drugs

PREVEX ® Felodipina

PREVEX ® is a drug based on felodipine.

THERAPEUTIC GROUP: Calcium antagonist with predominantly vascular effect.

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

Indications PREVEX ® Felodipina

PREVEX® ​​is indicated in the treatment of arterial hypertension, in monotherapy and combined therapy, and in angina pectoris.

Mechanism of action PREVEX ® Felodipine

The felodipine contained in PREVEX ® taken orally, is absorbed almost completely at the level of the gastro-enteric tract, making itself however bioavailable only for 15% of the dose taken. The tablets with gradual release, allow an improvement of the absorption kinetics, guaranteeing an extension of the therapeutic effect up to 24 hours.

Like the other calcium antagonists belonging to the dihydropyridine family, felodipine is able to selectively identify and bind L-type calcium channels expressed on the surface of vascular smooth muscle cells, preventing calcium entry and subsequent contraction. This effect, performed on peripheral arterioles, guarantees a significant reduction in vascular resistance, with a consequent drop in blood pressure; performed at the coronary level, it allows an improvement in cardiac vascular flow, with better oxygenation of the myocardial mass.

The aforementioned actions, also combined with a modest natriuretic and diuretic activity, justify the use of PREVEX ® in the treatment of hypertension and angina pectoris.

Felodipine, once its function is over, is metabolized in the liver into compounds lacking in antihypertensive efficacy, and subsequently eliminated above all through the urine.

Studies carried out and clinical efficacy

1. ANTIPERENSIVE EFFECTIVENESS OF THE FELODIPIN IN THE DIFFERENT BANDS OF AGE

This study evaluates the effectiveness of the treatment of high blood pressure with felodipine in patients of young age and elderly. Although the therapeutic effects seem to be common (ensuring a decrease in blood pressure of about 10 mmHg after a single dose, and of 20 mmHg following chronic intake), in elderly patients there is a reduction in the elimination of the drug, resulting in increase in half-life. In any case, these modest changes in the pharmacokinetic profile do not appear to alter the normal therapeutic properties of felodipine.

2. FELODIPINA WITH CONTROLLED RELEASE: what is the real duration?

Since the expiry of the patent for this active ingredient, the introduction of a large number of generic drugs with felodipine with gradual release has been observed. Although in most cases it refers to a prolonged therapeutic action for at least 24 hours, in reality its average duration seems to be around 18 hours. This characteristic should not be underestimated, since - taking the tablet once a day in the morning - a lack of blood pressure control in the early morning hours could compromise the patient's health and increase the incidence of vascular diseases.

3. FELODIPINA AND ANTI-INFLAMMATORY ACTIVITIES

Acta Pharmacol Sin. 2008 Sep; 29 (9): 1051-9.

In addition to the now characterized antihypertensive effect, felodipine appears to play a protective action against inflammatory diseases. This study, together with others in the literature, defines the baselines of this mechanism, probably characterized by a reduction in adhesion molecules and pro-inflammatory factors such as NF-kB.

Method of use and dosage

PREVEX ® Felodipine 5/10 mg tablets: 10 mg per day are generally used to treat high blood pressure and angina pectoris. This dosage can be halved in case of good pressure control.

In some cases, in order to reduce the transient increase in heart rate after taking PREVEX ®, the doctor may decide to resort to the concomitant administration of a beta blocker.

IN ANY CASE, BEFORE TAKING PREVEX ® Felodipina - THE PRESCRIPTION AND CONTROL OF ITS OWN DOCTOR IS NECESSARY.

Warnings PREVEX ® Felodipina

Given the hepatic involvement in the metabolism of felodipine, particular attention should be paid in case of therapy on patients suffering from liver disease of varying degrees. In fact, the reduction in the functionality of this organ could alter the normal pharmacokinetic properties of the active ingredient, resulting in an enhancement of the antihypertensive effect, with a possible increase in side effects.

Furthermore, some of the most common side effects associated with antihypertensive therapy - such as dizziness, headache and drowsiness - could cause a drop in the patient's perceptive and reactive capacities, making the driving of vehicles and the use of machinery dangerous.

PREGNANCY AND BREASTFEEDING

The various studies published in the literature - which show teratogenic and mutagenic effects of calcium antagonists on the fetus, when taken during pregnancy - suggest to absolutely avoid the use of these drugs, including PREVEX ® during the whole gestation period. Furthermore, the possibility that the active ingredient is partly secreted in breast milk exposes the baby to risks during the breastfeeding phase; therefore, it would be necessary to avoid taking it or suspend breastfeeding during the therapy period.

Interactions

PREVEX ® is contraindicated in case of hypersensitivity to one of its components or severe impairment of liver function.

PREVEX ® Felodipina Contraindications

Plasma levels of felodipine could go against significant variations in the case of concomitant administration of inducers or inhibitors of hepatic metabolism.

More precisely, the studies currently present in the literature show an increase in the plasma levels of felodipine following cimetidine administration, and a significant decrease in the case of concomitant intake of barbiturates, carbamezepine and other metabolic inducers. Inevitably, the variation in plasma concentrations of the active ingredient results in an unpredictability of the therapeutic effect and the related side effects.

Felodipine appears to alter the normal plasma digoxin concentration.

Undesirable effects - Side effects

The side effects associated with PREVEX ® therapy appear to be rare and in any case clinically irrelevant and transient. Among the most common, hot flushes, headaches, palpitations, dizziness, asthenia, rashes, increased diuresis and edema can be mentioned.

More serious reactions are decidedly more rare, and they mainly concern particular categories of patients at risk.

Note

PREVEX ® is salable only under medical prescription.