Term
|
Definition
interrupt DNA and RNA biosynthesis.
mainly in S-phase.
Structure similarity to normal cellular metabolites |
|
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Term
|
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. |
|
|
Term
| oral or topical low-dose antimetabolites use |
|
Definition
| maintenance and palliative cancer therapy. |
|
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Term
| Antimetabolites (toxicity) |
|
Definition
Myelosuppression
gastrointestinal ulcerations
hair loss
nausea and vomiting |
|
|
Term
| Dose-limoting toxicity for antimetabolites for all classes |
|
Definition
|
|
Term
| Antimetabolites (classification) |
|
Definition
Folate (folic acid) antagonists
Pyrimidine antagonists
Purine antagonists |
|
|
Term
| Which antimetabolites are phosphorylated inside the body into nucleotide form in order to be cytotoxic.) |
|
Definition
Pyrimidine antagonists
Purine antagonists |
|
|
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 |
|
Definition
|
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Term
| Folate (folic acid) antagonists MOA |
|
Definition
block active site of DHFR enzyme that reduce folic acid to its active form.
decrease methylation --> decrease DNA/RNA --> cytotoxic in S-phase |
|
|
Term
| Typical folate antagonists |
|
Definition
Methotrexate/leucovorin
Pemetrexed
Pralatrexate |
|
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Term
|
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 |
|
|
Term
| What type of inhibitor is methotrexate |
|
Definition
| competitive due to structure similarity to folic acid |
|
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Term
|
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. |
|
|
Term
| MTX dose-dependent toxicity |
|
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
|
Definition
Renal toxicity
Immunosuppression.
Hepatotoxicity. |
|
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Term
|
Definition
(folic acid agonist) given with folic acid antagonists to protect healthy cells and reduce bone marrow suppression.
Treat MTX overdose |
|
|
Term
|
Definition
|
|
Term
|
Definition
inhibits 3 enzymes used in purine and pyrimidine synthesis
1. thymidylate synthase (TS)
2. dihydrofolate reductase (DHFR)
3. glycinamide ribonucleotide formyltransferase |
|
|
Term
| Pemetrexed + cisplatin treat |
|
Definition
|
|
Term
|
Definition
| non-small cell lung cancer. |
|
|
Term
| pemetrexed dose-limiting toxicity |
|
Definition
|
|
Term
|
Definition
Mental fatigue and sleepiness.
Nausea and vomiting.
Diarrhea.
Oral mucositis (mouth, throat, or lip sores).
Loss of appetite.
Skin rash.
Constipation |
|
|
Term
| Supplement with Pemetrexed |
|
Definition
| Folic acid and vitamin B12 supplementation appears to reduce toxicity, while not interfering efficacy |
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