Enap tablets 2, 5 mg 60 pcs. pack (enalapril)

Latin name

ENAP

Release form

Tablets are white or almost white, round, biconvex, with a bevel.



packaging 10 pcs - blisters (6) - packs of cardboard.

Pharmacological action

Antihypertensive drug, ACE inhibitor. The mechanism of action is associated with inhibition of ACE activity, which leads to a decrease in the formation of angiotensin II.

enalapril is a derivative of two amino acids:L-alanine and L-proline. After absorption, oral enalapril is hydrolyzed to enalalrylate, which inhibits ACE. The mechanism of its action is associated with a decrease in the formation of angiotensin I from angiotensin I, a decrease in the plasma content of which leads to an increase in the blood plasma renin activity (due to elimination of the negative reverse reaction to changes in renin production) and a decrease in aldosterone secretion. Since ACE is identical to the kininase II enzyme, enalapril can also block the destruction of bradykinin, a peptide that has a powerful vasopressor effect. The value of this effect in the mechanism of action of enalapril has not been fully established.

The antihypertensive effect of enalapril is associated primarily with the suppression of RAAS activity, which plays an important role in the regulation of blood pressure. Despite this, enalapril has an antihypertensive effect even in patients with arterial hypertension and a low concentration of renin.

Against the background of enalapril, the blood pressure level decreases regardless of the position of the body (both lying and standing) without a significant increase in heart rate. Symptomatic orthostatic hypotension is rare. In some patients, achieving optimal BP reduction may require several weeks of therapy. Abrupt abolition of enalapril was not accompanied by a rise in blood pressure.

Effective inhibition of ACE activity usually occurs 2-4 hours after a single oral administration of enalapril. The time of onset of antihypertensive action when taken orally is usually 1 hour, reaches a maximum in 4-6 hours. The duration of action depends on the dose. When used in recommended doses, the antihypertensive effect and hemodynamic effects are maintained for at least 24 hours.

In patients with essential hypertension, a decrease in blood pressure is accompanied by a decrease in heart rate and an increase in cardiac

output, while heart rate does not change or does not change significantly. Renal blood flow increases, but the glomerular filtration rate

does not change. However, in patients with an initially low glomerular filtration rate, its level usually increased.

In patients with diabetic / nondiabetic nephropathy, enuminapril decreased albuminuria / proteinuria and renal excretion of IgG by enalapril.

In patients with chronic heart failure (CHF) treated with cardiac glycosides and diuretics

, the use of enalapril is accompanied by a decrease in OPS and blood pressure, increased cardiac output, while reducing heart rate (usually in patients with chronic heart failure, heart rate is increased). The jamming pressure of the pulmonary capillaries is also reduced. With prolonged use, enalapril increases exercise tolerance and reduces the severity of heart failure (evaluated according to NYHA criteria). Enalapril in patients with mild to moderate heart failure slows its progression, as well as slows down the development of dilatation of the left ventricle. With left ventricular dysfunction, enalapril reduces the risk of developing major ischemic outcomes (including the incidence of myocardial infarction and the number of hospitalizations for unstable angina).

Indications

- essential hypertension

- chronic heart failure (as part of combination therapy)

- prevention of clinically severe heart failure in patients with asymptomatic left ventricular dysfunction (as part of combination therapy)

- prevention of coronary artery diseaseov with dysfunction of the left ventricle in order to reduce the incidence of myocardial infarction and reduce the frequency of hospitalizations for unstable angina.

Contraindications

- history of angioedema, associated with the use of ACE inhibitors

- hereditary Quincke's edema or idiopathic angioedema edema

- simultaneous use with aliskiren in patients with diabetes mellitus or impaired renal function (CC

- porphyria

- pregnancy

- lactation (breast) years (efficacy and safety have not been established)

- lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome

- hypersensitivity to enalapril and other components of eparata

- hypersensitivity to other ACE inhibitors.

Caution should be used in patients with bilateral renal artery stenosis or stenosis of a single kidney artery with primary hyperaldosteronism, hyperkalemia after kidney transplantation with aortic stenosis and / or mitral stenosis (with hemodynamic impairment), hypertrophic obstructive cardiomyopathy (GO) and with diarrhea, vomiting) with systemic diseases of the connective tissue (including scleroderma, systemic lupus erythematosus) coronary heart disease with inhibition of bone marrow hematopoiesis erebrovaskulyarnymi diseases (including in cerebrovascular insufficiency) diabetic kidney disease (proteinuria - more than 1 g / d) hepatic failure patients following a salt-restricted diet or being on hemodialysis concurrently with immunosuppressants and diuretics in elderly patients (over 65).

Use during pregnancy and lactation

The use of EnapВ®, like other ACE inhibitors, is not recommended in the first trimester of pregnancy. The use of ACE inhibitors, including EnapВ®, in the II and III trimesters of pregnancy is contraindicated.

Epidemiological data on the risk of teratogenic effects of ACE inhibitors during pregnancy do not allow the conclusion to be drawn. However, the likelihood of teratogenic effects cannot be ruled out. If necessary, the use of ACE inhibitors, the patient must be transferred to therapy with another antihypertensive drug with a proven safety profile for pregnant women.

When confirming pregnancy, EnapВ® should be discontinued as soon as possible.

Taking ACE inhibitors in the second and third trimesters of pregnancy can cause fetotoxic effects (impaired renal function, oligohydramnios, delayed ossification of the bones of the skull) and neonatal toxic effects (renal failure, arterial hypotension, hyperkalemia).

If the patient took an ACE inhibitor in the II and III trimesters of pregnancy, it is recommended to conduct an ultrasound of the kidneys and bones of the fetal skull.

In those rare cases where the use of an ACE inhibitor during pregnancy is considered necessary, periodic ultrasound should be performed to evaluate the amniotic fluid index. If oligohydramnion is detected during ultrasound, it is necessary to stop taking the drug. Patients and the doctor should be aware that oligohydramnios develops with irreversible damage to the fetus. If ACE inhibitors are used during pregnancy and the development of oligohydramnios is observed, then depending on the gestational age, a stress test, a non-stress test or determination of the biophysical profile of the fetus may be required to assess the functional state of the fetus.

Newborns whose mothers took ACE inhibitors during pregnancy should be monitored due to possible arterial hypotension. Enalapril, which crosses the placenta, can be partially removed from the blood circulation of the newborn using peritoneal dialysis, theoretically it can be removed by exchange blood transfusion.

Enalapril and enaprilat are determined in trace milk in breast milk, therefore, if it is necessary to use the drug EnapВ® during lactation, breast-feeding should be discontinued.

Composition

1 tab. enalapril maleate 2.5 mg

Excipients: sodium bicarbonate - 1.3 mg, lactose monohydrate - 64.9 mg, corn starch - 11.2 mg, hyprolose - 1.25 mg, talc - 3 mg, magnesium stearate - 0.85 mg.

Dosage and administration

The drug is taken orally, regardless of food intake, preferably at the same time of day. Tablets should be washed down with a small amount of liquid.

Arterial hypertension

The initial dose is 5 to 20 mg 1 time / day, depending on the severity of the arterial hypertension. In case of mild arterial hypertension, the recommended initial dose is 5-10 mg / day.

In patients with severe activation of RAAS (for example, with renovascular hypertension, loss of electrolytes and / or dehydration, decompensation of heart failure, or severe arterial hypertension), an excessive decrease in blood pressure at the beginning of treatment is possible. 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.

Prior diuretic therapy in high doses can lead to dehydration and an increased risk of developing arterial hypotension at the start of Enap® therapy with a recommended starting dose of 5 mg / day. Treatment with diuretics should be discontinued 2-3 days before the start of the use of Enap®. Caution should be exercised when using Enap®, monitor kidney function and serum potassium.

Typically, the maintenance dose is 20 mg 1 time / day.

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

Chronic heart failure and left ventricular dysfunction

The initial dose is 2.5 mg 1 time / day, and treatment should be started under close medical supervision.

Enap® for the treatment of heart failure can be used simultaneously with diuretics and / or beta-blockers, 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 - 20 mg / day, which is prescribed either once, or in 2 doses, depending on the tolerability of the drug. Dose selection is carried out within 2-4 weeks. The maximum daily dose is 40 mg in 2 divided doses.

Week Dose in mg / day

Week 1 1-3 days: 2.5 mg / day * in 1 dose

4-7 days: 5 mg / day in 2 doses

Week 2 10 mg in 1-2 doses

Week 3 and 4 20 mg in 1-2 doses

* Special precautions should be observed in patients with impaired renal function, taking diuretics.

Given the risk of developing arterial hypotension and renal failure (much less commonly observed), blood pressure and kidney function should be carefully monitored before and after the start of Enap®. In patients taking diuretics, the doses of the latter should be reduced, if possible, before starting the use of Enap®. 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 for discontinuation of the drug.

Impaired renal function

In patients with impaired renal function, increase the intervals between doses and / or reduce the dose of Enap®.

KK Initial daily dose of

from 80 ml / min to 30 ml / min 5 mg-10 mg

from 30 ml / min to 10 ml / min 2.5-5 mg

less than 10 ml / min 2.5 mg on dialysis days *

* 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

Elderly patients are more likely to have a more pronounced antihypertensive effect and a longer duration of the drug, which is associated with a decrease in the rate of excretion of enalapril, therefore, the recommended starting dose is 1.25 mg.

In elderly patients, the dose is selected depending on the function of the kidneys.

Side effects

Classification of the frequency of development of side effects (WHO): very often ( 1/10), often ( 1/100 and

From the hemopoietic system: infrequently - anemia (including aplastic and hemolytic), rarely - neutropenia, decreased hemoglobin and hematocrit, thrombocytopenia, agranulocytosis, inhibition of bone marrow hematopoiesis, pancytopenia, lymphadenopathy, and. metabolism: infrequently - hypoglycemia.

From the nervous system: very often - dizziness often - headache, depression infrequently - confusion, insomnia, drowsiness, paresthesia, increased irritability, wereting о rarely - change in the nature of dreams, sleep disturbances.

From the sensory organs: often - a change in taste perception is infrequent - tinnitus is very rare - blurred vision.

From the cardiovascular system: often - a pronounced decrease in blood pressure (including . orthostatic hypotension), syncope, chest pain, heart rhythm disturbances, angina pectoris infrequently - palpitations, myocardial infarction or stroke (due to a sharp decrease in blood pressure in patients at high risk) rarely - Raynaud's syndrome.

From the respiratory system: very often - cough infrequently - rhinorrhea, sore throat and hoarseness, bronchospasm / bronchial asthma rarely - shortness of breath, lung infiltrates, rhinitis, allergic alveolitis / eosinophilic pneumonia.

From the digestive system: very often - nausea often - diarrhea, abdominal pain, flatulence infrequently - ileitis, intestinal obstruction, pancreatitis, vomiting, constipation, anorexia, dry oral mucosa, peptic ulcer rarely - impaired liver and biliary function, hepatitis (hepatocellular or cholestatic), including liver necrosis, cholestatic jaundice, stomatitis / aphthous ulcers, glossitis is very rare - angioedema of the intestine.

From the skin: often - skin rash infrequently - increased sweating, skin itching, alopecia rarely - erythema multiforme, Stevens-Johnson syndrome, exfoliative dermatitis, toxic epidermal necrolysis, pemphigus, erythroderma.

A symptom complex has been described that may include fever, myalgia / myositis, arthralgia / arthritis, serositis, vasculitis, increased ESR, leukocytosis and eosinophilia, a positive test for antinuclear antibodies. Skin rashes, photosensitization reactions, or other skin manifestations may occur.

From the urinary system: infrequently - impaired renal function, proteinuria, renal failure rarely - oliguria.

From the reproductive system: infrequently - decreased potency rarely - gynecomastia.

From the musculoskeletal system: infrequently - muscle cramps.

From the laboratory side: often - hyperkalemia, increased serum creatinine concentration infrequently - hyponatremia, increased serum urea concentration rarely - increased liver transaminases and bilirubin concentration.

Allergic reactions: often - hypersensitivity reactions / angioedema of the face, lips, tongue, pharynx and / or larynx infrequently - skin itching, urticaria.

Other: frequency unknown - syndrome of inadequate secretion of ADH.

Adverse events identified during the post-marketing use of Enap®, but a causal relationship with the drug has not been established: urinary tract infections, upper respiratory tract infections, bronchitis, cardiac arrest, atrial fibrillation, herpes zoster, melena, ataxia, pulmonary embolism and pulmonary infarction, hemolytic anemia, including hemolysis in patients with glucose-6-phosphate dehydrogenase deficiency.

Drug Interaction

The risk of arterial hypotension, hyperkalemia, and renal dysfunction (including acute renal failure) is higher in the case of double RAAS blockade, ie. with the concomitant use of angiotensin II receptor antagonists, ACE inhibitors or aliskiren, compared with the use of one of the above groups. If necessary, the simultaneous use of drugs is recommended to control blood pressure, kidney function and water-electrolyte balance.

Concomitant use of enalapril with aliskiren in patients with diabetes mellitus or impaired renal function (AC

ACE inhibitors reduce potassium under the action of diuretics, concomitant use of enalapril, diuretic table salt, as well as the use of other drugs that help to increase the content of potassium in the blood plasma (eg, heparin) can lead to hyperkalemia. Simultaneously Osty Application ostorozhnost It should observe and regularly kontrolyrovat Contents serum potassium.

Predshestvuyuschaya diuretics in therapy High doses of lead can u k Reduction and Increase BCC line development arteryalnoy hypotension IN TIME beginning enalapril therapy. Excessive antihypertensive action can be reduced by abolishing diuretics, increasing water or table salt consumption, as well as providing low dose enalapril treatment.

The use of beta-blockers, alpha-blockers, ganglioblockers, methyldopa, slow calcium channel blockers, nitroglycerin, or other nitrates may further reduce BP when co-administered with enalapril.

A transient increase in serum lithium concentration and the development of lithium intoxication have been observed with the use of ACE inhibitors with lithium drugs. The use of thiazide diuretics may lead to an additional increase in serum lithium concentration and the risk of lithium intoxication with the use of ACE inhibitors. Concomitant use of enalapril with lithium is not recommended. When using such a combination, serum lithium concentrations should be carefully monitored.

The concomitant use of some anesthetics, tricyclic antidepressants and antipsychotics (antipsychotics) with ACE inhibitors can lead to a further decrease in blood pressure.

Concomitant administration of NSAIDs (including selective COX-2 inhibitors) may attenuate the antihypertensive effect of ACE inhibitors or angiotensin II receptor antagonists. NSAIDs and ACE inhibitors have an additive effect on increasing serum potassium, which can lead to reversible impairment of kidney function, especially in patients with existing renal impairment.

In rare cases, acute renal failure may occur, especially in patients with impaired renal function (e.g., in elderly patients or with severe hypovolemia, including against the use of diuretics). Before starting therapy, it is necessary to complete CCC. During treatment, it is recommended that kidney function be monitored.

Epidemiological studies suggest that the concomitant use of ACE inhibitors and hypoglycemic agents (insulin and hypoglycemic agents for oral administration) may increase the hypoglycemic effect with the risk of hypoglycemia. More often, hypoglycemia develops in the first weeks of therapy in patients with impaired renal function.

Ethanol enhances the antihypertensive effect of ACE inhibitors.

Sympathomimetics can reduce the antihypertensive effect of ACE inhibitors.

Safe co-administration of enalapril with acetylsalicylic acid (as an antiplatelet agent), thrombolytics and beta blockers.

Reduces the action of medicines containing theophylline.

Co-administration of allopurinol, cytostatics and immunosuppressants (including methotrexate, cyclophosphamide) with ACE inhibitors may increase the risk of leukopenia. When used with allopurinol, the risk of an allergic reaction is increased, especially in patients with impaired renal function.

Co-administration of cyclosporine with ACE inhibitors may increase the risk of hyperkalemia.

Antacids can reduce the bioavailability of ACE inhibitors.

When using ACE inhibitors, incl. enalapril, in patients receiving in / in gold preparations (sodium aurothiomalate), a symptom complex was included, including facial skin hyperemia, nausea, vomiting, arterial hypotension.

No clinically relevant pharmacokinetic interaction of enalapril with hydrochlorothiazide, furosemide, digoxin, timolol, methyldopa, warfarin, indomethacin, sulindac and cimetidine was observed.

When co-administered with propranolol, the concentration of enalaprilat in the serum is reduced, but this effect is clinically insignificant.

Overdose

Symptoms: after about 6 hours after ingestion - a pronounced decrease in blood pressure up to the development of collapse, impaired water-electrolyte balance, renal failure, hyperventilation, tachycardia, palpitations, bradycardia, bradycardia. Serum concentrations of enalaprilat in the blood plasma after administration of enalapril 300 mg and 440 mg in doses exceeded the usual therapeutic concentrations by 100 and 200 times, respectively.

Treatment: The patient should be moved to a horizontal position with a low head. In mild cases, gastric lavage and intake of activated charcoal are indicated in more serious cases - infusion of 0.9% sodium chloride solution, plasma substitutes, if necessary - in / in the introduction of catecholamines. It is possible to remove enalaprilat by hemodialysis, the elimination rate is 62 ml / min. Patients with bradycardia resistant to therapy are shown arrhythmia. Serum electrolyte content and serum creatinine concentration should be carefully monitored.

Storage conditions

The drug should be stored out of the reach of children, protected from moisture, at a temperature not exceeding 25 ° C.

Expiration

3 years.

Deystvuyuschee substances

enalapril

dosage form

dosage form

tablets

KRKA d.d. Novo mesto AO, Slovenia



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