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30 Cards in this Set

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bladder toxicity, alopecia, lymphocytopenia, immunosuppresion, hemorrhagic cystitis from ACROLEIN, secondary neoplasm,
CYCLOPHOSPHAMIDE
IFOSFAMIDE

less ADRs with oral Cyclophosphamide, <> Innapropriate secretion of ADH can cause water intoxication
not vesicant, toxicity mainly hemotological
MELPHALAN
alkylating agents with renal toxicities
CYCLOPHOSPHAMIDE
IFOSFAMIDE
BUSULFAN
BCNU (carmustine)
CCNU (lomustine)
CISPLATINUM
CARBOPLATIN
use MESNA (2-mercaptoethanesulfonate) to conjugate toxic metabolites in urine, to wash-out to prevent toxicity
CYCLOPHOSPHAMIDE
alkylating agents used in breast cancer
CYCLOPHOSPHAMIDE
CHLORAMBUCIL
THIOTEPA
works in all patients, even patients deficient in mismatch repair protein when the other two don't work
OXALIPLATIN
nitrosoureas
BCNU (carmustine)
CCNU (lomustine)
methyl-CCNU (semustine)
STREPTOZOCIN
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
BCNU (carmustine)
alkylating agents for testicular cancer
IFOSFAMIDE
CISPLATINUM
slowest acting nitrogen mustard, must be converted by liver to active metabolite: Phenylacetic Acid Mustard
CHLORAMBUCIL
marrow ablative therapy, multiple myeloma, breast, ovary

enter cell via amino acid transporter pump
MELPHALAN
MECHLORETHAMINE
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
cross BBB, good for brain tumors, also good for Hodgkin and non-Hodgkin, Multiple myeloma and melanoma (also small cell lung for Lomustine)
nitrosoureas
local reaction from extravasation = vesicant, can tx with ice compress and thiosulfate
MECHLORETHAMINE
triazines
DACARBAZINE
PROCARBAZINE
TEMOZOLOMIDE
require initial activation by P450, Monofunctional alkylating agent causing depurination and DNA breaks
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
BUSULFAN
delayed (21 days) leukopenia and thrombocytopenia LUNG, LIVER and KIDNEY TOXICITIES
BCNU (carmustine)
lower NAD in beta cell of Langerhans islet
STREPTOZOCIN
IV mode
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
ADRs such as severe nausea, nephrotoxicity, ototoxcity
CISPLATINUM (Carboplatin less side effects but can cause myelosuppressio and hearing loss)
are alkylating agents CCS?
no
alkylating agents MOA
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)
enter cell via amino acid transporter pump
MELPHALAN
alkyl sulfonate
BUSULFAN
name the group of alkylating agents that cause secondary leukemias
nitrosoureas
name the compound that causes secondary lymphomas
CYCLOPHOSPHAMIDE
aziridines
THIOTEPA
HEXAMETHYLMELAMINE
alkylating agent with GI toxicities
THIOTEPA
MELPHALAN
BUSULFAN
alkylating agent with LIVER toxicity
BUSULFAN
CARMUSTINE
alkylating agent with lung toxicity
CARMUSTINE