Index of drugs

Hypertension. Symptomatic heart failure. Short-term (6-week) treatment of haemodynamically stable patients within 24 hours of the onset of acute myocardial infarction. Kidney disease in patients with hypertension and type II diabetes mellitus with nephropathy beginning.

1 tabl contains 5 mg, 10 mg or 20 mg of lisinopril dihydrate.

Angiotensin converting enzyme inhibitor. The angiotensin convertase is an enzyme that converts angiotensin I to angiotensin II, which has a strong vasodilator effect and increases blood pressure. Angiotensin II also increases the secretion of aldosterone by the adrenal cortex. Inhibition of angiotensin converting activity results in a decrease in angiotensin II concentration in the blood plasma and a reduction in the secretion of aldosterone, which may cause a small increase in serum potassium. After oral administration, the maximum concentration in the blood occurs after about 7 hours (this time is prolonged in patients with acute myocardial infarction), the absorption is about 25%. Lisinopril does not bind to serum proteins other than the circulating angiotensin converting enzyme (ACE). Lisinopril is not metabolized and is excreted completely unchanged in the urine. For multiple dosing, the effective half-life at steady-state is 12.6 h. Hepatic impairment in patients with cirrhosis results in decreased absorption (around 30%), but increased exposure (about 50%) compared to healthy subjects due to decrease in clearance. In subjects with severe hepatic impairment (creatinine clearance 5-30 ml / min) a 4.5-fold increase in mean AUC was observed. Patients with heart failure are more exposed to lisinopril than healthy subjects (125.5% increase in AUC), but the absorption is reduced (on average by 60%). Elderly patients have increased blood levels and higher AUC (approximately 60%) compared to younger patients.

Hypersensitivity to the components of the preparation, other angiotensin converting enzyme inhibitors or any of the excipients. Occurrence of angioedema in the past due to the use of ACE inhibitor. Hereditary or idiopathic angioneurotic edema. Second or third 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).

The probability of hypotension is higher in the case of decreased intravascular volume (as a result of diuretic therapy, salt-restricted diet, dialysis, diarrhea, vomiting), severe renin-dependent hypertension, heart failure with or without renal insufficiency (particularly more severe heart failure, which reflects the use of high doses of loop diuretics, hyponatremia, renal dysfunction), ischemic heart disease or cerebrovascular disease; in this group of patients, starting treatment and adjusting doses should be carried out under close medical supervision. In some patients with heart failure, with normal or low blood pressure, there may be an additional reduction in blood pressure after administration of lisinopril; if hypotension becomes symptomatic, it may be necessary to reduce the dose or discontinue treatment with lisinopril. Do not start treatment with lisinopril in patients with acute myocardial infarction if there is a risk of further severe haemodynamic deterioration following the use of a vasodilator. Caution should be exercised when administering lisinopril to patients with mitral valve stenosis and stenosis of the left ventricle outflow tract as is the case with aortic stenosis or hypertrophic cardiomyopathy. In patients with heart failure and concomitant renal insufficiency, initiation of treatment with ACE inhibitors may cause further deterioration of renal function (usually reversible).In patients with bilateral renal artery stenosis or stenosis of the artery supplying blood to one kidney that has increased urea and serum creatinine, treatment should be started with a small dose and gradually increased, and if necessary, the dose should be reduced or discontinued (and or) lisinopril. In acute myocardial infarction, treatment with lisinopril should not be initiated in patients with renal impairment (creatinine> 177μmol / l and / or proteinuria> 500 mg / 24 h); if renal dysfunction develops during treatment, withdrawal of lisinopril should be considered. In patients who develop angioneurotic edema of the face, limbs, lips, tongue, glottis (or the entire larynx), the drug should be immediately discontinued, appropriate treatment should be instituted and the patient monitored until the symptoms disappear completely (black patients are more likely to develop it) ). In patients with dialysis using membranes with high permeability (eg, AN 69) anaphylactoid reactions have been reported; in these patients, other dialysis membranes or other antihypertensive agents should be used. Anaphylactoid reactions have also been reported in patients during LDL-scintigraphy with dextran sulfate or during desensitisation (eg Hymenoptera venom); in these patients, lisinopril should be temporarily discontinued. In case of jaundice or a significant increase in liver enzymes, lisinopril should be discontinued and appropriate measures should be taken. Special care should be taken in patients with collagenosis, using immunosuppressants, taking Allopurinol or procainamide or in patients who coexist with these factors, especially in the case of pre-existing renal dysfunction (periodic monitoring of white blood cell counts is recommended). In black patients, the drug may be less effective. In patients treated with lisinopril, anesthesia with agents with antihypertensive properties, there is a greater risk of hypotension. Due to the risk of hyperkalemia, the drug should be used with caution in patients with renal insufficiency, diabetes mellitus as well as in the case of concomitant use of potassium-sparing diuretics, potassium supplements or a potassium salt substitute, drugs that increase the concentration of potassium (eg heparin); if you need to use these medicines at the same time, you should check the potassium levels. Simultaneous use of lithium is not recommended. There are limited data on efficacy and safety in pediatric patients> 6 years with hypertension, but no data on use in other indications. Use in indications other than hypertension is not recommended. Use in children with severe renal impairment is not recommended (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.

Use in the first trimester of pregnancy is not recommended. The preparation is contraindicated in the second and third trimester of pregnancy. In women planning pregnancy, an alternative antihypertensive treatment should be started with an established safety profile during pregnancy. If during treatment it turns out that the patient is pregnant, the drug should be discontinued immediately and, if necessary, alternative therapy should be started. The use of the drug during breastfeeding is not recommended.

Orally.Hypertension (the drug can be used alone or in combination with other antihypertensive agents).Adults: the usual starting dose is 10 mg.In patients with high activity of the renin-angiotensin-aldosterone system (especially with renovascular hypertension, salt deficiency and / or intravascular volume depletion, decompensated heart failure or severe hypertension) the starting dose should be reduced to 2.5-5 mg and start treatment under strict medical supervision. The usual maintenance dose is 20 mg / day. If the desired effect is not achieved within 2-4 weeks, the dose can be increased. The maximum dose used in long-term, controlled clinical trials was 80 mg / day. In patients concomitantly treated with diuretics, if possible, the diuretic should be discontinued 2-3 days before treatment with lisinopril. For patients who can not take their diuretic, treatment with lisinopril should be started at a dose of 5 mg. Renal function and blood potassium should be monitored. If necessary, treatment with a diuretic may be resumed. Subsequent doses of lisinopril should be determined on the basis of changes in the pressure value.Hypertension in children and adolescents aged 6-16: the recommended starting dose is 2.5 mg once a day in patients with a 20-50 kg (maximum dose is 20 mg / day) and 5 mg once a day in patients with an average of 50 kg (the maximum dose is 40 mg / day). In children and adolescents, no doses greater than 0.61 mg / kg (or above 40 mg) were tested. In children with impaired renal function, a lower starting dose or a longer interval between doses should be considered.Heart failure (the drug can be used in combination with diuretics, digitalis glycosides and ß-blockers). The starting dose is 2.5 mg once a day, which should be given under close medical supervision. The dose should be increased gradually, by no more than 10 mg once, no more frequently than every 2 weeks. The maximum dose is 35 mg once a day.Acute myocardial infarctionPatients should receive standard treatment, i.e. thrombolytics, antiaggregates, ß-blockers; together with lisinopril, intravenous or transdermal administration of glycerol trinitrate. Treatment with lisinopril should be started within 24 hours after the onset of infarction symptoms. Treatment should not be started if the systolic blood pressure is <100 mmHg. The initial dose of lisinopril is 5 mg orally, followed by 5 mg after 24 h, 10 mg after 48 h and then 10 mg once a day. Patients with a systolic blood pressure of 120 mmHg or less at the beginning of treatment during the first 3 days after the infarction should receive 2.5 mg orally. The maintenance dose is 10 mg / day. If hypotension occurs (blood pressure systolic 100 mmHg or less), 5 mg may be given as a daily maintenance dose, temporarily reducing it to 2.5 mg if necessary. In case of prolonged hypotension (systolic blood pressure <90 mmHg for more than 1 hour) the preparation should be discontinued. Treatment should be continued for 6 weeks, and then reassess the patient's condition. Patients who develop symptoms of heart failure should continue to take the medicine.Renal complications in diabetes. In patients with hypertension, type II diabetes mellitus with nephropathy starting the dose is 10 mg once a day, if necessary, the dose can be increased to 20 mg once a day to achieve diastolic blood pressure <90 mmHg.
In patients with renal impairment, the dose should be determined according to the creatinine clearance: creatinine clearance 31-80 ml / min 5-10 mg per day; clearance 10-30 ml / min 2.5-5 mg per day; clearance below 10 ml / min (including dialysis patients) 2.5 mg daily. The dose can be gradually increased depending on your blood pressure (the maximum daily dose is 40 mg).
Use once a day, every day at the same time. Food does not affect the absorption of the drug.