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Actifol 5, a derivative of tetrahydrofolic acid, bypasses dihydrofolate reductase for its conversion, allowing it to remain active even when this enzyme is inhibited by drugs such as methotrexate. This mechanism supports purine and pyrimidine synthesis in normal cells, enabling DNA replication despite the presence of folic acid antagonists.
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✅ Description:
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✔️ Folinic acid (Calcium Folinate) is prescribed for:
- Mitigating toxicity and addressing the effects of impaired Methotrexate elimination.
- Treating megaloblastic anemia caused by folate deficiency, such as in conditions like sprue or nutritional deficiencies.
- Managing megaloblastic anemia associated with pregnancy and infancy.
✔️ Pharmacology
Folinic acid, a 5-formyl derivative of tetrahydrofolic acid, is easily converted into other reduced folic acid derivatives like tetrahydrofolate, allowing it to exhibit equivalent vitamin activity to folic acid. Unlike folic acid, folinic acid does not require dihydrofolate reductase for activation, making it functional even in the presence of enzyme inhibitors like methotrexate.
While initially understood as merely aiding rescue therapy during methotrexate treatment, it was later discovered that folinic acid could reactivate dihydrofolate reductase directly, even in the presence of methotrexate. This effect, believed to involve polyglutamylation of methotrexate and dihydrofolate in malignant cells, selectively reactivates normal cells’ DNA synthesis. By facilitating some purine and pyrimidine synthesis, folinic acid helps maintain normal DNA replication processes.
✔️ Dosage:
- Reduction of adverse effects from folic acid antagonists (e.g., methotrexate, trimethoprim):
- 5–15 mg tablet every 6 hours for 2–3 days.
- Megaloblastic anemia:
- One 5–15 mg tablet daily, as directed by a physician.
✔️ Common side effects may include:
- Allergic reactions, such as sudden itchy rashes (hives), and swelling of the face, hands, or throat, could impair swallowing or breathing.
- Rare occurrences of seizures or fainting.
✔️ Actifol 5 is contraindicated in:
- Patients with hypersensitivity to Calcium Folinate or other components of the formulation.
- Pernicious anemia or other megaloblastic anemia caused by Vitamin B12 deficiency.
✔️ Overdose Effects
- No adverse effects have been reported in cases of excessive folinic acid administration. However, excessive doses may negate the therapeutic effects of folic acid antagonists.
- Supportive care is recommended in cases of overdose.
✔️ Pregnancy and Lactation
- No adequate clinical studies exist regarding the use of Actifol 5 in pregnant or breastfeeding women.
- Since many medications are excreted in human milk, caution is advised when administering Calcium Folinate to nursing mothers
✔️ Precautions and Warnings
- Calcium Folinate may mask pernicious anemia or megaloblastic anemia due to Vitamin B12 deficiency.
- Use with methotrexate or 5-fluorouracil must be under the supervision of an experienced clinician.
- Macrocytosis caused by certain cytotoxic agents (e.g., hydroxycarbamide, cytarabine) should not be treated with Actifol 5
- In epileptic patients on phenobarbital, phenytoin, primidone, or succinimides, Actifol 5 may reduce plasma levels of these medications, increasing seizure risk.
✔️ Storage
- Store below 30°C.
- Protect from light and keep out of reach of children.
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