Mechanism of Action and Pharmacokinetics of Cyclophosphamide Quiz

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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?

Hemorrhagic cystitis Signup and view all the answers

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

Mesna Signup and view all the answers

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

Due to their ability to penetrate the CNS Signup and view all the answers

What is the primary mechanism of action of nitrosoureas?

Inhibition of DNA replication Signup and view all the answers

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

Actively dividing cells Signup and view all the answers

What is the major excretory route for Dacarbazine and Temozolomide?

Kidney Signup and view all the answers

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

Temozolomide Signup and view all the answers

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

Nucleophilic groups in DNA Signup and view all the answers

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