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19 Cards in this Set
- Front
- Back
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Name the 2 drugs we talked about in class that kill cells at a specific stage in cell replication. How are they administered?
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5-fluorouracil
cytarabine Drugs must be administered by slow infusion or on a daily schedule for several days |
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Mechanisms of resistance to anti-neoplastic drugs. (5 of them)
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Decreased uptake
Increased efflux Inactivation Alteration of drug target Altered DNA repair |
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General side effects of anti-neoplastics
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Bone marrow suppression
Ulceration of the mouth and GI tract Alopecia (hair loss) Decreased resistance to infection Infertility Teratogenic effects (birth defects) Increased serum uric acid, potassium, phosphate, and calcium Nausea, vomiting, anorexia |
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Drug used to decrease the incidence of mucositis? Why does it work?
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PALIFERMIN (KEPIVANCETM)
Recombinant keratinocyte growth factor (KGF) KGF increases proliferation of endothelial cells (but not hematopoietic cell lineages, because they lack KGF receptor). |
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DRUGS USED TO CONTROL NAUSEA ASSOCIATED WITH CANCER CHEMOTHERAPY. How do they work? Are they useful for every emesis?
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Ondansetron and Granisetron.
Serotonin 5HT3 receptor antagonists. ACUTE EMESIS, usually controlled with 5HT3 antagonists and steroids. DELAYED EMESIS, Less frequent, but poorly controlled. |
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The 3 nitrogen mustard alkylating agents are:
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MECHLORETHAMINE:
CYCLOPHOSPHAMIDE: MELPHALAN: |
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Nitrogen mustards are highly reactive w/ ?
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water
proteins nucleic acids (Guanine bases of DNA) |
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This nitrogen mustard has the following characteristics:
Short half life in blood (few minutes) A vesicant (blistering agent) Must be administered parenterally |
Mechlorethamine
(not good for solid tumors because of short half-life) |
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This nitrogen mustard has the following characteristics:
Can be administered orally Half life about 6 hours Relatively platelet sparing Less likely than other mustards to produce secondary leukemias A prodrug that requires hepatic oxidation |
Cyclophosphamide
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Can melphalan be administered orally? Compare its halflife to mechlorethamine.
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Longer half life (several hours)
can be given orally |
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Toxic substance that is created when cyclophosphamide is administered? What does it cause?
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Acrolein
Hemorrhagic cystitis |
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Used to treat cyclophosphamide-induced hemorrhagic cystitis that is not controlled by hydration and diuresis.
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MESNA (MESNEX®)
Treatment of hemorrhagic cystitis that frequently occurs with usual doses of ifosphamide. Binds w/ acrolein! |
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Other alkylating agents that ARE NOT nitrogen mustards?
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NITROSOUREAS
TEMOZOLOMIDE BUSULFAN |
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Especially useful for treatment of CNS cancers. Delayed bone marrow suppression.
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NITROSOUREAS: Carmustine and Lomustine
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Treatment of anaplastic astrocytoma refractory to nitrosoureas
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TEMOZOLOMIDE
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Selective for granulocytes: used to treat chronic myelocytic leukemia. Unusual toxicity: pulmonary fibrosis
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BUSULFAN
(causes Busulfan lung) |
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What drug has these characteristics?
Wide spectrum of activity against blood and solid tumors Little effect on bone marrow Highly emetic. Requires use of antiemetic drugs Ototoxicity: High frequency hearing loss Renal toxicity: can be prevented with adequate hydration and diuresis |
CISPLATIN
(minimal effect on bone marrow is important because this is what limits dosage of most other antineoplastics) |
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WHAT DRUG IS USED AS PROTECTION AGAINST RENAL TOXICITY OF CISPLATIN? How does it work?
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AMIFOSTINE
-SH group reacts w/ cisplatin Cell needs alkaline phosphatase (AP) to add that -SH Normal cells have this AP Cancer cells do not! |
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MECHANISMS FOR DEVELOPMENT OF RESISTANCE TO ALKYLATING AGENTS (3 methods)
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1.)Decreased uptake, loss of choline uptake system
2.)Increased biotransformation, increased glutathione or metallothionein biosynthesis 3.) Altered DNA repair |
