Irumed, 20 mg, tablets, 30 pcs.

Compound

Lisinopril Irumed tablet 5 mg x30

Trade name: Irumed International name: Lisinopril

Release forms: tablets 5, 10, 20 mg (blisters)

Composition: lisinopril dihydrate 5.445/10.89/21.78 mg mg [equiv. 5/10/20 mg lisinopril anhydrous]

Pharmacological group: ACE inhibitor

Pharmacological group according to ATK: C09AA03 (Lisinopril)

Pharmacological action: vasodilating, hypotensive, diuretic, potassium-sparing, ACE blocking,

Indications: Arterial hypertension (including symptomatic), CHF, early treatment of acute myocardial infarction in hemodynamically stable patients (as part of combination therapy). As part of combination therapy for acute myocardial infarction (in the first 24 hours, with stable hemodynamic parameters). Diabetic nephropathy.

Dosage regimen: Orally, for arterial hypertension - 5 mg 1 time per day. 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 (increasing the dose above 20 mg/day usually does not lead to a further decrease in blood pressure). The maximum daily dose is 80 mg. For heart failure, start with 2.5 mg once, followed by increasing the dose by 2.5 mg after 3-5 days. In the elderly, a more pronounced long-term hypotensive effect is often observed, which is associated with a decrease in the rate of elimination of lisinopril (it is recommended to start treatment with 2.5 mg/day). In chronic renal failure, cumulation occurs when filtration decreases to less than 50 ml/min (the dose should be reduced by 2 times; with CC less than 10 ml/min, the dose should be reduced by 75%). For persistent arterial hypertension, long-term maintenance therapy of 10-15 mg/day is indicated, for heart failure - 7.5-10 mg/day.

Contraindications: Hypersensitivity to lisinopril or other ACE inhibitors, pregnancy, lactation.

Side effects: From the cardiovascular system: decreased blood pressure, arrhythmias, chest pain, rarely - orthostatic hypotension, tachycardia. From the nervous system: dizziness, headache, increased fatigue, drowsiness, twitching of the muscles of the limbs and lips, rarely - asthenia, mood lability, confusion. From the digestive system: nausea, dyspepsia, loss of appetite, change in taste, abdominal pain, diarrhea, dry mouth. From the hematopoietic organs: leukopenia, thrombocytopenia, neutropenia, agranulocytosis, anemia (decreased Hb, erythrocytopenia). Allergic reactions: angioedema, skin rashes, itching. Laboratory indicators: hyperkalemia, hyperuricemia, rarely - increased activity of “liver” transaminases, hyperbilirubinemia. Other: “dry” cough, decreased potency, rarely - acute renal failure, arthralgia, myalgia, fever, swelling (of the tongue, lips, limbs), impaired development of the fetal kidneys.

Pharmacodynamics: ACE inhibitor, reduces the formation of angiotensin II from angiotensin I. A decrease in the content of angiotensin II leads to a direct decrease in the release of aldosterone. Reduces bradykinin degradation and increases Pg synthesis. Reduces peripheral vascular resistance, blood pressure, preload, pressure in the pulmonary capillaries, causes an increase in IOC and an increase in myocardial tolerance to stress in patients with CHF. Dilates arteries more than veins. Some effects are explained by effects on tissue renin-angiotensin systems. With long-term use, hypertrophy of the myocardium and the walls of resistive arteries decreases. Improves blood supply to ischemic myocardium. ACE inhibitors extend life expectancy in patients with CHF and slow down the progression of LV dysfunction in patients who have suffered a myocardial infarction without clinical manifestations of HF. The onset of action is after 1 hour. The maximum effect is determined after 6-7 hours, duration is 24 hours. In arterial hypertension, the effect is noted in the first days after the start of treatment, a stable effect develops after 1-2 months.

Pharmacokinetics: Absorption - 30% (6-60%), bioavailability - 25%. Weakly binds to plasma proteins. Permeability through the BBB and placental barrier is low. Cmax - about 90 ng/ml, TCmax - 7 hours. It is practically not metabolized and is excreted unchanged by the kidneys. T1/2 - 12 hours.

Special instructions: Special caution is required when prescribing to patients with bilateral renal artery stenosis or stenosis of the artery of a single kidney (possible increase in the concentration of urea and creatinine in the blood), patients with ischemic heart disease or cerebrovascular disease, with decompensated CHF (possible arterial hypotension, myocardial infarction, stroke) . In patients with CHF, the resulting arterial hypotension can lead to deterioration of renal function. When using drugs that lower blood pressure in patients undergoing major surgery or during anesthesia, lisinopril can block the formation of angiotensin II, secondary to the compensatory release of renin. The safety and effectiveness of lisinopril in children has not been established. Before starting treatment, it is necessary to compensate for the loss of fluid and salts. Use during pregnancy is contraindicated, except in cases where other drugs cannot be used or are ineffective (the patient should be informed of the potential risk to the fetus). Carefully. History of angioedema during therapy with ACE inhibitors, hereditary or idiopathic angioedema, aortic stenosis, cerebrovascular diseases (including cerebrovascular insufficiency), coronary artery disease, coronary insufficiency, severe autoimmune systemic connective tissue diseases (including SLE , scleroderma), suppression of bone marrow hematopoiesis, diabetes mellitus, hyperkalemia, bilateral renal artery stenosis, stenosis of the artery of a single kidney, condition after kidney transplantation, renal failure, Na+-restricted diet, conditions accompanied by a decrease in blood volume (including diarrhea, vomiting ), elderly age, age under 18 years (safety and effectiveness of use have not been studied).

Interaction: Slows down the excretion of Li+ drugs. NSAIDs, estrogens, and adrenergic agonists reduce the hypotensive effect. When used simultaneously with potassium-sparing diuretics and K+ drugs, hyperkalemia is possible. Combined use with beta-blockers, BMCCs, diuretics and other antihypertensive drugs increases the severity of the hypotensive effect. Antacids and cholestyramine reduce absorption from the gastrointestinal tract. Myelotoxic drugs - a risk of severe inhibition of bone marrow hematopoiesis.

Drug registration number: P No. 015433/01

Date of registration (re-registration) of the drug: December 22, 2003

Directions for use and doses

Orally, before or after meals, 1 time per day, preferably at the same time.
Essential hypertension. The initial dose is 10 mg once a day, maintenance dose is 20 mg/day, maximum dose is 40 mg/day.

To fully develop the effect, a 2-4 week course of treatment with the drug may be required (this should be taken into account when increasing the dose). If the use of the drug at the maximum dose does not cause a sufficient therapeutic effect, then an additional prescription of another antihypertensive agent is possible.

In patients who have previously taken diuretics, they must be discontinued 2–3 days before starting the drug. If it is impossible to stop treatment with diuretics, the initial dose of lisinopril should be 5 mg/day.

For renovascular hypertension or other conditions with increased RAAS function, Irumed® is prescribed at an initial dose of 2.5–5 mg per day under the monitoring of blood pressure, renal function, and serum potassium concentration.

The maintenance dose is set depending on blood pressure.

In patients with renal failure and patients on hemodialysis, the initial dose is set depending on the creatinine Cl level. The maintenance dose is determined depending on blood pressure (under the control of renal function, potassium and sodium levels in the blood).

Doses for renal failure. Doses are determined depending on the creatinine Cl value, as shown in the table:

Table

In chronic heart failure, it is possible to use lisinopril simultaneously with diuretics and/or cardiac glycosides. If possible, the dose of the diuretic should be reduced before starting lisinopril. The initial dose is 2.5 mg 1 time per day, then it is gradually increased (by 2.5 mg after 3-5 days) to 5-10 mg per day. The maximum daily dose is 20 mg.

Acute myocardial infarction (as part of combination therapy in the first 24 hours with stable hemodynamic parameters). In the first 24 hours - 5 mg, then - 5 mg every other day, 10 mg every two days and then 10 mg 1 time per day, orally. In patients with acute myocardial infarction, use the drug for at least 6 weeks.

At the beginning of treatment or during the first 3 days after acute myocardial infarction in patients with low sBP (120 mmHg or lower), a lower dose of 2.5 mg should be prescribed. In case of decreased blood pressure (sBP ≤100 mm Hg), the daily dose of 5 mg can, if necessary, be temporarily reduced to 2.5 mg. In case of prolonged pronounced decrease in blood pressure (sBP <90 mm Hg for more than 1 hour), treatment with the drug should be discontinued.

Diabetic nephropathy. In patients with non-insulin-dependent diabetes mellitus, 10 mg of lisinopril is used once a day. The dose, if necessary, can be increased to 20 mg 1 time per day in order to achieve dBP values ​​below 75 mmHg. in a sitting position.

In patients with insulin-dependent diabetes mellitus, the same dosage is used to achieve dBP values ​​below 90 mmHg. in a sitting position.

Irumed, 20 mg, tablets, 30 pcs.

Symptomatic hypotension.

Most often, a pronounced decrease in blood pressure occurs with a decrease in fluid volume caused by diuretic therapy, a decrease in salt content in food, dialysis, diarrhea or vomiting (see “Interactions” and “Side effects”). In patients with chronic heart failure with or without concurrent renal failure, symptomatic arterial hypotension may develop. It was more often detected in patients with severe heart failure as a result of the use of large doses of diuretics, hyponatremia or impaired renal function. In such patients, treatment should be started under the strict supervision of a physician (with caution in selecting the dose of the drug and diuretics). Similar rules must be followed in patients with coronary artery disease and cerebrovascular insufficiency, in whom a sharp decrease in blood pressure can lead to myocardial infarction or stroke. If a pronounced decrease in blood pressure develops, the patient should be placed in the “lying” position and, if necessary, a 0.9% sodium chloride solution should be administered intravenously. A transient hypotensive reaction is not a contraindication for taking the next dose of the drug.

When using the drug, 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 reason to stop treatment. If arterial hypotension becomes symptomatic, it is necessary to reduce the dose of the drug or discontinue treatment with Irumed®.

In acute myocardial infarction.

The use of standard therapy (thrombolytics, acetylsalicylic acid, beta-blockers) is indicated. Irumed® can be used in conjunction with intravenous administration or with the use of transdermal nitroglycerin systems.

Treatment with lisinopril should not be used in patients with acute myocardial infarction (at risk of further serious hemodynamic deterioration after use of vasodilators). These are patients with SBP - 100 mm Hg. or lower or cardiogenic shock. During the first 3 days after myocardial infarction, the dose should be reduced if SBP is 120 mm Hg. or lower. Maintenance doses should be reduced to 5 mg or temporarily to 2.5 mg if SBP is 100 mmHg. or lower.

If arterial hypotension persists (SBP less than 90 mmHg for more than 1 hour), treatment with Irumed should be discontinued.

Renal dysfunction.

In patients with chronic heart failure, a pronounced decrease in blood pressure after initiation of treatment with ACE inhibitors may lead to a further deterioration of renal function. Cases of acute renal failure have been reported. In patients with bilateral renal artery stenosis or stenosis of the artery of a solitary kidney who received ACE inhibitors, there was an increase in serum urea and creatinine levels, usually reversible after discontinuation of treatment. This was more common in patients with renal failure.

Lisinopril is not used for acute myocardial infarction in patients with severe renal dysfunction, as determined by measuring serum creatinine concentrations greater than 177 mmol/L and/or proteinuria greater than 500 mg/day. If renal dysfunction develops during the use of the drug (serum creatinine concentration exceeding 265 mmol/l or doubling the value before treatment), the physician should assess the need for further use of Irumed®.

Hypersensitivity/Angioedema.

Angioedema of the face, extremities, lips, tongue, epiglottis and/or larynx, which may occur during any period of treatment, is rarely observed in patients treated with an ACE inhibitor, including lisinopril. In this case, treatment should be stopped as soon as possible and the patient should be monitored until complete regression of symptoms. In cases where swelling occurs only on the face and lips, the condition most often resolves without treatment, but antihistamines may be prescribed. Angioedema with laryngeal edema can be fatal. Swelling of the tongue, epiglottis or larynx may cause airway obstruction, so appropriate therapy (0.3–0.5 ml of 1:1000 SC epinephrine solution) and/or measures to ensure airway patency should be immediately carried out. It was noted that in patients of the Negroid race taking ACE inhibitors, angioedema developed more often than in patients of other races. Patients who have a history of angioedema not associated with previous treatment with ACE inhibitors may be at increased risk of developing it during treatment with an ACE inhibitor (see also “Contraindications”).

Anaphylactoid reactions during desensitization to hymenopterans.

In patients taking ACE inhibitors, a life-threatening anaphylactoid reaction may extremely rarely occur during desensitization to hymenopterans. This can be avoided by temporarily stopping ACE inhibitor treatment before each desensitization.

Patients on hemodialysis.

Anaphylactoid reactions have also been observed in patients undergoing hemodialysis using high-permeability membranes (for example AN 69®), who are simultaneously taking ACE inhibitors. In such cases, the use of a different type of dialysis membrane or another antihypertensive drug should be considered.

Cough.

When using ACE inhibitors, a dry, prolonged cough was noted, which disappears after stopping treatment with ACE inhibitors. In the differential diagnosis of cough, cough caused by the use of an ACE inhibitor must also be taken into account.

Surgery/General anesthesia.

When used in patients undergoing major surgery or during general anesthesia, lisinopril may block the formation of angiotensin II secondary to compensatory renin release. A pronounced decrease in blood pressure, which is considered a consequence of this mechanism, can be eliminated by increasing the volume of blood volume. Before surgery (including dental surgery), the surgeon/anesthetist should be informed about the use of an ACE inhibitor.

Serum potassium.

In some cases, hyperkalemia was observed. Risk factors for the development of hyperkalemia include renal failure, diabetes mellitus, and concomitant use of potassium-sparing diuretics (spironolactone, triamterene, or amiloride), potassium supplements, or salt substitutes containing potassium, especially in patients with impaired renal function. If the simultaneous use of lisinopril and the above-mentioned drugs is considered necessary, they should be used with caution, regularly monitoring the level of potassium in the blood serum.

In patients at risk of symptomatic hypotension (those on a low-salt or salt-free diet) with or without hyponatremia, as well as in patients who have received high doses of diuretics, the above-mentioned conditions (loss of fluid and salts) must be compensated and monitored before starting treatment effect of the initial dose of Irumed® on blood pressure.

Impact on the ability to drive vehicles and machinery.

There is no data on the effect of Irumed®, used in therapeutic doses, on the ability to drive vehicles and machines, however, it must be taken into account that dizziness may occur.