Pharmaceutical form | Enalapril 10mg Tablets. There are 10 tablets in a blister. 2 blisters are packed in a cardboard box together with an enclosed leaflet. |
Active ingredient | Enalapril 10mg |
Pharmacotherapeutic group | ACE inhibitor. |
Arterial hypertension (including renovascular), chronic heart failure (as part of combination therapy). Essential hypertension. Chronic heart failure (as part of combination therapy). Prevention of the development of clinically severe heart failure in patients with asymptomatic left ventricular dysfunction (as part of combination therapy). Prevention of coronary ischemia in patients with left ventricular dysfunction in order to reduce the incidence of myocardial infarction and reduce the incidence of hospitalizations for unstable angina. |
Package leaflet (information for patients)
Tradename
Enalapril
Dosage form
Tablets 10mg
Description
Round, flat, beveled to the edge white tablets with an imprint in the form of the brand name "V" on one side.
Structure
Active ingredient: Enalapril 10 mg
Excipients: microcrystalline cellulose 102, calcium stearate, aerosil ® 200 (hydrophilic pyrogenic silicon dioxide).
Pharmacotherapeutic group
ACE inhibitor
Pharmacological properties
pharmachologic effect
An ACE inhibitor is an antihypertensive agent. Inhibits the formation of angiotensin I angiotensin II and eliminates its vasoconstrictor effect. The drug gradually lowers blood pressure without causing changes in heart rate and minute blood volume. Reduces the total peripheral vascular resistance, reduces afterload. It also reduces preload, lowers pressure in the right atrium and pulmonary circulation. The drug reduces left ventricular hypertrophy. The drug reduces the tone of the efferent arterioles of the renal glomeruli, thereby improving intraglomerular hemodynamics, and prevents the development of diabetic nephropathy.
The time of the onset of the hypotensive effect when taken orally is 1 hour, it reaches a maximum after 4-6 hours and lasts up to 24 hours. In some patients, in order to achieve an optimal level of blood pressure, therapy is necessary for several weeks. In chronic heart failure, a noticeable clinical effect is observed with prolonged treatment - 6 months or more.
Pharmacokinetics
After oral administration, approximately 60% of enalapril is absorbed from the gastrointestinal tract. It is metabolized in the liver with the formation of an active metabolite - enalaprilat. The maximum concentration of enalaprilat in the blood serum is reached 3-4 hours after administration.
The connection with plasma proteins of enalaprilat is 50-60%. The maximum concentration in the blood plasma of enalapril is achieved after 1 hour, enalaprilat - 3-4 hours. Enalaprilat easily passes through the histohematological barriers, excluding the BBB, a small amount penetrates the placenta and into breast milk. The half-life of enalaprilat is 11 hours. It is excreted mainly by the kidneys - 60% (20% - in the form of enalapril and 40% - in the form of enalaprilat), through the intestines - 33% (6% - in the form of enalapril and 27% - in the form of enalaprilat). Removed by hemodialysis (speed
62 ml / min) and peritoneal dialysis.
After 4 days, after receiving the drug half-life enalaprilat Art abiliziruetsya and is 11h.
It is excreted by the kidneys.
Indications for use
-treatment of arterial hypertension;
-treatment of clinically expressed heart failure;
- prevention of clinically significant heart failure in patients with asymptomatic left ventricular dysfunction (ejection fraction ≤ 35%).
Method of administration and dosage
The drug should be taken at the same time of the day (regardless of food intake) with a small amount of liquid.
The dosage regimen is set individually depending on the patient's condition.
In the treatment of arterial hypertension, the drug is prescribed at an initial dose of 5 mg / day (in this case, it is recommended to use the dosage form of Enalapril - 5 mg tablets). After taking the initial dose, patients should be under medical supervision for 2 hours and an additional 1 hour until blood pressure stabilizes. Dose adjustment is carried out depending on the achieved clinical effect. Usually, the maintenance daily dose ranges from 10 - 20 mg, in exceptional cases - up to 40 mg in 1 or 2 doses. In the case of prescribing to patients simultaneously receiving diuretics, diuretic treatment should be discontinued 2 to 3 days before enalapril is prescribed. The initial dose for patients who received diuretics is 2.5 mg 1 time / day. When the initial dose of the drug is 2.5 mg, it is recommended to use the dosage form of Enalapril - tablets
2.5 mg.
With asymptomatic left ventricular dysfunction, the recommended initial dose of the drug is 2.5 mg 2 times / day, in this case it is recommended to use the dosage form of Enalapril - 2.5 mg tablets. Dose adjustment is possible depending on the patient's condition. The average maintenance dose is 10 mg 2 times / day.
In chronic heart failure, the recommended initial dose of the drug is 2.5 mg 1 time / day, in this case it is recommended to use the dosage form of Enalapril - 2.5 mg tablets. The dose of the drug should be increased gradually until the maximum clinical effect is achieved; on average, it takes 2 to 4 weeks to find the optimal dose. The average maintenance dose is 2.5-10 mg 1 time / day, the daily maximum maintenance dose is 40 mg (divided into 2 doses).
In the treatment of arterial hypertension in kidney disease, the dosage regimen is set depending on the severity of renal dysfunction or on the values of creatinine clearance. The initial dose of the drug should be gradually increased until a satisfactory clinical effect is achieved. When creatinine clearance is 80-30 ml / min, the dose is usually 5-10 mg / day, creatinine clearance is 30-10 ml / min - 2.5-5 mg / day (if 2.5 mg is prescribed, it is recommended to use the dosage form of Enalapril - tablets 2.5 mg).
The duration of treatment depends on the effectiveness of therapy. With a too pronounced decrease in blood pressure, the dose of the drug is gradually reduced.
Side effects
The following side effects are presented in accordance with the following gradations of the frequency of their occurrence: very often (> 1/10); often (> 1/100, <1/10); infrequently (> 1/1000, <1/100); rarely (> 1/10000, <1/1000); very rare (<1/10000) (including individual messages), unknown frequency (it is not possible to determine the frequency of occurrence from the available data).
On the part of the blood: rarely - anemia (including aplastic and hemolytic), neutropenia, decreased hemoglobin, decreased hematocrit, thrombocytopenia, agranulocytosis, bone marrow suppression, pancytopenia, lymphadenopathy, autoimmune diseases.
From the endocrine system: unknown - ADH secretion disorder syndrome.
Metabolic disorders: infrequently - hypoglycemia.
From the nervous system and psyche: often - depression, headache; rarely - confusion, drowsiness, insomnia, nervousness, paresthesia, vertigo, sleep disorder, abnormal dreams.
From the side of the organs of vision: very often - blurred vision.
From the side of the cardiovascular system: very often - dizziness; often - hypotension (including orthostatic hypotension), syncope, chest pain, rhythm disturbances, angina pectoris, tachycardia; rarely - postural hypotension, tachycardia, myocardial infarction or stroke (possibly as a result of excessive pressure reduction in patients with high risk) pheno changed Raynaud.
From the respiratory system: very often - cough; often - shortness of breath; rarely - runny nose, sore throat and hoarseness, bronchospasm / asthma, pulmonary infiltrates, rhinitis, allergic al Veolia / eosinophilic pneumonia.
From the side of the digestive tract: very often - nausea; often - diarrhea, abdominal pain, change in taste; rarely - intestinal obstruction, pancreatitis, vomiting, dyspepsia, constipation, anorexia, stomach irritation, dry mouth, peptic ulcers, stomatitis / aphthous ulcers, glossitis; very rarely - angioedema of the intestine.
From the digestive system: rarely - liver failure, hepatitis hepatocellular or cholestatic, hepatitis, including necro os, cholestasis (including jaundice).
On the part of the skin and subcutaneous tissues: often - rash, hypersensitivity / angioedema of the face, extremities, lips, tongue, glottis and / or larynx; infrequently - increased sweating, itching, urticaria, alopecia ; rarely - erythema multiplex, Stevens- Johnson syndrome, exfoliative dermatitis, toxic epidermal non- rabbit, pemphigus, erythroderma.
The development of a complex symptom complex was reported, which included some or all of such manifestations as: fever, serositis, vasculitis, myalgia / myositis, arthralgia / arthritis, a positive test for antinuclear antibodies, increased ESR, eosinophilia and leukocytosis. As side effects can occur rash fotosensibil ization and other dermal reactions.
From the urinary system: infrequently - impaired renal function, renal failure, proteinuria; rarely oliguria.
On the part of the reproductive system: infrequently - their potency; rarely - gynecomastia.
General disorders: very often - asthenia; often - fatigue; infrequently - muscle cramps, hot flashes, ringing in the ears, feeling of discomfort, fever.
Changes in laboratory parameters: often - hyperkalemia, increased serum creatinine levels; rarely - an increase in the level of urea in the blood, hyponatremia, an increase in liver enzymes, bilirubin in the blood serum.
Contraindication
Hypersensitivity to enalapril and other ACE inhibitors, a history of angioedema, pregnancy (especially the second and third trimesters of pregnancy), lactation, children under 18 years of age (safety and efficacy have not been determined).
Renal failure: creatinine clearance less than 10 ml / min (for this dosage form).
The simultaneous use of angiotensin - converting enzyme inhibitors or ATP receptor blockers with Aliskiren in patients with diabetes mellitus or moderate / severe renal failure (GFR <60 ml / min / 1.73 m2) is contraindicated.
With caution: decreased renal and liver function, simultaneously with immunosuppressants, with bilateral renal artery stenosis.
Overdose
Data on overdose in humans are limited. The most characteristic features of an overdose registered to date are severe arterial hypotension, which begins approximately 6 hours after taking the pill, simultaneously with blockade of the renin- angiotensin system, stupor. Symptoms associated with an overdose of ACE inhibitors may include circulatory shock, electrolyte disturbances, kidney failure, hyperventilation, tachycardia, palpitations, bradycardia, headache, restlessness, and coughing.
The recommended treatment for overdose is intravenous saline. If hypotension occurs, the patient is laid horizontally with raised legs. Consideration should be given to intravenous infusion of angiotensin II and / or catecholamines. If the drug has been recently taken, measures should be taken to eliminate enalapril maleate (for example, vomiting, gastric lavage, administration of sorbents and sodium sulfate). Enalapril can be removed from the general circulation by hemodialysis. With therapy-resistant bradycardia, the use of pacemakers is indicated. You should constantly monitor the basic vital functions, the concentration of serum electrolytes and creatinine.
Precautions
Enalapril should be used with caution in patients with difficulty in the outflow of blood from the left ventricle of the heart, ischemic heart disease, cerebrovascular disease.
During treatment with enalapril, systematic monitoring of blood pressure and renal function is required in patients with heart failure. In patients receiving diuretics, the dose of diuretics, if possible, should be reduced before starting treatment with enalapril. During the treatment period, the serum potassium content should also be monitored. Arterial hypotension often develops against the background of hypovolemia, restriction of salt intake, during hemodialysis, against the background of diarrhea or vomiting, during surgery or anesthesia using compounds that cause arterial hypotension.
In cases where hypotension becomes persistent, the dose should be reduced and / or discontinued diuretic and / or enalapril.
In patients with bilateral stenosis of the renal arteries or stenosis of an artery of a solitary kidney, arterial hypotension that develops after starting treatment with enalapril can lead to a deterioration in renal function, an increase in the content of urea and creatinine in serum.
When prescribing enalapril, rare cases of angioedema are described (more often in patients of the Negroid race). In such cases, you should immediately stop treatment and establish constant monitoring of the patient until the symptoms disappear completely. At the same time, antihistamines have a positive effect. With the development of suffocation against the background of edema, a solution of epinephrine (adrenaline) 0.1% (0.3-0.5 ml) should be injected subcutaneously and / or measures should be taken to ensure airway patency.
In rare cases, taking ACE inhibitors against the background of hyposensitization with Hymenoptera allergens or dialysis using high-throughput membranes (for example, AN69) causes severe anaphylactoid reactions. In these patients, we recommend the use antigiperte nzivnyh means another class.
There have been reports of the occurrence of a reversible, unproductive cough I during treatment with ACE inhibitors.
In patients who received enalapril for 48 weeks, an increase in serum potassium levels of 0.02 meq / L is observed. When treating with enalapril, serum potassium should be monitored.
Interaction with other medicinal products
When concomitant administration of potassium-sparing diuretics or potassium supplements may develop hyperkalemia. With simultaneous use with diuretics, beta- blockers, methyldopa, nitrates, calcium channel blockers, hydralazine, prazosin, an increase in the hypotensive effect is possible. With simultaneous use with NSAIDs (including with acetylsalicylic acid), it is possible to reduce the effect of enalapril and increase the risk of developing renal dysfunction. With simultaneous use with ethanol, as well as agents for general anesthesia, the risk of developing arterial hypotension increases. Enalapril weakens the effect of drugs containing theophylline. With simultaneous use with lithium preparations, the elimination of lithium slows down and its effect increases. With simultaneous use with cimetidine, the half- life of enalapril is lengthened.
Dual blockade of the renin- angas otenzin - aldosteronovoy system
Based on the available data, dual blockade of RAAS using an ACE inhibitor, ARB II or Aliskiren cannot be recommended for any patient, especially for patients with diabetic nephropathy.
In patients with diabetes mellitus or moderate / severe renal impairment (GFR <60 ml / min / 1.73 m2), the simultaneous use of Aliskiren s and ACE or ARB II is contraindicated.
In some cases, when the combined use of an ACE inhibitor and ARB II is absolutely indicated, careful supervision of a specialist and mandatory monitoring of renal function, water-electrolyte balance, and blood pressure are necessary.
Gold preparations
There have been sporadic reports of nitritic reactions (symptoms include facial flushing, nausea, vomiting, and hypotension) in patients receiving injectable gold preparations (sodium aurothiomalate) and ACE inhibitors, including enalapril.
Antidiabetic medicines
Epidemiological studies suggest that the simultaneous use of ACE inhibitors and antidiabetic drugs (insulin, oral antidiabetic drugs) can lead to a marked decrease in blood sugar levels with the risk of hypoglycemia. This phenomenon is most likely to occur in patients with kidney damage during the first weeks of combination therapy.
Tricyclic antidepressants / antipsychotics / anesthetics / narcotics
The simultaneous use of certain anesthetics, tricyclic antidepressants and antipsychotics with ACE inhibitors can lead to an additional decrease in blood pressure.
Sympathomimetics
Decrease the Sympathomimetics may shat antihypertensive effect.
Acetylsalicylic acid, thrombolytics and β-blockers
Enalapril can be safely administered concomitantly with acetylsalicylic acid (at a cadiological dosage), thrombolytics and β-blockers.
Special instructions
It is used with extreme caution in patients with autoimmune diseases, diabetes mellitus, impaired liver function, severe aortic stenosis, subaortic muscle stenosis of unknown origin, hypertrophic cardiomyopathy, with loss of fluid and salts. In the case of previous treatment with saluretics, in particular in patients with chronic heart failure, the risk of orthostatic hypotension increases, therefore, before starting treatment with enalapril, it is necessary to compensate for the loss of fluid and salts.
With long-term treatment with enalapril, it is necessary to periodically monitor the peripheral blood picture. Sudden discontinuation of enalapril does not cause a sharp increase in blood pressure.
During surgical interventions during the treatment with enalapril, arterial hypotension may develop, which should be corrected by the introduction of a sufficient amount of liquid.
Before examining the function of the parathyroid glands, enalapril should be discontinued.
Influence on the ability to drive vehicles and control mechanisms
Caution is required when driving or performing other work requiring increased attention, as dizziness is possible, especially after taking the initial dose of enalapril.
Pregnancy and elbowing
Pregnancy
The use of ACE inhibitors is not recommended in the first trimester of pregnancy.
Except in those cases when it is impossible to replace the ACE inhibitor with another alternative therapy, patients planning a pregnancy should be transferred to antihypertensive therapy with drugs for which the safety profile for pregnant women is well understood. Upon the occurrence of pregnancy, ACE inhibitors should be stopped immediately, and appointed and, if necessary, naya antihypertensive therapy.
The use of ACE inhibitors is contraindicated in the second and third trimesters of pregnancy.
When using ACE inhibitors in the second and third trimesters of pregnancy, the manifestation of fetotoxic action (impaired renal function, oligohydramnios, delayed ossification of the skull bones) and neonatal toxicity (renal failure, hypotension, hyperkalemia) was established. In the event that an ACE inhibitor was taken from the second trimester of pregnancy, an ultrasound of the function of the kidneys and skull bones is recommended. In newborns whose mothers took ACE inhibitors, blood pressure must be carefully monitored to prevent the possible development of hypotension.
Lactation
During treatment, breastfeeding should be stopped.
Enalapril in very low concentrations passes into breast milk. Although the concentrations generated can be considered clinically insignificant, the use of this drug during breastfeeding is not recommended in the case of premature births, or in the first few weeks after birth due to the perceived risk of adverse effects on the cardiovascular system and kidneys, and not enough clinical experience.
When feeding an older child, the use of these drugs is possible if therapy is considered necessary for the mother and the child's condition is monitored in terms of the possible development of any adverse reactions.
Influence on the ability to drive vehicles and work with mechanisms
Does not affect.
Storage conditions
Store in a dry, dark place at a temperature not exceeding 25 ° C, out of the reach of children.
Shelf life
3 years. Do not use after the expiration date printed on the package.
Vacation conditions
On prescription.
Packaging
Enalapril 10mg Tablets. There are 10 tablets in a blister. 2 blisters are packed in a cardboard box together with an enclosed leaflet.