Enalapril Hexal, tablets 10 mg 20 pcs

An angiotensin-converting enzyme inhibitor.
ATC code: C09AA02

Pharmacological action

Pharmacodynamics

ACE inhibitor. Enalapril, a metabolite of enalapril, has pharmacological activity. It suppresses the formation of angiotensin II and eliminates its vasoconstrictor effect. It decreases total peripheral vascular resistance, systolic and diastolic blood pressure (BP), post- and preload on myocardium.

Dilates the arteries to a greater extent than the veins, and there is no reflex increase in heart rate.

It also reduces preload, decreases right atrial pressure in the small circulatory circle, reduces left ventricular hypertrophy. Reduces the tone of the renal tubular arterioles, thus reducing intra-column hemodynamics and prevents diabetic nephropathy. It does not affect the metabolism of glucose, lipoproteins and sexual function.

The maximum effect develops in 6-8 hours and lasts for 24 hours. Therapeutic effect is achieved after several weeks of treatment.

Indications

Heart failure, Edema, Hypertension (high blood pressure)

• Arterial hypertension;
• Cronic heart failure (in combination therapy)
• Left ventricular dysfunction

Active ingredient

Enalapril

Composition

10 mg tablets:

active ingredient:

enalapril maleate – 10.0 mg;

excipients:

sodium bicarbonate,

lactose monohydrate,

corn starch,

talc,

magnesium stearate,

iron oxide red.

How to take, the dosage

The drug may be used regardless of meals, with plenty of fluids.
Daily doses are usually taken in the morning, however, the drug can be divided into 2 times – morning and evening.
Simultaneous use of diuretics may increase the hypotensive effect.

Arterial hypertension:
The initial dose is 5 mg in the morning (1 tablet of 5 mg enalapril maleate). If at this dose blood pressure value does not normalize, the daily dose may be increased to 10 mg. The interval between dose increases should be at least 3 weeks.
The maintenance dose is usually 10 mg enalapril maleate.
The maximum daily dose should not exceed 40 mg daily (2 times 20 mg of enalapril maleate).

Chronic heart failure:
The initial dose is 2.5 mg in the morning. The dose should be increased gradually, depending on the patient’s condition.
The maintenance dose is usually 5 – 10 mg (1 – 2 tablets of 5 mg, or 1 tablet of 10 mg enalapril maleate). The maximum daily dose should not exceed 20 mg (2 tablets of 10 mg, or 1 tablet of 20 mg).

Left ventricular dysfunction:
The initial dose is 2.5 mg of enalapril maleate 2 times daily, the dose may be adjusted depending on the patient’s condition. The average maintenance dose is 10 mg 2 times per day.

Patients with moderate renal impairment (creatinine clearance 30 – 60 ml/min) and patients aged over 65 years:
The initial dose is 2.5 mg in the morning.
The maintenance dose is usually 5 – 10 mg (1 – 2 tablets of 5 mg or 1 tablet of 10 mg) of enalapril maleate per day. The maximum daily dose should not exceed 20 mg (2 tablets of 10 mg or 1 tablet of 20 mg) of enalapril.

Patients with significant renal dysfunction (creatinine clearance less than 30 ml/min) and those on hemodialysis:
The starting dose is 2.5 mg of enalapril maleate per day.
Patients on hemodialysis should take the drug after dialysis.
The maintenance dose is usually 5 mg (1 5 mg tablet) of enalapril per day. The maximum daily dose should not exceed 10 mg (1 tablet of 10 mg or 2 tablets of 5 mg) per day.
The drug may be used as monotherapy or in combination with other antihypertensive agents, especially diuretics.

Interaction

Allopurinol: decrease in the number of leukocytes in the blood, leukopenia.

Analgesics, nonsteroidal anti-inflammatory drugs (e.g., acetylsalicylic acid, indomethacin): weakening of the hypotensive effect of enalapril is possible.

Antihypertensive agents: increase the hypotensive effect of enalapril, especially with concomitant use of diuretics.

Anesthetics and narcotics: Increased reduction of blood pressure.

Potassium, potassium-saving diuretics (especially spironolactone, amiloride, triamterene), and other drugs such as heparin: increase serum potassium levels.

Baking salt: weakening of the antihypertensive effect.

Lithium: increased serum lithium levels (regular monitoring of lithium is necessary).

Orderal antidiabetic agents, insulin: In rare cases there may be an increase in hypoglycemic effect of oral antidiabetics (e.g., sulfonyl urea / biguanidine) and insulin. In such cases, reduction of the dose of antidiabetics is required.

Novocainamide: decrease in the number of leukocytes in the blood, leukopenia.

Cytostatics, immunosuppressants, systemic corticosteroids: decrease in blood leukocyte count, leukopenia.

Alcohol: increasing the effect of alcohol.

.

Special Instructions

Caution should be exercised when prescribing Enalapril Hexal in patients with decreased circulating blood volume (as a result of diuretic therapy, restriction of table salt intake, hemodialysis, diarrhea and vomiting) – the risk of sudden and pronounced BP decrease after using even the initial dose of ACE inhibitor is increased. Transient arterial hypotension is not a contraindication for continuation of treatment with the drug after BP stabilization. In case of repeated BP decrease, the dose should be reduced or the drug should be discontinued.

Enalapril should not be used in patients on dialysis with AN 69 polyacrylonitron membranes due to the possibility of anaphylactic reactions.

We should check renal function before starting the drug. Patients with impaired renal function should reduce the single dose or increase the intervals between doses.

Hypertension and laboratory parameters should be monitored before and during treatment, especially if there is salt and/or fluid loss, impaired renal function, severe or renal hypertension, heart failure and over 65 years of age.

The risk of orthostatic hypotension increases with prior treatment with diuretics, particularly in patients with chronic heart failure, so the loss of fluids and salts should be compensated before starting enalapril treatment.

In some patients with bilateral renal artery stenosis or stenosis of a single kidney, increased blood urea and serum creatinine were observed. The changes were reversible and the parameters returned to normal after discontinuation of treatment.

In newborns and infants who have had intrauterine exposure to ACE inhibitors should be closely monitored for the timely detection of marked BP decrease, oliguria, hyperkalemia and neurological disorders possible due to decreased renal and cerebral blood flow with ACE inhibitor-induced BP decrease. In oliguria, it is necessary to maintain BP and renal perfusion by administration of appropriate fluids and vasoconstrictors.
If angioedema of the face, extremities, lips or larynx develops, discontinue the drug immediately and consult a physician. Coughing may occur, which stops after discontinuation of the drug.

The sudden withdrawal of treatment does not lead to “withdrawal” syndrome (a sharp rise in BP).

The drug should be discontinued before parathyroid function study.

Before surgery (including dentistry), the surgeon/anesthesiologist should be warned about the use of ACE inhibitors.

The drug should be prescribed with caution in patients with diabetes because of the risk of hyperkalemia.

Instructions for participants of road traffic:
Treatment with enalapril may result in the development of individual reactions that may impair the patient’s ability to actively participate in traffic, which should also be borne in mind when operating machinery and operating devices that require increased attention. These effects are exacerbated when the dose is increased and when alcohol is taken.

.

Contraindications

Enalapril Hexal should not be used if

• high sensitivity to the drug and to other angiotensin-converting enzyme inhibitors;
• Angioneurotic edema in the history, including against the ACE inhibitors;
• stenosis (unilateral or bilateral) of the renal arteries;
• liver or renal disease;
• pregnancy, lactation;
• age below 18 years (effectiveness and safety not established).

.

Side effects

Most side effects are temporary and do not require discontinuation of the drug.

Cardiovascular system disorders:
In the beginning of therapy rarely: arterial hypotension (including orthostatic), dizziness, weakness, visual disturbances and very rarely – chest pain, angina pectoris, palpitations, pulmonary artery thromboembolism.

Respiratory system disorders:
Unproductive dry cough, interstitial pneumonitis, bronchospasm, dyspnea, rhinorrhea, pharyngitis.

Gastrointestinal tract:

Dry mouth, anorexia, dyspeptic disorders (nausea, diarrhea or constipation, vomiting. abdominal pain), intestinal obstruction, pancreatitis, liver and biliary excretion disorders, hepatitis, jaundice.

Nervous system disorders:
In rare cases, headache, dizziness, weakness, increased fatigue, drowsiness, stunned consciousness may occur; very rarely (when taken in high doses) – depression, sleep disturbance, peripheral neuropathy and paresthesia, muscle cramps, nervousness, tinnitus and blurred vision. These disorders are temporary and normalize after discontinuation of the drug.

Recreational renal function:
Rarely, renal function abnormalities, proteinuria, development of hyperkalemia and hyponatremia, as well as taste changes (the phenomena are temporary and normalize after discontinuation of the drug).

Concerning the reproductive system:
Very rare when used in high doses – impotence.

Allergic reactions:
Skin rash, angioedema of the face, extremities, lips, tongue, vocal cleft and/or larynx, dysphonia, exfoliative dermatitis, erythema multiforme exudative erythema (including Stevens-Johnson syndrome).including Stevens-Johnson syndrome), toxic epidermal necrolysis, vesicular rash, pruritus, urticaria, photosensitization, serosis, vasculitis, myositis, arthralgia, arthritis, stomatitis.

Laboratory findings:
There may be a decrease in hemoglobin, hematocrit and platelet count. Anemia, thrombocytopenia, neuropathy, elevated urea concentrations, hypercreatininemia, eosinophilia may develop in very rare cases, especially in patients with impaired renal function, diffuse connective tissue diseases, or during simultaneous therapy with allopurinol, novocainamide or immunosuppressors; in single cases – increase of liver transaminases activity, agranulocytosis or pancytopenia.
The values of the above laboratory parameters should be regularly monitored before and during treatment, especially in patients in risk group.

.

Overdose

Symptoms: marked decrease of blood pressure, up to development of collapse, myocardial infarction, acute cerebral circulation disorder or thromboembolic complications, convulsions, stupor.

Treatment: the patient is transferred to the horizontal position with a low headboard. In mild cases gastric lavage and oral administration of saline solution are indicated, in more severe cases – measures aimed at BP stabilization: intravenous infusion of physiological solution, plasma substitutes, angiotensin II administration, hemodialysis if necessary (elimination rate of enalaprilat averages 62 ml/min).

.

Similarities

Berlipril 5, Renipril, Enam, Enap, Renitec, Berlipril 20, Berlipril 10, Enalapril Hexal, Enalapril FPO, Enalapril Renewal, Berlipril