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Antineoplastic I & II
N/A
23
Pharmacology
Professional
11/10/2013

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Term
Antimetabolites
Definition
interrupt DNA and RNA biosynthesis.

mainly in S-phase.

Structure similarity to normal cellular metabolites
Term
Antimetabolites (USE)
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.
Term
Antimetabolites (toxicity)
Definition
Myelosuppression
gastrointestinal ulcerations
hair loss
nausea and vomiting
Term
Dose-limoting toxicity for antimetabolites for all classes
Definition
Myelosuppression
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
Folate
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
Term
Methotrexate (MOA)
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
Term
MTX use
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)
Term
MTX toxicity
Definition
Renal toxicity
Immunosuppression.
Hepatotoxicity.
Term
Leucovorin
Definition
(folic acid agonist) given with folic acid antagonists to protect healthy cells and reduce bone marrow suppression.
Treat MTX overdose
Term
Pemetrexed Brand name
Definition
Alimta
Term
Alimta MOA
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
pleural mesothelioma
Term
Pemetrexed mono therapy
Definition
non-small cell lung cancer.
Term
pemetrexed dose-limiting toxicity
Definition
low blood cell count
Term
Alimta SE
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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