ATC categoryCardiology, angiology
ATC subcategoryAngiotensin-converting enzyme (ACE) inhibitors
Each tablet contains:
active ingredient: lisinopril (as dihydrate) – 5 mg;
excipients: sodium starch glycolate, magnesium stearate, microcrystalline cellulose.
ACE inhibitor, reduces the formation of angiotensin II from angiotensin I. Reduction of angiotensin II leads to a direct reduction of aldosterone release. It reduces the degradation of bradykinin and increases the synthesis of prostaglandins. It reduces the total peripheral vascular resistance, blood pressure (BP), preload, pressure in the pulmonary capillaries, causing an increase in cardiac output and increase tolerance to myocardial stress in patients with chronic heart failure. Artery expands to a greater extent than veins. Some effects are explained by the influence on the tissue renin-angiotensin system. With prolonged use reduces myocardial hypertrophy and arterial wall of the resistive type. It improves blood flow to ischemic myocardium.
ACE inhibitors prolong the life expectancy of patients with chronic heart failure, slow the progression of left ventricular dysfunction in patients with myocardial infarction without clinical manifestations of heart failure. Antihypertensive effect starts after approximately 6 hours and stored for 24 hours. Duration of the effect is also dependent on the dose. Onset of action -. 1 hour maximum effect is determined after 6-7 hours. When hypertension effect noted in the first days after the start of treatment, stable effect develops in 1-2 months. With a sharp lifting of the drug was observed pronounced increase in blood pressure.
In addition to lowering blood pressure lisinopril reduces albuminuria. Patients with hyperglycemia contributes to the normalization of the function of the damaged glomerular endothelium.
Lisinopril does not affect the blood glucose concentration in diabetic patients and leads to increased incidence of hypoglycemia.
Distribution. Almost does not bind to plasma proteins. The maximum plasma concentration (90 ng / mL) was reached after 7 hours. The permeability of the blood-brain and placental barrier is low.
Metabolism. Lisinopril is not biotransformed in the body.
Withdrawal. Excreted by the kidneys unchanged. The half-life is 12 hours.
For patients with chronic heart failure of absorption and clearance of lisinopril reduced.
For patients with renal insufficiency lisinopril concentrations several times greater than the concentration in the blood plasma of the volunteers, and there is an increase in the time to achieve maximum blood plasma concentration and increase the half-life.
Elderly patients drug concentration in plasma and area under the curve in a 2-fold greater than in younger patients.
Chronic heart failure (in a combination therapy for the treatment of patients taking drugs digitalis and / or diuretics);
Early treatment of acute myocardial infarction (within 24 hours with stable hemodynamics to maintain these parameters and prevent left ventricular dysfunction and heart failure);
Diabetic nephropathy (insulin-dependent reduction of albuminuria in patients with normal blood pressure and insulin dependent patients with hypertension).
Full effect is usually 2-4 weeks from start of treatment that should be considered when increasing the dose. When there is insufficient clinical effect of the drug can be combined with other antihypertensive agents.
If the patient has received prior treatment with diuretics, the use of these drugs should be discontinued for 2-3 days prior to the use of lisinopril. If this is not feasible, then the initial dose of lisinopril should not exceed 5 mg per day. In this case, after the first dose recommended medical supervision for several hours (maximum action is reached after about 6 hours), since it may be a marked reduction in blood pressure.
If renovascular hypertension or other conditions with increased activity of the renin-angiotensin-aldosterone system is also advisable to assign a low initial dose – 2.5-5 mg per day, under close medical supervision (control of blood pressure, kidney function, potassium concentration in blood serum). Maintenance dose, continuing strict medical control, should be determined depending on the dynamics of blood pressure.
In renal failure because the lisinopril excreted through the kidneys, the initial dose should be determined according to the creatinine clearance, then according to the reaction, should be set in a maintenance dose of frequent monitoring of renal function, potassium, sodium in serum.
When hypertension is a persistent long-term maintenance of 10-15 mg / day therapy.
In chronic heart failure – start with 2.5 1 mg once a day, followed by increasing doses of 2.5 mg every 3-5 days before the usual supporting daily dose of 5-20 mg. The dose should not exceed 20 mg per day.
In the elderly often observed more pronounced prolonged hypotensive effect, which is associated with a decrease in the rate of excretion of lisinopril (recommended to start treatment with 2.5 mg / day).
Acute myocardial infarction (in combination therapy)
On the first day – 5 mg orally, followed by 5 mg every other day, 10 mg every two days and then 10 mg 1 time per day. In patients with acute myocardial infarction drug use for at least 6 weeks.
At the beginning of treatment or during the first 3 days after acute myocardial infarction in patients with low systolic blood pressure (120 mmHg or lower) it is necessary to appoint a lower dose – 2.5 mg. In the case of reducing blood pressure (systolic blood pressure less than or equal to 100 mm Hg), the daily dose is 5 mg can, if necessary, temporarily reduced to 2.5 mg. In the case of long pronounced reduction in blood pressure (systolic blood pressure below 90 mm Hg more than 1 hour), lisinopril treatment should be discontinued.
Patients with non-insulin dependent diabetes mellitus 10 mg lisinopril applied 1 time a day. The dose may, if necessary, be increased to 20 mg 1 time per day in order to achieve values of the diastolic blood pressure below 75 mm Hg in a sitting position. Patients with insulin-dependent diabetes is the same dosage, in order to achieve the diastolic blood pressure below 90 mm Hg values in a sitting position.
Tablets are contain lactose, therefore the drug should not be taken by patients with rare hereditary disorders such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption. Precautions expressed violations kidney function, bilateral renal artery stenosis or stenosis of the artery only kidneys with progressive azotemia, condition after kidney transplantation, renal failure, azotemia, hyperkalemia, aortic stenosis, hypertrophic obstructive cardiomyopathy, primary hyperaldosteronism, arterial hypotension, cerebrovascular diseases (including .ch cerebrovascular insufficiency), ischemic heart disease, coronary artery disease, autoimmune systemic diseases of connective tissue (including scleroderma, systemic lupus erythematosus).; inhibition of medullary hematopoiesis; a diet with sodium restriction: hypovolemic conditions (including as a result of diarrhea, vomiting); in old age.
The most common side effects: dizziness, headache (in 5-6% of patients), fatigue, diarrhea, dry cough (3%), nausea, vomiting, orthostatic hypotension, skin rashes, chest pain (1.3%).
Other side effects (frequency <1%)
On the part of the immune system: (0.1%), angioedema (face, lips, tongue, larynx or epiglottis, the upper and lower limbs).
Cardio-vascular system: marked reduction of blood pressure, orthostatic hypotension, renal failure, cardiac arrhythmias, heart palpitations.
On the part of the central nervous system: fatigue, drowsiness, muscle jerking of the limbs and lips.
From hemopoiesis system: leucopenia, neutropenia, agranulocytosis, thrombocytopenia, prolonged treatment – a slight decrease in hemoglobin concentration and hematocrit, erythropenia.
Laboratory indicators: hyperkalemia, azotemia, hyperuricemia, hyperbilirubinemia, increased activity of “liver” enzymes, especially when there is a history of kidney disease, diabetes, and renovascular hypertension.
Rare side effects (less than 1%)
Cardio-vascular system: palpitations; tachycardia; myocardial infarction; cerebrovascular stroke in patients with an increased risk of disease, as a result of pronounced reduction in blood pressure.
From the digestive system: dry mouth, anorexia, dyspepsia, changes in taste, abdominal pain, pancreatitis, hepatocellular or cholestatic jaundice, hepatitis.
For the skin: rash, increased sweating, itching, alopecia.
From the urinary system: renal failure, oliguria, anuria, acute renal failure, uremia, proteinuria.
Immune system: a syndrome including acceleration of erythrocyte sedimentation rate (ESR), arthralgia and appearance of antinuclear antibodies.
On the part of the central nervous system: asthenic syndrome, mood lability, confusion, reduced potency.
Other: myalgia, fever, disturbance of fetal development.
Lisinopril crosses the placenta. No data on the penetration of lisinopril passes into breast milk. For the period of drug treatment should be abolished breastfeeding.
Symptoms (occur when receiving a single dose of 50 mg and above): marked reduction of blood pressure; dry mouth, drowsiness, urinary retention, constipation, anxiety, irritability.
Treatment: symptomatic therapy, intravenous fluids, controlling blood pressure, fluid and electrolyte balance and normalize the latter.
Lisinopril can be removed from the body by hemodialysis.
Lisinopril reduces potassium excretion from the body in the treatment of diuretic.
It requires special care while applying the drug with:
– Potassium-sparing diuretics (spironolactone, triamterene, amiloride), potassium, Vice-salt containing potassium (increased risk of hyperkalemia, especially with impaired renal function), so that they can jointly appoint only on the basis of individual judgment of the prescribing physician with regular monitoring of potassium levels serum and renal function.
Caution may be used together:
– Diuretics: with the additional administration of a diuretic to a patient receiving lisinopril usually comes an additive antihypertensive effect – the risk of significant decrease in blood pressure;
– With other antihypertensive agents (additive effect);
– A non-steroidal anti-inflammatory drugs (. Indomethacin, etc.), estrogens and adrenostimulyatorov – reduced antihypertensive effect of lisinopril;
– Lithium (lithium excretion may be reduced, so you should regularly monitor the concentration of lithium in blood serum);
– With antacids and colestyramine – reduce absorption in the gastrointestinal tract.
Alcohol enhances the effect of the drug.
Most often pronounced decrease blood pressure occurs at lower fluid volume caused by the diuretic therapy, reducing the amount of salt in the diet, dialysis, vomiting or diarrhea. In patients with chronic heart failure with simultaneous renal failure or without her, perhaps marked reduction in blood pressure. It is often diagnosed in patients with severe stage of chronic heart failure as a result of application of high doses of diuretics, hyponatremia or impaired renal function. In these patients, treatment with lisinopril should start under close medical supervision (with caution in selection of dosage and diuretics).
Such rules must be followed in the appointment of patients with ischemic heart disease, cerebrovascular insufficiency, in which a sharp decrease in blood pressure can lead to heart attack or stroke.
The transient hypotensive response is not a contraindication to receiving the next dose of the drug.
In the application of lisinopril in some patients with chronic heart failure but with normal or low blood pressure may experience a decrease in blood pressure, which is usually not a cause for discontinuation of treatment.
Prior to treatment lisinopril, if possible, should be to normalize the concentration of sodium and / or compensate for the lost volume of liquid carefully control the action of lisinopril on the initial dose of the patient.
In the case of renal artery stenosis (especially in bilateral stenosis or in the presence of artery stenosis single kidney) and circulatory failure due to lack of sodium and / or liquid Lisinopril use may lead to renal function, acute renal failure, which is usually irreversible after discontinuation of the drug.
In acute myocardial infarction
The application of standard therapy (thrombolytics, acetylsalicylic acid, beta-blockers). Lisinopril may be used in conjunction with intravenous or transdermal nitroglycerin therapeutic application systems.
Surgery / general anesthesia
With extensive surgical interventions, as well as the use of other drugs that cause a decrease in blood pressure, lisinopril, blocking the formation of angiotensin II of, can cause unpredictable pronounced reduction in blood pressure.
In elderly patients, the same dose results in a higher concentration of drug in the blood, so extra care is required when determining dosage.
Since it is impossible to eliminate the potential risk of agranulocytosis, requires periodic monitoring of blood picture. In applying the drug in a dialysis polyacryl-nitrile membrane can occur anaphylactic shock, it is recommended that a different type of dialysis membrane or appointment of other antihypertensive agents.
Effects on ability to drive vehicles and mechanisms
No data on the effect of lisinopril on the ability to drive vehicles and mechanisms applied in therapeutic doses, however, be aware that you may experience dizziness, so be careful.
1 blister packet with 24 tablets in the cardboard box.
3 years. Do not use after the expiration date.
To be dispensed with prescription.
Store at a room temperature (15-250C), in a dry place, out of the reach of children. Protect from light.