Folinic
Generic Name
Folinic acid (Leucovorin calcium)
Manufacturer
Various generic manufacturers (e.g., Pfizer, Sandoz, Mylan)
Country
Globally manufactured (e.g., USA, India, European countries)
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Price Details
Current market pricing information
| Variant | Unit Price | Strip Price |
|---|---|---|
| folinic 10 mg injection | ৳ 625.00 | N/A |
Description
Overview of the medicine
Folinic acid (leucovorin calcium) is a reduced form of folic acid that is metabolically active. It is used as a "rescue" agent to protect healthy cells from the toxic effects of high-dose methotrexate and as an adjunct in cancer chemotherapy with fluorouracil to enhance its cytotoxic effects. It is also used to treat megaloblastic anemia due to folate deficiency where oral therapy is not feasible.
Uses & Indications
Dosage
Adults
Highly variable. For methotrexate rescue, usually 10-15 mg/m² IV/IM/oral every 6 hours for 10 doses, starting 24 hours after methotrexate. For colorectal cancer with fluorouracil, typically 200 mg/m² IV over 2 minutes, followed by fluorouracil. For megaloblastic anemia, 1 mg daily.
Elderly
No specific dosage adjustment, but careful monitoring of renal function and general health status is recommended due to potential age-related decline in organ function.
Renal_impairment
Use with caution. Patients with severe renal impairment may require dosage adjustment and extended duration of leucovorin rescue due to delayed methotrexate excretion.
How to Take
Folinic acid injection is administered intravenously (IV) or intramuscularly (IM). For IV administration, it can be given as a slow IV injection or infusion. Ensure proper dilution if required and follow specific protocol for methotrexate rescue.
Mechanism of Action
Folinic acid does not require reduction by dihydrofolate reductase (DHFR) and is therefore unaffected by DHFR inhibitors like methotrexate. It acts as a bypass, providing the necessary reduced folate cofactors required for DNA synthesis and repair, thus rescuing healthy cells from methotrexate toxicity. When used with fluorouracil, it stabilizes the binding of fluorodeoxyuridine monophosphate to thymidylate synthase, thereby enhancing the cytotoxic effect of fluorouracil.
Pharmacokinetics
Onset
Rapid, typically within minutes for IV administration.
Excretion
Excreted primarily via the kidneys (80-90% in urine) and some via feces.
Half life
The parent drug (Leucovorin) has a half-life of about 0.7 hours; the active metabolite (5-methyltetrahydrofolate) has a terminal half-life of about 6 hours.
Absorption
Rapidly absorbed after intramuscular (IM) or intravenous (IV) administration. Peak plasma concentrations are reached within 10 minutes (IV) to 40 minutes (IM).
Metabolism
Rapidly converted to 5-methyltetrahydrofolate and other active reduced folates, primarily in the liver and intestinal mucosa.
Side Effects
Contraindications
- Pernicious anemia or other megaloblastic anemias due to vitamin B12 deficiency (as it may mask the neurological symptoms while improving hematological parameters)
- Known hypersensitivity to folinic acid or any component of the formulation
Drug Interactions
Methotrexate
Used as a rescue agent to reduce methotrexate toxicity, but timing is critical. Improper timing can reduce methotrexate's efficacy.
Fluorouracil (5-FU)
Enhances the cytotoxic and therapeutic effects of fluorouracil, potentially leading to increased toxicity (e.g., severe diarrhea, stomatitis). Dosage adjustment of fluorouracil may be necessary.
Trimethoprim/Pyrimethamine
Counteracts the antimicrobial effects of these antifolate drugs by providing exogenous folates.
Antiepileptics (e.g., Phenobarbital, Phenytoin, Primidone)
May reduce the plasma concentrations of certain antiepileptic drugs, potentially leading to increased seizure frequency. Monitoring of antiepileptic drug levels is recommended.
Storage
Store unopened vials at controlled room temperature (20-25°C), protected from light. Reconstituted solutions should be used immediately or stored under refrigeration (2-8°C) for a specified period (e.g., 24 hours).
Overdose
Folinic acid is generally well-tolerated. High doses may lead to gastrointestinal disturbances (e.g., nausea, vomiting) or allergic reactions. Management is supportive and symptomatic; there is no specific antidote for folinic acid overdose.
Pregnancy & Lactation
Pregnancy Category C. Should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is unknown if folinic acid is excreted in human milk; use with caution in nursing mothers.
Frequently Asked Questions
Common questions about this medicine
Pack Sizes
Shelf Life
Typically 2-3 years for unopened vials, stored according to manufacturer's instructions. Reconstituted solutions have a shorter shelf life (e.g., 24 hours at room temperature).
Availability
Hospitals, clinics, retail pharmacies
Approval Status
Approved by major regulatory bodies (e.g., FDA, EMA, DGDA)
Patent Status
Off-patent, available generically
WHO Essential Medicine
YesClinical Trials
Folinic acid (leucovorin) has been extensively studied in numerous clinical trials, particularly in oncology, for its role in methotrexate rescue and as a modulator of fluorouracil activity. Its efficacy and safety are well-established through decades of clinical use.
Lab Monitoring
- Serum methotrexate levels (essential for rescue therapy)
- Complete Blood Count (CBC) with differential
- Renal function tests (serum creatinine, BUN)
- Liver function tests (ALT, AST, bilirubin)
Doctor Notes
- Essential for methotrexate high-dose therapy rescue; timing and dosing are critical.
- Enhances fluorouracil efficacy but also its toxicity, requiring careful monitoring.
- Not suitable for pernicious anemia without concurrent Vitamin B12 therapy.
Patient Guidelines
- Inform your doctor about all medications you are taking, including over-the-counter drugs and herbal supplements.
- Report any unusual or severe side effects immediately.
- Strictly adhere to the prescribed dosage and schedule, especially during cancer therapy.
- Do not stop the medication without consulting your doctor.
Missed Dose Advice
If a dose is missed, especially during methotrexate rescue therapy, contact your doctor immediately. Missing a dose could have serious consequences. Do not double the next dose.
Driving Precautions
Folinic acid is generally not expected to impair the ability to drive or operate machinery. However, if you experience dizziness, fatigue, or other adverse effects, avoid such activities until you feel well.
Lifestyle Advice
- Maintain adequate hydration as advised by your healthcare provider, especially during methotrexate therapy.
- Follow a balanced diet to support overall health during cancer treatment.
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