Product image of Leucovorin (Calcium Folinate Pentahydrate) supplied by GNH India

Leucovorin

Active Ingredient:
Calcium Folinate Pentahydrate
Origin:
EU

Leucovorin (Calcium Folinate Pentahydrate)

Calcium Folinate Pentahydrate, the active ingredient in Leucovorin, is a folate analog presented as an oral formulation for systemic use. It is employed to correct folate deficiency and to mitigate toxicity from high‑dose methotrexate or certain fluoropyrimidine regimens in oncology and hematology patients.

GNH India supplies Leucovorin as a licensed, GDP‑compliant international pharmaceutical supplier serving hospitals, oncology centres, transplant centres and pharmacies worldwide. The company adheres to stringent quality standards and provides regulatory documentation for global distribution, ensuring reliable supply chains and timely delivery.

Manufacturer / TM Owner

Pfizer Pharma Gmbh

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Indications & Clinical Uses

Leucovorin is used to address folate‑related pathways and mitigate chemotherapy‑induced toxicity.

  • Methotrexate toxicity rescue: restores folate pools to reduce hematologic and mucosal toxicity.
  • Adjunctive therapy after high‑dose methotrexate: supports normal cell recovery during cancer treatment.
  • Enhancement of 5‑fluorouracil efficacy: stabilizes intracellular folate to improve drug activity.
  • Folate deficiency: supplies reduced folate to patients with inadequate dietary or metabolic folate levels.

How It Works

  • Leucovorin provides folinic acid, a reduced form of folic acid that bypasses the dihydrofolate reductase step. By directly entering the folate cycle, it replenishes tetrahydrofolate cofactors required for nucleotide synthesis, thereby supporting DNA replication and repair in normal cells and counteracting the effects of antifolate chemotherapy agents.

Side Effects

Leucovorin is generally well tolerated, but adverse reactions can occur.

Common Side Effects

  • Nausea: mild to moderate upset stomach.
  • Diarrhea: loose stools that may be transient.
  • Rash: skin redness or mild itching.
  • Headache: occasional dull or throbbing pain.

Serious or Rare Side Effects

  • Anaphylactic reaction: severe allergic response requiring immediate medical attention.
  • Stevens‑Johnson syndrome: rare skin and mucous membrane disorder.
  • Pancytopenia: marked reduction in blood cell counts.
  • Hepatic dysfunction: abnormal liver enzyme elevations.
  • Renal failure: impaired kidney function in susceptible individuals.

Precautions & Warnings

Leucovorin should be used with appropriate clinical monitoring.

  • Renal impairment: adjust use if kidney function is reduced.
  • Hepatic disease: monitor liver enzymes during therapy.
  • Concomitant antifolates: assess timing to avoid antagonism.
  • Pregnancy and lactation: safety not established; consult a physician.
  • Pediatric use: dose and safety require specialist oversight.
  • Store at ambient temperature: keep below 25 °C, in the original container, protected from moisture and direct sunlight.

Avoid Interactions

Leucovorin may interact with several drug classes.

Major Interactions (Avoid)

  • High‑dose methotrexate: inappropriate timing can diminish rescue effect.
  • Other antifolates (e.g., pemetrexed): may counteract therapeutic action.
  • Oral contraceptives: folate supplementation can reduce contraceptive efficacy.

Moderate Interactions (Monitor Closely)

  • Antiepileptic drugs (phenytoin, carbamazepine): may increase folate metabolism, requiring dose review.
  • High‑dose vitamin C: can affect folate stability and absorption.

Frequently Asked Questions

Leucovorin is employed as an antidote to reverse the toxic effects of high‑dose methotrexate, as an adjunct after such chemotherapy, to enhance the activity of 5‑fluorouracil, and to treat patients with folate deficiency. It supplies a reduced form of folate that supports normal cellular function during and after chemotherapy.

Calcium Folinate, the active form of folinic acid, bypasses the dihydrofolate reductase step and directly enters the folate cycle. This restores tetrahydrofolate pools, enabling DNA synthesis and repair in healthy cells, thereby counteracting the inhibition caused by antifolate drugs such as methotrexate.

The dose of Leucovorin is individualized and must be prescribed by a qualified healthcare professional. The prescriber determines the amount, frequency, and duration based on the specific indication, patient characteristics, and concurrent therapies.

Safety data for Leucovorin during pregnancy and lactation are limited, and the product is classified as having an unknown pregnancy category. Women who are pregnant, planning to become pregnant, or breastfeeding should discuss potential risks and benefits with their physician before using this medication.

To order Leucovorin, submit an enquiry on the product page at gnhindia.com, specifying the required quantity. GNH India works with hospitals, pharmacies, and procurement teams worldwide, verifies trade or institutional credentials, and then provides pricing, availability, shipping details (including any cold‑chain requirements), and necessary import documentation.

Leucovorin (folinic acid) is a reduced folate that bypasses the enzymatic step blocked by antifolate drugs, whereas folic acid requires conversion by dihydrofolate reductase. This makes Leucovorin more effective for rescuing cells from methotrexate toxicity and for enhancing fluoropyrimidine activity, while standard folic acid is primarily used for general dietary supplementation.

Leucovorin should be stored at ambient temperature, preferably below 25 °C, in its original packaging to protect it from moisture and direct sunlight. Keep the container tightly closed and out of reach of children. No refrigeration is required for the oral formulation.

Leucovorin is administered orally in tablet or liquid form, as directed by the prescribing clinician. The medication is taken with or without food, according to the specific dosing schedule provided, and should be swallowed whole unless a liquid formulation is prescribed.

Serious adverse reactions, although rare, include anaphylaxis, Stevens‑Johnson syndrome, severe hepatic or renal dysfunction, and pancytopenia. Patients should seek immediate medical attention if they experience symptoms such as difficulty breathing, widespread rash, jaundice, dark urine, or unexplained bruising or bleeding.

Leucovorin is contraindicated in individuals with known hypersensitivity to folinic acid or any of its excipients. Caution is also advised for patients with severe renal or hepatic impairment, and it should be avoided in combination with certain antifolate agents when rescue timing cannot be ensured.

Published by

GNH India Pharmaceuticals Limited

Licensed pharmaceutical supplier

Last updated:

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