Term
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Definition
interrupt DNA and RNA biosynthesis.
mainly in S-phase.
Structure similarity to normal cellular metabolites |
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Term
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Definition
combination chemotherapy as solid tumors and some hematologic cancers
are particularly effective in the treatment of leukemias
Colon, rectal, breast, stomach, lung, pancreatic
immunosuppressant in transplantations to control rejection reactions. |
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Term
oral or topical low-dose antimetabolites use |
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Definition
maintenance and palliative cancer therapy. |
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Term
Antimetabolites (toxicity) |
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Definition
Myelosuppression gastrointestinal ulcerations hair loss nausea and vomiting |
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Term
Dose-limoting toxicity for antimetabolites for all classes |
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Definition
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Term
Antimetabolites (classification) |
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Definition
Folate (folic acid) antagonists
Pyrimidine antagonists
Purine antagonists |
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Term
Which antimetabolites are phosphorylated inside the body into nucleotide form in order to be cytotoxic.) |
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Definition
Pyrimidine antagonists
Purine antagonists |
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Term
needed to synthesize DNA, repair DNA, and methylate DNA. It acts as co-enzyme in the one-carbon transfer during the biosynthesis of purine and pyrimidine |
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Definition
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Term
Folate (folic acid) antagonists MOA |
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Definition
block active site of DHFR enzyme that reduce folic acid to its active form.
decrease methylation --> decrease DNA/RNA --> cytotoxic in S-phase |
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Term
Typical folate antagonists |
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Definition
Methotrexate/leucovorin Pemetrexed Pralatrexate |
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Term
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Definition
binds and inhibits the enzyme dihydrofolate reductase (DHFR), and thus prevents the conversion of dietary folate to tetrahydrofolate.
tetrahydrofolate is essential for purine and pyrimidine synthesis, synthesis of amino acids serine and methionine |
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Term
What type of inhibitor is methotrexate |
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Definition
competitive due to structure similarity to folic acid |
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Term
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Definition
Chemotherapy breast, head and neck, leukemia, lymphoma, lung, osteosarcoma, bladder, and trophoblastic neoplasms Autoimmune disorders Rheumatoid arthritis, Juvenile dermatomyositis, psoriasis, psoriatic arthritis, lupus, sarcoidosis, Crohn's disease, and many forms of vasculitis. |
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Term
MTX dose-dependent toxicity |
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Definition
Myelosuppression (Thrombocytopenia and Leukopenia). Gastrointestinal toxicity (Oral mucositis is early sign of GI toxicity. Severe mucositis, Small bowel ulceration & bleeding, Diarrhea - requires cessation to prevent perforation of gut) |
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Term
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Definition
Renal toxicity Immunosuppression. Hepatotoxicity. |
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Term
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Definition
(folic acid agonist) given with folic acid antagonists to protect healthy cells and reduce bone marrow suppression. Treat MTX overdose |
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Term
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Definition
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Term
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Definition
inhibits 3 enzymes used in purine and pyrimidine synthesis 1. thymidylate synthase (TS) 2. dihydrofolate reductase (DHFR) 3. glycinamide ribonucleotide formyltransferase |
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Term
Pemetrexed + cisplatin treat |
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Definition
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Term
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Definition
non-small cell lung cancer. |
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Term
pemetrexed dose-limiting toxicity |
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Definition
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Term
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Definition
Mental fatigue and sleepiness. Nausea and vomiting. Diarrhea. Oral mucositis (mouth, throat, or lip sores). Loss of appetite. Skin rash. Constipation |
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Term
Supplement with Pemetrexed |
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Definition
Folic acid and vitamin B12 supplementation appears to reduce toxicity, while not interfering efficacy |
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