Mechanism of Action and Pharmacokinetics of Cyclophosphamide Quiz

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Questions and Answers

What is the cytotoxic step in the mechanism of action of cyclophosphamide?

  • Metabolism to active compounds
  • Formation of hydroxylated intermediates
  • Reaction with DNA (correct)
  • Excretion in the urine

How are cyclophosphamide and ifosfamide primarily biotransformed in the liver?

  • To acrolein
  • To toxic metabolites
  • To phosphoramide mustard
  • To hydroxylated intermediates (correct)

Which enzyme plays a primary role in the metabolism of ifosfamide?

  • CYP450 2E1
  • CYP450 3A4 (correct)
  • CYP450 1A2
  • CYP450 2C9

What is the unique toxicity associated with both cyclophosphamide and ifosfamide?

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

Which compound is used to neutralize the toxic metabolites responsible for bladder toxicity?

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

Why are nitrosoureas like carmustine and lomustine primarily used in the treatment of brain tumors?

<p>Due to their ability to penetrate the CNS (D)</p> Signup and view all the answers

What is the primary mechanism of action of nitrosoureas?

<p>Inhibition of DNA replication (B)</p> Signup and view all the answers

In which type of cells is the cytotoxicity of nitrosoureas primarily expressed?

<p>Actively dividing cells (D)</p> Signup and view all the answers

What is the major excretory route for Dacarbazine and Temozolomide?

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

Which drug does not require the CYP450 system for metabolic transformation?

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

What is responsible for the alkylating activity of MTIC (methyltriazenoimidazole carboxamide)?

<p>Nucleophilic groups in DNA (C)</p> Signup and view all the answers

Which drug is used in the treatment of brain tumors like glioblastomas and astrocytomas?

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

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