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54 Cards in this Set
- Front
- Back
- 3rd side (hint)
Mechlorethamine |
Alkylating nitrogen mustard -lacks ring structure -first nitrogenous mustard -dose limiting: leukopenia & thrombocytopenia -need intact veins or else result in necrosis via extravasasion |
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Cyclophosphamide* |
Alkylating nitrogen mustard *most widely used alkylating agent -activated by CYP2B -acute myelosuppression -elimination: hepatic metabolism -wide use cancer, autoimmune disorders
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Ifosfamide |
Alkylating nitrogen mustard -similar to cyclophosphamide -activated by CYP3A4 -activated more slowly therefore requires higher dose --> increased risk of cytotoxicity -most neurotoxic of the class -acute myelosuppression
adverse: hemorrhagic cystitis - |
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Melphalan |
Alkylating nitrogen mustard |
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Chlorambucil |
-Alkylating nitrogen mustard. -More stable and orally available than Mechlorethamine . -acute myelosuppression |
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Hexamethylamine |
Alyklating ethlinimine |
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Thiotepa |
Alyklating ethylenemine -myelosuppression -forms DNA cross links |
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Busulfan |
Alkylating sulfonate -MOA: myelosuppression -used in high-dose regimen -treats chronic myelogenous leukemia |
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Carmustine |
Alkylating nitosource |
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Lomustine |
Alkylating nitosource |
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Streptozotocin |
Alkylating nitosource -antibiotic -treats pancreatic islet cell carcinoma, carcinoid tumor -MOA: methylnitrosourea moiety attached to glucose |
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Dacarbazine |
Alkylating triazine -adds methyl group to DNA -activated by CYP -prototype -combination therapy for Hodgkin's lymphoma |
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Temozolomide |
-Alkylating triazine -prodrug of carbazine -standard in combination with radiation therapy -malignant glioma and astrocytoma/brain tumors -not cell cycle specific |
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Methotrexate |
Antimetabolite: folic acid analog Treats: RA MOA: 1)inhibits DHFR --> S phase in B and T cells 2) block thymidylate and purine synthesis -mitosis
-1/2 intrathecal drugs for meningismus/seizures
Adverse: hepatotoxicity, myelosuppression, GI effects
-can accumulate in 3rd spaces: ascites, pleural effusion, subcutaneous edema
-antidote: leukovorin, pholynic acid |
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5-FU |
-Anti metabolite pyramidine analog -Inhibit thymidylate synthesis -5-10% of population lack hepatic enzyme that deactivated 5-FU - |
5-flurouridine |
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Floxuridine |
Anti metabolite pyramidine analog |
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Cytarabine; Ara-C; Cytosine arabinoside |
-Anti metabolite pyramidine analog -most important anti metabolite for AML(acute myeloid leukemia) -intrathecal dose for meningeal/lymphomatous leukemia -CdK is rate limiting activating enzyme -disrupts base-pairing -adverse: myelosuppression, cerebellar/cerebral toxicity
-2 of 2 Intrathecal drugs |
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6-Mercaptopurine |
-Anti metabolite purine analog -MOA: inhibit purine synthesis -mitosis |
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Thioguanine |
Anti metabolite purine analog |
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Cladribine |
Anti metabolite purine analog |
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Fludarabine |
-Anti metabolite purine analog(HGPRT) -affects granulocyte lineage(phagocyte) -adverse: neutropenia --> infection -affects CD+4 --> HIV-like immunosuppression-->opportunistic infection
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Vinca alkaloids |
Vincristine, vinblastine, vinorelbine
Anti-mitosis agents: metaphase -binds beta tubulin blocking polymerization with alpha tubulin -motorized spindle not intact. Cell arrest in metaphase: chromosomes do not align
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Paclitaxel |
Anti-mitotic taxane. Stabilizes microtubule--> tubulin polymerization. Inhibits M phase Myelosuppression dose limiting |
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Docetaxel |
Anti-mitotic taxane. Stabilizes microtubule--> tubulin polymerization. Inhibits M phase Myelosuppression dose limiting |
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Topotecan |
-captothecin analog -MOA: Binds topoisomerase I inhibits re-ligation -ovarian cancer and small cell lung carcinoma -neutropenia |
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Irinotecan |
-camptothecan analog -Binds topoisomerase I -colorectal cancer -adverse: delayed diarrhea, myelosuppression |
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Etoposide |
Epipodophyllotoxin MOA: binds Topoisomerase II |
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Teniposide |
Epipodophyllotoxin MOA: binds Topoisomerase II |
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Doxorubicin* |
-Anthracycline/tumor antibody MOA: binds Topoisomerase II -solid tumors - |
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Epirubicin* |
-Anthracycline/tumor antibody MOA: binds Topoisomerase II -solid tumors |
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Danunorubicin |
-Anthracycline/tumor antibody -MOA: binds Topoisomerase II -acute leukemia |
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Idarubicin |
Anthracycline/tumor antibody MOA: binds Topoisomerase II -acute leukemia |
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Mitomycin |
-Tumor antibody -ONLY DRUG FOR ANAL CANCER |
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Bleomycin |
-Tumor antibody -adverse: pulmonary fibrosis, cumulative dose => 250 units |
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Dactinomycin |
-Tumor antibody -solid tumors in children -choriocarcinoma in women -binds dsDNA -one of most potent antitumor agent -adverse: anorexia, hematopoietic suppression, proctitis, diarrhea, glossitis, cheilitis |
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Carboplatin |
Platinum agent |
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Cisplatin |
-Platinum agent -nephrotoxicity |
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Carboplatin |
-Platinum agent -myelosuppression |
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Oxaliplatin |
-Platinum agent -neuropathy |
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Mitoxantrone |
-(Natural product:anthracenedione) -acute myelogenous leukemia, breast/prostate cancer |
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Mitoxantrone |
-(Natural product:anthracenedione) -acute myelogenous leukemia, breast/prostate cancer |
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Hydroxyurea |
-Inhibits ribonucleotide reductase -S phase -substituted urea |
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Procarbazine |
-Alkylating agent: methylhydrazine derivative -Hodgkin's disease -adverse: blocks catecholamine synthesis, HTN, carcinogenic, teratogenic |
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Mitotane |
-hormone antagonist: adrenocortical suppressant -adrenal cortical cancer |
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Gemcitabine |
-Pyrimidine analog anti-metabolite -metastatic pancreatic; non-squamous, non-small cell lung; ovarian; and bladder cancer -myelosuppression |
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Capecitabine |
-pyrimidine analog antimetabolite -prodrug of 5-FU -treats metastatic breast and colorectal cancer -adverse effect: Hand-foot syndrome: erythema, desquamation, pain, sensitive palms and soles |
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Platinum |
-Ovarian, head and neck, bladder, esophagus, lung, colon cancer -MOA: binds DNA --> distort. Form adducts--> recognition by MisMatch Repair enzyme --> apoptosis |
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Estramustine |
-natural product: hormone agent -MOA: damages microtubules -prostate cancer -myelosuppression, hypercalcemia, hypersensitivity, angioedema -estrogen effects:gynecomastia, impotence |
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Ixabepilone |
-natural product: Epothilones -MOA: damages microtubules (like taxane) -breast cancer -similar toxicity as taxane |
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Premetrexed |
-Knocks out purine/pyrimidine synthesis -needs to be supplemented with Vit B and folic acid to limit toxicity |
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Alkylating agents |
-need p53 to work -not phase specific? |
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Nitro source alkylating |
-one of few groups that are active against CNS |
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Camptothecins |
-freezes topoisomerase -adverse: criggler najar or Gilbert's -diarrhea toxicity: cholinergic mediated -atropine = prophylaxis for diarrhea - |
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Anthracyclines |
-dose-limiting: cardiotoxicity: ROOS --> myocytes high in O2 - |
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