PREFOLIC ® is a calcium mefolinate based drug
THERAPEUTIC GROUP: All other therapeutic products - Detoxifying substances for cytostatic treatments
Indications PREFOLIC ® Calcium mefolinate
PREFOLIC ® is indicated in the prophylaxis and treatment of folate deficiencies, due to increased need or reduced absorption.
The same drug can be used in the treatment of aminopterin and methotrexate side effects.
Mechanism of action PREFOLIC ® Calcium mefolinate
Calcium mefolinate, 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 anemia, neurological disorders, cardiovascular diseases and malformations in the unborn.
The aforesaid active principle, taken orally, 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 single carbon units, also justifies the enormous biological importance of this molecule, involved together with vitamin B12 in:
- Detoxification from homocysteine, a molecule with a strong toxic potential and 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 for all cells in active replication such as those of the immune and hematopoietic systems.
Studies carried out and clinical efficacy
1. ANTICOAGULANT THERAPY AND METHYL TETRAHYDROFOLATE
Blood Coagul Fibrinolysis. 2009 Jun; 20: 297-302.
Erythrocyte folate and 5-methyltetrahydrofolate levels decline during 6 months of oral anticoagulation with warfarin.
Sobczya „ska-Malefora A, Harrington DJ, Lomer MC, Pettitt C, Hamilton S, Rangarajan S, Shearer MJ.
Study that demonstrates how treatment with oral anticoagulants can, after about 6 months of therapy, reduce the concentrations of 5 methyltetrahydrofolate, thus compromising numerous biological functions including erythropoiesis. In these patients, a supplementation is therefore recommended to avoid pathological deficiencies. .
2. FOLATE METABOLISM AND AUTISM
Mol Psychiatry. 2012 Jan 10.
Cerebral folate receptor autoantibodies in autism spectrum disorder.
Frye RE, Sequeira JM, Quadros EV, James SJ, Rossignol DA.
Very interesting experimental evidence that demonstrates the presence of antibodies to the brain receptor for folate in patients with autism. This result could have very important repercussions from a clinical point of view, in the management of the therapy of the autistic patient.
3.FOLIC ACID OR 5 METHYL TETRAHYDROFOLATE
Clin Pharmacokinet. 2010 Aug 1; 49: 535-48.
Folic acid and L-5-methyltetrahydrofolate: comparison of clinical pharmacokinetics and pharmacodynamics.
Pietrzik K, Bailey L, Shane B.
Important pharmacokinetic work that demonstrates the advantages derived from the assumption 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 ®
Gastro-resistant tablets of 19.18 mg of 5 methyltetrahydrofolate of calcium, equal to 15 mg of acid;
Solution for injection 19.18 mg of 5 calcium methyltetrahydrofolate, equal to 15 mg of acid or 63.93 mg of 5 calcium methyltetrahydrofolate, equal to 50 mg of acid.
The dosage schedule must be defined by the specialist doctor based on the characteristics of the patient, the clinical picture and the therapeutic indication for which it is intended to be used.
Warnings PREFOLIC ® Calcium mefolinate
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 any intravenous administration.
PREFOLIC ® contains lactose therefore its intake 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 deficiencies, provided that such intake is done under strict medical supervision.
Interactions
No clinically relevant drug interactions are currently known, although some active ingredients such as anticonvulsants and antiepileptics could limit intestinal absorption of tetrahydrofolate.
On the other hand, the possible antagonizing effects associated with the use of dihydrofolate reductase inhibitor drugs are reduced.
Contraindications PREFOLIC ® Calcium mefolinate
The use of PREFOLIC ® is contraindicated in patients hypersensitive to the active substance or to one of its excipients.
Undesirable Effects - Side Effects
Although therapy with PREFOLIC ® is free of particular side effects, it is possible to observe, especially in atopic patients and treated with PREFOLIC ® injectable, the appearance of allergic reactions such as fever, arterial hypotension, dermatological manifestations, tachycardia, bronchospasm and in the most severe cases anaphylactic shock.
Note
PREFOLIC ® can only be sold with a medical prescription.
The information on PREFOLIC ® Calcium mepholinate published on this page may be out of date or incomplete. For a correct use of this information, see the Disclaimer and useful information page.
