Alkylating Agents Flashcards
Mechlorethamine (1)
Alkylating agent; spontaneous conversion to active metabolites in body fluids or enzymatically converted in liver
Cyclophosphamide (Cytoxan) (1)
Alkylating agent; conversion by hepatic cytochrome P450 to active metabolite phosphoramide mustard
Ifosfamide (1)
Alkylating agent; conversion by hepatic cytochrome P450 to active metabolite phosphoramide mustard
Mechlorethamine (2)
Hodgkin’s disease, topically for treatment of cutaneous T-cell lymphoma
Cyclophosphamide (Cytoxan) (2)
Most widely used alkylating agent (broad clinical spectrum); singly or in combination for ALL, CLL, non-Hodgkin’s lymphoma, and breast, lung, and ovarian cancer
Ifosfamide (2)
Sarcoma and testicular cancer
Mechlorethamine (3)
Severe nausea and vomiting, myelosuppression (leucopenia, thrombocytopenia)
Cyclophosphamide (Cytoxan) (3)
Hemorrhagic cystitis (bladder irritation) due to acrolein (toxic drug metabolite); adequate hydration and administration of MESNA (2-mercaptoethane sulfonate) minimizes problem. Nausea, vomiting, myelosuppression
Ifosfamide (3)
Hemorrhagic cystitis (bladder irritation) due to acrolein (toxic drug metabolite); adequate hydration and administration of MESNA (2-mercaptoethane sulfonate) minimizes problem. Nausea, vomiting, myelosuppression
Carmustine (1)
Alkylating agent
Lomustine (1)
Alkylating agent
Carmustine (2)
Brain tumors (cross blood-brain barrier)
Lomustine (2)
Brain tumors (cross blood-brain barrier)
Carmustine (3)
Renal toxicity, pulmonary fibrosis. Profound myelosuppression, severe nausea and vomiting
Lomustine (3)
Renal toxicity, pulmonary fibrosis. Profound myelosuppression, severe nausea and vomiting
Decarbazine (1)
Alkylating agent; prodrug activated by liver cytochromes
Temozolomide (1)
Alkylating agent; nonenzymatic conversion to methylhydrazine at physiologic pH
Decarbazine (2)
Part of ABVD for Hodgkin’s disease; also, malignant melanoma. IV ADMIN
Temozolomide (2)
Malignant gliomas ORAL ADMIN
Decarbazine (3)
Nausea and vomiting, myelosuppression (neutropenia, thrombocytopenia), flu-like symptoms (fever, fatigue)
Temozolomide (3)
Nausea and vomiting, myelosuppression (neutropenia, thrombocytopenia), flu-like symptoms (fever, fatigue)
Cisplatin (1)
covalently bind nucleophilic sites on DNA (e.g., guanine N7); converted to active cytotoxic forms by reacting with water to form (+)charged, hydrated intermediates that react with DNA guanine, forming inter- and intrastand cross-links
Carboplatin (1)
covalently bind nucleophilic sites on DNA (e.g., guanine N7); converted to active cytotoxic forms by reacting with water to form (+)charged, hydrated intermediates that react with DNA guanine, forming inter- and intrastand cross-links
Oxaliplatin (1)
covalently bind nucleophilic sites on DNA (e.g., guanine N7); converted to active cytotoxic forms by reacting with water to form (+)charged, hydrated intermediates that react with DNA guanine, forming inter- and intrastand cross-links
Cisplatin (2)
Testicular, ovarian, cervical, and bladder cancers; also useful in treatment of head and neck cancer, and lung carcinoma
Carboplatin (2)
Ovarian cancer
Oxaliplatin (2)
Gastric and colorectal cancer
Cisplatin (3)
Nephrotoxicity, ototoxicity, peripheral motor and sensory neuropathy at high doses. Myelosupression. Severe nausea and vomiting
Carboplatin (3)
Myelosuppression (thrombocytopenia)
Oxaliplatin (3)
Peripheral sensory neuropathy (cold-induced). Neutropenia