Enalapril Hexal pills 5 mg N20
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Active ingredients
Enalapril
Release form
Pills
Composition
1 tablet contains: Active substance: enalapril maleate 5 mg. Auxiliary substances: lactose monohydrate - 106 mg, magnesium carbonate - 71.645 mg, gelatin - 7.8 mg, crospovidone - 7.8 mg, magnesium stearate - 1.755 mg.
Pharmacological effect
Pharmacodynamics Enalapril is an angiotensin-converting enzyme (ACE) inhibitor used to treat hypertension, heart failure, 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 administered orally is 1 hour, which reaches a maximum after 4-6 hours and lasts up to 24 hours. Some patients need therapy for several weeks to achieve optimal blood pressure. 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 long-term use (from 3-4 weeks of treatment), left ventricular hypertrophy and myofibrils of resistive-type arteries decrease, left ventricular dilatation slows down and blood supply to the ischemic myocardium improves, metabolism improves and the incidence of arrhythmias improves, there is a marked after the restoration of blood supply to the heart muscle. 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 "cancel" (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. Pharmacokinetics Absorption When administered 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. Distribution 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%. Withdrawal Undergoes biotransformation in the liver with the formation of an 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 hours. 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.
Indications
arterial 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).
Contraindications
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); pregnancy. breastfeeding period. Enalapril Hexal should be used with caution when patients have 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 (includingscleroderma, 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 dialysis patients using high-flow membranes (such as AN69); during desensitization; in patients of the Negroid race; with apheresis of low density lipoprotein.
Precautionary measures
During treatment, psoriasis may worsen. During pheochromocytoma, propranolol can only be used after taking an alpha blocker. After a long course of treatment, propranolol should be discontinued gradually, under the supervision of a physician. during anesthesia, you must stop taking propranolol or find a remedy for anesthesia with minimal negative inotropic effects. The impact on the ability to drive vehicles and control mechanisms of patients whose activities require increased attention, the question of the use of propranolol on an outpatient basis should be addressed only after evaluating the individual response of the patient.
Use during pregnancy and lactation
The use of the drug Enalapril Hexal during pregnancy is not recommended. When pregnancy occurs, taking the drug Enalapril Hexal should be stopped immediately. ACE inhibitors can cause disease or death of the fetus or newborn when prescribed in the second and third trimesters of pregnancy. The use of ACE inhibitors during this period was accompanied by a negative effect on the fetus and newborn, including the development of arterial hypotension, renal failure, hyperkalemia and / or hypoplasia of the skull bones in the newborn. Perhaps the development of oligohydramnios, apparently due to a decrease in renal function of the fetus. This complication can lead to contracture of the limbs, deformation of the bones of the skull, including its facial part, and lung hypoplasia. When prescribing Enalapril Hexal, it is necessary to inform the patient about the potential risk to the fetus.Enalapril, which crosses the placenta, can be partially removed from the circulation of the newborn by peritoneal dialysis; theoretically, it can be removed through exchange transfusions. It is recommended to carefully monitor newborns and infants who have been exposed to prenatal exposure to the drug Enalapril Hexal to timely detect a pronounced decrease in blood pressure, oliguria, hyperkalemia and neurological disorders, possibly due to a decrease in renal and cerebral blood flow while reducing blood pressure caused by ACE inhibitors. In oliguria, it is necessary to maintain blood pressure and renal perfusion by administering appropriate fluids and vasoconstrictor drugs. Enalapril and enalaprilat are excreted in breast milk in trace concentrations, with the use of the drug in therapeutic doses, the effect on the child is unlikely. However, the use of the drug is contraindicated in breastfeeding premature babies and in the first few weeks after birth due to the risk of side effects in the newborn from the side of the cardiovascular system and kidneys, as well as due to the lack of sufficient clinical experience. If necessary, the appointment of the drug Enalapril Hexal nursing mothers should decide on the termination of breastfeeding.
Dosage and administration
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 in time. In no case should not double the dose. Dosing regimen is selected individually.
Side effects
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 is very common: 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. Of the central nervous system often: headache, depression; infrequently: dizziness, drowsiness, insomnia, irritability, confusion, paresthesia, vertigo; seldom: unusual dreams, sleep disturbance. 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). On the part of 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. On the part of the urogenital system infrequently: renal dysfunction, renal failure, proteinuria, impotence, an increase in the concentration of urea in the blood plasma; rarely: oliguria, gynecomastia. On the part of the organ of vision very often: blurred vision.On the part of 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. On the part of the endocrine system, the frequency is unknown: the syndrome of inadequate secretion of antidiuretic hormone. Allergic reactions are 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. Others 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.
Overdose
Symptoms: headache, marked reduction in blood pressure, up to the development of collapse, myocardial infarction, acute cerebrovascular accident or thromboembolic complications, convulsions, stupor, tachycardia, palpitations, heart palpitations, dizziness, bradycardia, heartbeat, kidney failure, heart failure, kidney failure, heart failure, kidney failure, heart rate, kidney failure, heart failure, renal failure, an inadequate heartbeat, renal failure, an inadequate heartbeat, kidney failure, heart failure, renal insufficiency, heartbeat, kidney failure, heart failure, renal failure, an inadequate heartbeat, renal insufficiency, heartbeat, kidney failure, heart rate, kidney failure, heart failure, kidney failure, heart failure, kidney failure, heart failure, kidney failure, heart failure 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).
Interaction with other drugs
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 . 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, accordingly, its toxic effects are enhanced. 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 face 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.
special instructions
It is used with extreme caution in patients with autoimmune diseases, diabetes mellitus, abnormal liver function, severe aortic stenosis, subaortic muscular stenosis of unknown origin, hypertrophic cardiomyopathy, with loss of fluids and salts. In the case of prior 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 salt. During long-term treatment with enalapril, it is necessary to periodically monitor the pattern of peripheral blood. Sudden discontinuation of enalapril does not cause a sharp increase in blood pressure. During surgical interventions during the period of treatment with enalapril, hypotension may develop, which should be corrected by administering a sufficient amount of fluid.