Enam - instructions for use, doses, side effects, contraindications

Description:white or almost white round tablets with bevelled edges, embossed with "EMT" on one side and number "2.5" or "5", or "10" or "20" and the dividing risk on the other side.

Pharmacotherapeutic group:Angiotensin-converting enzyme (ACE) inhibitor.

ATX: & nbsp

C.09.A.A.02 Enalapril

Pharmacodynamics:

Enam® belongs to the group of ACE inhibitors, it has an antihypertensive effect, the development mechanism of which is associated with a decrease in the formation of angiotensin II from angiotensin I, a decrease in its concentration leads to a direct decrease in the secretion of aldosterone. This reduces the overall peripheral resistance of blood vessels, systolic and diastolic blood pressure (BP), post- and preload on the myocardium. Expands arteries more than veins, with a reflex increase in the number of cardiac contractions is not noted. Reduces the degradation of bradykinin, increases the synthesis of prostaglandins. The hypotensive effect is more pronounced with a high plasma renin concentration than with normal or reduced plasma renin.

Decrease in 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 and against a background of reduced blood pressure. Strengthens coronary and renal blood flow. With prolonged use, hypertrophy of the left ventricle of the heart decreases. Reduces the tone of the walls of arteries of resistive type. Prevents the progression of chronic heart failure (CHF), slows the development of dilatation of the left ventricle, inhibits the development of diabetic nephropathy. Improves the blood supply of the ischemic myocardium.

Reduces the aggregation of platelets. Reduces the duration of life in patients with CHF, slows the progression of left ventricular dysfunction in patients with myocardial infarction, without clinical manifestations of heart failure.Has some diuretic effect. Reduces intra-cerebral hypertension, slowing the development of glomerulosclerosis and the risk of chronic renal failure.

Pharmacological activity is formed by the hydrolysis metabolite enalapril - enalaprilate, which inhibits ACE.

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. Some patients need therapy for several weeks to achieve the optimal level of blood pressure. With CHF, a noticeable clinical effect is observed with long-term treatment - 6 months. and more.

Pharmacokinetics:

After ingestion, absorption is 60%. Eating does not affect absorption. In the liver is metabolized to form an active metabolite of enalaprilat, which is a more effective ACE inhibitor than enalapril. The connection with plasma proteins enalaprilata - 50-60%. Time to reach the maximum concentration (Teshah) of enalapril - 1 h, enalaprilat - 3-4 hours. Equilibrium concentration of the drug (Css) in plasma is achieved after 4 days. Enalaprilat easily passes through the histohematological barriers, excluding the blood-brain barrier, a small amount penetrates through the placenta and into breast milk.

The half-life (T1 / 2) of enalaprilate -11h. It is excreted mainly by the kidneys

- 60% (20% in the form of enalapril and 40% in the form of enalaprilate), 33% through the intestine (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:

Various forms of hypertension, including renovascular hypertension. Enam is effective in chronic heart failure (as part of combination therapy).

Contraindications:

- Hypersensitivity to enalapril or other ACE inhibitors.

- Pregnancy and lactation.

- Angioedema with a history of therapy with ACE inhibitors, hereditary or idiopathic angioedema.

- Age to 18 years (effectiveness and safety not established).

Carefully:

Aortic stenosis, cerebrovascular diseases (including cerebrovascular insufficiency), ischemic heart disease, coronary insufficiency, severe autoimmune systemic connective tissue disease (including systemic lupus erythematosus, scleroderma), inhibition of bone marrow hematopoiesis, diabetes mellitus, hyperkalaemia, bilateral stenosis of the renal arteries, artery stenosis of a single kidney, condition after kidney transplantation, renal and / or liver failure, sodium restricted diet , A condition associated with decreased blood volume (including diarrhea, vomiting),primary aldosteronism, advanced age.

Dosing and Administration:

Inside, regardless of food intake.

With monotherapy of hypertension - the initial dose of 5 mg once a day. In the absence of effect after 1-2 weeks, the dose is increased by 5 mg. After the initial dose, patients should be under medical supervision for 2 hours and an additional 1 hour until BP stabilizes. If necessary, and a sufficiently good tolerability dose can be increased to 40 mg / day for 1-2 doses. After 2-3 weeks pass to the maintenance dose - 10-40 mg / day, divided into 1-2 admission. With moderate hypertension, the average daily dose is about 10 mg. The maximum daily dose of the drug is 40 mg.

If Enam is prescribed to patients receiving diuretics, the diuretic should be discontinued 2-3 days before the drug is prescribed. If this is not possible, then the initial dose of Enam should be 2.5 mg / day.

Patients with hyponatraemia (the concentration of sodium in the serum is less than 130 mmol / l) or the concentration of serum creatinine in excess of 0.14 mmol / l, the initial dose is 2.5 mg once a day.

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

When chronic heart failure the initial dose is 2.5 mg once, then the dose is increased by 2.5-5 mg every 3-4 days according to the clinical response to the maximum tolerated dose (depending on blood pressure), but not more than 40 mg / day, once , or in 2 admission. In patients with low systolic pressure (less than 110 mm Hg), therapy should be started with a dose of 1.25 mg. The dose should be selected within 2-4 weeks or in shorter terms. The average maintenance dose is 5-20 mg / day for 1-2 doses.

When chronic renal failure cumulation occurs with a decrease in filtration of less than 10 ml / min. When creatinine is cleared 80-30 ml / min, the dose is usually 5-10 mg / day, the creatinine clearance of 30-10 ml / min is 2.5-5 mg / day, 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 the drug is gradually reduced.

Side effects:

From the cardiovascular system: excessive reduction in blood pressure, orthostatic collapse, rarely - chest pain, angina pectoris, myocardial infarction (usually associated with marked decrease in blood pressure), arrhythmias (atrial brady or tachycardia, atrial fibrillation), palpitation, thromboembolism of the pulmonary artery branches.

From the digestive system: dry mouth, decreased appetite, dyspeptic disorders (nausea, diarrhea or constipation, vomiting, abdominal pain), intestinal obstruction, pancreatitis, impaired liver function and bile secretion, hepatitis, jaundice.

From the respiratory system: unproductive "dry" cough, interstitial pneumonitis, bronchospasm, dyspnea, rhinorrhea, pharyngitis.

From the nervous system: dizziness, fainting, headache, weakness, insomnia, paresthesia, anxiety, depression, confusion, increased fatigue, drowsiness (2-3%), very rarely when used in high doses - nervousness, depression, paresthesia.

From the sense organs: disturbances of the vestibular apparatus, hearing and vision impairment, tinnitus.

Allergic reactions: skin rash, angioedema, facial edema, extremities, lips, tongue, glottis and / or throat, dysphonia, exfoliative dermatitis,

multiforme exudative erythema (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), pemphigus (pemphigus), itching, urticaria, photosensitivity, serositis, vasculitis, myositis, arthralgia, arthritis,stomatitis, glossitis. Very rarely - angioedema, edema of the gastrointestinal tract (including intestinal edema).

From the laboratory indicators: hyperkreatininemia, increased urea concentration, increased activity of "hepatic" transaminases, hyperbilirubinemia, hyperkalemia, hyponatremia, decreased hemoglobin and hematocrit, increased erythrocyte sedimentation rate, thrombocytopenia, neutropenia, agranulocytosis (in patients with autoimmune diseases), eosinophilia. There have been reports of cases of hypoglycemia in patients with diabetes who took insulin and oral hypoglycemic medications.

From the urinary system: impaired renal function, proteinuria. Other: alopecia, decreased libido, "flushes" of blood to the face.

Overdose:

Symptoms: excessive reduction of blood pressure, up to the development of collapse, myocardial infarction, acute cerebrovascular accident 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 shown,in more serious cases - measures aimed at stabilizing blood pressure: intravenous injection of 0.9% sodium chloride solution, plasma substitutes, if necessary - intravenous angiotensin II, hemodialysis (enalaprilate removal rate - 62 ml / min).

Interaction:

Strengthens the action of ethanol, slows the excretion of lithium.

Weaken the effect of medicines containing theophylline.

Hypotensive action reduces non-steroidal anti-inflammatory drugs, estrogens; strengthen - diuretics, other antihypertensive drugs (beta-blockers, methyldopa, nitrates, slow calcium channel blockers (BCCC), hydralazine, prazozin), medicines for general anesthesia, ethanol. Potassium-sparing diuretics and potassium-containing medicines increase the risk of hyperkalemia.

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

Immunosuppressants, allopurinol, cytotoxic drugs increase hematotoxicity.

With simultaneous use of ACE inhibitors and preparations of gold (sodium aurotomy malate) describes a symptom complex, which includes facial flushing, nausea, vomiting and lowering blood pressure.

Simultaneous reception with insulin and oral hypoglycemic drugs increases the risk of developing hypoglycemia.

Special instructions:

Caution should be exercised in appointing patients with reduced circulating blood volume (BCC) resulting from diuretic therapy, while limiting consumption of table salt, hemodialysis, diarrhea and vomiting, as the risk of a sudden and severe decrease in blood pressure after applying even an initial dose of an ACE inhibitor is increased. Transient hypotension is not a contraindication for continuing treatment with the drug after stabilizing blood pressure. In the case of a re-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 of dialysis, should be carried out depending on the level of blood pressure.

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

It should be carefully monitored for patients with decompensated CHF, coronary heart disease and cerebrovascular diseases, 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 an indication of angioedema development in the anamnesis have an increased risk of its development with the administration of ACE inhibitors.

For newborns and infants who have been exposed to the intrauterine effect of ACE inhibitors, careful monitoring is recommended to timely detect a marked decrease in blood pressure, oliguria, hyperkalemia and neurological disorders, possibly due to a reduction 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 impaired renal function, single dose should be reduced or intervals between enalapril intake increased.

Before the study of parathyroid gland functions enalapril should be canceled. Care should be taken when doing physical exercises or in hot weather (the risk of dehydration and excessive blood pressure lowering due to a decrease in BCC).

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

During the treatment period, care must be taken when driving vehicles and engaging in other potentially dangerous activities requiring increased concentration and speed of psychomotor reactions (possibly dizziness, especially after taking the initial dose of an ACE inhibitor in patients taking diuretic medicines).

Form release / dosage:

Tablets of 2.5 mg, 5 mg, 10 mg and 20 mg.

Packaging:

Tablets 2.5 mg.

For 10 tablets in an aluminum strip.Two strips are packed in a cardboard box with instructions for use.

Tablets 5 mg, 10 mg, 20 mg.

For 10 tablets in an aluminum strip. For 2, 5, 6 or 10 strips packed in a cardboard box with instructions for use.

Storage conditions:

List B.

In a dry, protected from light place 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 N014189 / 01

Date of registration:18.03.2009

The owner of the registration certificate:Dr. Reddy's Laboratories Ltd.Dr. Reddy's Laboratories Ltd. India

Manufacturer: & nbsp

Dr. Reddy`c Laboratoris Ltd. India

Information update date: & nbsp23.10.2015

Illustrated instructions

Instructions

Enam® (Enam®)