Lisinoton, tablets 5 mg 28 pcs

Lysinoton is an ACE inhibitor and reduces the formation of angiotensin II from angiotensin I. Reduction of angiotensin II leads to a direct reduction of aldosterone release. Reduces bradykinin degradation and increases prostaglandin synthesis.

Recreases RPS, BP, preload, pulmonary capillary pressure, causes an increase in the minute blood volume and increases myocardial tolerance to exercise in patients with chronic heart failure. Dilates arteries more than veins.

Some effects are explained by the effect on tissue renin-angiotensin systems. Long-term use reduces myocardial hypertrophy and resistive arterial wall hypertrophy. It improves the blood supply to the ischemic myocardium.

The ACE inhibitors prolong life expectancy in patients with chronic heart failure and slow the progression of left ventricular dysfunction in patients who have had myocardial infarction without clinical manifestations of heart failure.

After a single dose of the drug, the antihypertensive effect develops in 1 hour, reaches a maximum in 6-7 hours and lasts for 24 hours. The duration of the effect also depends on the size of the dose taken. In arterial hypertension, the effect is noted in the first days after the start of treatment, a stable effect develops after 1-2 months.

When the drug is abruptly withdrawn, no pronounced increase in BP was observed.

Lysinoton decreases albuminuria. In patients with hyperglycemia it normalizes the function of the damaged glomerular endothelium. It does not affect the blood glucose concentration in patients with diabetes mellitus and does not lead to increased incidence of hypoglycemia.

Indications

Active ingredient

Composition

The tablets are round, biconvex, white, incised.

The active ingredient:

Excipients:

How to take, the dosage

The drug is taken orally.

In patients with arterial hypertension who are not receiving other hypotensive agents, 5 mg once daily is prescribed. If there is no effect, the dose is increased every 2-3 days by 5 mg to an average therapeutic dose of 20-40 mg/day (an increase in dose over 40 mg/day usually does not lead to further BP reduction). The usual daily maintenance dose is 20 mg. The maximum daily dose is 40 mg.

The full effect usually develops in 2-4 weeks from the beginning of treatment, which should be taken into account when increasing the dose. If the clinical effect is insufficient, the drug may be combined with other hypotensive agents.

If the patient received prior treatment with diuretics, their administration should be stopped 2-3 days before starting Lisinoton. If diuretics cannot be stopped, the starting dose of Lisinoton should not exceed 5 mg/day.

In this case, a physician monitoring for several hours after the first dose is recommended (maximum effect reached after about 6 hours), because a pronounced decrease in BP may develop.

In renovascular hypertension or other conditions with increased RAAS activity it is also reasonable to prescribe lower initial dose – 2.5-5 mg/day under increased medical control (BP control, renal function, serum potassium concentration). The maintenance dose should be determined depending on the BP dynamics.

In case of renal insufficiency, since lisinopril is excreted by kidneys, the initial dose should be determined depending on the CKR, then a maintenance dose should be established according to the response with frequent monitoring of renal function, serum potassium and sodium concentrations.

In persistent arterial hypertension, long-term maintenance therapy with the drug at a dose of 10-15 mg/day is indicated.

In chronic heart failure, the initial dose is 2.5 mg once daily with subsequent dose increases by 2.5 mg after 3-5 days to the usual maintenance daily dose of 5-20 mg. The daily dose should not exceed 20 mg.

Elderly patients often have a more pronounced long-term hypotensive effect due to decreased excretion rate of lisinopril. Therefore in this category of patients it is recommended to start treatment with a dose of 2.5 mg/day.

In acute myocardial infarction (as part of combined therapy) 5 mg is prescribed in the first day, then 5 mg every other day, 10 mg every two days and then 10 mg once daily. In patients with acute myocardial infarction, the drug should be used 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) the preparation should be prescribed in dose 2.5 mg.

If the blood pressure decreases (systolic BP ≤100 mmHg) while taking Lisinoton the daily dose of 5 mg can be temporarily reduced to 2.5 mg.

In case of prolonged marked BP decrease (systolic BP <90 mmHg for more than 1 hour), treatment with Lisinoton should be discontinued.

Interaction

When used concomitantly with diuretics, lisinopril decreases potassium excretion.

Particular caution should be exercised when prescribing Lisinoton with potassium-saving diuretics (spironolactone, triamterene, amiloride), potassium, salt substitutes containing potassium because the risk of hyperkalemia increases, especially with impaired renal function.

These combinations should therefore only be prescribed based on the individual decision of the physician, with regular monitoring of serum potassium levels and renal function.

Additive antihypertensive effect develops when used concomitantly with diuretics and other antihypertensive drugs.

Concomitant use with NSAIDs (including indomethacin), estrogens, and adrenostimulants decreases the antihypertensive effect of lisinopril.

Concomitant use with lithium may decrease excretion of lithium, therefore serum lithium concentration should be monitored regularly.

Simultaneous use with antacids and colestiramine decreases gastrointestinal absorption of lisinopril.
Simultaneous use with ethanol increases the effect of lisinopril.

Special Instructions

The most common cause of marked BP decline is a decrease in fluid volume caused by diuretic therapy, salt reduction, dialysis, diarrhea, or vomiting.

In chronic heart failure with or without concomitant renal failure, a marked decrease in BP may occur. More often pronounced BP decrease is detected in patients with severe stage of chronic heart failure, as a consequence of using high-dose diuretics, hyponatremia or impaired renal function.

In these patients, treatment with Lisinoton should be started under strict medical supervision (with caution to select the dose of the drug and diuretics).

The same rules should be followed when prescribing Lisinoton in patients with coronary heart disease, cerebrovascular insufficiency, in whom a rapid decrease in BP may lead to myocardial infarction or stroke.

Transient hypotensive reaction is not a contraindication for the next dose of the drug.
When using Lisinoton, some patients with chronic heart failure but with normal or lower BP may experience a decrease in BP, which is usually not a reason to discontinue treatment.

Before starting treatment with Lisinoton, if possible, sodium concentration should be normalized and/or lost fluid volume should be replenished, and the effect of the initial dose of Lisinoton on the patient should be carefully monitored.

In cases of renal artery stenosis (particularly with bilateral stenosis or in the presence of artery stenosis of the single kidney), as well as circulatory failure due to lack of sodium and/or fluid, use of Lisinoton may lead to impaired renal function, acute renal failure, which is usually irreversible after drug withdrawal.

In acute myocardial infarction, standard therapy (thrombolytics, acetylsalicylic acid, beta-adrenoblockers) is indicated. It is possible to use Lisinoton together with IV administration or with the use of therapeutic transdermal nitroglycerin systems.

In major surgical interventions, as well as in the use of other drugs that cause BP reduction, lisinopril, by blocking angiotensin II formation, may cause a pronounced unpredictable decrease in BP.

In elderly patients, the use of standard doses leads to higher blood concentrations of the drug, so extra caution is required in determining the dose, although no differences in the antihypertensive effect of Lisinoton have been identified in elderly and younger patients.

Because the potential risk of agranulocytosis cannot be excluded, periodic monitoring of blood counts is required.

Anaphylactic shock may occur when the drug is used in dialysis with a polyacrylonitrile membrane, so either a different type of dialysis membrane or the administration of other antihypertensive agents is recommended.

Influence on driving and operating ability

There are no data on the effect of lisinopril on driving and operating ability, but it should be taken into account that dizziness may occur, so caution should be exercised.

Contraindications

. Caution should be exercised when the drug is prescribed in severe renal function impairment, bilateral renal artery stenosis or artery stenosis of the sole kidney with progressive azotemia, condition after renal transplantation, renal failure, azotemia, hyperkalemia, aortic estuary stenosis, hypertrophic obstructive cardiomyopathy, primary hyperaldosteronism arterial hypotension, cerebrovascular diseases (including cerebrovascular insufficiency), coronary heart disease, coronary insufficiency, autoimmune systemic connective tissue diseases (including scleroderma, systemic lupus erythematosus), bone marrow hematopoiesis inhibition, hypovolemic conditions (including those resulting from diarrhea, vomiting); patients on a sodium-restricted diet, elderly patients.

Side effects

Cardiovascular system: often – orthostatic hypotension, chest pain (1-3%); rarely (< 1%) – marked BP decrease, palpitations, tachycardia, myocardial infarction, cerebrovascular stroke in patients with increased risk of disease due to marked BP decrease.

CNS: frequently – dizziness, headache (5-6%), weakness, rarely (< 1%) – fatigue, drowsiness, convulsive twitching of the limbs and lips, asthenic syndrome, mood swings, confusion, decreased potency.

The digestive system: frequently – nausea, vomiting, diarrhea; rarely (< 1%) – dry mouth, anorexia, dyspepsia, changes in taste, abdominal pain, pancreatitis, hepatocellular or cholestatic jaundice, hepatitis.

Respiratory system: often (3%) – dry cough.

Blood system: probably – leukopenia, neutropenia, agranulocytosis, thrombocytopenia, with prolonged treatment – a slight decrease in the concentration of hemoglobin and hematocrit, erythrocytopenia.

Immune system disorders: (0.1%) angioedema (face, lips, tongue, larynx or epiglottis, upper and lower extremities); rare (< 1%) – syndrome including acceleration of CRP, arthralgia and appearance of antinuclear antibodies.

Urinary system disorders: rare (< 1%) – renal dysfunction, oliguria, anuria, acute renal failure, uremia, proteinuria.

Dermatological reactions: frequently – skin rash, rarely (< 1%) – urticaria, sweating, itching, alopecia.

Laboratory: hyperkalemia, azotemia, hyperuricemia, hyperbilirubinemia, increased liver enzymes activity (especially if there is a history of renal disease, diabetes and renovascular hypertension).

Other: rare (< 1%) – myalgia, fever, impaired fetal development.

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Overdose

Symptoms: marked BP decrease, dry mouth, drowsiness, urinary retention, constipation, anxiety, increased irritability (occurs with a single dose of 50 mg).

Treatment: if necessary, symptomatic therapy (intravenous fluid administration, control and normalization of BP, water-electrolyte balance) is carried out.

Lisinopril is eliminated from the body by hemodialysis.

Pregnancy use

The use of Lisinopril during pregnancy is contraindicated. Lisinopril penetrates through the placenta. If pregnancy is established, the drug should be discontinued as soon as possible.

The use of ACE inhibitors during the second and third trimesters of pregnancy has adverse effects on the fetus (marked BP decrease, renal failure, hyperkalemia, skull hypoplasia, fetal death are possible).

There are no data about negative effects of the drug on the fetus in case of I trimester use. Newborns and infants who have been intrauterine exposed to ACE inhibitors are recommended to be closely monitored for timely detection of marked BP decrease, oliguria, hyperkalemia.

There are no data on permeation of Lisinopril into breast milk. If it is necessary to prescribe the drug during lactation, breastfeeding should be discontinued.

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