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Leucovorin (leucovorin calcium) 

Indications 

• Methotrexate Overdose: Leucovorin is used to diminish the toxic effects of methotrexate and other folic acid antagonists by rescuing normal cells. 
• Megaloblastic Anemia: Treatment of megaloblastic anemia due to folic acid deficiency when oral therapy is not feasible. 
• Colorectal Cancer: Used in combination with 5-fluorouracil (5-FU) to enhance the effectiveness in treating colorectal cancer. 
• Folic Acid Deficiency: Helps in conditions requiring folic acid supplementation when the deficiency is due to dihydrofolate reductase inhibitors. 

Dosage and Administration 

• Take Leucovorin exactly as prescribed by your doctor. 
• Swallow the tablet whole with a full glass of water. If prescribed for use with methotrexate, follow the specific timing and dosage instructions provided by your healthcare provider. 
• Maintain regular appointments with your doctor for monitoring and adjustments. 
• Do not skip doses or alter the dosage without consulting your doctor. 
• Avoid taking Leucovorin simultaneously with oral folic acid supplements without medical advice, as this can affect its efficacy. 
• Do not crush or chew the tablets, as this can alter their effectiveness. 
• Avoid using Leucovorin if you are allergic to any of its ingredients. 

Mechanism of Action 

Leucovorin is a form of folic acid that helps in the synthesis of nucleic acids and proteins. It works by providing a source of tetrahydrofolate, bypassing the block caused by dihydrofolate reductase inhibitors like methotrexate. This allows for the rescue of normal cells from the toxic effects of methotrexate and enhances the effects of fluoropyrimidines like 5-FU in cancer treatment. 

Contraindications 

• Allergy to Leucovorin: Do not use it if you have had an allergic reaction to leucovorin or any other ingredients in the tablet. 
• Pernicious Anemia or Other Megaloblastic Anemias: Avoid use in megaloblastic anemias due to vitamin B12 deficiency, as it can mask the symptoms and potentially worsen the condition. 
• Severe Gastrointestinal Toxicity: Not recommended for patients experiencing severe gastrointestinal toxicity. 

Side Effects 

Common Side Effects 

• Nausea 
• Vomiting 
• Diarrhea 
• Stomatitis (inflammation of the mouth and lips) 
• Fatigue 

Serious Side Effects 

• Severe allergic reactions (e.g., rash, itching, swelling, difficulty breathing) 
• Seizures 
• Syncope (fainting) 
• Severe diarrhea (indicative of possible gastrointestinal toxicity) 

Precautions 

• Regular Monitoring: Frequent blood tests may be required to monitor blood counts and folate levels. 
• Use with Chemotherapy: Carefully follow the timing and dosing schedule when used in combination with chemotherapy drugs like methotrexate and 5-FU. 
• Allergic Reactions: Be aware of any signs of allergic reactions and seek immediate medical attention if they occur. 
• Hydration: Ensure adequate fluid intake to prevent dehydration, especially if experiencing gastrointestinal side effects. 
• Pregnancy and Breastfeeding: Discuss with your doctor if you are pregnant, planning to become pregnant, or breastfeeding. 

Storage Instructions 

• Store Leucovorin tablets at room temperature between 20°C to 25°C (68°F to 77°F). 
• Keep the tablets in the original container to protect from light and moisture. 
• Keep out of reach of children. 
• Do not use the tablets after the expiration date on the label. 

References 

https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/040347s010lbl.pdf