PREFOLIC ® Calcium Mepholinate

PREFOLIC ® is a calcium mefolinate based drug

THERAPEUTIC GROUP: All other therapeutic products - Detoxifying substances for cytostatic treatments

IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects

Indications PREFOLIC ® Calcium mefolinato

PREFOLIC ® is indicated in the prophylaxis and treatment of folate deficiencies, due to increased need or reduced absorption.

The same medicine can be used in the treatment of side effects from aminopterin and methotrexate.

Mechanism of action PREFOLIC ® Calcium mefolinato

Calcium Mepholinate, active ingredient of PREFOLIC ®, is a salt of N5-methyl tetrahydrofolate, a particularly valuable active ingredient in the treatment of folate deficiency states, often responsible for megaloblastic anemias, neurological disorders, cardiovascular diseases and birth defects.

The aforementioned active ingredient, taken by mouth, reaches the intestinal environment unaltered, where thanks to the presence of specific transporters it is absorbed in the form of mono and diglutamates to be immediately reconverted into 5-methyltetrahydrofolate, a biologically active form.

Its chemical activity, important in the transfer of monocarbonous units, also justifies the enormous biological relevance of this molecule, involved together with vitamin B12 in:

Homocysteine detoxification, a molecule with a strong toxic potential and an independent risk factor for cardiovascular diseases;
Synthesis of methyl groups, necessary for the correct functioning of numerous enzymes and biological molecules;
Synthesis of purines and in particular of thymine, necessary for the biosynthesis of nucleic acids, therefore to all the cells in active replication such as those of the immune and hematopoietic system.

Studies carried out and clinical efficacy

1. ANTICOAGULANT THERAPY AND METHYLTETRAIDROFOLATE

Blood Coagul Fibrinolysis. 2009 Jun; 20 (4): 297-302.

Study demonstrating that treatment with oral anticoagulants may, after about 6 months of therapy, reduce concentrations of 5-methyltetrahydrofolate, thus compromising numerous biological functions including erythropoiesis. In these patients, therefore, supplementation useful to avoid pathological deficiencies is recommended.

2. METABOLISM OF FOLATE AND AUTISM

Mol Psychiatry. 2012 Jan 10.

Very interesting experimental evidence showing the presence of anti-brain receptor antibodies to folate in patients with autism. This result could have very important clinical repercussions in the management of autistic patient therapy.

3. FOLIC ACID OR 5 METHYLTHRAIDROPHOLATE

Clin Pharmacokinet. 2010 Aug 1; 49 (8): 535-48.

Important pharmacokinetic work demonstrating the advantages derived from the intake of methyltetrahydrofolate compared to that of folic acid, concretized with the reduction of interactions with drugs that inhibit the activity of dihydrofolate reductase.

Method of use and dosage

PREFOLIC ®

19.18 mg gastro-resistant tablets of calcium methyltetrahydrofolate, equivalent to 15 mg of acid;

Solution for injection 19.18 mg of calcium methyltetrahydrofolate, equivalent to 15 mg of acid or 63.93 mg of calcium methyltetrahydrofolate, equal to 50 mg of acid.

The dosing schedule must be defined by the specialist doctor based on the characteristics of the patient, the clinical picture and the therapeutic indication for which its use is foreseen.

Warnings PREFOLIC ® Calcium mefolinato

The different pharmaceutical forms envisaged for PREFOLIC ® require important precautions such as: avoid chewing gastro-resistant tablets, given the sensitivity of the active ingredient to the gastric environment, request the intervention of health personnel for the possible intravenous administration.

PREFOLIC ® contains lactose therefore its use is not recommended in patients with lactose intolerance, lactase enzyme deficiency or glucose / galactose malabsorption syndrome.

PREFOLIC ® injectable instead contains parahydroxybenzoates, excipients characterized by a strong allergenic power.

PREGNANCY AND BREASTFEEDING

PREFOLIC ® could be used during pregnancy and in the subsequent period of breastfeeding, also to compensate for any deficiency, provided this is done under strict medical supervision.

Interactions

No clinically relevant drug interactions are currently known, although some active ingredients such as anticonvulsants and antiepileptics may limit the intestinal absorption of tetrahydrofolate.

The possible antagonizing effects associated with the use of dihydrofolate reductase inhibitor drugs are reduced.

Contraindications PREFOLIC ® Calcium mefolinato

The use of PREFOLIC ® is contraindicated in patients who are hypersensitive to the active ingredient or to one of its excipients.

Undesirable effects - Side effects

Despite the fact that PREFOLIC ® therapy has no particular side effects, it is possible to observe, especially in atopic patients treated with injectable PREFOLIC ®, the appearance of allergic reactions such as fever, arterial hypotension, dermatological manifestations, tachycardia, bronchospasm and in more severe cases anaphylactic shock.