Enalozid mono

General characteristics. Structure:

Active ingredient: enalapril;

1 tablet contains maleate enalapril in terms of 100% substance of 5 mg or 10 mg;

excipients (tablets on 5 mg): lactose, monohydrate, starch corn, povidone, calcium stearate.

excipients (tablets on 10 mg): lactoses monohydrate, starch corn, povidone, calcium stearate.

Pharmacological properties:

Pharmacodynamics. Inhibitor of an angiotensin-converting enzyme (APF). Эналозид® Mono treats group of anti-hypertensive means. Pharmacological activity the enalapril metabolite - enalaprilat has. It suppresses formation of angiotensin II and eliminates its vasoconstrictive action, causes gradual decrease in systolic and diastolic arterial pressure without essential change of heart rate and minute volume of blood, reduces a hypertrophy of a left ventricle, increases a renal blood stream, improves function of kidneys and interferes with progressing of a diabetic nephropathy.

Pharmacokinetics. After intake from digestive tract about 60% of enalapril are absorbed. Meal does not influence its absorption. The therapeutic effect develops in 1 hour after reception, reaches a maximum in 4 - 6 hours and proceeds for 24 hours. Enalapril is exposed to hydrolysis with formation of enalaprilat which maximum concentration in blood is observed in 3 - 4 hours. The elimination half-life of enalaprilat makes 11 hours. Drug is removed by kidneys (60%) and with a stake (33%). At patients with a heavy renal failure the elimination half-life of enalaprilat increases. Gets through a placenta and into breast milk. It is brought out of an organism at a hemodialysis.
Pharmaceutical characteristics.

Main physical and chemical properties: tablets of color, white or white with a creamy shade, with a flat surface, a facet and risky, or without risks.

Indications to use:

Essential hypertensia, renovascular hypertensia, heart failure.

Route of administration and doses:

Drug can be accepted irrespective of meal. The dose of drug should be korrigirovat according to a condition of the patient and his requirements. Duration of treatment depends on its efficiency and is defined by the doctor.

Indications                    the Recommended daily dosages

                              Initial dose            Maintenance dose                 Maximum dose

Essential       Once 5 mg,        10 - 20 mg, in exclusive       40 mg once silt
hypertensia           sometimes 2 times on 5 mg    cases of 40 mg once            and 2 times on 20 mg
                                                                     or 2 times on 20 mg
Cordial              Once 2,5                                                     mg 5 - 10 mg 20 mg
insufficiency

Renovascular          2,5 - 5 mg *                        5 - 10                               mg 10 - 20 mg *
hypertensia
 

* The initial and maximum daily dose is defined depending on an indicator of clearance of creatinine. If it exceeds 0,5 ml/sec. (30 ml/min.), then an initial dose of 5 mg/days, maximum – 20 mg/days if the clearance is lower than 0,5 ml/sec. (30 ml/min.), an initial dose of 2,5 mg/days, maximum – 10 mg/days.

In case of purpose of Enalozida® to the Mono patients receiving at the same time diuretics, the initial dose of drug has to make 2,5 mg/days. Further increase in a dose is possible.

For patients of advanced age the recommended initial dose makes 1,25 mg, at the same time at this category of patients more expressed hypotensive effect and lengthening of time of effect of drug is more often observed that it is connected with reduction of speed of removal of enalaprilat.

The patient with a hyponatremia (concentration of ions of sodium in blood serum less than 130 mmol/l) the initial dose of Enalozida® Mono has to make 2,5 mg 1 times/days.

Selection of a dose has to be carried out within 2 – 4 weeks or to shorter terms. An average maintenance dose of 5 - 20 mg/days for 1 – 2 reception.

Drug is used both in monotherapy, and in combination with other anti-hypertensive means.

Features of use:

With care it is necessary to appoint Enalozid® Mono at primary hyper aldosteronism, a bilateral stenosis of renal arteries, a stenosis of an artery of the only kidney, a hyperpotassemia, a state after transplantation of a kidney, an aortal stenosis, a mitral stenosis with disturbances of a hemodynamics, an idiopathic hypertrophic subaortal stenosis, diseases of connecting fabric, the coronary heart disease (CHD), cerebrovascular diseases, a diabetes mellitus, a renal failure (a proteinuria more than 1 g/days), a liver failure, at a concomitant use with immunodepressants and saluretics, at patients of advanced age (65 years are more senior).

If there is a high risk of development of arterial hypotension (vomiting, diarrhea, use of a hemodialysis, treatment by diuretics, heavy heart failure), then such patient should give the first dose of drug in medical institution and to watch the patient not less than 5 hours. During observation the patient has to be in a prone position.

Treatment of patients with suspicion of renovascular hypertensia is recommended to be carried out in specialized hospitals.

It is necessary to exercise careful medical control at purpose of Enalozida® to Mono patients with heavy heart failure, an ischemic heart disease and diseases of vessels of a brain at which sharp decrease in the ABP can lead to a myocardial infarction, a stroke or a renal failure.

With care appoint Enalozid® to Mono patients with a reduced volume of the circulating blood (as a result of therapy by diuretics, at restriction of consumption of table salt, carrying out a hemodialysis, diarrhea and vomiting) since the risk of the sudden and expressed decrease in the ABP after use even of the minimum dose of APF inhibitor is increased. Tranzitorny arterial hypotension is not a contraindication for continuation of treatment of Enalozidom® Mono after stabilization of the ABP. In case of the repeated expressed decrease in the ABP it is necessary to reduce a dose or to cancel drug.

At purpose of Enalozida® the Mono patients who are on a hemodialysis should consider that use of high-flowing dialysis membranes increases risk of development of anaphylactic reaction. Correction of the mode of dosing in days, free from dialysis, has to be carried out depending on the ABP level. Before reception of Enalozida® Mono control of the ABP, level of hemoglobin, potassium, creatinine, urea, activity of liver enzymes, availability of protein in urine is necessary.

Patients with the instruction on development of a Quincke's disease in the anamnesis have an increased risk of its development at reception of APF inhibitors.

The sudden termination of reception of Enalozida® Mono does not lead to a withdrawal (sharp raising of the ABP).

At an oliguria maintenance of the ABP and renal perfusion by administration of the corresponding liquids and vasoconstrictors is necessary.

Before a research of function of Enalozid® epithelial bodies Mono it is necessary to cancel.

During treatment of Enalozidom® Mono increase in content of potassium in blood serum, especially at patients with a chronic renal failure, a diabetes mellitus is possible, at co-administration of kaliysberegayushchy diuretics (Spironolactonum, amiloride and Triamterenum it is not recommended to appoint) or potassium drugs. Such patients should be informed on need of the address to the doctor at emergence of muscular weakness and arrhythmia. During treatment of Enalozidom® Mono it is necessary to be careful when performing physical exercises at hot weather since there is a risk of development of dehydration and excessive decrease in the ABP because of decrease in volume of the circulating blood. During treatment of Enalozidom® Mono it is not recommended to take alcoholic beverages.

Before surgical intervention (including stomatology) it is necessary to warn the surgeon/anaesthesiologist about use of APF inhibitors.

Lactose therefore this drug is not recommended to be accepted to patients with inborn intolerance of a galactose, with deficit of lactase or disturbance of absorption of glucose or a galactose is a part of the tablets Enalozida® Mono.

Ability to influence speed of response at control of motor transport or work with other mechanisms. During treatment it is necessary to abstain from control of motor transport and occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions since dizziness, especially after an initial dose of APF inhibitor and at the patients accepting diuretic means is possible.

Side effects:

The side effects observed during treatment of Enalozidom® Mono are usually poorly expressed, have passing character and do not demand drug withdrawal.

From cardiovascular system: excessive decrease in the ABP, an orthostatic collapse, is rare - a retrosternal pain, stenocardia, a myocardial infarction (are usually connected with the expressed decrease in the ABP), arrhythmias (wander - or tachycardia, atrial fibrillation), a heart consciousness, a thromboembolism of branches of a pulmonary artery, pain in heart, a syncope, Reynaud's syndrome.

From the central nervous system: dizziness, a headache, sleeplessness, weakness, increased fatigue, drowsiness (2-3%), very seldom confusion of consciousness, increased fatigue, is very rare at use of high doses - a hyperexcitability, a depression, paresthesias.

From sense bodys: disturbance of a vestibular mechanism, hearing disorder, taste, sonitus.

From organs of sight: perhaps temporary vision disorder, xanthopsias, in rare instances visual hallucinations.

From the alimentary system: dryness in a mouth, anorexia, dispeptic frustration (nausea, diarrhea or a lock, vomiting, pains in a stomach), intestinal impassability, pancreatitis, an abnormal liver function and a zhelchevydeleniya, hepatitis (hepatocellular or cholestatic), jaundice.

From respiratory system: unproductive dry cough, intersticial pneumonitis, bronchospasm/asthma, asthma, rhinorrhea, pharyngitis, pharyngalgia, hoarseness of a voice.

Allergic reactions: skin rash, Quincke's disease of the person, extremities, lips, language, glottis and/or throat, dysphonia, polymorphic erythema, exfoliative dermatitis, Stephens-Johnson's syndrome, toxic epidermal necrolysis, pempigus, itch, small tortoiseshell, photosensitization, serositis, vasculitis.

From laboratory indicators: a giperkreatininemiya, increase in content of urea, increase in activity of "hepatic" transaminases, a hyperbilirubinemia, a hyperpotassemia, a hyponatremia, decrease in concentration of hemoglobin and a hematocrit, increase in the blood sedimentation rate (BSR), thrombocytopenia, a neutropenia, an agranulocytosis (at patients with autoimmune diseases), an eosinophilia.

From an urinary system: renal failure, proteinuria.

From a musculoskeletal system: muscular spasms, muscular weakness, mialgiya, dorsodynias, arthralgias are possible.

Endocrine disturbances: a syndrome of disturbance of secretion of antidiuretic hormone, a hypoglycemia at patients who accept antihyperglycemic means.

Others: an alopecia, decrease in a libido, inflows, stomatitis, a glossitis, the increased sweating, decrease in a potentiality.

Chances of paradoxical reaction in the form of increase in arterial pressure at enalapril use.

Interaction with other medicines:

Co-administration with non-steroidal anti-inflammatory drugs (NPVS) can lead to decrease in hypotensive effect of Enalozida® Mono;
joint appointment with kaliysberegayushchy diuretics can cause a hyperpotassemia;
simultaneous use of Enalozida® of lithium, Mono with salts, leads to delay of release of lithium;
the concomitant use of drug with febrifugal and anesthetics can reduce efficiency of Enalozida® Mono;
Эналозид® Mono weakens effect of the drugs containing theophylline;
Cimetidinum extends the period of action of Enalozida® Mono;

estrogen reduces efficiency of drug;
at use with nimodipiny emergence of disturbances of a cordial rhythm, strengthening of congestive heart failure is possible;
at the combined appointment with Allopyrinolum, cytostatics, immunodepressants, system corticosteroids the leukopenia, anemia, a pancytopenia is possible;
at co-administration with pressor amines - mutual easing of effects;

during treatment it is forbidden to take alcoholic beverages as alcohol strengthens hypotensive effect of drug.

Contraindications:

Hypersensitivity to enalapril and other components of drug;
the Quincke's disease in the anamnesis connected with purpose of APF inhibitors;
bilateral stenosis of renal arteries or renal artery stenosis of the only kidney;
primary hyper aldosteronism;
stenosis of the aortal or mitral valve, hypertrophic cardiomyopathy;
collagenoses; porphyria;
heavy hepatic disturbances (prekoma, hepatic coma); period of pregnancy and feeding by a breast;
children's age up to 18 years (due to the lack of sufficient clinical experience).

Overdose:

Overdose symptoms: excessive decrease in the ABP up to development of a collapse, a myocardial infarction, an acute disorder of cerebral circulation or tromboembolic episodes, spasms, a stupor.

Treatment: the patient is transferred to horizontal position with a low headboard, it is necessary to call immediately the doctor if the accepted dose exceeds established. In mild cases the gastric lavage and intake of saline solution, in more serious cases - the actions directed to stabilization of the ABP, intravenous administration of normal saline solution, plasma substitutes, if necessary - intravenous administration of angiotensin II, a hemodialysis are shown (enalaprilat removal speed - 62 ml/min.).
Use during pregnancy and feeding by a breast.

It is contraindicated to use at pregnancy. At the occurred pregnancy reception of enalapril should be stopped immediately. Enalapril is emitted in breast milk. In need of its use in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination.
Children.

Safety and efficiency of use of drug for treatment of children are not established therefore children should not appoint it up to 18 years.

Storage conditions:

Period of validity. 3 years. Not to use drug after the termination of the period of validity specified on packaging. To store in the unavailable to children, protected from light place at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in the blister. On 2 blisters enclosed in a pack.