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Chemotherapy
Chemo One Liners
| Question | Answer |
|---|---|
| Constant proportion of cell population killed rather than a constant number | Log-kill hypothesis |
| Treatment with cancer chemotherapy at high doses every 3-4 weeks, too toxic to be used continuously | Pulse therapy |
| Toxic effect of anticancer drug can be lessened by rescue agents | Rescue therapy |
| Drug used concurrently with toxic anticancer agents to reduce renal precipitation of urates | Allopurinol |
| Pyrimidine analog that causes "Thymine-less death" given with leucovorin rescue | 5-flouracil (5-FU) |
| Drug used in cancer therapy causes Cushing-like symptoms | Prednisone |
| Side effect of Mitomycin | SEVERE myelosuppression |
| MOA of cisplatin | Alkylating agent |
| Common toxicities of cisplatin | Nephro and ototoxicity |
| Analog of hypoxanthine, needs HGPRTase for activation | 6-mercaptopurine (6-MP) |
| Interaction with this drug requires dose reduction of 6- MP | Allopurinol |
| May protect against doxorubicin toxicity by scavenging free radicals | Dexrazoxane |
| Blows DNA (breaks DNA strands), limiting SE is pulmonary fibrosis | Bleomycin |
| Bleomycin+vinblastine+etoposide+cisplatin produce almost a 100% response when all agents are used for this neoplasm | Testicular cancer |
| ABVD regimen used for HD, but appears less likely to cause sterility and secondary malignancies than MOPP | Adriamycin (doxorubicin) +bleomycin, vinblastine +dacarbazine |
| Regimen used for non-Hodgkin's lymphoma | CHOP (cyclophosphamide, doxorubicin, vincristine, and prednisone) plus rituximab |
| Regimen used for breast cancer | CMF (cyclophosphamide, methotrexate, and fluorouracil) and tamoxifen if ER+ |
| Alkylating agent, vesicant that causes tissue damage with extravasation | Mechlorethamine |
| Anticancer drug also used in RA, produces acrolein in urine that leads to hemorrhagic cystitis | Cyclophosphamide |
| Prevention of cyclophosphamide induced hemorrhagic cystitis | Hydration and mercaptoethanesulfonate (MESNA) |
| Microtubule inhibitor that causes peripheral neuropathy, foot drop (eg. ataxia), and "pins and needles" sensation | Vincristine |
| Interact with microtubules (but unlike vinca which prevent disassembly of tubules), it stabilizes tubulin and cells remain frozen in metaphase | Paclitaxel (taxol) |
| Toxicities include nephrotoxicity and ototoxicity, leading to a severe interaction with aminoglycosides | Cisplatin |
| Agent similar to cisplatin, less nephrotoxic, but greater myelosuppression | Carboplatin |
| Converts asparagine to aspartate and ammonia, denies cancer cells of essential AA (asparagine) | L-asparaginase |
| Used for hairy cell leukemia, it stimulates NK cells | Interferon alpha |
| Anti-androgen used for prostate cancer | Flutamide (Eulexin) |
| Anti-estrogen used for estrogen receptor + breast cancer | Tamoxifen |
| Aromatase inhibitor used in breast cancer | Letrozole, anastrozole |
| Newer estrogen receptor antagonist used in advanced breast cancer | Toremifene (Fareston) |
| Some cell cycle non-specific drugs | Alkylating agents (eg., mechlorethamine, cyclophosphamide), antibiotics (doxorubicin, daunorubicin), cisplatin, nitrosourea |
| Anti-emetics used in association with anti-cancer drugs that are 5-HT3 (serotonin receptor subtype ) antagonists | Odansetron, granisetron |
| Nitrosoureas with high lipophilicity, used for brain tumors | Carmustine (BCNU) and lomustine (CCNU) |
| Produces disulfiram-like reaction with ethanol | Procarbazine |
| Extravasation causes tissue necrosis | Vesicants |
| Carmustine has what toxicity | irritant |
| Dacarbazine has what toxicity | irritant |
| Etoposide has was toxicity | irritiant |
| Streptozocin has what toxicity | irritant |
| Paclitaxel has what toxicity | irritant |
| Decreased cellular uptake is a mechanism of resistance of what two drugs? | methotrexate and cytarabine |
| anthracyclines,vinca alkaloids, topoisomerase II inhibitors and taxanes have what mechanism of resistance? | Increased effluxof the drug due to MDR |
| Alteration in what target enzyme = resistance to methotrexate? | dihydrofolate reductase |
| What enzyme is altered in irinotecan resistance? | topoisomerase I |
| What enzyme is altered in cytarabine resistance? | DNA polymerase |
| What enzyme is altered in etoposide and doxorubicin resistance? | topoisomerase II |
| What enzyme is altered in flurouracil resistance? | thymidylate synthetase |
| What chemo drug must be activated by the liver? | cyclophosphamide |
| What chemo drug is metabolized by DPD? | Flurouracil |
| What chemo drug is metabolized by cytidine deaminase? | cytarabine |
| What drug is converted it's active form, SN-38? | irinotecan |
| What two classes of drugs can have resistance by increased glutathione/glutathione S transferase | alkylating agents and cisplatin |
| What drug has cerebellar toxicity? | cytarabine (Ara-C) |
| What two drugs cause encephaopathy? | Ifosfamide and l-asparaginase |
| 2 drugs that cause myelopathy | Vincristine and cytarabine |
| 3 drugs that cause neuropathy | taxanes, cytarabine and eptoposide |
| What chemo drug causes cardiac necrosis at high doses? | Cyclophosphamide |
| Breast, leukemia, lymphoma, bone marrow transplant all use | Cyclophosphamide. Very immunosuppressive, can be used in rheumatic dx |
| What drug is structurally similar to cyclophosphamide and requires liver enzyme activation? | Ifosfamide |
| What drug produces the urotoxic metabolite acrolein? | Ifosfamide and cyclophosphamide |
| What crosses the BBBs the source of neurotoxicity | Ifosfamide |
| lethargy, confusion, encephalopathy, ATN, neutropenia and hemorrhagic cystitis are side effects of | Ifosfamide |
| What treatment stops the effects of Ifosfamide toxicity? | Methylene blue |
| What is used to counteract the effects of acrolein in the bladder? | Mesna |
| What cell cycle are antimetabolites most effective? | S phase |
| What drug inhibits DNA synthesis of thymidylate and purines | Methotrexate |
| Methotrexate binds to what increasing the chance of drug interactions | albumin |
| What drug distributes to third spaces | Methotrexate |
| What can cross to the brain in high doses? | Methotrexate |
| What provides reduced folates to bypass blockade of DHFR | Leucovorin |
| Acidic urine pH is a risk factor for toxicity of what? | Methotrexate |
| What drug given 10 days prior to methotrexate may reduce toxicity? | L-asparaginase |
| Prevents cells from entering S-phase and reduces the effects of methotrexate | L-asparaginase |
| What drug forms a phosphorylated nucleotide, falsely incorporates into DNA and terminates chain elongation | Cytarabine |
| Cytarabine is an analogue of what | pyrimidine |