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30 Cards in this Set
- Front
- Back
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bladder toxicity, alopecia, lymphocytopenia, immunosuppresion, hemorrhagic cystitis from ACROLEIN, secondary neoplasm,
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CYCLOPHOSPHAMIDE
IFOSFAMIDE less ADRs with oral Cyclophosphamide, <> Innapropriate secretion of ADH can cause water intoxication |
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not vesicant, toxicity mainly hemotological
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MELPHALAN
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alkylating agents with renal toxicities
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CYCLOPHOSPHAMIDE
IFOSFAMIDE BUSULFAN BCNU (carmustine) CCNU (lomustine) CISPLATINUM CARBOPLATIN |
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use MESNA (2-mercaptoethanesulfonate) to conjugate toxic metabolites in urine, to wash-out to prevent toxicity
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CYCLOPHOSPHAMIDE
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alkylating agents used in breast cancer
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CYCLOPHOSPHAMIDE
CHLORAMBUCIL THIOTEPA |
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works in all patients, even patients deficient in mismatch repair protein when the other two don't work
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OXALIPLATIN
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nitrosoureas
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BCNU (carmustine)
CCNU (lomustine) methyl-CCNU (semustine) STREPTOZOCIN |
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activated by spontaneous breakdown, bifunctional alkylating agents reacting with G, C and A base <> can also modify DNA repair enzymes so inhibit DNA, RNA and protein synthesis
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BCNU (carmustine)
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alkylating agents for testicular cancer
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IFOSFAMIDE
CISPLATINUM |
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slowest acting nitrogen mustard, must be converted by liver to active metabolite: Phenylacetic Acid Mustard
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CHLORAMBUCIL
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marrow ablative therapy, multiple myeloma, breast, ovary
enter cell via amino acid transporter pump |
MELPHALAN
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MECHLORETHAMINE
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Hodgkin (part of MOPP, see Vincristine) and non-Hodgkin, lymphomas and lung carcinoma (infusion for) metastatic carcinoma resulting in effusion
enter cell via amino acid transporter pump |
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cross BBB, good for brain tumors, also good for Hodgkin and non-Hodgkin, Multiple myeloma and melanoma (also small cell lung for Lomustine)
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nitrosoureas
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local reaction from extravasation = vesicant, can tx with ice compress and thiosulfate
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MECHLORETHAMINE
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triazines
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DACARBAZINE
PROCARBAZINE TEMOZOLOMIDE require initial activation by P450, Monofunctional alkylating agent causing depurination and DNA breaks |
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CML, myeloproliferative d/o such as severe thrombocytosis, polycythemia vera, adjunctive tx in myelofibrosis, used with other drugs like Alopurinol in very high dose to wipe out bone marrow in prep for marrow transplant
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BUSULFAN
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delayed (21 days) leukopenia and thrombocytopenia LUNG, LIVER and KIDNEY TOXICITIES
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BCNU (carmustine)
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lower NAD in beta cell of Langerhans islet
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STREPTOZOCIN
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IV mode
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CYCLOPHOSPHAMIDE (IV or PO)
IFOSFAMIDE MELPHALAN MECHLORETHAMINE (IV, intra-peritoneal, pleural, pericardial) THIOTEPA (IV, intracavity, intravesicular or directly into tumor) BCNU (carmustine) STREPTOZOCIN DACARBAZINE PROCARBAZINE (PO too) Platinum analogs |
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ADRs such as severe nausea, nephrotoxicity, ototoxcity
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CISPLATINUM (Carboplatin less side effects but can cause myelosuppressio and hearing loss)
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are alkylating agents CCS?
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no
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alkylating agents MOA
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substitute alkyl group for active H atom, toxic to rapid growing cells, dose-limiting factor is myelosuppression, reduce women fertility, impair men fertility, chronic use may cause irreversible marrow damage and leukemogenesis, RESISTANCES: 1- decrease permeability of cells, 2-production of Glutathione S-transferase as false target for alkylation, 3-possibly increasing activity of DNA repair systems; TOXICITY: 1-immunosuppression, 2-destruction of GI epithelium and mucositis, possible diarrhea, ADRs: N&V, need Odansetron as antiemetic Tx, amenorrha, impaired spermatogenesis, teratogenesis, alopecia, pulmonary fibrosis, hemorrhagic cystitis (cyclophosphamide and ifosfamide)
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enter cell via amino acid transporter pump
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MELPHALAN
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alkyl sulfonate
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BUSULFAN
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name the group of alkylating agents that cause secondary leukemias
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nitrosoureas
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name the compound that causes secondary lymphomas
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CYCLOPHOSPHAMIDE
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aziridines
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THIOTEPA
HEXAMETHYLMELAMINE |
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alkylating agent with GI toxicities
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THIOTEPA
MELPHALAN BUSULFAN |
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alkylating agent with LIVER toxicity
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BUSULFAN
CARMUSTINE |
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alkylating agent with lung toxicity
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CARMUSTINE
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