What is Leucovorin?

Folic acid (vitamin B9) is turned into leucovorin, which is also called folinic acid.

Leucovorin does not require to be activated by dihydrofolate reductase.

This means it can get around some barriers in the folate metabolic route.

It’s mostly used as a rescue agent that can help mitigate the adverse effects of high-dose methotrexate.

Fluorouracil (5-FU) can be used more effectively to treat cancer with this chemosensitizer.

A supplement that adds folate to the body when it is lacking or too much antifolate is being used.

Overview

Description

Leucovorin is an important supporting drug in chemotherapy treatments.

By adding folate to cells that have lost it, it protects them from the harmful effects of folate antagonists, such as methotrexate.

It is also used to enhance the cancer-fighting effects of drugs like 5-FU, which prevent cancer cells from replicating their DNA when they divide rapidly.

Uses / Indications

Rescue therapy following high-dose methotrexate to mitigate damage in healthy cells.

Adjuvant therapy in colorectal cancer with 5-fluorouracil (5-FU) to augment anticancer effectiveness.

Managing toxicity from folate antagonists includes handling overdoses of methotrexate, Trimethoprim, or pyrimethamine.

Management of megaloblastic anaemia resulting from folate insufficiency in particular clinical contexts.

Benefits

During the chemotherapeutic treatment with methotrexate, it safeguards healthy cells.

Used in conjunction with 5-FU, it improves the response to chemotherapy.

Reverses the harmful effects of antifolate promptly and efficiently.

The medication is well-tolerable and poses a lower chance of serious adverse reactions.

Crucial in the field of pediatric oncology, particularly for patients suffering from leukemia.

Side Effects

How Does It Work?

Leucovorin is the usual folate rescue agent that is often used with methotrexate and 5-fluorouracil (5-FU).

It can get around dihydrofolate reductase (DHFR) and restore folate stores that have been lost.

Levoleucovorin is the active L-isomer of leucovorin. It is more bioavailable and potent.

This means it can be used in smaller doses but still offers the same therapeutic benefits.

Folic acid looks a lot like methotrexate. However, it can’t help methotrexate because it relies on DHFR activity.

Methotrexate blocks this activity. Calcium folinate is just another name for leucovorin, and it works the same way.

If leucovorin rescue isn’t enough for severe methotrexate toxicity, glucarpidase can help.

It quickly breaks down methotrexate, offering another way to detoxify.

How to Use / Dosage Guidelines

Give leucovorin 24 hours following high-dose methotrexate, usually 10-15 mg/m² every 6 hours.

For colorectal cancer, administer 20-500 mg/m² IV before or with 5-FU.

To treat antifolate toxicity, provide 3-15 mg/day IV/IM until hematologic recovery.

Under medical supervision, the medication is administered either intravenous (IV) or intramuscular (IM).

The dose and length of treatment are determined by methotrexate levels, renal function, and patient response.

When Not to Use

A hypersensitivity that is known to exist to leucovorin or calcium folinate

Both pernicious anaemia and B12-deficiency anaemia have the potential to conceal symptoms.

Methotrexate administered intravenously at the same time poses a risk of lethal neurotoxicity.

Drug Interactions

Safety Advice

General Instructions

A medical professional always carries out administration.

Look out for any adverse responses, such as a rash, convulsions, or difficulty breathing.

Ensure that you consume a sufficient amount of water throughout your methotrexate cycles.

Make sure to report any unusual signs of infection, such as exhaustion or bruises.

Special Dietary & Lifestyle Tips

Maintaining proper hydration is especially important during methotrexate treatment.

Consume no alcohol because it may affect liver function.

Dietary folate-rich foods include citrus fruits, lentils, and leafy greens.

Folic acid should not be used for self-injecting without an expert lookout.

During chemotherapy, remain consistent with your schedule.

Comparison with Similar Agents

Precautions & Warnings

In methotrexate rescue treatments, it should not be confused with folic acid.

Reversing methotrexate-induced nephrotoxicity is not possible with leucovorin.

People who are prone to seizures should be cautious when taking anti-epileptic medications.

Avoid intrathecal administration if possible.

Patients with folate analogue allergies may experience cross-reactivity.

Compatibility with Other Medicines

Storage

Keep in the fridge at 2°C to 8°C (36°F to 46°F).

Keep out of the light.

Don’t freeze

Use reconstituted solutions within the time limit that is indicated (usually 12 to 24 hours, depending on how stable they are).

Safely throw away solutions that you don’t need.