Folic Acid Analogues: MTX and Pemetrexed

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Questions and Answers

What is the main mechanism of action of purine analogs like 6-Mercaptopurine and 6-Thioguanine?

  • They inhibit the activity of topoisomerase enzymes, leading to DNA damage.
  • They intercalate into DNA, preventing transcription and replication.
  • They inhibit the synthesis of DNA by interfering with the biosynthesis of purine bases. (correct)
  • They alkylate and crosslink DNA strands, leading to cell death.

Which of the following is a common adverse effect of purine analog drugs like 6-Mercaptopurine and 6-Thioguanine?

  • Bone marrow suppression (correct)
  • Neurotoxicity
  • Cardiotoxicity
  • Hepatorenal toxicity

Why is allopurinol often given to patients receiving cancer chemotherapy with drugs like 6-Mercaptopurine?

  • Allopurinol inhibits xanthine oxidase, which metabolizes 6-Mercaptopurine, leading to higher plasma levels.
  • Allopurinol enhances the antitumor activity of 6-Mercaptopurine by inhibiting purine synthesis.
  • Allopurinol protects against the cardiotoxic effects of 6-Mercaptopurine.
  • Allopurinol prevents the formation of uric acid, which can lead to gout and kidney stones during chemotherapy. (correct)

Which of the following is a potential drug interaction with methotrexate that can lead to toxicity?

<p>Concomitant use of NSAIDs like aspirin (B)</p> Signup and view all the answers

How can toxicity from methotrexate be managed?

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

Which of the following leukemias is 6-Thioguanine commonly used to treat?

<p>Acute myeloid leukemia (D)</p> Signup and view all the answers

Which enzyme does methotrexate inhibit in mammalian cells?

<p>Dihydrofolate reductase (B)</p> Signup and view all the answers

What is the primary dose-limiting toxicity of methotrexate and pemetrexed?

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

Which drug is indicated for the treatment of non–small cell lung cancer and mesothelioma, in combination with cisplatin?

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

What is the management strategy known as leucovorin rescue used for?

<p>Reducing methotrexate toxicity to normal cells (D)</p> Signup and view all the answers

What adverse effect can long-term use of methotrexate cause?

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

How can alkalinization of urine help in reducing methotrexate toxicity?

<p>Reduce renal toxicity (C)</p> Signup and view all the answers

What is the mechanism of action of nitrogen mustard prodrugs like cyclophosphamide and ifosfamide?

<p>Require activation by hepatic cytochrome P450 enzymes (A)</p> Signup and view all the answers

Which type of cancer is non-Hodgkin lymphoma commonly treated with?

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

What adverse effect is commonly associated with nitrogen mustard agents like cyclophosphamide and ifosfamide?

<p>Hemorrhagic cystitis (D)</p> Signup and view all the answers

Which sulfhydryl compound is often coadministered to prevent hemorrhagic cystitis caused by nitrogen mustard agents?

<p>2-mercaptoethanesulfonate (Mesna) (A)</p> Signup and view all the answers

Which platinum analog is used to treat colorectal cancer?

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

What is the main adverse effect associated with cisplatin among the platinum analogs?

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

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