drugs

CARDIOVASC ® Lercanidipine hydrochloride

CARDIOVASC ® is a drug based on Lercanidipine hydrochloride.

THERAPEUTIC GROUP: Calcium antagonist with predominantly vascular effect.

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

Indications CARDIOVASC ® Lercanidipine hydrochloride

CARDIOVASC® is a drug indicated for the treatment of mild or moderate essential hypertension.

Mechanism of action CARDIOVASC ® Lercanidipine hydrochloride

CARDIOVASC ® presents as active principle lercanidipine, a molecule belonging to the dihydropyridine family. This substance is rapidly and totally absorbed in the intestine and transported in the blood, where it reaches a maximum peak between the second and third hours. The therapeutic action of lercanidipine is mainly due to the S enantiomer, capable of binding and blocking the a1 receptors of slow-type calcium channels, inhibiting the incoming flow of this element and thus preventing the contraction of smooth muscle fibrocells. The antihypertensive effect is therefore due to a precise action of the active principle on the arteriolar muscle cells, which allows a significant reduction of peripheral vascular resistance (vasodilatory effect).

Lercanidipine is characterized by a slow and prolonged action, guaranteed by the permanence at the level of the cellular membranes, at the end of which, after about 24 hours, it is metabolized by the hepatic cytochromes and eliminated in equal parts through feces and urine.

Studies carried out and clinical efficacy

1. THE POSSIBLE ROLE OF LERCANIDIPINE

Although still in the phase of in vitro experimentation, lercanidipine appears to be able to prevent the proliferation and differentiation of arteriolar smooth muscle cells. This particular ability could not only assist the antihypertensive effect exerted by the muscle relaxant action, but also reduce the vascular thickening, responsible for the worsening of the hemodynamic properties.

2. CALCIUM ANTAGONISTS AND PERIPHERAL EDEMA: the advantages of lercanidipine

Lercanidipine appears to be among the safest dihydropyridine-structure calcium antagonists currently used in clinical practice. An important study in meta-analysis shows that the incidence of peripheral edema and consequent suspension of drug therapy is decidedly reduced in patients treated with lercanidipine compared to other calcium antagonists.

3. THE EFFECTIVENESS OF COMBINED THERAPY IN THE TREATMENT OF HYPERTENSION

Administration of calcium antagonists and inhibitors of the renin-angiotensin system appears to be one of the most promising drug combinations in the treatment of hypertension. Several studies seem to agree on the greater efficacy and safety of the combined therapy compared to the monotherapy with one of the two drugs, even in hypertensive patients with metabolic and organic complications. However, the effectiveness of the synergy between lercanidipine and enalapril in the prevention of cardiovascular events remains to be clarified.

Method of use and dosage

CARDIOVASC ® 10 mg tablets of lercanidipine: for the treatment of mild to moderate essential hypertension, we recommend taking one tablet a day. Under strict medical supervision, the daily dose could be increased to 2 tablets, if satisfactory pressure drops were not reached after two weeks of therapy.

The intake should be carried out at the latest 15 minutes before a meal, as the size and type of nutrients ingested could alter the normal pharmacokinetic profile of CARDIOVASC ®

IN ANY CASE, BEFORE TAKING CARDIOVASC ® Lercanidipine hydrochloride - THE REQUIREMENT AND CHECK OF YOUR DOCTOR IS NECESSARY.

Warnings CARDIOVASC ® Lercanidipine hydrochloride

Before and during the administration of CARDIOVASC ® a careful monitoring of the arterial pressure should be performed in order to correctly set the treatment plan and the relative dosage.

A reduction in the therapeutic dose may be necessary in patients with liver disease, for whom the reduced functionality of cytochromial enzymes could cause a decrease in the inactivation of lercanidipine, with consequent strengthening of the therapeutic effects. The same argument is naturally replicable for the use of drugs and molecules capable of interfering with the activity of the cytochrome CYP 3A4.

Particular caution should be taken in the case of patients suffering from renal insufficiency, ventricular dysfunction, cardiac ischemia and dysfunction of the atrial sinus node.

CARDIOVASC ® presents lactose among the excipients, which could be dangerous in patients with lactase deficiency, galactosemia or glucose / galactose malabsorption syndrome.

Some symptoms related to CARDIOVASC ® therapy such as dizziness, headache, asthenia and somnolence, albeit rare, could reduce the patient's perceptive and reactive capacities, making the driving of vehicles and the use of machinery dangerous.

PREGNANCY AND BREASTFEEDING

Despite the presence of experimental studies conducted on animals, which show the absence of teratogenic and mutagenic effects of lercanidipine on the fetus, fetal malformations, growth retardation observed for other active ingredients of the same therapeutic category and of similar chemical structure, and l absence of human clinical trials, suggest avoiding the use of CARDIOVASC ® during the entire period of pregnancy.

The contraindications also extend to the period of breastfeeding, given the possible secretion of the drug in breast milk with effects not studied or foreseeable.

Interactions

As is known, the cytochrome hepatic enzymes responsible for the metabolism of lercanidipine are highly susceptible to the inhibiting and inducing action of various drugs and molecules, therefore CARDIOVASC ® could interact with:

  1. Beta blockers with hepatic metabolism (metopropole), phenytoin, astemizole, amiodarone and other CYP 3A4 inducers, resulting in increased activity of this enzyme and relative reduction in plasma levels and biological efficacy of lercanidipine;
  2. CYP3A4 inhibitors, such as grapefruit juice and cyclosporin, with increased bioavailability of lercanidipine, and potentiation of therapeutic effects.

In both cases an adjustment of the dosage may be necessary in order to reduce the potential side effects.

Furthermore, the antihypertensive effect of CARDIOVASC ® could be enhanced by the concomitant administration of antihypertensive drugs and alcohol.

Contraindications CARDIOVASC ® Lercanidipine hydrochloride

CARDIOVASC ® is contraindicated in case of hypersensitivity to one of its components, severe liver disease and nephropathy, congestive heart failure, angina pectoris and recent heart attack. Contraindications inevitably extend to women during the period of pregnancy and lactation, or during fertile age in the absence of protective contraceptive therapy.

Undesirable effects - Side effects

The administration of CARDIOVASC ® appears to be well tolerated, with an incidence of adverse reactions that does not exceed 2%. Among the most common effects are dizziness, peripheral edema, tachycardia, palpitations and headache. Rather, clinically relevant symptoms appear, such as vascular, nervous, cutaneous and gastro-intestinal symptoms.

The aforementioned effects may be more frequent - and also accompanied by serious complications, such as increased angina episodes and myocardial infarction - in particular groups of patients at risk.

Note

CARDIOVASC ® can be sold only under medical prescription.