Antineoplastics - Alkylating Agents Flashcards
(30 cards)
Prodrug activated by CYP450-2B6
AE: hemorrhagic cystitis due to toxic metabolite Acrolein
Alkylating Agent
Cyclophosphamide, nitrogen mustard
Vesicant; no longer used
Alkylating Agent
Mechlorethamine
Used for Brain tumors and Lymphomas
Carbustine (IV) and Lomustine (oral); highly lipophilic –> cross BBB
AE: pulmonary fibrosis and Renal failure
Used for CML
Busulfan
Prodrug metabolized by CYP450-3A4 to Chloroacetaldehyde
Ifosfamide
AE of Ifosfamide
Neurotoxicity, nephrotoxicity, hemorrhagic cystitis
AE: oral ulceration, pulmonary fibrosis, hepatotoxicity
Melphalan
Given with Amifostine to reduce nephrotoxicity
Cisplatin
AE of Platinum compounds
Peripheral neuropathy, electrolyte disturbances, anaphylactic rxns
Alkylating Agent MOA
Alkylation at N7 position of Guanine; on single or both via cross-linking (intrastrand or b/t both)
Curative therapy for Testicular Cancer
Vinblastine + Cisplatin + Bleomycin
A Methylhydrazine
Procarbazine
AE of Procarbazine
Disulfiram-like rxn, metabolite is MAOI
Leukemogenic, mutagenic, teratogenic
Are Alkylating Agents cell-cycle specific or cell cycle non-specific?
Cell cycle non-specific
Alkylating agents that cause pulmonary fibrosis
Busulfan
Melphalan
Carmustine
Lomustine
Causes Oral ulceration
Melphalan
Cause hemorrhagic cystitis
Ifosfamide
Cyclophosphamide
Cross BBB
Carmustine
Lomustine
Vesicant
Mechlorethamine
Decarbazine
Given with Mesna to prevent?
Mesna prevents Hemorrhagic cystitis by Cyclophosphamide
Metabolite of Ifosfamide
Chloroacetaldehyde
Metabolite of Cyclophosphamide
Acrolein: irritates bladder mucosa
Nitrogen Mustards
Cyclophosphamide, Ifosfamide, Mechlorethamine, Melphalan
Used for Multiple Myeloma
Melphalan
