Enalapril Hexal tablets 10 mg 50 pcs. (enalapril)

Packaging

50 pcs

Pharmacological action of

ATX code: C09AA02

Pharmacological properties of

Pharmacodynamics

Enalapril - an angiotensin converting enzyme (ACE) inhibitor, used to treat arterial hypertension, heart failure, diabetic nephropathy. The clinical effect of enalapril is due to the suppression of ACE activity and, as a consequence, a decrease in the formation of angiotensin II from angiotensin I in tissues and circulating blood. A decrease in the concentration of angiotensin II, in turn, leads to vasodilation, a decrease in the secretion of aldosterone, an increase in the potassium content and the concentration of renin in blood plasma.

The hemodynamic consequences of these changes are a decrease in total peripheral vascular resistance (OPSS), systolic and diastolic blood pressure, increased cardiac output, decreased post-and preload on the myocardium. Enalapril expands arteries more than veins, however, there is no reflex increase in heart rate (HR). Reduces the degradation of bradykinin, increases the synthesis of prostaglandins. The antihypertensive effect is more pronounced with a high concentration of renin than with a normal or reduced level. The time of onset of the antihypertensive effect when taken orally is 1 hour, which reaches a maximum after 4-6 hours and lasts up to 24 hours.

Some patients require therapy for several weeks to achieve optimal blood pressure (BP). In chronic heart failure, a noticeable clinical effect is observed with prolonged treatment - 6 months or more. The duration of the therapeutic effect is dose-dependent.

The vasodilating and some diuretic effect of enalapril are also provided by the blockade of the destruction of bradykinin, which, in turn, stimulates the synthesis of vasodilating and renal prostaglandins. An increase in the content of bradykinin both in blood plasma and locally in the organs and tissues of the body blocks the pathological processes that occur in chronic heart failure in the myocardium, kidneys, and smooth muscles of blood vessels. At the same time, there is an increase in coronary and renal blood flow, with prolonged use (from 3-4 weeks of treatment), left ventricular hypertrophy and myofibrils of the arterial wall walls decrease in resistance, dilatation of the left ventricle slows down and blood supply to the ischemic myocardium improves, metabolism improves and the incidence of arrhythmias noted after restoration of blood supply to the heart muscle.

Due to the moderate diuretic effect of the drug, intracranial hypertension is reduced, the development of glomerulosclerosis slows down and the risk of chronic renal failure decreases.

A decrease in blood pressure within the therapeutic range (not lower than 110/60 mm Hg) does not affect cerebral circulation: blood flow to the brain is maintained at a good level and against a background of low blood pressure.

Sudden cancellation of treatment does not lead to a "withdrawal" syndrome (a sharp increase in blood pressure).

Enalapril does not cause metabolic disorders, does not affect glucose metabolism, does not increase the concentration of uric acid, does not change the profile of blood lipoproteins. Enalapril may reduce the hypokalemic effect of thiazide diuretics.

Pharmacokinetics

Absorption

When taken orally, enalapril is rapidly absorbed, the maximum plasma concentration is reached within 1 hour.

Enalapril is well absorbed from the gastrointestinal tract (GIT), within 1 hour (maximum 4-8 hours) after oral administration, a therapeutic effect is achieved. Eating does not affect the absorption of the drug.

Distribution of

In patients with normal renal function, the equilibrium concentration of enalapril in blood plasma is reached 2-3 days after the start of administration. Does not cumulate. Communication with blood plasma proteins is about 50%.

Excretion of

It undergoes biotransformation in the liver with the formation of an active metabolite - enalaprilat, the maximum concentration of which is determined 4 hours after administration. Enalapril is excreted mainly through the kidneys - 60% (20% - as enalapril and 40% - as enalaprilat), through the intestines - 33% (6% - as enalapril and 27% - as enalaprilat). The half-life (T1 / 2) is 11 hours.

In patients with creatinine clearance (CC) of less than 30 ml / min, T1 / 2 of enalapril is increased. Decreased renal secretion of enalapril may increase hydrolysis to enalaprilat and increase extrarenal excretion of the drug.

Enalapril hydrolysis rate may decrease in patients with impaired liver function without reducing the therapeutic effect.

Crosses the placental barrier. Excreted in breast milk. Almost does not penetrate the blood-brain barrier. It does not accumulate in any tissues and organs.

Indications

arterial hypertension

chronic heart failure (as part of combination therapy)

prevention of the development of clinically severe heart failure in patients with asymptomatic dysfunction of the left ventricle (as part of combination therapy).

Special instructions

Use with extreme caution in patients with autoimmune diseases, diabetes mellitus, impaired liver function, 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 developing orthostatic hypotension is increased, therefore, before starting treatment with enalapril, it is necessary to compensate for the loss of fluid and salts.

With prolonged treatment with enalapril, it is necessary to periodically monitor the picture of peripheral blood. The sudden cessation 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.

Composition

1 tablet contains:

active substance: enalapril maleate 5.0 mg / 10.0 mg / 20.0 mg excipients: sodium bicarbonate 2.6 mg / 5.1 mg / 10.2 mg lactose monohydrate 129 , 8 mg / 124.6 mg / 117.8 mg corn starch 22.4 mg / 21.4 mg / 13.9 mg talc 6.0 mg / 6.0 mg / 6.0 mg hyprolose 2.5 mg / - / - magnesium stearate 1.7 mg / 1.7 mg / 1.7 mg iron oxide red - / 1.2 mg / 0.1 mg iron oxide yellow - / - / 0.3 mg.

Dosage and Administration

Enalapril Hexal is administered orally, regardless of food intake, it is necessary to drink plenty of fluids. Treatment with Enalapril Hexal is carried out for a long time. The dose of the drug should be adjusted in accordance with the patient's condition.

The drug Enalapril Hexal should be taken at the same time of the day, usually in the morning, but the drug Enalapril Hexal can be divided into two doses.

Following the first dose, patient monitoring and regular measurement of blood pressure over the next few hours is recommended. If there is a high risk of developing arterial hypotension, then such a patient should be given the first dose of Enalapril Hexal in a medical institution and observe the patient for at least 5 hours. During observation, the patient should be in the “lying” position.

If you skip taking the next dose of Enalapril Hexal, you must take the missed dose as soon as possible. If the time is approaching the next dose of Enalapril Hexal, you should skip the forgotten dose and take the next dose on time. In no case should you double the dose.

The dosage regimen is selected individually.

Side effects

According to the World Health Organization (WHO), unwanted effects are classified according to their frequency of development as follows: very often (? 1/10), often (from? 1/100 to <1/10), infrequently (from? 1 / 1,000 to <1/100), rarely (from? 1 / 10,000 to <1 / 1,000), very rarely ( <1 / 10,000) the frequency is unknown - according to the available data, establish the frequency of occurrence without representing moose is possible.

From the cardiovascular system

very often: dizziness

often: marked decrease in blood pressure (including orthostatic), syncope, pain in the chest, arrhythmia, tachycardia,

angina pectoris infrequently: palpitations, myocardial infarction, stroke, including secondary after the development of severe hypotension

rarely: thromboembolism of the branch of the pulmonary artery, Raynaud's syndrome.

From the central nervous system

often: headache, depression

infrequently: dizziness, drowsiness, insomnia, irritability, confusion, paresthesia, vertigo

rarely: unusual dreams, sleep disturbance.

From the respiratory system

very often: cough

often: shortness of breath

infrequently: rhinorrhea, sore throat, hoarseness, bronchospasm (bronchial asthma)

rarely: infiltration in the lungs, rhinitis, allergic alveolitis, (eosinophilic).

From the digestive system

very often: nausea

often: diarrhea, abdominal pain, taste disorder

infrequent: intestinal obstruction, pancreatitis, vomiting, dyspepsia, constipation, anorexia, peptic ulcer, dry oral mucosa, irritable bowel syndrome

rare: stomatitis / aphthous ulcers, glossitis, liver failure, hepatitis (hepatitis) ( , cholestasis, jaundice, an increase in the activity of “hepatic” transaminases and bilirubin in the blood plasma

is very rare: intestinal angioedema.

From the genitourinary system

infrequently: impaired renal function, renal failure, proteinuria, impotence, an increase in the concentration of urea in the blood plasma

rarely: oliguria, gynecomastia.

On the part of the organ of vision

very often: visual impairment.

On the part of the hematopoietic system and lymphatic system

infrequently: anemia (including aplastic, hemolytic)

rare: neutropenia, thrombocytopenia, agranulocytosis, inhibition of bone marrow hematopoiesis, pancytopenia, decreased hemoglobin, decreased hematocrit, lymphadenopathy, autoimmune diseases.

From the endocrine system

, frequency is unknown: syndrome of inadequate secretion of antidiuretic hormone.

Allergic reactions

often: urticaria, skin rash, exanthema, hypersensitivity reactions / angioedema (angioedema of the face, limbs, lips, tongue, pharynx and / or larynx is described)

infrequently: increased sweating, sore skin, itching, rarely: erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), exfoliative dermatitis, pemphigus, erythroderma.

A symptom complex is described, which may include fever, myalgia and arthralgia, serositis, vasculitis, increased erythrocyte sedimentation rate, leukocytosis and eosinophilia, skin rash, positive test for antinuclear antibodies. A symptom complex is also described, which includes hyperemia of the skin of the face, nausea, vomiting, and arterial hypotension and can develop with the simultaneous use of ACE inhibitors and gold preparations (sodium aurothiomalate) intravenously.

Other

very common: asthenia

often: fatigue, hyperkalemia, increased creatinine in the blood increased blood urea concentration.

Drug Interactions

The simultaneous use of ACE inhibitors with other agents acting on the renin-angiotensin-aldosterone system (RAAS) increases the risk of hypotension, hyperkalemia and impaired renal function (including acute renal failure).

As with other ACE inhibitors and angiotensin II receptor antagonists, the combined use of enalapril and aliskiren is contraindicated in patients with diabetes mellitus or renal failure (CC less than 60 ml / min).

Mutual enhancement of action while the use of enalapril with other antihypertensives.

Concomitant use with nitroglycerin or other nitrates, or other vasodilators, tricyclic antidepressants, antipsychotics, general anesthetics, narcotic drugs leads to an increase in the antihypertensive effect.

With the simultaneous use of enalapril with diuretics (thiazide or "loop" diuretics), an increase in the antihypertensive effect is possible. The simultaneous use of enalapril and potassium-sparing diuretics (such as spironolactone, eplerenone, triamteren, amiloride), potassium preparations or potassium-containing substitutes for edible salt, as well as the use of other drugs that increase the potassium content in blood plasma (for example, heparin) are not recommended.

The simultaneous use of non-steroidal anti-inflammatory drugs (NSAIDs) (including selective cyclooxygenase-2 inhibitors (COX-2)) can weaken the antihypertensive effect of antihypertensive drugs, due to an increase in potassium in the blood plasma, which leads to a reversible impairment of renal function, fluid retention. Thus, the antihypertensive effect of angiotensin II receptor antagonists or ACE inhibitors can be attenuated by NSAIDs, including COX-2 inhibitors.

NSAIDs and ACE inhibitors have an additive effect on increasing serum potassium, which can lead to impaired renal function, especially in patients with impaired renal function. This effect is reversible. Joint use should be carried out with caution in patients with impaired renal function.

The simultaneous use of enalapril and lithium preparations is not recommended, since the concentration of lithium in the blood plasma increases and, accordingly, there is an increase in its toxic effects. With the simultaneous use of enalapril and lithium preparations, it is necessary to control the concentration of lithium in the blood plasma.

Concomitant use with thiazide diuretics leads to an increase in the concentration of lithium salts in blood plasma.

With the simultaneous use of enalapril with gold preparations for parenteral administration (sodium aurothiomalate), a symptom complex may occur, including facial flushing, nausea, vomiting, arterial hypotension.

Reduces the effects of theophylline-containing drugs.

Concomitant use with insulin and hypoglycemic agents for oral administration increases the risk of hypoglycemia.

Immunosuppressants, allopurinol, cytostatics enhance hematotoxicity.

Medications that inhibit bone marrow function, increase the risk of neutropenia and / or agranulocytosis.

Ethanol enhances the antihypertensive effect of enalapril.

Enalapril can be used simultaneously with acetylsalicylic acid (as an antiplatelet agent), thrombolytics and -adrenergic blockers. Concomitant use with other ACE inhibitors may increase the risk of hyperkalemia. Antacids may decrease the bioavailability of ACE inhibitors. Sympathomimetics may reduce the antihypertensive effect of ACE inhibitors.

Overdose

Symptoms: headachele, pronounced decrease in blood pressure, up to the development of collapse, myocardial infarction, acute disorders of cerebral circulation or thromboembolic complications, convulsions, stupor, tachycardia, palpitations, dizziness, bradycardia, palpitations, renal failure.

Treatment: symptomatic. The patient is placed in a low head position. In mild cases, gastric lavage and intake of activated charcoal are shown, in more severe cases, measures aimed at stabilizing blood pressure: intravenous administration of 0.9% sodium chloride solution, plasma substitutes, connection of artificial rhythm driver with bradycardia-resistant (drug-induced bradycardia) elimination of enalapril averages 62 ml / min).

Storage Conditions

List B. Keep dry, out of reach of children at a temperature of 15 to 25 ° C.

Shelf life

3 years.

Deystvuyushtee substance

Эnalapril

Terms and conditions

prescription

dosage form

tablets

Possible product names

enalapril hexal tablets 10 mg 50 pcs.

Salyutas Pharma GmbH, Switzerland



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