Ednit - instructions for use, dose, side effects, contraindications

auxiliary substances: sodium hydroxide, silicon dioxide colloid, magnesium stearate,povidone, talc, crospovidone, microcrystalline cellulose, lactose monohydrate.

Description:

Tablets 2.5 mg Round flat white tablets with bevel. On the one side - risk, on the other - marking "ED 2.5".

Tablets 5 mg Round flat white tablets with bevel. On the one side - risk, on the other - marking "ED 5".

Tablets 10 mg Round flat white tablets with bevel. On the one side - risk, on the other - marking "ED 10".

Tablets 20 mg Round flat white tablets with bevel. On the one side - risk, on the other - marking "ED 20".

Pharmacotherapeutic group:inhibitor of angiotensin-converting enzyme (ACE).

ATX: & nbsp

C.09.A.A.02 Enalapril

Pharmacodynamics:

Ednit ® is an antihypertensive drug whose mechanism of action is associated with a decrease in the formation of angiotensin II from angiotensin I, a decrease in its content leads to a direct decrease in the release of aldosterone. This reduces the overall peripheral vascular resistance, systolic and diastolic blood pressure (BP), post- and prdnagruzka on the myocardium. Expands arteries more than veins, with a reflex increase in heart rate (heart rate) is not noted. Reduces the degradation of bradykinin.The hypotensive effect is more pronounced with high renin activity of blood plasma than normal or reduced its activity. Reduction of blood pressure within the therapeutic limits does not affect cerebral circulation, blood flow in the vessels of the brain is maintained at a sufficient level against the background of reduced pressure. Strengthens coronary and renal blood flow. With long-term use, myocardial hypertrophy of the left ventricle and myocytes of the walls of arteries of resistive type decrease, prevents the progression of heart failure and slows down the development of dilatation of the left ventricle. Improves the blood supply of the ischemic myocardium.

Reduces the aggregation of platelets. Lengthens life expectancy in patients with chronic heart failure, slows the progression of left ventricular dysfunction in patients who underwent myocardial infarction, without clinical manifestations of heart failure.

Has some diuretic effect. Reduces intramedular hypertension, slowing the development of glomerulosclerosis and the risk of chronic renal failure.

The time of onset of the hypotensive effect with ingestion is 1 hour, it reaches a maximum after 4-6 hours and lasts up to 24 hours.In some patients, in order to achieve optimal blood pressure, therapy is needed for several weeks. In chronic heart failure, a noticeable clinical effect is observed with long-term treatment - 6 months or more.

Pharmacokinetics:

After ingestion, 60% of the drug is absorbed. Eating does not affect the absorption of enalapril.

Enalapril binds up to 50% with plasma proteins. Is a "prodrug": enalapril It is rapidly metabolized in the liver, as a result of its hydrolysis, an active metabolite enalaprilate, which is a more active ACE inhibitor than enalapril. Bioavailability of the drug is 40%. The maximum concentration of enalapril in the blood plasma is achieved after 1 hour, enalaprilata - after 3-4 hours. Enalaprilat easily passes through the histohematological barriers, excluding the blood-brain barrier, a small amount penetrates the placenta and into the breast milk.

The half-life of enalaprilata is about 11 hours. enalapril mainly kidneys 60% (20% in the form of enalapril and 40% in the form of enalaprilata), through the intestine - 33% (6 % in the form of enalapril and 27 % in the form of enalaprilate).

It is removed during hemodialysis (rate 62 ml / min) and peritoneal dialysis.

Indications:

- arterial hypertension;

- chronic heart failure (as part of combination therapy);

- prevention of chronic heart failure in patients with asymptomatic dysfunction of the left ventricle.

Contraindications:

Hypersensitivity to enalapril and other ACE inhibitors, history of angioedema, associated with treatment with ACE inhibitors, and hereditary or idiopathic angioedema, porphyria, pregnancy, lactation, age under 18 (efficacy and safety not established), lactose intolerance , deficiency of lactase or glucose-galactose malabsorption (since the composition of the drug includes lactose).

Carefully:

Primary hyperaldosteronism, bilateral stenosis of the renal arteries, stenosis of the single kidney artery, hyperkalemia, condition after kidney transplantation, aortic stenosis, mitral stenosis (with hemodynamic disorders), idiopathic hypertrophic subaortic stenosis, systemic connective tissue diseases, coronary heart disease,cerebrovascular diseases, diabetes mellitus, renal insufficiency (proteinuria more than 1 g / day), liver failure, patients with a salt-limited or hemodialysis diet, simultaneous use with immunosuppressants and saluretic drugs, elderly patients (over 65), oppression of bone marrow hematopoiesis , conditions accompanied by a decrease in the volume of circulating blood (including diarrhea and vomiting).

Dosing and Administration:

Take inside regardless of the time of eating, squeezed with enough liquid.

At monotherapy of an arterial hypertensia the initial dose - 5 mg once a day. If there is no clinical effect, after 1-2 weeks the dose is increased by 5 mg. After taking the initial dose, patients should be under medical supervision for 2 hours and an additional 1 hour until blood pressure stabilizes. If necessary, and a fairly good tolerability dose can be increased to 40 mg per day for 1 -2 admission. After 2-3 weeks pass to a maintenance dose of 10-40 mg per day, divided into 1-2 doses. With a moderate degree of arterial hypertension, the average daily dose is about 10 mg. The maximum daily dose is 40 mg.

If Ednit® is given to patients who are concurrently receiving diuretics, treatment with a diuretic should be discontinued 2-3 days before the Ednit® product is used. If this is not possible, the initial dose of Ednit® should be 2.5 mg / day. Patients with hyponatremia (concentration of sodium ions in the serum of less than 130 mmol / l) or with an increase in creatinine concentration in the serum of more than 0.14 mmol / l appoint Ednit® at an initial dose of 2.5 mg once a day.

With Renovascular hypertension, the initial dose is 2.5 - 5 mg / day. The maximum daily dose is 20 mg.

In chronic heart failure, the initial dose of Ednit® is 2.5 mg once, then the dose is increased by 2.5 to 5 mg every 3-4 days according to the clinical response to the maximum tolerated dose (depending on blood pressure), but not above 40 mg / day once or in 2 divided doses. In patients with low systolic blood pressure (less than 110 mm Hg), therapy should be started at a dose of 1.25 mg / day (1/2 tablet 2.5 mg). Selection of the dose should be carried out within 2-4 weeks or if necessary and the opportunity in a shorter time. The average maintenance dose is 5-20 mg / day for 1-2 doses.In elderly people, the more pronounced hypotensive effect and lengthening of the duration of the Ednit® action are more frequent, which is associated with a decrease in the elimination rate of the drug, therefore the recommended initial dose for elderly patients is 1.25 mg / day.

To prevent the development of chronic heart failure with asymptomatic violation of the function of the left ventricle - 2.5 mg 2 times a day. The dose is selected taking into account the tolerability up to 20 mg / day, divided into 2 doses.

In chronic renal failure, cumulation of enalapril occurs with a decrease in filtration of less than 10 ml / min. When creatinine clearance (CC) is 80-30 ml / min, the dose of Ednit® should be 5-10 mg / day, with a decrease in QC to 30-10 ml / min., 2.5-5 mg / day, with a QC less than 10 ml / min - 1,25-2,5 mg / day only on dialysis days.

The duration of treatment depends on the effectiveness of therapy. With too pronounced decrease in blood pressure, the dose of Ednit® is gradually reduced.

The drug is used in both monotherapy and in combination with. other antihypertensive agents.

Side effects:

From the cardiovascular system: excessive decrease in blood pressure, orthostatic collapse; rarely - chest pain, stenocardia,myocardial infarction or stroke (usually associated with a pronounced decrease in blood pressure); extremely rare - arrhythmia (atrial or bradi- tachycardia, atrial fibrillation), palpitations, thromboembolism of pulmonary artery branches, Raynaud's syndrome.

From the central nervous system: dizziness, headache, fatigue, insomnia, anxiety, confusion, fatigue, sleepiness (2-3%); very rarely with high doses - nervousness, depression, paresthesia.

From the sense organs: disturbance of balance, hearing and vision impairment, tinnitus.

From the digestive system: dry mouth, anorexia, dyspeptic disorders (nausea, diarrhea or constipation, vomiting, abdominal pain), ileus, pancreatitis, liver dysfunction and biliary excretion, hepatitis (hepatocellular or cholestatic), jaundice, very rarely - stomatitis, glossitis.

From the respiratory system: nonproductive dry cough, sore throat, hoarseness, pulmonary infiltrates, interstitial pneumonitis, bronchospasm, dyspnea, rhinorrhea, pharyngitis.

Allergic reactions: skin rash, angioneurotic edema of the face, extremities, lips, tongue,a glottis and / or a larynx; very rarely - polymorphic erythema, exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, pemphigus, pruritus, urticaria, photosensitivity, serositis, vasculitis, myositis, arthralgia, arthritis, intestinal angioedema.

From the laboratory indicators: hyperkreatininemia, increased urea levels, increased activity of "hepatic" enzymes, hyperbilirubinemia, hyperkalemia, hyponatremia, hypoglycemia in patients with diabetes mellitus taking hypoglycemic agents for ingestion or insulin.

In some cases, a decrease in the concentration of hemoglobin and hematocrit, an increase in the rate of erythrocyte sedimentation (ESR), thrombocytopenia, neutropenia, agranulocytosis (in patients with autoimmune diseases), eosinophilia are noted.

From the urinary system: impaired renal function; rarely - proteinuria. Other: alopecia, decreased libido, impotence, "hot flashes".

Overdose:

Symptoms: a marked decrease in blood pressure up to the development of collapse, myocardial infarction, acute impairment of cerebral circulation or thromboembolic complications; convulsions, stupor. Treatment: patient is transferred to a horizontal position with a low headboard.In mild cases, gastric lavage and ingestion of saline are indicated. In more severe cases, measures aimed at stabilizing blood pressure are recommended: intravenous administration of 0.9% sodium chloride solution, plasma substitutes, and if necessary - angiotensin II, hemodialysis (enalapril removal rate averages 62 ml / min).

Interaction:

With simultaneous application of Ednit® with non-steroidal anti-inflammatory drugs (NSAIDs), including selective inhibitors of cyclooxygenase-2 (COX-2), hypotensive effect can be reduced; with potassium-sparing diuretics (spironolactone, triamterene, amiloride) can lead to hyperkalemia; with lithium salts - to slowing the excretion of lithium in the blood plasma (control of the concentration of lithium in blood plasma is shown). .

In some patients with impaired renal function and takingyusttheir HPVP, including, COX-2 inhibitors, concomitant use of ACE inhibitors may lead to further impairment of kidney function. These changes are reversible.

Simultaneous administration of Ednit® with NSAIDs may decrease the effectiveness of the drug. Enalapril weakens the effect of medicines containing theophylline.

The hypotensive effect of enalapril is enhanced by diuretics, beta-blockers, methyldopa, nitrates, blockers of "slow" calcium channels, hydralazine, prazozin. Immunosuppressants, allopurinol, cytotoxic drugs increase hematotoxicity.

Drugs that cause bone marrow depression, increase the risk of developing neutropenia and / or agranulocytosis up to death.

The combined use of ACE inhibitors and hypoglycemic agents (insulin, hypoglycemic agents for prima) can enhance the hypoglycemic effect of the latter with the risk of developing hypoglycemia. This is most often observed during the first weeks of joint use, as well as in patients with renal insufficiency. In patients with diabetes, who take hypoglycemic agents for ingestion and insulin, blood glucose control is necessary, especially during the first month of joint use with ACE inhibitors.

Symptomocomplex, which includes red face, nausea, vomiting and arterial hypotension,is described in rare cases when the gold preparation is used for intravenous administration (sodium aurotomy malate) and ACE inhibitors (enalapril).

Special instructions:

Caution should be exercised when prescribing patients with reduced circulating blood volume (as a result of diuretic therapy, limiting intake of salt, hemodialysis, diarrhea and vomiting) - the risk of a sudden and severe decrease in blood pressure after applying even an initial dose of an ACE inhibitor is increased. Transient arterial hypotension is not a contraindication for the continuation of treatment with the drug after stabilization of blood pressure, in the case of a repeated expressed decrease in blood pressure should reduce the dose or cancel the drug.

With the development of excessive reduction in blood pressure, the patient is transferred to a horizontal position with a low headboard, if necessary, 0.9% sodium chloride solution and plasma-substituting drugs are administered.

The use of high-flow dialysis membranes increases the risk of developing an anaphylactic reaction. Correction of the dosing regimen on days free from dialysis should be performed depending on the blood pressure.

Before and after treatment with ACE inhibitors, control of blood pressure, blood counts (hemoglobin, potassium, creatinine, urea, activity of "hepatic" enzymes), protein concentration in the urine is necessary.

It should be carefully monitored for patients with severe heart failure, coronary heart disease and cerebrovascular disease, in which a sharp decrease in blood pressure can lead to myocardial infarction, stroke, or renal dysfunction. Sudden abolition of treatment does not lead to the syndrome of "withdrawal" (a sharp rise in blood pressure).

Patients with a history of angioedema have an increased risk of developing it with ACE inhibitors.

For newborns and infants who have undergone intrauterine exposure to ACE inhibitors, careful monitoring is recommended to timely detect a marked decrease in blood pressure, oliguria, hyperkalemia and neurological disorders, possibly due to a decrease in renal and cerebral blood flow with a decrease in blood pressure caused by ACE inhibitors. In oliguria it is necessary to maintain blood pressure and renal perfusion by introducing appropriate fluids and vasoconstrictive drugs.

In patients with reduced renal function, a single dose should be reduced or intervals between doses should be increased.

Before the study of the function of parathyroid glands Ednit® should be canceled.

During the period of treatment it is not recommended to drink alcoholic beverages, since alcohol enhances the hypotensive effect of the drug.

Caution should be exercised when performing physical exercises in hot weather (risk of dehydration and excessive blood pressure lowering due to decreased circulating blood volume).

Before surgery (including dentistry), it is necessary to alert the surgeon / anesthesiologist about the use of ACE inhibitors.

Effect on the ability to drive transp. cf. and fur:When there are side effects from the central nervous system, it is not recommended to drive vehicles, as well as performing work associated with an increased risk

Form release / dosage:

Tablets, 2.5 mg, 5 mg, 10 mg, 20 mg

Packaging:

10 tablets in a blister of AL/ PA / PVC and aluminum foil. 2 blisters with instructions for use in a cardboard bundle.

Storage conditions:

List B.

At a temperature of no higher than 25 ° C. Keep out of the reach of children!

Shelf life:

3 years

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N012649 / 01

Date of registration:02.06.2010

The owner of the registration certificate:GEDEON RICHTER, OJSC GEDEON RICHTER, OJSC Hungary

Manufacturer: & nbsp

GEDEON RICHTER OJSC Hungary

Representation: & nbspGEDEON RICHTER OJSC GEDEON RICHTER OJSC Hungary

Information update date: & nbsp21.10.2015

Illustrated instructions

Instructions

Ednit® (Ednyt®)