CONVERTEN ® Enalapril maleate

CONVERTEN ® is a drug based on Enalapril maleate.

THERAPEUTIC GROUP: Antihypertensives - ACE inhibitors not associated

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

Directions CONVERTEN ® Enalapril maleate

CONVERTEN ® is used both in monotherapy and in combination therapy to treat high blood pressure.

CONVERTEN ® can also be used in the treatment of symptomatic heart failure and in the prevention of this disease in high-risk patients with asymptomatic left ventricular dysfunction and with an ejection fraction of less than 35%.

Mechanism of action CONVERTEN ® Enalapril maleate

The oral intake of CONVERTEN ® ensures a good absorption of its active ingredient enalapril, estimated at around 60% of the dose taken. Despite the plasmatic peak of this molecule is recorded already after an hour from the assumption, so that the active principle can carry out its own biological action must necessarily be metabolized in its active form, known as enalaprilat, whose plasmatic peak is observed only after 4 hours after taking CONVERTEN ® oral In light of the aforementioned pharmacokinetic properties, the antihypertensive effect of the drug starts about an hour after taking it, to optimize around the fourth / sixth hour when the levels of the pharmacologically active principle are maximum. The antihypertensive effect is mainly due to the inhibitory action of enalaprilat on the ACE enzyme, with a consequent decrease in the levels of angiotensin II and aldosterone, responsible for the increase in peripheral vascular resistance and hydrosaline retention. Furthermore, several studies show that this active ingredient can reduce microalbuminuria and urinary IgG secretion in patients suffering from diabetic nephropathy, and above all reduce progressive cardiac dilation in patients with mild and moderate heart failure, preventing the progression of the disease.

Once its action is over, the active ingredient is eliminated mainly through the urine in the form of 40% enalaprilat and 20% enalpril.

Studies carried out and clinical efficacy

1 ENALAPRIL / FOLIC ACID, WINNING COMBINATION

This study conducted on about 430 patients suffering from hypertension and treated with concomitant administration of enalapril (10mg) and folic acid (400mcg), shows how this combination can be more effective - compared to the drug alone - in reducing systolic and diastolic blood pressure and in balancing blood sugar levels in patients with hyperglycemia.

2. ENALAPRIL / HYDROCHLOROTHIAZIDE IN THE TREATMENT OF HYPERTENSION

In most therapeutic protocols for hypertension recourse is made to the concomitant administration of more antihypertensive drugs. This Russian study, carried out on almost 8000 patients suffering from hypertension and cardiovascular complications, has shown how the combined hydrochlorothiazide / enalapril therapy, at constant dosage, guarantees a decrease in blood pressure levels up to reaching the standard values and aggressors in as many as 77% of patients treated.

3. ENALAPRIL AND TREATMENT OF DIABETIC NEPHROPATHY

One of the therapeutic indications of ACE inhibitors consists in the treatment of diabetic nephropathy. The study in question shows how the administration of enalapril can be particularly effective both in reducing blood pressure and in reducing proteinuria in patients with diabetic nephropathy.

Method of use and dosage

CONVERTEN ® enalapril maleate 5/20 mg tablets:

for the treatment of arterial hypertension, doses of between 5 and 20 mg are recommended, using tablets taken once a day. It is necessary to consider that the precise formulation of the dosage should be established by the doctor after a careful evaluation of the severity of the disease, the possible susceptibility to the drug and the presence of interfering factors with the therapeutic procedure (concomitant or previous administration of diuretics, old age, volume-depleted patients or patients with kidney diseases)
for the treatment of heart failure and left ventricular dysfunction, the dosage generally tends to fall; the appropriate therapeutic scheme must however be decided by the doctor, taking into account the history of the patient's pathology and the possible association with other drugs active on the cardiovascular system.

IN ANY CASE, BEFORE TAKING CONVERTEN ® Enalapril maleate - THE REQUIREMENT AND CHECK OF YOUR DOCTOR IS NECESSARY.

Warnings CONVERTEN ® Enalapril maleate

Particular attention in the correct dosage formulation should be placed in case of concomitant administration of antihypertensive drugs, in particular diuretics. In fact, the depletion of the blood volume induced by these drugs could increase the incidence of hypovolemic episodes accompanied by hypotensive crises. Furthermore, any conditions of hyperkalemia could occur following the simultaneous intake of potassium-sparing diuretics; we therefore recommend constant monitoring of blood levels of potassium and blood pressure.

The same monitoring modalities, with the addition of creatinine, should be undertaken in case of use of CONVERTEN by patients with reduced renal function and subjected to enalapril therapy, in which given the renal metabolism of the active ingredient, could be sufficient inferior doses of the drug.

It would also be advisable to frequently monitor the blood levels of granulocytes in immunocompromised patients under CONVERTEN ® therapy in order to minimize the possible occurrence of neutropenia or agranulocytosis, which in rare cases has been observed following the administration of ACE inhibitors.

The different therapeutic efficacy of ACE inhibitors, therefore also of enapril, among black and Caucasian patients, could be explained by the low basal renin levels in blacks, which greatly reduce the therapeutic efficacy of this medicinal category.

It is also important to remember that some of the side effects associated with antihypertensive therapy, such as dizziness, headache and drowsiness, could reduce the patient's perceptive and reactive capacities, making it dangerous to use machinery and drive vehicles.

PREGNANCY AND BREASTFEEDING

The various studies present in the literature suggest a potential increase in the risk of teratogenicity and fetal toxicity when taking ACE inhibitors during the period of pregnancy; therefore it is not recommended for use during the entire gestation period, opting for drugs with a higher safety profile.

Both enalapril and enalaprilat are secreted in breast milk, with effects not yet clarified, thus suggesting the interruption of lactation during CONVERTEN ® therapy

Interactions

Enalapril, contained in CONVERTEN ®, can interact with numerous other active ingredients, sometimes causing a significant variation in the normal functionality of the drug.

As already mentioned, enalapril can interact with:

potassium-sparing drugs and potassium supplements, evidently increasing the blood levels of this mineral;
diuretics and antihypertensive drugs, mutually enhancing the hypotensive efficacy;
non-steroidal anti-inflammatory drugs, reducing their therapeutic effect;
antidiabetic drugs, with an increase in their hypoglycemic action, probably due to an improved insulin sensitivity;
lithium, increasing its cytotoxicity.

Contraindications CONVERTEN ® Enalapril maleate

CONVERTEN ® is contraindicated in case of hypersensitivity to one of its components, in the case of angioedema, severe impairment of renal function and during the period of pregnancy and lactation.

CONVERTEN ® contains lactose; therefore, it should not be taken by patients with lactose / galactose intolerance, malabsorption and lactase deficiency.

Undesirable effects - Side effects

Side effects observed during CONVERTEN ® therapy are generally transient and clinically irrelevant. The most common ones include cough, headache, depression, dizziness, blurred vision, abdominal pain, nausea and hypotension.

In particular categories of patients at risk, potentially dangerous side effects, such as angioedema, hypoglycemia, neutropenia, anemia and renal dysfunction, may occur.

In case of hypersensitivity to the drug, dermatological reactions may occur - such as skin rashes and erythemas, accompanied by fever, pruritus and facial angioedema - which could hinder normal respiratory capacity.