ENALAPRIL PILLS 20MG
ENALAPRIL PILLS 20MG - 50 tabs
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Mechanism of action
Enalapril is an angiotensin-converting enzyme (ACE) inhibitor used to treat hypertension, heart failure, and diabetic nephropathy. The clinical effect of enalapril is due to the suppression of ACE activity and, as a result, a decrease in the formation of angiotensin II from angiotensin I in tissues and circulating blood. The decrease in the concentration of angiotensin II, in turn, leads to vasodilation, a decrease in the secretion of aldosterone, an increase in the potassium content and the concentration of renin in the blood plasma.
The hemodynamic consequences of these changes are a reduction in total peripheral vascular resistance (OPS), systolic and diastolic blood pressure, an increase in cardiac output, a decrease in post- and preload on the myocardium.Enalapril expands the arteries to a greater extent than the veins, while there is no reflex increase in heart rate (HR). Reduces the degradation of bradykinin, increases the synthesis of prostaglandins. The antihypertensive effect is more pronounced with a high concentration of renin than with its normal or reduced level. The time of onset of the antihypertensive effect when taken orally is 1 hour, which reaches a maximum after 4-6 hours and lasts up to 24 hours.
In some patients, therapy for several weeks is necessary to achieve optimal blood pressure (BP). In chronic heart failure, a noticeable clinical effect is observed with prolonged treatment - 6 months or more. The duration of therapeutic action is dose-dependent.
The vasodilating and some diuretic effect of enalapril is also provided by the blockade of bradykinin destruction, which, in turn, stimulates the synthesis of vasodilating and renal prostaglandins. The increase in the content of bradykinin in the blood plasma and locally in the organs and tissues of the body blocks the pathological processes occurring in chronic heart failure in the myocardium, kidneys, and vascular smooth muscle. At the same time, there is an increase in coronary and renal blood flow, with prolonged use (from 3-4 weeks of treatment), left ventricular hypertrophy and myofibrils of resistive-type arteries decrease,dilatation of the left ventricle is slowed down and the blood supply to the ischemic myocardium improves, metabolism improves and the incidence of arrhythmias, which occur after the restoration of blood supply to the heart muscle, decreases.
Due to the moderate diuretic effect of the drug, intraglomerular hypertension is reduced, the development of glomerulosclerosis is slowed down and the risk of chronic renal failure is reduced.
Reducing blood pressure in the therapeutic range (not lower than 110/60 mmHg. Art.) Does not affect cerebral circulation: blood flow to the brain is maintained at the proper level and against the background of low blood pressure.
Sudden cancellation of treatment does not lead to the syndrome of "cancellation" (a sharp rise in blood pressure).
Enalapril does not cause metabolic disorders, does not affect glucose metabolism, does not increase the concentration of uric acid, does not change the profile of blood lipoproteins. Enalapril may reduce the hypokalemic effect of thiazide diuretics.
When ingestion enalapril is rapidly absorbed, the maximum concentration in the blood plasma is reached within 1 hour.
Enalapril is well absorbed from the gastrointestinal tract (GIT), a therapeutic effect is achieved within 1 hour (maximum 4-8 hours) after ingestion. Eating does not affect the absorption of the drug.
In patients with normal renal function, the equilibrium plasma concentration of enalapril is reached 2-3 days after the start of administration. Does not accumulate. Communication with proteins of a blood plasma about 50%.
Subjected to biotransformation in the liver with the formation of the active metabolite - enalaprilat, the maximum concentration of which is determined 4 hours after administration. Enalapril is eliminated mainly through the kidneys - 60% (20% - in the form of enalapril and 40% - in the form of enalaprilat), through the intestine - 33% (6% - in the form of enalapril and 27% - in the form of enalaprilat). The half-life (T1 / 2) is 11 h.
In patients with creatinine clearance (CK) of less than 30 ml / min, T1 / 2 enalapril increases. Reduced renal secretion of enalapril may increase hydrolysis to enalaprilat and increase extrarenal excretion of the drug.
The rate of hydrolysis of enalapril may decrease in patients with impaired liver function without reducing the therapeutic effect.
It penetrates the placental barrier. It is excreted in breast milk. Practically does not penetrate the blood-brain barrier. Does not accumulate in any tissues and organs.
- hypersensitivity to enalapril and other ACE inhibitors, as well as to any other component of the drug;
lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome;
history of angioedema edema associated with a previous use of ACE inhibitors, hereditary angioedema, or idiopathic angioedema;
simultaneous use of enalapril and aliskiren in patients with diabetes mellitus or renal insufficiency (QA less than 60 ml / min);
- age up to 18 years (efficacy and safety not established);
• breastfeeding period.
Carefully Enalapril Hexal should be used in patients with bilateral renal artery stenosis or arterial stenosis of a single kidney, primary hyperaldosteronism, hyperkalemia, or a condition after kidney transplantation; cerebrovascular diseases (including cerebrovascular insufficiency); coronary heart disease (CHD), recent myocardial infarction (up to 3 months); chronic heart failure, aortic and / or mitral stenosis (with impaired hemodynamic parameters), hypertrophic obstructive cardiomyopathy; hypovolemic condition (associated with long-term diuretic administration, the presence of a diet with salt restriction, diarrhea or vomiting, hemodialysis, after surgery); severe autoimmune systemic diseases of the connective tissue (including scleroderma, systemic lupus erythematosus); in the suppression of bone marrow hematopoiesis; with liver failure; in old age (over 65); diabetes; in case of renal failure (proteinuria - more than 1 g / day); with simultaneous use with immunosuppressants and diuretics; in patientsundergoing dialysis using high-flow membranes (such as AN69®); during desensitization; in patients of the Negroid race; with apheresis of low density lipoprotein.
According to the World Health Organization (WHO), undesirable effects are classified according to their development frequency as follows: very often (≥1 / 10), often (from ≥1 / 100 to <1/10), infrequently (from ≥1 / 1,000 to <1/100), rarely (from ≥1 / 10,000 to <1 / 1,000), very rarely (<1 / 10,000); frequency is unknown - according to the available data it was not possible to establish the frequency of occurrence.
Since the cardiovascular system
very often: dizziness;
often: pronounced decrease in blood pressure (including orthostatic), syncopal conditions, chest pain, arrhythmia, tachycardia, angina pectoris;
infrequently: palpitations, myocardial infarction, stroke, incl. secondary after the development of severe hypotension;
seldom: thromboembolism of a branch of a pulmonary artery, Raynaud's syndrome.
From the side of the central nervous system
often: headache, depression;
infrequently: dizziness, drowsiness, insomnia, irritability, confusion, paresthesia, vertigo;
seldom: unusual dreams, sleep disturbance.
On the part of the respiratory system
very often: cough;
often: shortness of breath;
infrequently: rhinorrhea, sore throat, hoarseness, bronchospasm (bronchial asthma);
rarely: lung infiltration, rhinitis, allergic alveolitis, (eosinophilic pneumonia).
From the digestive system
very often: nausea;
often: diarrhea, pain in the abdominal cavity, a violation of taste sensations;
infrequently: intestinal obstruction, pancreatitis, vomiting, dyspepsia, constipation, anorexia, peptic ulcer, dryness of the oral mucosa, irritable bowel syndrome;
rarely: stomatitis / aphthous ulcers, glossitis, liver failure, hepatitis (including liver necrosis), cholestasis, jaundice, increased activity of “liver” transaminases and plasma bilirubin;
very rarely: intestinal angioedema.
From the genitourinary system
infrequently: renal dysfunction, renal failure, proteinuria, impotence, increase in plasma urea concentration;
rarely: oliguria, gynecomastia.
On the part of the organ of vision
very often: blurred vision.
From the hematopoietic system and the lymphatic system
infrequently: anemia (including aplastic, hemolytic);
rarely: neutropenia, thrombocytopenia, agranulocytosis, inhibition of bone marrow hematopoiesis, pancytopenia, decrease in hemoglobin, decrease in hematocrit, lymphadenopathy, autoimmune diseases.
From the endocrine system
unknown frequency: syndrome of inadequate secretion of antidiuretic hormone.
often: urticaria, skin rash, rash, hypersensitivity reactions / angioedema (described angioedema of the face, extremities, lips, tongue, pharynx and / or larynx);
infrequently: increased sweating, pruritus, urticaria, alopecia;
rarely: erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), exfoliative dermatitis, pemphigus, erythroderma.
Symptom complex is described, which may include fever, myalgia and arthralgia, serositis, vasculitis, increased erythrocyte sedimentation rate, leukocytosis and eosinophilia, skin rash, positive test for antinuclear antibodies. Also described is a symptom complex, which includes flushing of the skin of the face, nausea, vomiting and arterial hypotension and may develop with the simultaneous use of ACE inhibitors and gold preparations (sodium aurothiomalate) intravenously.
very often: asthenia;
often: increased fatigue, hyperkalemia, increased concentration of creatinine in the blood;
infrequently: muscle twitching, tinnitus (tinnitus), hyperemia (redness of the skin), malaise, fever, dysphonia, hypoglycemia, hyponatremia, increased blood urea concentration.
The simultaneous use of ACE inhibitors with other agents acting on the renin-angiotensin-aldosterone system (RAAS) increases the risk of arterial hypotension, hyperkalemia and renal dysfunction (including acute renal failure).
As in the case of other ACE inhibitors and angiotensin II receptor antagonists, the combined use of enalapril and aliskiren is contraindicated in patients with diabetes mellitus or renal failure (CC less than 60 ml / min).
Mutual enhancement of action with simultaneous use of enalapril with other antihypertensives.
Simultaneous use with Nitroglycerin or other nitrates, or other vasodilators, tricyclic antidepressants, neuroleptics, general anesthetics, narcotic drugs leads to increased antihypertensive effect.
With the simultaneous use of enalapril with diuretics (thiazide or "loop" diuretics), an antihypertensive effect may be enhanced. The simultaneous use of enalapril and potassium-saving diuretics (such as spironolactone, eplerenone, triamterene, amiloride), potassium preparations or potassium-containing salt substitutes is not recommended, as well as the use of other drugs that increase the content of potassium in the blood plasma (eg, heparin).
The simultaneous use of nonsteroidal anti-inflammatory drugs (NSAIDs) (including selective cyclooxygenase-2 inhibitors (COX-2)) can weaken the antihypertensive effect of antihypertensive drugs, due to an increase in potassium in the blood plasma, which leads to reversible renal dysfunction, fluid retention . Thus, the antihypertensive effect of angiotensin II receptor antagonists or ACE inhibitors can be weakened by NSAIDs, including COX-2 inhibitors.
NSAIDs and ACE inhibitors have an additive effect on the increase in serum potassium, which can lead to a deterioration in renal function, especially in patients with impaired renal function. This effect is reversible.Combined use should be carried out with care at patients with a renal failure.
The simultaneous use of enalapril and lithium preparations is not recommended, since the concentration of lithium in the blood plasma increases and, consequently, an increase in its toxic effects is observed. With the simultaneous use of enalapril and lithium preparations, it is necessary to control the concentration of lithium in the blood plasma.
Simultaneous use with thiazide diuretics leads to an increase in the concentration of lithium salts in the blood plasma.
With the simultaneous use of enalapril with gold preparations for parenteral administration (sodium aurothiomalate), a symptom complex may occur, including facial flushing, nausea, vomiting, arterial hypotension.
Weaken the effect of drugs containing theophylline.
Simultaneous intake with insulin and hypoglycemic means for oral administration increases the risk of hypoglycemia.
Immunosuppressants, Allopurinol, cytotoxic drugs enhance hematotoxicity.
Drugs that inhibit bone marrow function increase the risk of developing neutropenia and / or agranulocytosis.
Ethanol enhances the antihypertensive effect of enalapril.
Enalapril can be used simultaneously with Acetylsalicylic acid (as an antiplatelet agent), thrombolytic agents and β-blockers. Concurrent use with other ACE inhibitors may increase the risk of developing hyperkalemia.Antacids can reduce the bioavailability of ACE inhibitors. Sympathomimetics can reduce the antihypertensive effect of ACE inhibitors.
How to take, the course of administration and dosage
Enalapril Hexal is administered orally, regardless of the meal, you need to drink plenty of fluids. Treatment with Enalapril Hexal is carried out for a long time. The dose of the drug should be adjusted in accordance with the patient's condition.
The drug Enalapril Hexal should be taken at the same time of the day, usually in the morning, but the administration of the drug Enalapril Hexal can be divided into two doses.
After taking the first dose, it is recommended to observe the patient and regularly measure blood pressure over the next few hours. If there is a high risk of arterial hypotension, then such a patient should be given the first dose of Enalapril Hexal in a hospital and observe the patient for at least 5 hours. During the observation, the patient should be in the "lying" position.
When you skip the next dose of Enalapril Hexal, you must take the missed dose as quickly as possible. If the next dose of Enalapril Hexal is coming, you should skip the reception of the forgotten dose and take the next dose on time. In no case should not double the dose.
Dosing regimen is selected individually.
Symptoms: headache, marked decrease in blood pressure, up to the development of collapse,myocardial infarction, acute cerebrovascular accident or thromboembolic complications, convulsions, stupor, tachycardia, heart palpitations, dizziness, bradycardia, feeling of heartbeat, kidney failure, cough, anxiety.
Treatment: symptomatic. The patient is transferred to the "lying" position with a low head. In mild cases, gastric lavage and ingestion of Activated carbon are shown, in more severe cases, measures aimed at stabilizing blood pressure: intravenous administration of 0.9% sodium chloride solution, plasma substitutes, connection of an artificial pacemaker with bradycardia resistant to drug therapy, hemodialysis (rate enalapril excretion averages 62 ml / min).
During treatment, it is necessary to conduct regular monitoring of blood pressure, heart rate and electrocardiogram, clinical analysis of blood, potassium, creatinine, urea, activity of “liver” enzymes in blood plasma, protein content in urine.
Care must be taken when prescribing to patients with reduced blood volume (as a result of diuretic therapy, while limiting salt intake, hemodialysis, diarrhea and vomiting) - the risk of sudden and pronounced decrease in blood pressure after even the initial dose of Enalapril Hexal is increased. Transient arterial hypotension is not a contraindication to continue treatment.drug Enalapril Hexal after stabilization of blood pressure. In case of repeated pronounced decrease in blood pressure, reduce the dose or discontinue the drug.
With the development of an excessive decrease in blood pressure of the patient is transferred to the "lying" position with a low head, if necessary, 0.9% sodium chloride solution and plasma-substituting drugs are administered.
The use of high-capacity dialysis membranes (including AN69®) increases the risk of an anaphylactic reaction. Correction of the dosing regimen in the days free from dialysis should be carried out depending on blood pressure.
Patients who took ACE inhibitors during apheresis of low-density lipoprotein (LDL) using dextran sulfate, in rare cases, developed anaphylactoid reactions. Therefore, this method should not be used in patients receiving ACE inhibitors.
You should carefully monitor patients with decompensated chronic heart failure, coronary heart disease, cerebrovascular diseases, in which a sharp decrease in blood pressure can lead to myocardial infarction, stroke or renal dysfunction.
Sudden cancellation of treatment does not lead to the syndrome of "cancellation" (a sharp rise in blood pressure).
In patients withcoronary heart disease orcerebrovascular insufficiency treatment should begin by prescribing low doses of the drug.
It should be borne in mind that patients withdiabetes mellitus with noralalbuminuria, the drug Enalapril Hexal is prescribed only after the determination of the functional renal reserve, with micro- and macroalbuminuria - without prior determination. In patients withreduced kidney function should reduce the single dose or increase the intervals between doses. In patients with diabetes, it is necessary to regularly monitor the concentration of glucose in the blood, especially against the background of hypokalemia.
During the period of treatment with Enalapril Hexal, it is possibleincrease in potassium in the blood serum, especially in patients with chronic renal failure, diabetes mellitus, with the simultaneous appointment of potassium-saving diuretics (spironolactone, eplerenone, triamterene, amiloride is not recommended) or potassium preparations. Such patients should be informed about the need to consult a doctor when muscle weakness and arrhythmia appear.
With the use of ACE inhibitors may develop dry cough. Coughing bouts are persistent, but quickly disappear after drug withdrawal. This feature should be considered in the differential diagnosis of cough. If necessary, treatment can be continued.
During the period of desensitization to wasp or bee venom in patients receiving Enalapril Hexal, hypersensitivity reactions may develop. In order to avoid such reactions, it is recommended to temporarily discontinue treatment with ACE inhibitors prior to each desensitization procedure.
Before surgery (including dentistry) it is necessary to warn the surgeon / anesthesiologist about the use of the drug Enalapril Hexal.
In rare cases, against the background of the applicationACE inhibitors cholestatic jaundice occurs, with the progression of which fulminant necrosis of the liver develops, sometimes with a fatal outcome. If jaundice occurs and the activity of “liver” transaminases increases with the use of the drug Enalapril Hexal, the treatment should be stopped. In patients taking ACE inhibitors, there have been cases of neutropenia / agranulocytosis, thrombocytopenia and anemia.
In patients with normal renal function in the absence of other complications, neutropenia rarely develops. Enalapril Hexal should be used with great caution in patients with connective tissue diseases (including systemic lupus erythematosus, scleroderma) who are simultaneously receiving immunosuppressive therapy, allopurinol or procainamide, as well as with a combination of these factors, especially for existing disorders of renal function. Such patients may develop severe infections that are not susceptible to intensive antibiotic therapy.
If patients still take Enalapril Hexal, it is recommended to periodically monitor leukocytes in the blood. The patient should be warned that in the event of any signs of infection, you should consult a doctor. In the event of angioedema of the face, it is usually sufficient to discontinue the therapy and prescribe an antihistamine to the patient.
Angioedema of the tongue, pharynx, or larynx may be fatal. When angioedema of the tongue, pharynx or larynx, which can lead to obstruction of the respiratory tract, it is necessary to immediately administer epinephrine (0.3-0.5 ml of epinephrine (adrenaline) solution subcutaneously in a 1: 1000 ratio) and maintain the airway patency (intubation or tracheostomy).
Among patients of the Negroid race, receiving therapy with an ACE inhibitor, the incidence of angioedema is higher than among patients of a different race. Patients with a history of angioedema, not associated with the use of ACE inhibitors, have an increased risk of developing angioedema when taking any ACE inhibitor.
There is no experience of using the drug in patients after kidney transplantation, so treatment with Enalapril Hexal is not recommended in patients after kidney transplantation.
Influence on ability to steer vehicles, mechanisms
When taking the drug Enalapril Hexal, caution should be exercised when driving and engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.
Light orange biconvex oblong tablets with lighter and darker patches with a smooth surface with a notch on one side and the inscription "EN 20" and a notch on the opposite side at an angle of 140 degrees ("Snap-tab").
List B. Store in a dry place inaccessible to children at a temperature of from 15 to 25 ° C.