Composition, form of production and packaging
Tablets of white color, round, flat, with a facet, with a risk on one side and labeling "ED10" - on the other.
1 tab.
enalapril maleate 10 mg
Excipients: sodium hydroxide, silicon dioxide colloid, magnesium stearate, povidone, talc, crospovidone, microcrystalline cellulose, lactose monohydrate.
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (10) - packs of cardboard.
Tablets of white color, round, flat, with a facet, with a risk on one side and labeling "ED2.5" - on the other.
1 tab.
enalapril maleate 2.5 mg
Excipients: sodium hydroxide, silicon dioxide colloid, magnesium stearate, povidone, talc, crospovidone, microcrystalline cellulose, lactose monohydrate.
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (10) - packs of cardboard.
Tablets of white color, round, flat, with a facet, with a risk on one side and labeling "ED20" - on the other.
1 tab.
enalapril maleate 20 mg
Excipients: sodium hydroxide, silicon dioxide colloid, magnesium stearate, povidone, talc, crospovidone, microcrystalline cellulose, lactose monohydrate.
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (10) - packs of cardboard.
Tablets of white color, round, flat, with a facet, with a risk on one side and labeling "ED5" - on the other.
1 tab.
enalapril maleate 5 mg
Excipients: sodium hydroxide, silicon dioxide colloid, magnesium stearate, povidone, talc, crospovidone, microcrystalline cellulose, lactose monohydrate.
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (10) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2010.
PHARMACHOLOGIC EFFECT
Antihypertensive drug, the mechanism of its action is associated with a decrease in the formation of angiotensin II from angiotensin I, which leads to a direct reduction in the release of aldosterone. At the same time, the overall peripheral vascular resistance (OPSS), systolic and diastolic blood pressure (BP), post- and preload of the myocardium decrease. 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 the 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 necessary 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 is rapidly metabolized in the liver as a result of its hydrolysis, an active metabolite enalaprilat is formed, which is a more active inhibitor of ACE than enalapril. Bioavailability of the drug is 40%. C max enalapril in blood plasma is achieved after 1 hour, enalaprilata - after 3-4 hours. Enalaprilat easily passes through the histohematetic barriers, excluding blood-brain, a small amount penetrates the placental barrier and into breast milk.
T 1/2 of enalaprilat is about 11 hours. Enalapril is excreted mainly with 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
- arterial hypertension;
- chronic heart failure (as part of combination therapy);
- prevention of chronic heart failure in patients with asymptomatic left ventricular dysfunction.
DOSING MODE
Take ingestion, regardless of the time of ingestion, with a sufficient amount of liquid.
At monotherapy of an arterial hypertensia the initial dose - 5 mg 1 times / sut. 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 sufficiently good tolerability dose can be increased to 40 mg / day for 1-2 doses. After 2-3 weeks pass to a maintenance dose of 10-40 mg / day and divided into 1-2 admission. With a moderate degree of arterial hypertension, the average daily dose is about 10 mg. The maximum daily dose is 40 mg.
In the case of administering the Ednit drug to patients who are concurrently receiving diuretics, treatment with a diuretic should be discontinued 2-3 days before the application of the Ednit drug. 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 1 time / day.
With Renovascular hypertension, the initial dose is 2.5-5 mg / day. The maximum daily dose is 20 mg.
For 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 more than 40 mg / day once or in 2 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 tablets, 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, more pronounced hypotensive effect and lengthening of the duration of the Ednit drug effect are more frequent, which is associated with a decrease in the rate of excretion 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 / day. The dose is selected taking into account the tolerance to 20 mg / day in 2 divided doses.
In chronic renal failure, cumulation of enalapril occurs with a decrease in filtration of less than 10 ml / min. At CC 80-30 ml / min, the dose of Ednit should be 5-10 mg / day, with a decrease in CK to 30-10 ml / min - 2.5-5 mg / day, with a CK of 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 EFFECT
From the cardiovascular system : excessive reduction in blood pressure, orthostatic collapse, rarely - chest pain, angina, myocardial infarction or stroke (usually associated with a pronounced decrease in blood pressure); extremely rare - arrhythmias (atrial brady or tachycardia, atrial fibrillation), palpitations, thromboembolism of the pulmonary artery branches, Raynaud's syndrome.
From the central nervous system and peripheral nervous system : dizziness, headache, weakness, insomnia, anxiety, confusion, fatigue, drowsiness (2-3%); very rarely with high doses - nervousness, depression, paresthesia.
From the sense organs : imbalance, hearing and vision impairment, tinnitus.
On the part of the digestive system : dry mouth, anorexia, dyspeptic disorders, nausea, diarrhea or constipation, vomiting, abdominal pain, intestinal obstruction, pancreatitis, liver and biliary dysfunction, hepatitis (hepatocellular or cholestatic), jaundice, rarely - stomatitis , glossitis, increased activity of liver enzymes.
On the part of the respiratory system : unproductive dry cough, sore throat, hoarseness, pulmonary infiltrates, interstitial pneumonitis, bronchospasm, dyspnea, rhinorrhea, pharyngitis.
Allergic reactions : skin rash, angioedema, swelling of the face, limbs, lips, tongue, glottis and / or larynx; extremely rare - erythema multiforme, exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, pemphigus, pruritus, urticaria, photosensitivity, serositis, vasculitis, myositis, arthralgia, arthritis, intestinal angioedema.
On the part of metabolism : hypercreatininaemia, increased urea in the blood, hyperbilirubinemia, hypoglycemia in diabetic patients taking hypoglycemic agents for ingestion or insulin.
From the side of the water-electrolyte balance : hyperkalemia, hyponatremia.
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.
From the urinary system : a violation of the kidneys, rarely - proteinuria.
Other : alopecia, decreased libido, impotence, "hot flashes".
CONTRAINDICATIONS
- history of angioedema, associated with treatment with ACE inhibitors, and hereditary or idiopathic angioedema;
- porphyria;
- Pregnancy and the period of breastfeeding;
- Children under 18 years of age (effectiveness and safety not established);
lactose intolerance;
- deficiency of lactase or glucose-galactose malabsorption (because the composition of the drug includes lactose).
- Hypersensitivity to enalapril and other ACE inhibitors.
With caution: 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, ischemic heart disease, cerebrovascular diseases , diabetes mellitus, renal failure (proteinuria more than 1 g / day), liver failure, patients who follow a diet with restricted iem salt or hemodialysis, simultaneous with immunosuppressants and saluretikami, older patients (over 65 years), inhibition of bone marrow hematopoiesis, state, accompanied by a decrease in blood volume (including diarrhea and vomiting).
PREGNANCY AND LACTATION
The drug is contraindicated in pregnancy and during breastfeeding.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution appoint patients with renal insufficiency (proteinuria more than 1 g / day), as well as patients with bilateral stenosis of the renal arteries, stenosis of the artery of a single kidney and in a state after kidney transplantation.
In chronic renal failure, cumulation of enalapril occurs with a decrease in filtration of less than 10 ml / min. At CC 80-30 ml / min, the dose of Ednit should be 5-10 mg / day, with a decrease in CK to 30-10 ml / min - 2.5-5 mg / day, with a CK of less than 10 ml / min - 1.25-2.5 mg / day only on dialysis days.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Be wary appoint patients with hepatic insufficiency.
APPLICATION FOR CHILDREN
The drug is contraindicated in children under the age of 18 years.
APPLICATION IN ELDERLY PATIENTS
The drug is administered with caution to elderly patients.
In elderly people, more pronounced hypotensive effect and lengthening of the duration of the Ednit drug effect are more frequent, which is associated with a decrease in the rate of excretion of the drug, therefore the recommended initial dose for elderly patients is 1.25 mg / day.
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 continuing 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, hepatic enzyme activity) and protein concentration in the urine are 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 withdrawal of treatment does not lead to withdrawal syndrome (a sharp rise in blood pressure).
In patients with an indication of angioedema, a history of an increased risk of its development with the administration of ACE inhibitors.
For newborns and infants who have undergone intrauterine exposure to ACE inhibitors, careful monitoring is recommended to detect a marked decrease in blood pressure, oliguria, hyperkalemia and neurological disorders that are possible 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 impaired 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, incl. dental, it is necessary to warn the surgeon / anesthesiologist about the use of ACE inhibitors.
Impact on the ability to drive vehicles and manage mechanisms
When side effects from the central nervous system are not recommended, vehicle management, as well as performing work associated with increased risk.
OVERDOSE
Symptoms : marked decrease in blood pressure up to the development of collapse, myocardial infarction, acute disturbance of cerebral circulation or thromboembolic complications, seizures, stupor.
Treatment : the patient is transferred from 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 injection of 0.9% sodium chloride solution, plasma substitutes, and if necessary - angiotensin II, hemodialysis (enalapril removal rate averages 62 ml / min).
DRUG INTERACTION
With the simultaneous use of the Ednit drug with non-steroidal anti-inflammatory drugs (NSAIDs), incl. selective inhibitors of cyclooxygenase-2 (COX-2), possibly reducing the hypotensive effect; with potassium-sparing diuretics (spironolactone, triamterene, amiloride) can lead to hyperkalemia; with lithium salts - to slow down the excretion of lithium (shown control of the concentration of lithium in blood plasma).
In some patients with impaired renal function and receiving NSAIDs, incl. inhibitors of COX-2, the concomitant use of ACE inhibitors may lead to further impairment of renal function. These changes are reversible.
Simultaneous administration of Ednit with NSAIDs may decrease the effectiveness of the drug.
Enalapril weakens the effect of drugs containing theophylline.
The hypotensive effect of enalapril is enhanced by diuretics, ОІ-adrenoblockers, methyldopa, nitrates, blockers of "slow" calcium channels, hydralazine, prazosin. Immunosuppressants, allopurinol, cytostatics increase hematotoxicity.
Drugs that cause depression of bone marrow function, increase the risk of developing neutropenia and / or agranulocytosis up to death.
Joint use of ACE inhibitors and hypoglycemic agents (insulin, hypoglycemic agents for the duration of oral administration) may 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. Patients with diabetes who take hypoglycemic agents for ingestion and insulin need control of blood glucose, especially during the first month of joint use with ACE inhibitors.
Symptom, including facial flushing, nausea, vomiting, and hypotension, in rare cases described, when used together for the preparation of gold on / in the (sodium aurothiomalate) and ACE inhibitors (enalapril).
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
Storage conditions
List B.
Store at a temperature above 25 В° C in the reach of children.
Shelf life:
3 years.
Do not use after the expiry date printed on the package.
