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Pharmacological properties

lisinopril reduces the level of angiotensin ii and aldosterone in blood plasma, while increasing the concentration of the vasodilator bradykinin. lisinopril causes a decrease in OPS and hell, cardiac output may increase with constant heart rate, and renal blood flow may also increase.

Blood pressure begins to decrease 1 hour after ingestion, the maximum antihypertensive effect is achieved after 6 hours. The duration of lisinopril (about 24 hours) depends on the dose. With prolonged treatment, the effectiveness of the drug does not decrease. With a sharp cessation of treatment, large differences in blood pressure (withdrawal syndrome) do not occur.

Although the primary effect of lisinopril is associated with RAAS, the drug is effective in hypertension, which is characterized by a low renin content.

In addition to a direct decrease in blood pressure, lisinopril reduces albuminuria due to changes in the histology and hemodynamics of the glomerular apparatus of the kidneys. In controlled studies in patients with diabetes mellitus, neither fluctuations in the level of glucose in the blood nor the increase in hypoglycemia were detected.

It plays a positive role in restoring the function of damaged endothelium in patients with hyperglycemia.

Pharmacokinetics

Suction. With oral administration of lisinopril Cmax in plasma is reached after about 7 hours. Given the amount of drug excreted in the urine, the average absorption rate of lisinopril is about 25% when a dose of 5–80 mg is taken. Variability of indicators between patients can be from 6 to 60%. The absolute bioavailability of lisinopril is reduced to about 16% in patients with NYHA grade II – IV heart failure. Eating does not affect the absorption of lisinopril.

Distribution. In addition to binding to ACE, lisinopril does not bind to other plasma proteins. As animal studies show, lisinopril in small amounts penetrates the BBB.

Lisinopril is not metabolized and excreted exclusively by the kidneys unchanged. After increasing the dose, effective T½ is 12.6 hours. The clearance of lisinopril is about 50 ml / min in healthy volunteers. After removal of a significant amount of free active substance, a slower elimination of the fraction associated with ACE follows.

Impaired liver function. In patients with cirrhosis, the absorption of lisinopril slows down depending on impaired liver function by about 30% (as determined by excretion in the urine). On the other hand, its excretion decreases and leads to an increase in the effectiveness of lisinopril by 50%.

Impaired renal function. With impaired renal function, the excretion of lisinopril excreted by the kidneys decreases. This decrease has clinical significance only when the glomerular filtration level is 30 ml / min. If creatinine clearance is 30–80 ml / min, the average AUC increases by only 13%. If creatinine clearance is 5-30 ml / min, the average AUC increases by 4.5 times compared to the norm. Lisinopril can be removed by dialysis.

Heart failure. In the presence of heart failure, the effect of lisinopril increases (AUC increases by about 25%). On the other hand, the absolute bioavailability of lisinopril is reduced to about 16% in patients with heart failure.

Children. The pharmacokinetic profile of lisinopril was studied in 29 patients aged 6–16 years with hypertension, whose glomerular filtration rate was 30 ml / min / 1.73 m2. When taking a dose of 0.1-0.2 mg / kg body weight, the constant concentration of lisinopril in the blood plasma reached within 6 hours, as well as the degree of absorption based on excretion in the urine, were about 28%. Values ​​differed from those obtained in adult patients. AUC and C Valuesmax in children in this study coincide with the values ​​obtained in adults.

Elderly patients.In elderly patients, the level of lisinopril is usually higher due to impaired renal function, AUC is approximately 60% higher than in younger patients.

Indications

Essential Ag. heart failure (symptomatic treatment). acute myocardial infarction (short-term treatment (6 weeks) for hemodynamically stable patients no later than 24 hours after acute myocardial infarction). treatment of initial nephropathy in patients with type II diabetes mellitus, ag.

Application

Inside 1 time per day at the same time, regardless of food intake.

Essential hypertension

Initial dose. The recommended starting dose is usually 10 mg. Patients with very active RAAS (especially with renovascular hypertension, excessive excretion of sodium chloride and / or dehydration, cardiac decompensation, or severe hypertension) may experience an excessive decrease in blood pressure after taking the first dose. Therefore, at the beginning of treatment, such patients should be under the supervision of a doctor, the initial recommended dose is 2.5-5 mg. Patients with renal failure also need to reduce the initial dose (table).

Maintenance dose. The usual effective maintenance dose is 20 mg once daily. If when applying the prescribed dose within 2-4 weeks the desired therapeutic effect is not achieved, then the dose can be increased. The maximum daily dose should not exceed 80 mg.

If patients take diuretics, 2-3 days before starting lisinopril therapy, these drugs should be discontinued. If this is not possible, the initial dose of lisinopril should not exceed 5 mg / day, and it is recommended that the doctor monitor the condition of the patient after taking the first dose, since symptomatic hypotension may develop (maximum effect appears 6 hours after taking the drug).

At the beginning of treatment with lisinopril, arterial hypotension may develop. This is most likely in patients already using diuretics. Since dehydration and / or excessive excretion of sodium chloride is possible in these patients, the drug should be used with caution.

Heart failure. Lisinopril can be used simultaneously with diuretics and / or digitalis preparations. In this case, previously, if possible, the dose of the diuretic should be reduced. The initial dose of lisinopril, equal to 2.5 mg, can be gradually increased to a maintenance dose of 5–20 mg / day.

The recommended dose increase ratio after 2 weeks is not more than 10 mg.

The maximum daily dose of lisinopril is 35 mg / day.

Before starting treatment with lisinopril and during treatment, you should regularly monitor blood pressure, indicators of kidney function, the concentration of potassium and sodium in the blood, in order to avoid the development of arterial hypotension and the associated renal dysfunction.

Diabetic nephropathy. The daily dose for patients with non-insulin-dependent diabetes mellitus with hypertension is 10 mg at a time. If necessary, the dose can be increased to 20 mg / day in order to achieve optimal diastolic blood pressure (should be 90 mm RT. Art.).

Acute myocardial infarction. In the case of the use of lisinopril in the first 24 hours after myocardial infarction, the initial dose should be 5 mg, 5 mg should be re-prescribed after 24 hours, 10 mg after 48 hours, then the maintenance dose is 10 mg / day. The duration of treatment is 6 weeks. If necessary, treatment is carried out according to the usual scheme in such cases, for example, thrombolytic drugs, acetylsalicylic acid and β-adrenergic receptor blockers are prescribed.

With low systolic blood pressure (≤120 mmHg) or during the first 3 days after a heart attack, the drug is indicated in a low dose (2.5 mg / day), after which, if the patients condition allows, treatment can be continued at a higher dose. In the case of the development of arterial hypotension (systolic blood pressure ≤100 mm RT.Art.) it is recommended to reduce the maintenance dose to 5 mg / day, if necessary, with an intermediate reduction to 2.5 mg / day.

An indication for stopping treatment with lisinopril is ongoing arterial hypotension, when 1 h after the use of the drug, systolic blood pressure remains 90 mm Hg. Art.

With the development of heart failure, it is necessary to follow the dosage instructions outlined in the corresponding section.

Patients with impaired renal function. Since the elimination of lisinopril is carried out by the kidneys, the initial dose depends on creatinine clearance indicators, the maintenance dose depends on the clinical response and is selected by regularly measuring indicators of kidney function, potassium and sodium concentrations in the blood.

Creatinine clearance, ml / min Initial dose, mg / day
31–70 5–10
10–30 2,5–5
10 (including patients on hemodialysis) * 2,5*

* You can stop taking lisinopril during dialysis.

The dose and frequency of taking the drug is determined by the parameters for lowering blood pressure.

The maximum dose of lisinopril is 40 mg / day.

Use in elderly patients. In clinical trials, there was no difference in the efficacy or safety of treatment with lisinopril depending on age. Since elderly people often show a decrease in renal function, the dose indicated in renal failure should be determined.

Use in patients with a kidney transplant. There is no experience with lisinopril in patients immediately after a kidney transplant, therefore, treatment with Diroton is not recommended for such patients.

Contraindications

Hypersensitivity to the active or excipients of the drug. history of angioedema associated with previous treatment with other APF inhibitors. hereditary or idiopathic angioedema. stenosis of the aorta or mitral valve or hypertrophic cardiomyopathy with impaired hemodynamics. primary hyperaldosteronism. renal artery stenosis (bilateral or unilateral). cardiogenic shock. a condition with unstable hemodynamics after acute myocardial infarction. ii or iii trimester of pregnancy. use in patients undergoing hemodialysis using high-flow membranes (e.g. an 69). plasma creatinine level 220 μmol / l.

Side effects

As a rule, weakly expressed and short-term, discontinuation of treatment is necessary in extreme cases.

The following side effects may be noted, which are grouped by classes of organ systems and frequency of occurrence.

Organ system classes Side effects
Disorders from the blood and lymphatic system Inhibition of bone marrow function, anemia, thrombocytopenia, leukopenia, neutropenia, agranulocytosis, hemolytic anemia, lymphadenopathy
Immune System Disorders Autoimmune disease, angioedema
Endocrine disorders Inadequate Secretion Antidiuretic Hormone Syndrome
Disorders of nutrition and metabolism Hypoglycemia
Disorders of the nervous system Dizziness, headache, paresthesia, vertigo, taste disturbance, fainting
Mental disorders Mood changes, sleep disturbances, confusion, depression
Cardiological disorders Heart palpitations, myocardial infarction, possibly as a complication of excessive hypotension in high-risk patients
Vascular disorders Orthostatic

Tags: Lisinopril