Enam-N

Active material: Enalapril, Gidroxlorotiazid
When ATH: C09BA02
CCF: Antihypertensive drugs
When CSF: 01.09.16.03
Manufacturer: DR. REDDY`S LABORATORIES LTD. (India)

Pharmaceutical form, composition and packaging

Pills white or nearly white, round, with beveled edges; One side is smooth, another – stamping “S134”.

1 tab.
эnalaprila maleate10 mg
gidroxlorotiazid25 mg

Excipients: lactose monohydrate, pre-gelatinized starch, corn starch, Zinc acetate.

10 PC. – aluminum strips (2) – packs cardboard.
10 PC. – aluminum strips (3) – packs cardboard.
10 PC. – aluminum strips (10) – packs cardboard.

Pharmacological action

Combined antihypertensive drug.

Enalapril – ACE inhibitor. It is “prodrug”. The pharmacological activity of the metabolite has enalaprilat, which is formed by hydrolysis of enalapril, mechanism of action is associated with inhibition of ACE activity, leading to a decrease in the formation of angiotensin I into angiotensin II; as well as a decrease in aldosterone secretion, vasopressin; vasodilators decrease inactivation of bradykinin and atrial natriuretic factor, inhibition activity sympathoadrenal, suppression of hypertrophy of smooth muscles of arteries, hyperplasia and smooth muscle cell proliferation, thereby reducing systemic vascular resistance. Enalapril also causes a decrease in left ventricular hypertrophy, and reduces excretion of potassium in the urine. Favorably influences on carbohydrate and lipid metabolism, increasing the permeability of cell membranes to glucose and increasing the content of HDL. It has nephroprotective action. Reduces the excitability of the myocardium, tachycardia and the incidence of arrhythmia due to increased levels of potassium in the blood, also has a cardioprotective effect by reducing pre- and afterload on the myocardium and increase coronary blood flow. It improves circulation of the small circle, which contributes to the normalization of breath.

Gidroxlorotiazid – a drug with diuretic and hypotensive activity. Effect of the drug due to its effect on the reabsorption of sodium and chloride in the distal tubule. Thus excretion of sodium and chloride ions is increased by approximately an equal volume of. Strengthening natriuresis may be accompanied by loss of potassium ions, Magnesium, bicarbonate, delay calcium ions. After oral diuretic effect begins to show through 2 no, reaches through 4 hours and lasts about 6-12 no.

When combined effects of antihypertensive drugs complement each other, resulting in a therapeutic effect becomes more prolonged and severe. It is also shown, that the combined use of enalapril and hydrochlorothiazide reduces the loss of potassium in the urine.

Pharmacokinetics

Enalapril

Absorption, distribution

After oral administration about 60% enalapril is absorbed and Cmax plasma achieved by the end of the first hour, after which the concentration decreases rapidly. Absorption does not depend from taking screaming. The concentration of enalapril in the plasma is a linear function of the dose. The equilibrium state is established after 3-4 taking the drug. Plasma protein binding is about 50%.

Metabolism, deduction

Enalapril is metabolized primarily in the liver to the active metabolite enalaprilat, Cmax which plasma is later 3-4 h after administration. Report the news. T1/2 is about 11 no; during the elimination of the active metabolite – about 30-35 no.

Gidroxlorotiazid

Absorption

Hydrochlorothiazide is absorbed after oral administration in the 60-80%, Cmax in plasma is reached after 1.5-3 no, food intake on the absorption effect is insignificant.

Metabolism, deduction

Hydrochlorothiazide in the body is practically not metabolized, metabolites found in trace concentrations. When saving kidney function 60-75% of the administered dose excreted by the kidneys in an unmodified form for 24 no.

Pharmacokinetics in special clinical situations

In patients with cirrhosis the pharmacokinetics of hydrochlorothiazide changes were observed.

Indications

- Treatment of hypertension, requiring the use of combination therapy.

Dosage regimen

The dose and duration of therapy is determined individually. Treatment of hypertension should not be started with the use of a combination. Patients, have sufficient hypotensive effect can not be achieved with the help of enalapril monotherapy or hydrochlorothiazide, recommended intake of n-Enam 1 tablets 1 times / If necessary, the dose can be increased to 2 tablets 1 time /

Side effect

From the central and peripheral nervous system: headache, dizziness, fatigue, asthenia; very rarely when used in high doses – insomnia, increased nervous irritability, depression, disequilibrium, paresthesia, noise in ears.

The respiratory system: perhaps – dry cough, breathlessness.

From the digestive system: nausea, diarrhea, constipation, stomach ache; rarely – dysgeusia (metallic taste in mouth, ageusia); increase in liver enzymes and bilirubin.

Cardio-vascular system: hypotension, swoon, heartbeat, chest pain.

Allergic reactions: skin rashes, itch; may develop angioedema various localization (person, limbs, lips, language, larynx and pharynx). The reaction can occur at any time during the course of treatment.

From the laboratory parameters: proteinuria, giperglikemiâ, hyperkalemia, hypercalcemia, hyperuricemia, gipomagniemiya, giponatriemiya, chloropenia, kaliopenia, alkalosis, increase in urea, serum creatinine; sometimes – high cholesterol and triglycerides.

From the hematopoietic system: leukopenia, neutropenia, anemia, thrombocytopenia; in some cases – agranulocytosis, inhibition of myelopoiesis (in patients without a history of history, taking captopril and other ACE inhibitors, incl. Enalapril). In most cases the above states occur in patients with renal insufficiency, systemic connective tissue diseases, and vasculitis.

Other: very rarely when used in high doses – hair loss, reduced potency.

Contraindications Enam-H

- Angioedema, associated with ACE inhibitors, history;

- Anurija;

- Pregnancy;

- Lactation (breast-feeding);

- Hypersensitivity to the drug, ACE inhibitors or sulfonamides.

Use of the drug pregnancy and breastfeeding

The drug is contraindicated during pregnancy and lactation (breast-feeding).

The use of ACE inhibitors in the II and III trimester of pregnancy may impair fetal development, incl. incompatible with life. When using ACE inhibitors in the I trimester the risk of such disorders is minimal. If pregnancy occurs during therapy with the drug Enam-H as soon as possible to change the therapy.

Women of childbearing age You should be alerted about the need to stop the drug at the onset of pregnancy.

Application for violations of liver function

In appointing Enam-N should also be considered, that even a small change in fluid and electrolyte balance may provoke increased hepatic insufficiency. There were reports of severe adverse reactions in the liver in patients receiving ACE inhibitors (incl. enalapril), so in the event of jaundice patients should stop taking the drug and conduct appropriate therapy.

Application for violations of renal function

When renal artery stenosis in clinical trials of enalapril approximately 20% patients showed increase in urea and creatinine in the blood (usually reversible). If necessary, use of enalapril in this group of patients during the first few weeks of treatment is recommended careful monitoring of renal function.

It is not recommended to use the drug in patients with renal insufficiency (CC <80 ml / min).

Cautions

Simultaneous food intake does not affect the absorption of the components of the drug.

Against the background of the drug is prohibited to drink alcohol in connection with a possible increased hypotensive effect.

Hypotension

Before and during use Enam-H requires monitoring of blood pressure and renal function in connection with the possibility of “the effect of the first dose”. At risk of arterial hypotension (which may be associated with oliguria and / or progressive azotemia; rarely – with acute renal failure) refer patients with chronic heart failure, hyponatremia; Patients, taking high doses of diuretics; Patients, on dialysis; Patients with impaired water and electrolyte balance of various etiologies. At the beginning of therapy, these patients should be careful. The development of hypotension is not a reason for the complete withdrawal of the drug, but it requires the implementation of preventive measures (monitoring of electrolytes, FROM, renal function, Dosage adjustment Enam-H and taken him drugs).

If the patient's condition allows, it is desirable for 1-2 days before the start of the reception Enam-H to reduce the dose diuretics or completely cancel them. During the first two weeks of treatment and each time, when adjusted dose, Patients should be under medical supervision. Such monitoring is also required when administering the drug to patients with ischemic heart disease and cerebrovascular disease (in these patients hypotension can cause myocardial infarction and acute cerebrovascular disorders).

Aortalnыy stenosis

Enam-H should be used with caution in these patients (like any other peripheral vasodilator).

Kidney

When renal artery stenosis in clinical trials of enalapril approximately 20% patients showed increase in urea and creatinine in the blood (usually reversible). If necessary, use of enalapril in this group of patients during the first few weeks of treatment is recommended careful monitoring of renal function.

It is not recommended to use the drug in patients with renal insufficiency (CC <80 ml / min).

Endocrinological diseases

While taking hydrochlorothiazide sometimes marked increase in blood glucose, which may require increased doses of insulin or oral hypoglycemic agents. This effect is less pronounced when receiving hydrochlorothiazide with enalapril.

Receiving thiazide diuretics may increase the level of calcium in the blood, that should be considered during the investigation of the function of the parathyroid glands (before the study drug should be canceled).

Neutropenia / agranulocytosis

The appointment Enam-H should be periodic haematological monitoring in patients with systemic connective tissue, vasculitis and renal disease due to a higher risk of impaired hematopoiesis.

Anaphylactoid reactions

When treatment with ACE inhibitors (incl. and enalapril) described rare cases of angioedema face, limbs, lips, language, glottis, larynx. In this case, you should immediately remove the drug and take the necessary measures. If the swelling is limited to face and lips, the process usually resolves without treatment, if necessary, use antihistamines.

Use in patients with impaired hepatic function

In these patients may increase the duration of drug action, tk. Enalapril is metabolized in the liver. In appointing Enam-N should also be considered, that even a small change in fluid and electrolyte balance may provoke increased hepatic insufficiency. There were reports of severe adverse reactions in the liver in patients receiving ACE inhibitors (incl. enalapril), so in the event of jaundice patients should stop taking the drug and conduct appropriate therapy.

Effects on ability to drive vehicles and management mechanisms

As a result of treatment with enalapril may develop individual responses, which may impair the ability of patients to drive and engage in other activities, require high concentration and speed of psychomotor reactions. These effects increase with increasing dose, and while drinking alcohol.

Overdose

Symptoms: common – hypotension.

Treatment: the patient should be given a horizontal position with raised legs. In mild cases, inside the prescribed aqueous salt solutions. In severe cases, the patient is admitted in the hospital and carry out activities, to stabilize blood pressure (/ in the introduction of electrolyte solutions, plasma expanders). Perhaps the use of hemodialysis.

Drug Interactions

At simultaneous application with antihypertensive drugs other groups (beta-blockers, Calcium channel blockers, Diuretics, methyldopa, Alpha-blockers), as well as to increase the hypotensive effect of nitrates Enam-H.

While the use of diuretics may develop severe hypotension at the beginning of therapy.

Co-administration of analgesics, antipyretics and NSAIDs may reduce the hypotensive effect of the drug.

In an application Enam-N and potassium-sparing diuretics, or potassium products (if hypokalemia) Caution should be exercised and continuously monitor the concentration of potassium in the plasma, t. to. enalapril reduces the excretion of potassium from the body. It is desirable to avoid the use of potassium-sparing diuretics and medications for patients with renal insufficiency, receiving enalapril, in connection with the possibility of increasing the content of potassium in the blood.

In an application with lithium may slow excretion of lithium (is shown to control the concentration of lithium in the blood plasma); It was described cases of lithium toxicity while receiving lithium preparations, increases the excretion of sodium (including enalapril and hydrochlorothiazide).

In an application with allopurinol, prokaynamydom, GCS, cytostatics increases the risk of violations of the hematopoietic system (lekopeniya, neutropenia), and when taken with corticosteroids – the risk of electrolyte imbalance.

In an application Enam-H with oral hypoglycemic drugs or insulin preparations may require adjustment of the antidiabetic therapy (in connection with the influence of N on enam-glucose uptake in the tissues).

With simultaneous application of cimetidine action extends Enam-H.

Application Enam-H together with means for anesthesia may increase the hypotensive effects.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children at or above 25 ° C. Shelf life – 2 year.

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