Enap tablets 10mg, No. 60

Х Essential hypertension.
Х Chronic heart failure (as part of combination therapy).
Х Prevention of the development of clinically significant heart failure in patients with asymptomatic left ventricular dysfunction (as part of combination therapy).
Х Prevention of coronary ischemia in patients with left ventricular dysfunction in order to:
- reduce the incidence of myocardial infarction;
- reducing the frequency of hospitalizations for unstable angina.

Inside, regardless of the time of food intake, preferably at the same time of day, with a small amount of liquid.

Arterial hypertension

The initial dose is 5 to 20 mg once a day, depending on the severity of hypertension and the patient's condition. For mild arterial hypertension, the recommended starting dose is 5-10 mg / day.

In patients with severe activation of the RAAS (for example, with renovascular hypertension, salt loss and / or dehydration, decompensated heart failure or severe arterial hypertension), an excessive decrease in blood pressure is possible at the beginning of treatment. In such situations, it is recommended to start therapy with a low initial dose of 5 mg / day or less under the supervision of a physician.

Previous therapy with high doses of diuretics can lead to dehydration and an increased risk of arterial hypotension at the beginning of therapy with EnapЃ; the recommended starting dose is 5 mg / day. Diuretic treatment should be discontinued 2-3 days before the start of the use of EnapЃ. Care should be taken when using EnapЃ, to monitor renal function and serum potassium.

The usual maintenance dose is 20 mg once a day.

The dosage is selected individually, if necessary, it can be increased to a maximum daily dose of 40 mg.

CHF and left ventricular dysfunction

The initial dose of EnapЃ is 2.5 mg / day once; in this case, treatment must be started under the close supervision of a doctor.

The drug EnapЃ for the treatment of heart failure can be used simultaneously with diuretics and / or beta-blockers, and, if necessary, with cardiac glycosides. In the absence of symptomatic arterial hypotension at the beginning of therapy or after its correction, the dose should be increased gradually (by 2.5-5 mg every 3-4 days) to the usual maintenance dose of 20 mg / day, which is prescribed either once or in 2 doses. depending on the tolerability of the drug. The dose selection is carried out within 2-4 weeks. The maximum daily dose is 40 mg in 2 divided doses.

1st week: 1st-3rd day - 2.5 mg / day in 1 dose; 4-7th day - 5 mg / day in 2 divided doses.

2nd week: 10 mg / day in 1 or 2 divided doses.

3rd and 4th weeks: 20 mg / day in 1 or 2 divided doses.

Special precautions should be taken in patients with impaired renal function and taking diuretics.

Given the risk of developing arterial hypotension and renal failure (observed much less often), blood pressure and renal function should be carefully monitored before and after starting the use of EnapЃ. In patients taking diuretics, the dose of diuretics, if possible, should be reduced before taking EnapЃ. The development of arterial hypotension after taking the first dose does not mean that arterial hypotension will persist with prolonged use, and does not indicate the need to discontinue the use of the drug.

Special patient groups

Impaired renal function. In patients with impaired renal function, the intervals between use should be increased and / or the dose of EnapЃ should be reduced.

When Cl creatinine is from 30 to 80 ml / min, the initial dose is 5-10 mg / day; from 10 to 30 ml / min - 2.5Ц5 mg / day; less than 10 ml / min - 2.5 mg on the day of hemodialysis (enalaprilat is excreted during hemodialysis).

In the interval between hemodialysis sessions, the dose of the drug should be selected under the control of blood pressure.

Elderly patients. In elderly patients, a more pronounced antihypertensive effect and a prolongation of the drug action time are more often observed, which is associated with a decrease in the rate of elimination of enalapril, therefore the recommended initial dose is 1.25 mg. The dose is adjusted according to renal function.

Active ingredient:
Enalapril maleate 10.00 mg
Excipients: sodium bicarbonate 5.10 mg, lactose monohydrate 124.60 mg, corn starch 21.40 mg, talc 6.00 mg, magnesium stearate 1.70 mg, iron dye red oxide (E172) 1.20 mg

hypersensitivity to enalapril, other components of the drug or other ACE inhibitors;

a history of angioedema associated with previous use of ACE inhibitors, hereditary angioedema of Quincke or idiopathic angioedema;

simultaneous use with aliskiren in patients with diabetes mellitus or impaired renal function (Cl creatinine less than 60 ml / min);

porphyria;

lactase deficiency, lactose intolerance, glucose-galactose malabsorption syndrome (because EnapЃ contains lactose);

pregnancy;

breastfeeding period;

age up to 18 years (efficacy and safety have not been established).

With care: bilateral stenosis of the renal arteries or stenosis of the artery of a single kidney; primary hyperaldosteronism; hyperkalemia; condition after kidney transplantation; aortic stenosis and / or mitral stenosis (with hemodynamic impairment); hypertrophic obstructive cardiomyopathy (GOKMP); conditions with reduced BCC (including diarrhea, vomiting); systemic connective tissue diseases (including scleroderma, systemic lupus erythematosus); coronary heart disease; oppression of bone marrow hematopoiesis; cerebrovascular diseases (including cerebral circulation insufficiency); diabetes; renal failure (proteinuria - more than 1 g / day); liver failure; patients on a salt-restricted diet or on hemodialysis; simultaneous reception with immunosuppressants and diuretics;patients over 65 years of age.

Tradename:

EnapЃ

International non-proprietary name:

enalapril

Dosage form:

Pills

Composition

1 tablet 2.5 mg contains:
Active substance:
Enalapril maleate 2.50 mg
Excipients: sodium bicarbonate 1.30 mg, lactose monohydrate 64.90 mg, corn starch 11.20 mg, hyprolose 1.25 mg, talc 3, 00 mg, magnesium stearate 0.85 mg
1 tablet 5 mg contains:
Active substance:
Enalapril maleate 5.00 mg
Excipients: sodium bicarbonate 2.60 mg, lactose monohydrate 129.80 mg, corn starch 22.40 mg, hyprolose 2 , 50 mg, talc 6.00 mg, magnesium stearate 1.70 mg
1 tablet 10 mg contains:
Active ingredient:
Enalapril maleate 10.00 mg
Excipients:sodium bicarbonate 5.10 mg, lactose monohydrate 124.60 mg, corn starch 21.40 mg, talc 6.00 mg, magnesium stearate 1.70 mg, iron dye red oxide (E172) 1.20 mg
1 tablet 20 mg contains :
Active substance:
Enalapril maleate 20.00 mg
Excipients: sodium bicarbonate 10.20 mg, lactose monohydrate 117.80 mg, corn starch 13.90 mg, talc 6.00 mg, magnesium stearate 1.70 mg, iron oxide dye red (E172) 0.10 mg, iron dye yellow oxide (E172) 0.30 mg

Description

Tablets 2.5 mg. The tablets are white or almost white, round, biconvex, with a bevel.
Tablets 5 mg. Tablets are white or almost white, flat-cylindrical, with a score and a bevel.
Tablets 10 mg. The tablets are red-brown in color, flat-cylindrical, with a score and a chamfer. White and burgundy blotches are allowed on the surface and in the mass of the tablet.
Tablets 20 mg . Tablets are light orange, flat-cylindrical, with a score and a bevel. On the surface and in the mass of the tablet, white and maroon blotches are allowed.

pharmachologic effect

ACE inhibitor. It is a prodrug from which the active metabolite enalaprilat is formed in the body. It is believed that the mechanism of antihypertensive action is associated with competitive inhibition of ACE activity, which leads to a decrease in the rate of conversion of angiotensin I to angiotensin II (which has a pronounced vasoconstrictor effect and stimulates the secretion of aldosterone in the adrenal cortex). As a result of a decrease in the concentration of angiotensin II, a secondary increase in plasma renin activity occurs due to the elimination of negative feedback during the release of renin and a direct decrease in aldosterone secretion. In addition, enalaprilat appears to have an effect on the kinin-kallikrein system, preventing the breakdown of bradykinin. Due to the vasodilating effect, it reduces the OPSS (afterload),wedge pressure in the pulmonary capillaries (preload) and resistance in the pulmonary vessels; increases cardiac output and exercise tolerance. In patients with chronic heart failure, long-term use of enalapril increases exercise tolerance and reduces the severity of heart failure (assessed by NYHA criteria). Enalapril in patients with mild to moderate heart failure slows down its progression, and also slows down the development of left ventricular dilatation. In left ventricular dysfunction, enalapril reduces the risk of major ischemic outcomes (including the incidence of myocardial infarction and the number of hospitalizations for unstable angina).In patients with chronic heart failure, long-term use of enalapril increases exercise tolerance and reduces the severity of heart failure (assessed by NYHA criteria). Enalapril in patients with mild to moderate heart failure slows down its progression, and also slows down the development of left ventricular dilatation. In left ventricular dysfunction, enalapril reduces the risk of major ischemic outcomes (including the incidence of myocardial infarction and the number of hospitalizations for unstable angina).In patients with chronic heart failure, long-term use of enalapril increases exercise tolerance and reduces the severity of heart failure (assessed by NYHA criteria). Enalapril in patients with mild to moderate heart failure slows down its progression, and also slows down the development of left ventricular dilatation. In left ventricular dysfunction, enalapril reduces the risk of major ischemic outcomes (including the incidence of myocardial infarction and the number of hospitalizations for unstable angina).Enalapril in patients with mild to moderate heart failure slows down its progression, and also slows down the development of left ventricular dilatation. In left ventricular dysfunction, enalapril reduces the risk of major ischemic outcomes (including the incidence of myocardial infarction and the number of hospitalizations for unstable angina).Enalapril in patients with mild to moderate heart failure slows down its progression, and also slows down the development of left ventricular dilatation. In left ventricular dysfunction, enalapril reduces the risk of major ischemic outcomes (including the incidence of myocardial infarction and the number of hospitalizations for unstable angina).

Pharmacokinetics

When taken orally, about 60% is absorbed from the gastrointestinal tract. Simultaneous food intake does not affect absorption. It is metabolized in the liver by hydrolysis with the formation of enalaprilat, due to the pharmacological activity of which the hypotensive effect is realized. Plasma protein binding of enalaprilat is 50-60%. T1 / 2 of enalaprilat is 11 hours and increases with renal failure. After oral administration, 60% of the dose is excreted by the kidneys (20% as enalapril, 40% as enalaprilat), 33% is excreted through the intestines (6% as enalapril, 27% as enalaprilat). After intravenous administration of enalaprilat, 100% is excreted by the kidneys unchanged.

Side effect

From the nervous system: dizziness, headache, tiredness, fatigue; very rarely when used in high doses - sleep disorders, nervousness, depression, imbalance, paresthesia, tinnitus. From the side of the cardiovascular system: orthostatic hypotension, fainting, palpitations, pain in the region of the heart; very rarely, when used in high doses, hot flashes. From the digestive system: nausea; rarely - dry mouth, abdominal pain, vomiting, diarrhea, constipation, abnormal liver function, increased activity of hepatic transaminases, increased concentration of bilirubin in the blood, hepatitis, pancreatitis; very rarely when used in high doses - glossitis. From the hematopoietic system: rarely - neutropenia; in patients with autoimmune diseases - agranulocytosis. From the urinary system:rarely - renal dysfunction, proteinuria. From the respiratory system: dry cough. On the part of the reproductive system: very rarely, when used in high doses, impotence. Dermatological reactions: very rarely, when used in high doses, hair loss. Allergic reactions: rarely - skin rash, Quincke's edema. Others: rarely - hyperkalemia, muscle cramps.

Application during pregnancy and lactation

Contraindicated in pregnancy. With the onset of pregnancy, enalapril should be discontinued immediately. Enalapril is excreted in breast milk. If necessary, its use during lactation should decide on the termination of breastfeeding.

Application for violations of liver function

Use with extreme caution in patients with impaired liver function.

Application in children

The safety and efficacy of enalapril in children have not been established.

special instructions

It is used with extreme caution in patients with autoimmune diseases, diabetes mellitus, liver dysfunction, severe aortic stenosis, subaortic muscle stenosis of unknown origin, hypertrophic cardiomyopathy, with loss of fluid and salts. In the case of previous treatment with saluretics, in particular in patients with chronic heart failure, the risk of orthostatic hypotension increases, therefore, before starting treatment with enalapril, it is necessary to compensate for the loss of fluid and salts. With long-term treatment with enalapril, it is necessary to periodically monitor the peripheral blood picture. Sudden discontinuation of enalapril does not cause a sharp increase in blood pressure. During surgical interventions during the treatment with enalapril, the development of arterial hypotension is possible,which should be corrected by the introduction of a sufficient amount of fluid. Before examining the function of the parathyroid glands, enalapril should be discontinued. Influence on the ability to drive vehicles and mechanisms Care must be taken when driving vehicles or performing other work that requires increased attention, because dizziness is possible, especially after taking the initial dose of enalapril.

Drug interactions

With simultaneous use with immunosuppressants, cytostatics, the risk of developing leukopenia increases. With the simultaneous use of potassium-sparing diuretics (including spironolactone, triamterene, amiloride), potassium preparations, salt substitutes and dietary supplements containing potassium, hyperkalemia may develop (especially in patients with impaired renal function), because ACE inhibitors reduce the content of aldosterone, which leads to a retention of potassium in the body against the background of limiting the excretion of potassium or its additional intake into the body. With the simultaneous use of opioid analgesics and anesthetics, the antihypertensive effect of enalapril is enhanced. With the simultaneous use of 'loop' diuretics, thiazide diuretics, the antihypertensive effect is enhanced. There is a risk of developing hypokalemia.Increased risk of renal impairment. With simultaneous use with azathioprine, anemia may develop, which is due to inhibition of the activity of erythropoietin under the influence of ACE inhibitors and azathioprine. A case of the development of anaphylactic reaction and myocardial infarction with the use of allopurinol in a patient receiving enalapril is described. Acetylsalicylic acid in high doses can reduce the antihypertensive effect of enalapril. It has not been definitively established whether acetylsalicylic acid reduces the therapeutic efficacy of ACE inhibitors in patients with coronary artery disease and heart failure. The nature of this interaction depends on the course of the disease. Acetylsalicylic acid, by inhibiting COX and prostaglandin synthesis, can cause vasoconstriction,which leads to a decrease in cardiac output and a worsening of the condition of patients with heart failure receiving ACE inhibitors. With the simultaneous use of beta-blockers, methyldopa, nitrates, calcium channel blockers, hydralazine, prazosin, an increase in the antihypertensive effect is possible. With simultaneous use with NSAIDs (including with indomethacin), the antihypertensive effect of enalapril decreases, apparently due to the inhibition of prostaglandin synthesis under the influence of NSAIDs (which are believed to play a role in the development of the hypotensive effect of ACE inhibitors). The risk of developing impaired renal function increases; hyperkalemia is rarely observed. With the simultaneous use of insulin, hypoglycemic agents, sulfonylurea derivatives, hypoglycemia may develop.With the simultaneous use of ACE inhibitors and interleukin-3, there is a risk of developing arterial hypotension. With simultaneous use with clozapine, there are reports of the development of syncope. With simultaneous use with clomipramine, an increase in the action of clomipramine and the development of toxic effects have been reported. With simultaneous use with co-trimoxazole, cases of the development of hyperkalemia have been described. With simultaneous use with lithium carbonate, the concentration of lithium in the blood serum increases, which is accompanied by symptoms of lithium intoxication. With simultaneous use with orlistat, the antihypertensive effect of enalapril decreases, which can lead to a significant increase in blood pressure, the development of a hypertensive crisis. It is believed that with simultaneous use with procainamide, an increase in the risk of developing leukopenia is possible.With simultaneous use with enalapril, the effect of drugs containing theophylline decreases. There have been reports of the development of acute renal failure in patients after kidney transplantation with simultaneous use with cyclosporine. With simultaneous use with cimetidine, T1 / 2 of enalapril increases and its concentration in blood plasma increases. It is believed that it is possible to reduce the effectiveness of antihypertensive drugs when used simultaneously with erythropoietins. With simultaneous use with ethanol, the risk of developing arterial hypotension increases.With simultaneous use with cimetidine, T1 / 2 of enalapril increases and its concentration in blood plasma increases. It is believed that it is possible to reduce the effectiveness of antihypertensive drugs when used simultaneously with erythropoietins. With simultaneous use with ethanol, the risk of developing arterial hypotension increases.With simultaneous use with cimetidine, T1 / 2 of enalapril increases and its concentration in blood plasma increases. It is believed that it is possible to reduce the effectiveness of antihypertensive drugs when used simultaneously with erythropoietins. With simultaneous use with ethanol, the risk of developing arterial hypotension increases.