Enzix Tablets 10mg 2.5mg N30
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Active ingredients
Indapamide + Enalapril
Release form
Pills
Composition
Indapamide pills, film-coated white, round, biconvex (5 pieces in a blister) .1 tab. Indapamide 2.5 mg Auxiliary substances: lactose monohydrate - 76.96 mg, povidone K30 - 2.82 mg, crosspovidone - 0.88 mg, magnesium stearate - 0.88 mg , sodium lauryl sulfate - 0.44 mg, talc - 3.52 mg. The composition of the shell of pills of indapamide: hypromellose - 1.7222 mg, macrogol 6000 - 0.3445 mg, talc - 1.903 mg, titanium dioxide (E171) - 0.4303 mg. biconvex, with a risk on one side (5 pieces in a blister) .1 tab. enalapril maleate 10 mg Supplementary e substances: lactose monohydrate - 125 mg Magnesium Carbonate 84.6 mg Gelatin - 9.2 mg crospovidone - 9.2 mg magnesium stearate - 2 mg.
Pharmacological effect
An antihypertensive drug that contains two drugs in the same package: the ACE inhibitor, enalapril, and the diuretic, indapamide, Enalapril, the ACE inhibitor. It is a prodrug: Enalapril metabolite - enalaprilat has pharmacological activity. Inhibits the formation of angiotensin II from angiotensin I, which leads to a decrease in the content of aldosterone. At the same time, OPSS, systolic and diastolic blood pressure, post- and preload on the myocardium decrease. Enalapril dilates the arteries to a greater extent than the veins (with no reflex increase in heart rate), reduces bradykinin degradation, increases prostaglandin synthesis. The antihypertensive effect is more pronounced at high plasma renin levels than at normal or decreased levels. blood flow. Reducing blood pressure in therapeutic limits does not affect cerebral circulation, the blood flow in brain vessels is maintained at a sufficient level and against a background of reduced pressure. With prolonged use of enalapril, myocardial left ventricle and myocytes of resistive arteries decrease, which prevents progression of heart failure and slows dilatation of the left ventricle. Enalapril improves blood supply to the ischemic myocardium. Reduces platelet aggregation. It has some diuretic effect. The action of enalapril occurs after 1 h, reaches a maximum after 4-6 h and lasts up to 24 h. Indapamide is a thiazide-like diuretic with moderate strength and prolonged action.It has moderate saluretic and diuretic effects, which are associated with the blockade of reabsorption of sodium ions, chlorine, hydrogen, and to a lesser extent potassium ions in the proximal tubules and the cortical segment of the nephron's distal tubule. norepinephrine and angiotensin II; increase in the synthesis of prostaglandins with vasodilating activity; inhibition of calcium current in vascular smooth muscle cells. It helps to reduce left ventricular hypertrophy. At therapeutic doses, it does not affect lipid and carbohydrate metabolism (including in patients with concomitant diabetes mellitus). The antihypertensive effect of indapamide develops at the end of the first / beginning of the second week with regular use of the drug. After a single dose, the antihypertensive effect lasts for 24 hours. The simultaneous use of enalapril and indapamide leads to an increase in the antihypertensive effect of enalapril.
Pharmacokinetics
Enalapril AbsorptionAfter ingestion, about 60% is absorbed in the gastrointestinal tract. A simultaneous meal does not affect the absorption of enalapril. Cmax enalapril in plasma is reached after 1-2 h, enalaprilat after 3-4 h. The bioavailability of the drug is 40%. Distribution Binding to plasma proteins for enalaprilat is 50-60%. Enalaprilat easily passes through histohematogenous barriers, excluding BBB, small the amount penetrates the placental barrier and is excreted in breast milk. Metabolism Enalapril is rapidly and completely hydrolyzed in the liver to form an active metabolite, enalaprilat, which is a more active ACE inhibitor than enalapril. Excretion of T1 / 2 enalaprilat - about 11 hours. With urine output 60% (20% in the form of enalapril and 40% in the form of enalaprilat), with feces 33% (6% in the form of enalapril and 27% in the form of enalaprilat). Pharmacokinetics in In special clinical situations, in chronic renal failure, enalapril cumulation occurs when filtration decreases below 10 ml / min. Enalapril is removed during hemodialysis (62 ml / min) and peritoneal dialysis. Indapamide Absorption After ingestion, it is quickly and completely absorbed from the gastrointestinal tract. Meal somewhat slows down the rate of absorption, but does not affect its fullness.Cmax is achieved within 1-2 hours after ingestion. Bioavailability is high (93%). The distribution of Css is established after 7 days of regular intake. Binding to plasma proteins is 79%. Also associated with elastin smooth muscle of the vascular wall. It has significant Vd, penetrates through histohematogenous barriers (including placental) and into breast milk. Metabolism Metabolizes in the liver. Excretion of T1 / 2 averages 14-18 hours. With urine 60-80% is excreted in the form of metabolites (unchanged) about 5% is eliminated), with feces - 20%. Not cumulative. Pharmacokinetics in special clinical situations. Patients with renal insufficiency do not change pharmacokinetics.
Indications
- arterial hypertension.
Contraindications
Enalapril - a history of angioedema associated with treatment with ACE inhibitors; - porphyria; - pregnancy; - lactation; - children and adolescents under 18 years of age (efficacy and safety have not been established); - hypersensitivity to enalapril and other ACE inhibitors. Enalapril should be used with caution in case of primary hyperaldosteronism, bilateral renal artery stenosis, single kidney artery stenosis, hyperkalemia, a condition after kidney transplantation, conditions associated with BCC (including vomiting, diarrhea), with aortic stenosis, mitral stenosis (with hemodynamic disorders), idiopathic hypertrophic subaortic stenosis, systemic connective tissue diseases, CHD, cerebrovascular diseases, diabetes mellitus, renal failure (proteinuria - more 1 g / day), with liver failure, in patients on a salt-restricted diet or on hemodialysis, while taking it with immunosuppressants and saluretics, in elderly patients (over 65) ). Indapamide-anuria; - hypokalemia; - severe liver failure (including with encephalopathy); - severe renal failure; - pregnancy; - lactation period; - children and adolescents under 18 years of age (efficacy and safety have not been established); - simultaneous administration of drugs prolonging the QT interval; - hypersensitivity to the drug, other sulfonamide derivatives or other components of the drug. Indapamide should be used with caution in diabetes mellitus at the stage of decompensation, hyperuricemia (especially accompanied by gout and urate nephrolithiasis).
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 drug is contraindicated for use during pregnancy and lactation. If you need to use the drug Enzix during lactation, breastfeeding should be discontinued. For newborns and infants who have been exposed to intrauterine effects of ACE inhibitors, it is recommended that you carefully monitor for the timely detection of marked reduction in blood pressure, oliguria, hyperkalemia and neurological disorders, which may develop as a result of 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 injecting appropriate fluids and vasoconstrictor agents.
Dosage and administration
Enzix and Enzix Duo1 tab. enalapril (10 mg) and 1 tab. indapamide (2.5 mg) is taken orally in the morning at the same time. Depending on the dynamics of blood pressure indicators, the dose of enalapril can be increased up to 2 times a day. Enzix Duo Forte1 tab. enalapril (20 mg) and 1 tab. indapamide (2.5 mg) is taken orally in the morning at the same time. Depending on the dynamics of blood pressure indicators, the dose of enalapril can be increased up to 2 times a day. The maximum daily dose of enalapril is 40 mg, indapamide is 2.5 mg. In case of mild to moderate renal failure (CK 30-80 ml / min), enalapril dose should be 5-10 mg / day.
Side effects
EnalaprilS side of the central nervous system and peripheral nervous system: headache, dizziness, weakness, insomnia,anxiety, confusion, fatigue, drowsiness (2-3%); in some cases, when used in high doses, nervousness, depression, paresthesias. On the respiratory system: unproductive dry cough, interstitial pneumonitis, bronchospasm / bronchial asthma, shortness of breath, rhinorrhea, pharyngitis. of sight, tinnitus. From the digestive system: dry mouth, anorexia, dyspeptic symptoms (nausea, diarrhea or constipation, vomiting, abdominal pain), intestinal obstruction, pancreatitis, abnormal liver function and biliary excretion Lenia, hepatitis (hepatocellular or cholestatic), jaundice, increased liver transaminases, giperbilirubinemiya.So the cardiovascular system: an excessive fall in blood pressure, orthostatic collapse; rarely - chest pain, angina pectoris, myocardial infarction (usually associated with a pronounced decrease in blood pressure), arrhythmias (atrial brady- or tachycardia, atrial fibrillation), palpitations, thromboembolism of the pulmonary artery branches, pain in the heart area, fainting. , hyponatremia, hypoglycemia (in patients with diabetes mellitus). From the hematopoietic system: rarely - decrease in hematocrit and hemoglobin concentration, thrombocytopenia, neutropenia, agranulocytosis (in patients with autoimmune diseases), eosinophilia, increase in ESR. From the urinary system: impaired renal function, proteinuria, hypercreatininemia, increased urea content. From the reproductive system: decreased libido, hot flashes, reduced potency. Dermatological reactions: alopecia, photosensitization. Allergic reactions: skin rash, angioneurotic face, face sensitization. extremities, lips, tongue, glottis and / or larynx, dysphonia, erythema multiforme, exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, pemphigus, pruritus, urticaria, gray Zit, vasculitis, myositis, arthralgia, arthritis, stomatitis, glossitis; very rarely - intestinal angioedema. Indapamide For the central nervous system and peripheral nervous system: asthenia, nervousness, headache, dizziness, drowsiness, vertigo, insomnia, depression, paresthesia; rarely - increased fatigue, weakness, malaise,muscle spasm, tension, irritability, anxiety. On the digestive system: nausea, anorexia, dry mouth, gastralgia, vomiting, diarrhea or constipation, feeling of discomfort in the abdomen, pancreatitis are possible. side of the respiratory system: cough, pharyngitis, sinusitis, rhinorrhea; rarely - rhinitis. Cardio-vascular system: orthostatic hypotension, ECG, arrhythmia, palpitations, characteristic of hypokalemia. On the urinary system: an increase in the incidence of infection, nocturia, polyuria, urea nitrogen in plasma, hypercreatininemia. metabolism: hypokalemia, hyponatremia, hypochloremic alkalosis, hypercalcemia, glycosuria, sweating, weight loss. From the reproductive system: decreased potency, decreased libido. Allergic reactions: to naya rash, hives, itching, bleeding vaskulit.Prochie: flu-like symptoms, chest pain, back pain, infection, exacerbation of SLE.
Overdose
EnalaprilSymptomas: a pronounced decrease in blood pressure up to the development of collapse, myocardial infarction, acute cerebral circulation disorder or thromboembolic complications, convulsions, stupor. In mild cases, gastric lavage and ingestion of a saline laxative are indicated. In more severe cases, measures are taken to stabilize blood pressure: intravenous saline, plasma substitutes, angiotensin II, hemodialysis is possible. in some cases - an excessive decrease in blood pressure, dizziness, drowsiness, confusion, respiratory depression. Patients with cirrhosis of the liver may develop hepatic coma. Treatment: gastric lavage and / or administration of activated carbon, correction of water and electrolyte balance, symptomatic therapy. There is no specific antidote.
Interaction with other drugs
Enalapril The simultaneous use of enalapril and indapamide leads to an increase in the antihypertensive effect of enalapril. With simultaneous use of enalapril with NSAIDs,including selective COX-2 inhibitors, antipyretic analgesics may reduce the anti-hypertensive effect of enalapril. In some cases, patients with impaired renal function receiving NSAIDs, including selective COX-2 inhibitors, can lead to a further deterioration in renal function. These changes are reversible. The anti-hypertensive effect of enalapril is enhanced by diuretics, beta-adrenergic blockers, and others, and others, and methydopes, nitrates, and blockers of slow calcium channels of the dihydropyridine series, hydralazine, and prazosin. hyperkalemia. Enalapril weakens the effect of drugs containing theophylline. Immunosuppressants, allopurinol, cytostatics increase the hematotoxicity of anal App. Drugs that cause bone marrow depression, increase the risk of developing neutropenia and / or agranulocytosis. Enalapril helps slow lithium clearance (while using enalapril with lithium salts, control of lithium in plasma is shown.) Combined use of ACE inhibitors and hypoglycemic agents (insulin, hypoglycemic drugs (insulin, hypoglycemic drugs, oral hypoglycosis) drugs) may enhance the hypoglycemic effect of the latter with the risk of hypoglycemia. This is most common during the first 3 weeks of combined use, as well as in patients with renal insufficiency. In patients with diabetes who are receiving hypoglycemic drugs for oral administration and insulin, control of blood glucose level is necessary, especially during the first month of joint use with ACE inhibitors. Symptomocomplex, including facial flushing, nausea, vomiting and arterial hypotension, is described in rare cases with the joint use of gold preparations for parenteral use (sodium aurothiomalate) and ACE inhibitors (enalapril). Ethanol enhances the hypotensive effect of enalapril. Indapamide With simultaneous n When indapamide is used with saluretics, cardiac glycosides, gluco- and mineralocorticoids, tetracosactids, amphotericin B (w / w), and laxative drugs, the risk of hypokalemia increases. With simultaneous administration of indapamide with cardiac glycosides, it increasesthe probability of the development of glycosidic intoxication; with calcium preparations - hypercalcemia; with metformin - aggravation of lactic acidosis is possible. Indapamide helps to slow lithium clearance and thereby increase its concentration in blood plasma. Astemizol, erythromycin (w / w), pentamidine, sultoprid, terfenadine, vincamine, class I antiarrhythmic drugs (quinidine, disopyramide) class III (amiodarone, bretily, sotalol) when taken on the background of idapamide can lead to the development of arrhythmias of the pirouet type. NPVS, GCS, tetracosactide, sympathomimetics reduce the hypotensive effect of indapamide; baclofen - enhances. The combination of indapamide with potassium-sparing diuretics may be effective in some patients, but this does not completely preclude the development of hypo- or hyperkalemia, especially in patients with diabetes mellitus and renal failure. The ACE inhibitors while used with indapamide increase the risk of developing hypotension and / or acute renal failure (especially if there is a renal artery stenosis). Indapamide increases the risk of developing impaired renal function. EC with simultaneous use with iodine-containing contrast agents in high doses (dehydration of the body). Before using iodine-containing contrast agents in patients taking indapamide, it is necessary to restore fluid loss. Tricyclic antidepressants and antipsychotic drugs increase the hypotensive effect of indapamide and increase the risk of orthostatic hypotension. If you use indapamide with cyclosporine at the same time, it increases the effect of hypercreatininemia. coumarin or indandion) due to increased concentration of clotting factors Ia by reducing the BCC and enhance their production by the liver (may require dose correction) .Indapamid enhances the effect of non-depolarizing muscle relaxants.
special instructions
EnalaprilPatients need medical observation for 2 hours after taking the initial dose of the drug and an additional 1 hour until blood pressure stabilizes. Patients with decreased BCC (as a result of diuretic therapy, while limiting salt intake, hemodialysis, diarrhea,vomiting) when using enalapril (as well as other ACE inhibitors), even at the initial dose, the risk of a sudden and pronounced decrease in blood pressure increases. Transient arterial hypertension is not a contraindication for continuing treatment with the drug after stabilization of blood pressure. In the case of repeated pronounced decrease in blood pressure, reduce the dose or discontinue the drug. The use of high-strength dialysis membranes increases the risk of an anaphylactic reaction. In days free from dialysis, the dosage regimen should be adjusted depending on the level of blood pressure. Care should be taken to monitor the condition of patients with severe heart failure, IHD and vascular diseases of the brain. In such patients, a sharp decrease in blood pressure can lead to myocardial infarction, stroke, or impaired renal function. Sudden withdrawal of the drug does not lead to a sharp increase in blood pressure. Before testing the function of the parathyroid glands, enalapril should be canceled. appropriate treatment. Before surgical intervention (including dentistry), the patient must warn the surgeon / anesthesiologist about the use of ACE inhibitors. Before and during treatment with inhibitors PF requires periodic monitoring of blood pressure, blood counts (hemoglobin, potassium, creatinine, urea, liver transaminase activity), protein in the urine. the content of potassium and creatinine. Against the background of taking indapamide, the concentration of potassium, sodium, magnesium in blood plasma, pH, glucose, uric acid and atochnogo nitrogen. The most careful control is indicated for cirrhosis of the liver (especially with edema or ascites - the risk of developing metabolic alkalosis, which increases the manifestations of hepatic encephalopathy), coronary heart disease, heart failure, as well as in elderly patients. Patients with an increased QT interval on an ECG (congenital or developed on the background of any pathological process) also belong to an increased risk group.The first determination of potassium concentration in the blood should be carried out during the first week of treatment. Hypercalcemia during indapamide may be due to previously undiagnosed hyperparathyroidism. In patients with diabetes, it is extremely important to control blood glucose levels, especially in the presence of hypokalemia. Significant dehydration can lead to acute development renal failure (reduced glomerular filtration). Patients need to compensate for the loss of water and at the beginning of treatment carefully monitor kidney function. Indapamide can give a positive result during doping control. Patients with arterial hypertension and hyponatremia (due to receiving diuretics) should stop taking diuretics 3 days before starting taking ACE inhibitors (with If necessary, diuretic administration can be resumed a little later), or in such cases, initial low doses of ACE inhibitors are prescribed. When prescribing indapamide, it should be noted that sulfonamide derivatives may exacerbate the course of SC.Patient use. Pediatrics The efficacy and safety of enalapril and indapamide in children and adolescents under the age of 18 years have not been established. vehicles and occupations of potentially hazardous activities that require increased concentration and psychomotor speed, since dizziness is possible, especially after taking the initial dose of the drug.