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Chemotherapy

Chemo One Liners

QuestionAnswer
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
Created by: tessah10