Treatment of hypertension. Treatment of symptomatic heart failure. Short-term (6 weeks) treatment of haemodynamically stable patients within 24 hours of the onset of acute myocardial infarction. Treatment of kidney disease in patients with hypertension and type II diabetes with beginning nephropathy.
Composition:
1 tabl contains 5 mg, 10 mg or 20 mg lisinopril.
Action:
Angiotensin converting enzyme inhibitor. lisinopril is a peptidyl-dipeptidase inhibitor. It inhibits the activity of an angiotensin converting enzyme (ACE) that catalyzes the transformation of angiotensin I into a vasoconstrictive peptide - angiotensin II. Angiotensin II also stimulates the secretion of aldosterone through the adrenal cortex. Inhibition of ACE results in a decrease in angiotensin II concentration, which causes a weakening of vasodilator activity and a reduction of aldosterone secretion. The mechanism by which lisinopril lowers blood pressure is believed to mainly consist of inhibiting the renin-angiotensin-aldosterone system. The average absorption of lisinopril is approx. 25%. The food has no effect on the absorption of the drug. The maximum serum concentration is reached within approximately 7 hours. During multiple dosing, the effective half-life of the drug in the accumulation phase is approximately 12.6 hours. Lisinopril does not bind to serum proteins. It is not metabolised and is excreted completely unchanged in the urine. In patients with impaired renal function, excretion of lisinopril decreases depending on the degree of renal impairment. In patients with liver cirrhosis, the absorption of lisinopril is reduced, but due to decreased clearance, the exposure to the drug increases by approximately 50% compared to healthy subjects. In patients with circulatory insufficiency, the AUC is increased but the absorption of the preparation is reduced. Elderly patients have increased absorption and AUC.
Contraindications:
Hypersensitivity to lisinopril, other ingredients of the preparation or other ACE inhibitors. Angioneurotic edema caused by the use of ACE inhibitors. Hereditary or idiopathic angioneurotic edema. II and III trimester of pregnancy. Concomitant use with aliskiren in patients with diabetes mellitus or renal impairment (glomerular filtration rate, GFR <60 ml / min / 1.73 m2).
Precautions:
Do not start treatment with lisinopril in patients with acute myocardial infarction if there is a risk of further severe hemodynamic deterioration after using vasodilator - patients with systolic blood pressure ≤100 mm Hg or cardiogenic shock or patients with acute myocardial infarction and renal impairment ( blood creatinine> 177 μmol / l (or) proteinuria> 500 mg / 24 h). Particularly cautiously use in patients with impaired renal function; in patients with hepatic impairment (for jaundice or a significant increase in liver enzymes, lisinopril should be discontinued); in patients with bilateral renal artery stenosis or stenosis of the artery of the sole kidney, especially with concomitant hypertension (starting with low doses and carefully increasing the dose, discontinuing diuretics and monitoring renal function during the first weeks of treatment with lisinopril); in patients with severe renin-dependent hypertension, heart failure, at risk of hyperkalemia, in patients treated with diuretics, ischemic heart disease or cerebrovascular disease (treatment should be started and increased under strict medical supervision); with mitral stenosis and narrowing of the left ventricle outflow path, such as aortic stenosis or hypertrophic cardiomyopathy; in patients with vascular collagenosis treated with immunosuppressants, Allopurinol or procainamide, especially with a history of renal dysfunction. Caution in patients undergoing major surgery or during anesthesia with antihypertensive agents; in diabetic patients treated with oral antidiabetic agents or insulin, blood Glucose monitoring should be monitored during the first month of lisinopril use; in elderly patients with impaired renal function. Due to the risk of anaphylactic reactions in patients undergoing dialysis, high permeability membranes should not be used or an antihypertensive agent should be used from another group; in patients undergoing apheresis treatment with dextran sulphate, ACE inhibitors should be temporarily discontinued.In black patients, the risk of angioedema is higher than in patients of other breeds. In patients taking ACE inhibitors during desensitisation (eg Hymenoptera venom), anaphylactoid reactions have been observed. Lisinopril is not recommended in children for indications other than hypertension. Lisinopril is not recommended in children under 6 years of age and in children with severe renal impairment (GFR <30 ml / min / 1.73 m2). The concomitant use of ACE inhibitors, angiotensin II receptor antagonists or aliskiren increases the risk of hypotension, hyperkalaemia and renal dysfunction (including acute renal failure) - therefore, dual blocking of the RAA system is not recommended by concomitant use of ACE inhibitors, angiotensin II receptor antagonists or aliskiren. If the use of a dual RAA blockade is absolutely necessary, it should only be carried out under the supervision of a specialist, and the vital parameters of the patient, such as kidney function, electrolyte concentration and blood pressure should be closely monitored. In patients with diabetic nephropathy, ACE inhibitors and angiotensin II receptor antagonists should not be used concurrently.
Pregnancy and lactation:
It is not recommended during the first trimester of pregnancy. The use of the drug in the second and third trimester of pregnancy is contraindicated. The use of ACE inhibitors in the second and third trimester of pregnancy may cause worsening of renal function, oligohydramnios and delayed ossification of the skull in the fetus, in the newborn child - renal insufficiency, hypotension and hyperkalemia. If pregnancy is confirmed, ACE inhibitors should be discontinued immediately and alternative therapy initiated if necessary. It is not recommended to use the product during breastfeeding. It is recommended to use medications with a better known safety profile, especially when feeding newborns and premature babies.
Side effects:
Dosage:
Orally.Hypertension.The recommended starting dose is 10 mg; the usual maintenance dose is 20 mg once a day. If the desired effect is not achieved within 2-4 weeks, the dose may be increased. The maximum dose used in clinical trials was 80 mg. Hypertension in patients receiving diuretic therapy. When starting treatment with lisinopril, symptomatic hypotension may occur. 2-3 days before starting treatment with lisinopril, the diuretic should be discontinued. If the diuretic can not be discontinued, the starting dose of lisinopril is 5 mg; Renal function and serum potassium should be monitored. Subsequent doses of the drug are determined based on changes in blood pressure.Children (6-16 years). The recommended starting dose is 2.5 mg once a day in patients with a 20-50 kg and 5 mg in patients with b. ≥50 kg. The dose should be individually adjusted to the patient, up to 20 mg daily for patients with a 20-50 kg and 40 mg in patients with b. ≥50 kg. Doses> 0.61 mg / kg have not been studied in children. In children with impaired renal function, it is recommended to lower the initial dose and to prolong the interval between doses.Heart failure. Lisinopril should be used in combination with diuretics and, if possible, with digitalis preparations or beta-blockers. The starting dose is 2.5 mg once a day and should be given under close medical supervision to determine the initial effect on blood pressure. The dose of the drug should be increased: not more than 10 mg, not more often than every 2 weeks; up to the highest tolerated dose, up to a maximum of 35 mg once a day. In patients at high risk of symptomatic hypotension, such as hyponatraemic or hyponatremia-deficient patients, patients with circulating or receiving high-dose diuretic therapy should be corrected before starting treatment. Renal function and blood potassium should be monitored.Acute myocardial infarction. Patients should receive standard treatment, i.e. thrombolytics, Aspirin and β-blockers. At the same time, intravenous or transdermal glycerol trinitrate may be administered with lisinopril. Treatment should not be initiated in patients with systolic blood pressure <100 mmHg. The initial dose (within the first 3 days after the onset of an infarction) is 5 mg, subsequent doses are 5 mg after 24 hours, 10 mg after 48 hours and then 10 mg once a day.In patients with low systolic blood pressure (≤120 mmHg) at the beginning of treatment during the first 3 days after the infarction, a lower dose - 2.5 mg orally should be used. The maintenance dose is 10 mg once a day. If hypotension occurs (systolic blood pressure ≤100 mmHg), the maintenance dose can be reduced to 5 mg and temporarily to 2.5 mg if necessary. If hypotension persists, the drug should be discontinued. Treatment should be continued for 6 weeks, and then reassess the patient's condition.Renal complications of diabetes. In patients with hypertension and type II diabetes mellitus with nephropathy starting the recommended dose is 10 mg once a day. The dose can be increased to 20 mg once a day, if necessary, to achieve diastolic pressure below 90 mmHg.Patients with impaired renal function. Dosage should be determined based on creatinine clearance - initial doses: <10 ml / min (including dialysis patients) 2.5 mg; 10-30 ml / min 2.5-5 mg; 31-80 ml / min 5-10 mg. The dose may be gradually increased until the desired effect is achieved or up to a maximum dose of 40 mg / day. The drug should be used once a day, at the same time of the day; food has no effect on the absorption of the drug.