Lisinopril Stada, pills 5mg, 30pcs

Composition

1 tablet contains: Active ingredient: Lisinopril dihydrate 5,445 mg,10.89 mg and 21.78 mg (in terms of lisinopril 5 mg,10 mg and 20 mg, respectively); Excipients: Mannitol 12.5 mg/13,0 mg/30,0 mg, microcrystalline Cellulose 23,255 mg/25.0 mg/27,0 mg, Ludipress of LCE (lactose monohydrate 94,7–98,3%, povidone 3-4%) — 60,0 mg/61,0 mg/78,02 mg, Povidone—To 25 — 4.0 mg/4.5 mg/6.4 mg, Silicon dioxide colloid 2.5 mg/3,61 mg/6,0 mg, Magnesium stearate 1.3 mg/1.5 mg/2.2 mg, Croscarmellose sodium 5.0 mg/5.0 mg/5.0 mg, Calcium hydrogen phosphate 16,0 mg/25,5 mg/mg. 43,6

Pharmacological action

Lisinopril – cardioprotective, natriuretic, vasodilating, hypotensive.

Pharmacodynamics

ACE inhibitor, reduces the formation of angiotensin II from angiotensin I. A decrease in angiotensin II leads to a direct decrease in the release of aldosterone.

Reduces the degradation of bradykinin and increases the synthesis of prostaglandins.

Reduces total peripheral vascular resistance, blood pressure (BP), preload, pressure in the pulmonary capillaries, causes an increase in minute blood volume and increased myocardial load tolerance in patients with chronic heart failure.

Dilates the arteries to a greater extent than the veins. Some of the effects are attributed to effects on the tissue renin-angiotensin system.

With prolonged use, hypertrophy of the myocardium and arterial walls of the resistive type decreases. Improves blood supply to the ischemic myocardium.

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

The antihypertensive effect begins after approximately 6 hours and persists for 24 hours. The duration of the effect also depends on the dose. The action starts in 1 hour. The maximum effect is determined in 6-7 hours.

With 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 was abruptly discontinued, no significant increase in blood pressure was observed.

In addition to lowering blood pressure, lisinopril reduces albuminuria. In patients with hyperglycemia, it helps to normalize the function of damaged glomerular endothelium.

Lisinopril does not affect the concentration of glucose in the blood in patients with diabetes mellitus and does not lead to an increase in cases of hypoglycemia.

Pharmacokinetics

Suction. After oral use, about 25% of lisinopril is absorbed from the gastrointestinal tract.

Food intake does not affect the absorption of the drug. Absorption averages 30%, bioavailability-29%. Distribution. Almost does not bind to plasma proteins.

The maximum concentration in blood plasma (90 ng/ml) is reached after 7 hours. Blood-brain and placental barrier permeability is low.

Metabolism. Lisinopril is not biotransformed in the body.

Output. It is excreted unchanged by the kidneys. The elimination half-life is 12 hours.

Pharmacokinetics in selected groups of patients

In patients with chronic heart failure, lisinopril absorption and clearance are reduced.

In patients with renal insufficiency, the concentration of lisinopril is several times higher than the concentration in the blood plasma of volunteers, and there is an increase in the time to reach the maximum concentration in the blood plasma and an increase in the half-life.

In elderly patients, the concentration of the drug in the blood plasma and the area under the curve are 2 times greater than in young patients.

Indications

• Arterial hypertension (in monotherapy or in combination with other antihypertensive agents)
• Chronic heart failure (as part of combination therapy for the treatment of patients taking cardiac glycosides and / or diuretics)
• Acute myocardial infarction (early (in the first 24 hours) treatment of patients with stable hemodynamic parameters, to maintain these indicators and prevent left ventricular dysfunction and heart failure)
• Diabetic nephropathy (to reduce albuminuria in patients with type 1 diabetes mellitus with normal blood pressure and in patients with type 2 diabetes mellitus with arterial hypertension).

Contraindications

Hypersensitivity to lisinopril and/or other components of the drug, hypersensitivity to other ACE inhibitors, a history of angioedema, including those associated with the use of ACE inhibitors, hereditary angioedema or idiopathic angioedema, age up to 18 years (efficacy and safety have not been established), pregnancy, lactation, lactase deficiency, galactosemia, glucose-galactose malabsorption syndrome. With caution aortic stenosis, hypertrophic obstructive cardiomyopathy, hypotension, coronary heart disease, coronary insufficiency; diet with salt restriction, hyperkalemia; bilateral renal artery stenosis or stenosis of the artery of a single kidney with progressive azotemia, condition after kidney transplantation, renal failure (creatinine clearance less than 30 ml/min), hemodialysis using high-flow drugs dialysis membranes (AN 69®); primary hyperaldosteronism;cerebrovascular diseases, including cerebral circulatory failure; systemic connective tissue diseases (including scleroderma, systemic lupus erythematosus); suppression of bone marrow hematopoiesis; hypovolemic conditions (including as a result of diarrhea, vomiting); elderly age (over 65 years).

Side effects

Side effects are classified by frequency: common (1-10%), infrequent (0.1-1%), rare (0.01-0.1%), very rare (less than 0.01%). From the cardiovascular system: often-marked decrease in blood pressure, orthostatic hypotension; rarely-palpitation, tachycardia, Raynaud’s syndrome, myocardial infarction, cerebrovascular stroke in patients with an increased risk of the disease. From the central nervous system: often — dizziness, headache; not often-mood lability, paresthesia, drowsiness/insomnia; rarely-confusion; frequency not known-depression, fainting. From the side of the senses: not often-violations of taste and olfactory sensations. From the respiratory system: often-dry cough; not often-rhinitis; very rarely-bronchospasm, sinusitis, allergic alveolitis/eosinophilic pneumonia. From the digestive system: often — diarrhea, vomiting; not often-nausea, abdominal pain, dyspepsia; rarely-dryness of the oral mucosa; very rarely-pancreatitis, hepatocellular or cholestatic jaundice, hepatitis, isolated cases of liver failure. From the urinary system: often-impaired renal function; rarely-uremia, acute renal failure; very rarely-oliguria, anuria. From the reproductive system: rarely-decreased potency, gynecomastia. Hematopoietic disorders: rarely-decreased hemoglobin and hematocrit; very rarely-suppression of bone marrow function, anemia, thrombocytopenia, leukopenia, neutropenia, agranulocytosis, hemolytic anemia, lymphadenopathy. From the skin: not often-itching; rarely-rash, alopecia, psoriasis; very rarely-increased sweating, pemphigus. Allergic reactions: rarely — urticaria, angioedema (face, lips, tongue, larynx or epiglottis, upper and lower extremities); very rarely — toxic epidermal necrolysis, Stevens-Johnson syndrome, erythema multiforme, pseudolymphoma of the skin; in some cases — intestinal angioedema, a syndrome including fever, vasculitis, myalgia, arthralgia, acceleration of sedimentation rate red blood cell count (ESR) and positive test results for antinuclear antibodies, eosinophilia, leukocytosis, photosensitization. Laboratory parameters: infrequently-increased urea and creatinine concentrations, increased activity of “hepatic” transaminases, hyperkalemia; rarely-hyperbilirubinemia, hyponatremia. Others: not often-increased fatigue, asthenia; very rarely-hypoglycemia, autoimmune diseases; in some cases-inadequate secretion of antidiuretic hormone.

Interaction

Lisinopril can be used simultaneously with beta-blockers, acetylsalicylic acid (no more than 300 mg / day), thrombolytics, nitrates. Concomitant use of lisinopril with potassium-sparing diuretics (spironolactone, triamterene, amiloride), potassium preparations, potassium-containing salt substitutes, cyclosporine increases the risk of hyperkalemia, especially in patients with impaired renal function. Combined use is allowed only with regular monitoring of blood potassium and kidney function. When using lisinopril with other antihypertensive agents, including diuretics, beta-blockers, slow calcium channel blockers, etc., the additive antihypertensive effect should be taken into account. The combination of lisinopril with tricyclic antidepressants / antipsychotics, barbiturates, vasodilators, phenothiazines can lead to a pronounced decrease in blood pressure. Lisinopril slows down the elimination of lithium preparations, so you should regularly monitor the concentration of lithium in the blood. Antacids and colestyramine reduce the absorption of lisinopril in the gastrointestinal tract.Concomitant use of lisinopril with insulin and oral hypoglycemic agents increases the risk of hypoglycemia, especially during the first month of ACE inhibitor therapy. Nonsteroidal anti-inflammatory drugs, including selective cyclooxygenase-2 inhibitors, estrogens, and adrenomimetics reduce the antihypertensive effect of lisinopril. When ACE inhibitors and intravenous gold preparations (sodium aurothiomalate) are used simultaneously, a symptom complex is described, including facial hyperemia, nausea, vomiting, and a decrease in blood pressure. The combined use of lisinopril with selective serotonin reuptake inhibitors can lead to severe hyponatremia and a marked decrease in blood pressure. Combined use with allopurinol, procainamide, cytostatics can lead to leukopenia. Ethanol enhances the effect of the drug.

How to take, course of use and dosage

Inside, regardless of food intake,1 time a day in the morning, preferably at the same time. Dose selection is carried out until the optimal (target level) blood pressure is reached. The maintenance dose is determined depending on the dynamics of blood pressure. Do not increase the dose of the drug earlier than after 2 weeks (accelerated titration of the dose is allowed in patients with asymptomatic left ventricular dysfunction, initial and moderate heart failure, arterial hypertension and hospitalized patients). In arterial hypertension, the initial dose is 10 mg / day, the maintenance dose is 20 mg/day, and the maximum daily dose is 40 mg (increasing the dose above 40 mg / day usually does not lead to a further decrease in blood pressure). Previous diuretic therapy should be discontinued 2-3 days before the start of lisinopril use. If diuretics cannot be discontinued, the initial dose of lisinopril should not exceed 5 mg / day. In this case, after taking the first dose, medical monitoring is recommended for several hours, taking into account the maximum antihypertensive effect in 6-7 hours. For renovascular hypertension or other conditions with increased activity of the renin-angiotensin-aldosterone system, the initial dose is 5 mg per day, under strict medical supervision in a hospital setting (monitoring of blood pressure, kidney function, and serum potassium). The maintenance dose, while continuing strict medical monitoring, should be determined depending on the dynamics of blood pressure. In patients with renal insufficiency, since lisinopril is excreted through the kidneys, the initial dose is determined depending on creatinine clearance. Further, in accordance with the therapeutic effect and tolerability, a maintenance dose should be established in conditions of frequent monitoring of renal function, serum potassium and sodium levels.

* including patients on hemodialysis with persistent arterial hypertension, long-term maintenance therapy of 10-15 mg/day is indicated. In case of chronic heart failure (simultaneously with diuretics and/or cardiac glycosides) — lisinopril in a dose of 5-10 mg is used for maintenance therapy. The initial dose is 2.5 mg (2.5 mg or 5 mg tablets with a risk are used). The maximum daily dose is 20 mg. If absolutely necessary, increase the dose to 35 mg / day, for a period of at least 2 weeks, under the strict supervision of a doctor in a hospital setting. If possible, the diuretic dose should be reduced 2-3 days before starting lisinopril. Acute myocardial infarction (as part of combination therapy). On the first day, lisinopril is indicated only in patients with stable hemodynamic parameters-5 mg orally, then 5 mg after 1 day,10 mg after two days, and then 10 mg once a day. Patients with low systolic blood pressure (100-120 mm Hg) at the beginning of treatment and during the first 3 days after acute myocardial infarction should receive a dose of the drug no more than 2.5 mg per day. The course of treatment is at least 6 weeks. If blood pressure decreases (systolic blood pressure is less than or equal to 100 mm Hg), the daily dose of 5 mg should be temporarily reduced to 2.5 mg. In case of prolonged marked decrease in blood pressure (systolic blood pressure below 90 mm Hg for more than 1 hour), treatment with lisinopril should be discontinued. In diabetic nephropathy,10 mg of lisinopril is used once a day. If necessary, the dose can be increased to 20 mg once a day in order to achieve diastolic blood pressure values below 75 mm Hg in the sitting position for patients with type 2 diabetes and below 90 mm Hg in the sitting position for patients with type 1 diabetes.

Overdose

Symptoms:marked decrease in blood pressure, cough, dryness of the oral mucosa, dizziness, restlessness, increased irritability, drowsiness, vascular collapse, rapid breathing, palpitation, tachycardia, bradycardia, impaired water-electrolyte balance, renal failure, urinary retention. Treatment:gastric lavage, absorbing agents, giving the patient a horizontal position with raised legs, intravenous use of 0.9% sodium chloride solution, if necessary — vasopressors, blood pressure control, water-electrolyte balance, creatinine. With persistent bradycardia — the use of an artificial pacemaker. Hemodialysis is effective.

Special instructions

ACE inhibitor therapy should be initiated under the control of blood pressure, taking into account the maximum effect of lisinopril after 6-8 hours (in case of myocardial infarction 8-10 hours). Patients with heart failure (with or without renal failure) are at high risk of developing dangerous adverse reactions. In such cases, treatment with Lisinopril should be started under strict medical supervision in a hospital setting. Similar rules should also be followed when prescribing to patients with coronary heart disease, cerebrovascular insufficiency, in which a sharp decrease in blood pressure can lead to a myocardial infarction or stroke. Hypotension of the first dose may develop, in particular, in patients with high plasma renin activity (for example, against the background of high-dose diuretic therapy or congestive heart failure). A marked decrease in blood pressure occurs when the initial volume of circulating blood is reduced due to diuretic therapy, low-salt diet, hemodialysis, diarrhea and vomiting. Before starting treatment with Lisinopril, it is necessary to replenish the volume of circulating blood and normalize water and electrolyte disorders. Transient arterial hypotension is not a contraindication for taking the next dose of the drug. When Lisinopril is used, some patients with chronic heart failure with normal or low blood pressure may experience a decrease in blood pressure, which is not a reason to stop treatment. In cases of renal artery stenosis (especially bilateral stenosis, or stenosis of the artery of a single kidney), as well as in cases of circulatory failure due to a lack of sodium and/or fluid, the use of Lisinopril may lead to an increase in the concentration of urea and creatinine in the blood, impaired renal function, and acute renal failure. Treatment with Lisinopril in acute myocardial infarction is carried out against the background of standard therapy (thrombolytics, acetylsalicylic acid (no more than 300 mg / day), beta-blockers). Compatible with intravenous nitroglycerin and with the transdermal therapeutic nitroglycerin system (TTS). Surgical intervention/general anesthesia. With extensive surgical interventions, as well as with the use of other drugs that cause a decrease in blood pressure, Lisinopril, blocking the formation of angiotensin II, can cause a pronounced unpredictable decrease in blood pressure. Before surgery, including dental surgery, the surgeon/anesthesiologist should be informed about the use of an ACE inhibitor. In elderly patients, the same dose leads to a higher concentration of the drug in the blood plasma, so special care is required when determining the dose. Angioedema associated with the use of ACE inhibitors, including Lisinopril, may develop at any stage of treatment. With edema of the tongue, pharynx, larynx, airway obstruction can develop with a fatal outcome. If you experience the described complaints, you should immediately stop taking the drug and consult a doctor. In such cases, rapid subcutaneous use of a 0.1% epinephrine solution (0.3–0.5 ml), use of glucocorticosteroids, antihistamines, and/or measures to ensure airway patency is necessary. In patients with chronic heart failure and diabetes mellitus who simultaneously take potassium supplements, potassium-containing salt substitutes, potassium-sparing diuretics, or other drugs that increase the content of potassium ions in the serum (heparin), ACE inhibitors increase the risk of hyperkalemia. Taking Lisinopril, like all ACE inhibitors, may be accompanied by a dry cough, which stops with a reduction in the dose of the drug or discontinuation of MI treatment. Since the potential risk of agranulocytosis cannot be excluded, periodic monitoring of the blood picture is required. Patients taking ACE inhibitors may experience a life-threatening anaphylactoid reaction during desensitization with hymenopteran venom (bees and wasps). It is necessary to temporarily stop treatment with an ACE inhibitor before starting a course of desensitization. Anaphylactoid reactions may occur with simultaneous hemodialysis using high-flow membranes (including AN 69®), as well as during apheresis of low-density lipoproteins with adsorption on dextran sulfate. Consideration should be given to using a different type of dialysis membrane or other antihypertensive agent.In patients with diabetes mellitus, careful monitoring of blood sugar levels is required, especially during the first month of Lisinopril therapy;Caution should be exercised when exercising, hot weather (risk of dehydration and excessive blood pressure reduction due to reduced circulating blood volume). During the treatment period, it is not recommended to consume alcoholic beverages, as alcohol increases the hypotensive effect of the drug. Effect on the ability to drive vehicles and work with mechanisms There is no data on the effect of lisinopril in therapeutic doses on the ability to drive vehicles and mechanisms. However, it should be borne in mind that dizziness may occur, so caution should be exercised.

Form of production

Tablets 5,10 and 20 mg. 10 or 30 tablets in a contour cell package made of polyvinyl chloride film and aluminum foil. 2 or 3 contour cell packs of 10 tablets or 1 contour cell pack of 30 tablets together with the instructions for use in a cardboard pack.

Storage conditions

Store in a dry place protected from light and out of reach of children, at a temperature not exceeding 25°C.

Shelf life

3 years

Active ingredient

Lisinopril

Conditions of release from pharmacies

By prescription

Dosage form

Tablets