ELITEN ® Fosinopril

ELITEN ® is a drug based on fosinopril sodium salt

THERAPEUTIC GROUP: Antihypertensives - ACE inhibitors not associated

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

Indications ELITEN ® Fosinopril

ELITEN ® is indicated for the treatment of high blood pressure and heart failure. In both cases it is also possible to opt for a combined therapeutic treatment.

Mechanism of action ELITEN ® Fosinopril

Fosinopril in sodium salt, the active ingredient of ELITEN ® is absorbed in the first part of the small intestine for about 36% of the total dose taken per os. The active ingredient present in the drug is rapidly metabolized both at the level of the gastro-intestinal mucosa and at the liver level, where it is transformed into the biologically active form, known as fosinoprilat. This molecule reaches its maximum blood concentrations 3 hours after the oral administration of the prodrug.

The antihypertensive action exerted by the fosinoprilat materializes in the inhibition of the angiotensin I conversion enzyme, responsible for the degradation of the aforementioned decapeptide in angiotensin II, biologically active because it is responsible for the vasoconstrictor action at the arteriolar level and for stimulating the secretion of aldosterone, both important factors in the genesis of hypertension. In addition to the aforementioned action, fosinoprilat appears to be involved in the inhibition of a second enzyme, known as kininase II, necessary to degrade a molecule (bradykinin) with marked vasodilatory qualities.

Furthermore, several studies have demonstrated the cardioprotective effect of the active ingredient of ELITEN in terms of prevention and therapy of cardiac hypertrophy.

Fosinoprilat is distinguished from other ACE inhibitors - in addition to a prolonged half-life - by being a phosphinic derivative that can be effectively eliminated both by renal and hepatic pathways. This double route of excretion of the drug allows, in case of reduced functionality of one of the two organs, to be able to take advantage of the vicarious function of the other, ensuring the maintenance of a good elimination kinetic.

Studies carried out and clinical efficacy

1 FOSINOPRIL AND OSTEPOPOROSIS

According to this study, conducted on about 50 menopausal women, not all suffering from high blood pressure, the administration of fosinopril could reduce the normal bone demineralization that is observed in menopause, responsible for the increased incidence of osteoporotic events. If the results were confirmed by other studies, the hypothesis of the involvement of the renin-angiotensin system in bone metabolism could become increasingly accredited.

2. FOSINOPRIL AND INFLAMMATORY MARKERS

Recent studies have associated an anti-inflammatory effect with the administration of fosinopril, evidenced by the reduction of plasma levels of C-reactive protein. This preventive action against atherosclerosis and cardiovascular pathologies has been refuted by a recent study conducted on 621 patients in whom there was no statistically significant drop in this factor, even after 3 months of treatment.

Acta Cardiol. 2010 Jun; 65 (3): 309-14.

The study in question has evaluated the different efficacy of the combined therapy with amlodipine and fosinopril in single administration with respect to chronotherapy, ie the taking of the two drugs at different times of the day. The results show that chronotherapy can be more effective in reducing nocturnal pressure and restoring the correct pressure-based cycles.

Method of use and dosage

ELITEN ® 10mg tablets of fosinopril sodium salt:

for the treatment of arterial hypertension, the most effective dose seems to be that of 20 mg daily, taken in a single thing; however, in the initial phase, therapy should involve the administration of only one tablet per day. In the case of a reduced therapeutic effect, it would be advisable to adjust the dosage or combine another antihypertensive drug, such as a diuretic.

The correct dosage formulation should be established by the doctor after a careful evaluation of the pathological picture, of the possible administration of other antihypertensive drugs and of the physiological state of the patient, in order to avoid the appearance of side effects and maximize therapeutic efficacy.

IN ANY CASE, BEFORE TAKING ELITEN ® Fosinopril - THE REQUIREMENT AND CHECK OF YOUR DOCTOR IS NECESSARY.

Warnings ELITEN ® Fosinopril

The administration of ACE inhibitors, therefore also of ELITEN ® could be accompanied by facial, labial, lingual and laryngeal angioedema, preventing normal breathing. In these cases it would be necessary to provide for the immediate suspension of therapy and the implementation of the necessary practices to avoid suffocation. Moreover, this reaction, like dermatological ones, could occur with greater incidence in case of hypersensitivity to the active principle, which seems to be accentuated by the bite of some insects and the use of particular dialysis membranes.

Before starting therapy with ELITEN ® it would be necessary to monitor the electrolytes and blood pressure in order to establish the correct dosage and, if necessary, to correct the blood chemistry parameters.

Especially in the initial phase of treatment, it is possible to experience marked pressure drops, which could determine the onset of hypotensive crises, however transient; in these cases it would be advisable to review the dosage, in order to optimize the therapeutic efficacy and avoid the incidence of side effects. Therefore, in patients with heart failure, for whom the risk of hypotensive crisis has increased, the drug should be administered under strict medical supervision and possibly in a hospital setting.

The same should be done for particular categories of patients at risk, such as immunosuppressed, patients suffering from various types of renal and hepatic insufficiency, and collagen diseases, in which other plasma values should also be monitored, such as azotemia, creatininemia and granulocyte counts.

Some side effects of antihypertensive drugs and ACE inhibitors, such as dizziness, headache and drowsiness, could reduce the patient's normal reactive and perceptive capacities, making it dangerous to use machinery and drive vehicles.

PREGNANCY AND BREASTFEEDING

The side effects on the health of the fetus, described in the literature on experimental models and due to the administration of ACE inhibitors during the period of pregnancy, strongly advise against the intake of ELITEN ® during this period. Furthermore, considering the observed neonatal toxicity, it is advisable to stop breast-feeding in case of concomitant onset of drug therapy with ACE inhibitors.

Interactions

The therapeutic efficacy of fosinoprilat could be increased by the concomitant administration of antihypertensive drugs, tricyclic antidepressants, antipsychotics, anesthetics and diuretics. This action could be used for therapeutic purposes, in case of correct dosage formulation, but could be responsible for hypotensive crises as a consequence of incorrect dosages. For this reason it would be advisable to adjust the administered dose and monitor blood pressure levels. In the case of administration of potassium-sparing diuretics, monitoring of blood potassium levels should also be envisaged, to avoid situations of hyperkalemia potentially dangerous for the health of the patient.

The antihypertensive effect of ELITEN ® could be inhibited by the administration of non-steroidal anti-inflammatory drugs and drugs capable of increasing water-saline retention.

Fosinoprilat, as well as other ACE inhibitors, can assist the function of hypoglycemic drugs, allowing better glycemic control, probably through an enhancement of insulin sensitivity.

ELITEN ® may also increase lithium cytotoxicity.

Contraindications ELITEN ® Fosinopril

ELITEN ® is contraindicated in case of hypersensitivity to one of its components, in case of hereditary angioedema or associated with previous pharmacological treatments with ACE inhibitors, in case of severe impairment of renal and hepatic function and during the period of pregnancy and lactation.

Undesirable effects - Side effects

The side effects described for ELITEN ® are generally mild and transient. More frequently it is possible to find asthenia, chest pain, peripheral edema, headache and dry cough.

Clinically more relevant disorders are decidedly more rare and mainly concern particular categories of patients at risk (immunosuppressed, patients suffering from cardiac, renal and hepatic insufficiency), manifesting themselves with neutropenia followed by recurrent infections of the respiratory and gastro-intestinal tract, frequency alterations cardiac, orthostatic hypotension and alterations of some hematoclinic parameters.

Hypersensitivity to the active ingredient occurs mainly with angioedema and dermatological reactions.