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 (A)</p> Signup and view all the answers

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

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

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

<p>Glucuronidation by UGT1A9 (C)</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 (C)</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% (A)</p> Signup and view all the answers

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

<p>Parkinson's disease (A)</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 (C)</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 (B)</p> Signup and view all the answers

Which enzyme is inhibited by safinamide?

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

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

<p>Urine (C)</p> Signup and view all the answers

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

<p>3,4-dihydroxyphenylacetone (B)</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 (C)</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 (A)</p> Signup and view all the answers

Iron salts can reduce the bioavailability of carbidopa by:

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

What is the primary metabolite of tolcapone?

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

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

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

What percentage of tolcapone is found unchanged in urine?

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

Which enzyme is not involved in the metabolism of tolcapone?

<p>COMT (C)</p> Signup and view all the answers

What is a minor metabolite formed from tolcapone?

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

What are the most common adverse effects associated with tolcapone?

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

Which enzyme is primarily inhibited by tolcapone?

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

Which class of alkaloids is apomorphine related to?

<p>Aporphine alkaloids (A)</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 (C)</p> Signup and view all the answers

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