    What percentage of the urinary metabolites do the resulting glucuronides from the parent drug and the alkene isomer represent?

    <p>70% and 25%</p> Signup and view all the answers

    Which neurological condition is tolcapone indicated for as an adjunct therapy?

    <p>Parkinson's disease</p> Signup and view all the answers

    What effect does the nitro group have on the metabolism of the catechol of entacapone?

    <p>Blocks catechol-O-methyltransferase-mediated methylation</p> Signup and view all the answers

    In the cocrystal structure of tolcapone, what interaction does the catechol of tolcapone form?

    <p>Interaction with Mg2+ ion, hydrogen bond to Asn170, and ionic-dipole interaction with Glu199</p> Signup and view all the answers

    Which enzyme is inhibited by safinamide?

    <p>Monoamine oxidase</p> Signup and view all the answers

    What is the primary route of elimination for the metabolites of entacapone?

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

    Which compound may form directly by autooxidation of the parent drug carbidopa?

    <p>3,4-dihydroxyphenylacetone</p> Signup and view all the answers

    What is the main mechanism of action for tolcapone in the treatment of Parkinson's disease?

    <p>COMT inhibitor</p> Signup and view all the answers

    What are the most common adverse events in advanced Parkinson's disease patients treated with carbidopa?

    <p>Nausea and headache</p> Signup and view all the answers

    Iron salts can reduce the bioavailability of carbidopa by:

    <p>Chelating carbidopa</p> Signup and view all the answers

    Why does transfer not occur likely in the case of tolcapone?

    <p>Strong electron-donating effect of the nitro group</p> Signup and view all the answers

    What is the primary metabolite of tolcapone?

    <p>Glucuronide of the more sterically accessible phenol</p> Signup and view all the answers

    Which enzyme is responsible for mediating methylation to 3-Omethyl-tolcapone?

    <p>Catechol-O-methyltransferase</p> Signup and view all the answers

    What percentage of tolcapone is found unchanged in urine?

    <p>0.5%</p> Signup and view all the answers

    Which enzyme is not involved in the metabolism of tolcapone?

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

    What is a minor metabolite formed from tolcapone?

    <p>An aniline that is subsequently acetylated</p> Signup and view all the answers

    What are the most common adverse effects associated with tolcapone?

    <p>Nausea, anorexia, sleep disorder, vomiting</p> Signup and view all the answers

    Which enzyme is primarily inhibited by tolcapone?

    <p>Catechol-O-methyltransferase</p> Signup and view all the answers

    Which of the following is a dopamine receptor agonist used in the treatment of Parkinson's disease?

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

    What is the mechanism of action of apomorphine in the treatment of Parkinson's disease?

    <p>Stimulation of postsynaptic dopamine D2-type receptors</p> Signup and view all the answers

    Which class of alkaloids is apomorphine related to?

    <p>Aporphine alkaloids</p> Signup and view all the answers

    In the treatment of advanced Parkinson's disease, what is safinamide indicated for?

    <p>Hypomobility or 'off' episodes</p> Signup and view all the answers

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