About
Leucovorin, also known as folinic acid, is a formyl derivative of tetrahydrofolic acid. It is metabolically active and does not require reduction by dihydrofolate reductase, unlike folic acid. This property makes it effective in rescuing normal cells from the toxic effects of folic acid antagonists like methotrexate, by providing a source of reduced folates necessary for DNA and RNA synthesis.
Beyond its role as a rescue agent, leucovorin can also enhance the cytotoxic effects of fluorouracil in certain colorectal cancers, improving treatment outcomes. Its ability to bypass the dihydrofolate reductase enzyme makes it a crucial therapeutic agent in specific oncological and hematological settings.
Uses
- Rescue therapy after high-dose methotrexate administration.
- Counteracting the effects of other folic acid antagonists (e.g., pyrimethamine, trimethoprim).
- Palliative treatment of advanced colorectal cancer in combination with fluorouracil.
- Treatment of megaloblastic anemia due to folate deficiency when oral therapy is not feasible.
Directions For Use
Administered orally or intravenously. Dosage and schedule depend on the specific indication and concurrent chemotherapy regimen.
Benefits
- Reduces severe toxicity of methotrexate to normal cells.
- Enhances the efficacy of fluorouracil in colorectal cancer.
- Provides essential folates for cellular processes.
- Can reverse adverse effects of certain antifolate drugs.
- Available in both oral and injectable forms.
- Crucial component in specific chemotherapy protocols.
Side Effects
- Allergic reactions (rare)
- Fever
- Nausea
- Vomiting
- Diarrhea
- Stomatitis (when used with fluorouracil)
- Increased seizure frequency in epileptic patients
- Insomnia
- Agitation
- Depression
- Thrombocytopenia (rare)
- Leukopenia (rare)
Safety Measures
- Alcohol - No specific contraindication, but excessive alcohol consumption can interfere with folate metabolism.
- Pregnancy - Generally considered safe for use in pregnancy when indicated, especially for folate deficiency or as rescue therapy. Consult a physician.
- Breastfeeding - Considered compatible with breastfeeding, as it is a natural folate derivative. Consult a physician.
- Liver - No specific dosage adjustment required for liver impairment. Use with caution and monitor if severe hepatic dysfunction is present.
- Kidney - No specific dosage adjustment required for renal impairment. Monitor patients with severe renal dysfunction, especially during high-dose methotrexate rescue.
- Lung - No specific safety concerns related to lung conditions.
Disclaimer
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