Enalapril pills 20 mg 20 pcs
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Active ingredients
Enalapril
Release form
Pills
Composition
Enalapril maleate 20 mg. Auxiliary substances: corn starch, lactose (milk sugar), microcrystalline cellulose, colloidal silicon dioxide (Aerosil A – 300), calcium stearate.
Pharmacological effect
ACE inhibitor. It is a prodrug from which the active metabolite enalaprilat is formed in the body. The mechanism of antihypertensive action is believed to be associated with competitive inhibition of ACE activity, which leads to a decrease in the rate of angiotensin I conversion to angiotensin II (which has a pronounced vasoconstrictor effect and stimulates the secretion of aldosterone in the adrenal cortex). plasma by eliminating negative feedback during renin release and a direct decrease in aldosterone secretion. In addition, enalaprilat appears to have an effect on the kinin-kallikrein system, preventing the breakdown of bradykinin. Due to its vasodilator action, it reduces the congestion resistance (afterload), the wedging pressure in the pulmonary capillaries (preload) and the resistance in the pulmonary vessels; increases cardiac output and exercise tolerance. In patients with chronic heart failure, long-term use of enalapril increases exercise tolerance and reduces the severity of heart failure (assessed by NYHA criteria). Enalapril in patients with mild to moderate heart failure slows its progression and also slows the development of left ventricular dilatation. When left ventricular dysfunction enalapril reduces the risk of major ischemic outcomes (including the incidence of myocardial infarction and the number of hospitalizations for unstable angina).
Pharmacokinetics
When ingested, about 60% is absorbed from the gastrointestinal tract. Simultaneous food intake does not affect absorption. Metabolized in the liver by hydrolysis with the formation of enalaprilat, thanks to the pharmacological activity of which the hypotensive effect is realized. The binding of enalaprilat to plasma proteins is 50-60% .T1 / 2 enalaprilat is 11 h and increases in renal failure. After ingestion, 60% of the dose is eliminated by the kidneys (20% as enalapril, 40% as enalaprilat), 33% is excreted through the intestine (6% as enalapril, 27% as enalaprilat).After the on / in the introduction of enalaprilat 100% excreted by the kidneys unchanged.
Indications
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 hospitalization for unstable angina.
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
Angioedema in history, bilateral renal artery stenosis or renal artery stenosis of a single kidney, hyperkalemia, porphyria, simultaneous use with aliskiren in patients with diabetes or renal dysfunction (CC less than 60 ml / min), pregnancy, lactation (breastfeeding), childhood and adolescence to 18 years, hypersensitivity to enalapril and other ACE inhibitors.
Dosage and administration
When ingestion, the initial dose is 2.5-5 mg 1 time / day. The average dose is 10–20 mg / day in 2 divided doses. When administered intravenously, it is 1.25 mg every 6 hours. To detect excessive hypotension in patients with sodium deficiency and dehydration due to previous diuretic therapy, patients receiving diuretics, as well as renal failure impose an initial dose of 625 mg.With an inadequate clinical response, this dose can be repeated after 1 hour and continue treatment at a dose of 1.25 mg every 6 hours. The maximum daily dose for oral administration is 80 mg.
Side effects
On the part of the central nervous system and peripheral nervous system: dizziness, headache, fatigue, fatigue; very rarely when used in high doses - sleep disorders, nervousness, depression, imbalance, paresthesia, tinnitus. On the part of the cardiovascular system: orthostatic hypotension, syncope, heartbeat, pain in the heart area; very rarely when used in high doses - hot flashes. From the digestive system: nausea; rarely - dry mouth, abdominal pain, vomiting, diarrhea, constipation, abnormal liver function, increased activity of hepatic transaminases, increased concentration of bilirubin in the blood, hepatitis, pancreatitis; very rarely when used in high doses - glossitis. From the hematopoietic system: rarely - neutropenia; in patients with autoimmune diseases - agranulocytosis. From the urinary system: rarely - renal dysfunction, proteinuria. From the respiratory system: dry cough. From the reproductive system: very rarely used in high doses - impotence. Dermatological reactions: very rarely use in high doses - hair loss. Allergic reactions: rarely - skin rash, angioedema. Others: rarely - hyperkalemia, muscle cramps.
Overdose
Symptoms: a pronounced decrease in blood pressure up to the development of collapse, myocardial infarction, acute cerebral circulatory disorders or thromboembolic complications, convulsions, stupor. Treatment: the patient is transferred to a horizontal position with a low head. In mild cases, gastric lavage and ingestion of a saline solution are shown, in more severe cases, measures aimed at stabilizing blood pressure: intravenous saline, plasma substitutes, if necessary, angiotensin II administration, hemodialysis (enalaprylate elimination rate averages 62 ml / min ).
Interaction with other drugs
With simultaneous use with immunosuppressants, cytostatics, the risk of developing leukopenia increases. With simultaneous use of potassium-saving diuretics (including spironolactone, triamterene, amiloride), potassium preparations, salt substitutes and dietary supplements containing potassium, hyperkalemia may develop (especially in patients with impaired renal function), becauseACE inhibitors reduce aldosterone levels, which leads to a delay of potassium in the body against the background of limiting the excretion of potassium or its supplemental intake in the body. When opioid analgesics and anesthetics are used simultaneously, the antihypertensive effect of enalapril is enhanced. . There is a risk of hypokalemia. Increased risk of impaired renal function. When used simultaneously with azathioprine, anemia may develop, which is due to the inhibition of erythropoietin activity under the influence of ACE inhibitors and azathioprine. reduce the antihypertensive effect of enalapril. It is not fully established whether acetylsalicylic acid reduces therapeutic efficacy ngibitorov ACE in patients with coronary artery disease and heart failure. The nature of this interaction depends on the course of the disease. Acetylsalicylic acid, inhibiting COX and prostaglandin synthesis, can cause vasoconstriction, which reduces cardiac output and worsens the condition of heart failure patients receiving ACE inhibitors. When beta-blockers, methyldopes, nitrates are used simultaneously, calcium channel blockers, hydralazine, prazosin may increase antihypertensive action. When used simultaneously with NSAIDs (including with indomethacin), reduce tsya antihypertensive effect of enalapril, apparently by inhibiting NSAIDs influenced prostaglandin synthesis (which is believed to play a role in the development of hypotensive effect of ACE inhibitors). The risk of developing impaired renal function increases; hyperkalemia is rarely observed. If insulin is used at the same time, hypoglycemic agents of sulfonylurea derivatives may develop hypoglycemia. If ACP inhibitors and interleukin-3 are used simultaneously, there is a risk of arterial hypotension.use with clomipramine has been reported to increase the action of clomipramine and the development of toxic effects. When used simultaneously with co-trimoxazole, cases of hyperkalemia are described. When used simultaneously with lithium carbonate, the concentration of lithium in the blood serum increases, which is accompanied by symptoms of lithium intoxication. the antihypertensive effect of enalapril, which can lead to a significant increase in blood pressure, the development of hypertensive crisis. with simultaneous use with procainamide may increase the risk of leukopenia. When used with enalapril, the effect of drugs containing theophylline is reduced. There are reports of the development of acute renal failure in patients after kidney transplantation while using cyclosporin. enalapril and its concentration increases in the blood plasma. It is possible that a decrease in the effectiveness of antihypertensive drugs at the same time It is used with erythropoietins. When used simultaneously with ethanol, the risk of arterial hypotension is increased.
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, arterial hypotension may develop, which should be corrected by administering a sufficient amount of liquid.control mechanisms. Care must be taken when driving or doing other work that requires special attention, because dizziness may occur, especially after taking the initial dose of enalapril.