Lisinopril pills 20mg, 30pcs

Composition

Each tablet contains:

Active ingredient:

lisinopril dihydrate (equivalent to lisinopril) 2.5 mg,5 mg,10 mg or 20 mg;

Auxiliary substances:

lactose monohydrate of 77.5 mg/75,0 mg/70,0 mg/65,0 mg, respectively,

corn starch of 49.0 mg,

povidone 6.0 mg,

talc 3,13 mg,

magnesium stearate 1.3 mg,

dyes (sunset yellow 0.02 mg in tablets containing 2.5 mg and 5 mg lisinopril; dye azorubin 0.02 mg in tablets containing 10 mg lisinopril; titanium dioxide 0.02 mg in tablets containing 20 mg lisinopril).

Pharmacological action

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 (OPSS), blood pressure (BP), preload, pressure in the pulmonary capillaries, causes an increase in minute blood volume (MOC) and an increase in myocardial load tolerance in patients with chronic heart failure (CHF). Dilates the arteries to a greater extent than the veins. Some of the effects are attributed to effects on the tissue renin-angiotensin-aldosterone system (RAAS). 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 CHF, slow the progression of left ventricular (LV) dysfunction in patients who have had a myocardial infarction without clinical manifestations of heart failure (HF).

The antihypertensive effect begins in 1 hour. The maximum effect is observed after 6-7 hours. The antihypertensive effect persists for 24 hours. The duration of the effect also depends on the dose. With arterial hypertension, the effect is noted in the first days after the start of treatment, a stable effect develops after 1-2 months.

Pharmacokinetics

The average degree of lisinopril absorption is about 25%, with significant inter-individual variability (6-60%). Food does not affect the absorption of lisinopril.

The maximum plasma concentration of about 90 ng / ml is reached after 6 hours. Bioavailability – 25%. Weakly binds to plasma proteins. Permeability through the blood-brain barrier and placental barrier is low. It is practically not metabolized and is excreted unchanged by the kidneys. The elimination half-life is 12 hours. In patients with CHF, cirrhosis of the liver, and elderly patients, lisinopril absorption and clearance are reduced.

Impaired renal function leads to an increase in AUC (area under the plasma concentration – time curve) and the half-life of lisinopril, but these changes become clinically significant only when the glomerular filtration rate is less than 30 ml / min

. Pharmacokinetics in certain groups of patients

In patients with chronic heart failure, lisinopril absorption and clearance are reduced, with a bioavailability of 16%. In patients with renal insufficiency (creatinine clearance less than 30 ml/min), the concentration of lisinopril is several times higher than the concentration in blood plasma in healthy volunteers, and there is an increase in the time to reach the maximum concentration in blood plasma and an increase in the half-life.

In elderly patients, the concentration of lisinopril in blood plasma is increased by an average of 60% and the area under the concentration-time curve is 2 times larger than in young patients.

In patients with cirrhosis of the liver, the bioavailability of lisinopril is reduced by 30% and clearance is reduced by 50% compared to patients with normal liver function.

Indications

-essential and renovascular arterial hypertension (AH) (in monotherapy or in combination with other antihypertensive agents);- chronic heart failure (CHF) (as part of combination therapy);- early treatment of acute myocardial infarction in combination therapy (in the first 24 hours with stable hemodynamic parameters to maintain these indicators and prevent left ventricular dysfunction and heart failure); – diabetic nephropathy (reduced albuminuria in patients with type 1 diabetes mellitus with normal blood pressure and patients with type 2 diabetes mellitus with arterial hypertension).

Contraindications

-hypersensitivity to lisinopril, to other ACE inhibitors and components of the drug; – a history of angioedema, including against the background of the use of ACE inhibitors; – hereditary angioedema of Quincke or idiopathic edema; – pregnancy; – lactation;- age up to 18 years (efficacy and safety have not been established);- lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

With caution, aortic stenosis, hypertrophic obstructive cardiomyopathy, bilateral renal artery stenosis, single kidney artery stenosis, post-kidney transplant condition, severe renal insufficiency (creatinine clearance less than 30 ml/min), primary hyperaldosteronism, hypotension, bone marrow hematopoiesis suppression, hyponatremia (increased risk of hypotension in patients undergoing surgery). low-salt or salt-free diet), hypovolemic conditions (including diarrhea, vomiting), systemic connective tissue diseases (including systemic lupus erythematosus, scleroderma), diabetes mellitus, hyperkalemia, coronary heart disease, cerebrovascular diseases (including cerebral circulatory failure), severe chronic heart failure, hemodialysis using high-flow dialysis membranes (AN69®), and the elderly.

Side effects

The most common side effects are dizziness, headache, fatigue, diarrhea, dry cough, nausea.

From the cardiovascular system: marked decrease in blood pressure, chest pain, orthostatic hypotension, tachycardia, bradycardia, the appearance or aggravation of symptoms of heart failure, violation of atrioventricular conduction, myocardial infarction, palpitation sensation.

From the central nervous system: emotional lability, impaired concentration of attention, paresthesia, drowsiness, convulsive twitching of the muscles of the limbs and lips, increased fatigue, asthenic syndrome, confusion.

Hematopoieticdisorders: leukopenia, neutropenia, agranulocytosis, thrombocytopenia, anemia (decreased hemoglobin, hematocrit, erythropenia).

Respiratory systemdisorders: dyspnoea, dry cough, bronchospasm.

From the digestive system: dryness of the oral mucosa, anorexia, dyspepsia, taste changes, abdominal pain, pancreatitis, jaundice (hepatocellular or cholestatic), hepatitis.

From the skin: increased sweating, alopecia, photosensitization, pruritus.

From the genitourinary system: impaired renal function, oliguria, anuria, acute renal failure, uremia, proteinuria, decreased potency.

Allergic reactions: angioedema of the face, extremities, lips, tongue, epiglottis and / or larynx, skin rashes, urticaria, fever, positive results of the antinuclear antibody test, increased ESR, eosinophilia, leukocytosis, intestinal angioedema.

Other: myalgia, arthralgia/arthritis, vasculitis.

With the simultaneous use of ACE inhibitors and gold preparations (sodium aurothiomalate) intravenously, a symptom complex is described, including facial hyperemia, nausea, vomiting and arterial hypotension.

Laboratory parameters: hyperkalemia, hyponatremia, increased activity of “hepatic” transaminases, hyperbilirubinemia, hypercreatininemia, increased urea concentration.

Interaction

When used concomitantly with potassium-sparing diuretics (spironolactone, triamterene, amiloride), potassium preparations, salt substitutes containing potassium, the risk of hyperkalemia increases, especially in patients with impaired renal function. Therefore, they can be co-administered only on the basis of an individual doctor’s decision, with regular monitoring of serum potassium and kidney function. When used concomitantly with beta-blockers, slow calcium channel blockers, diuretics and other antihypertensive agents, the antihypertensive effect of the drug is enhanced.

Lisinopril can be used simultaneously with beta-blockers, acetylsalicylic acid (in doses less than 300 mg / day), thrombolytics, nitrates.

When used concomitantly with vasodilators, barbiturates, phenothiazines, tricyclic antidepressants – ethanol-increased antihypertensive effect of the drug.

When used concomitantly with nonsteroidal anti-inflammatory drugs (NSAIDs) (including selective cyclooxygenase – 2 inhibitors), estrogens, and adrenostimulants, the antihypertensive effect of lisinopril decreases.

When used concomitantly with lithium preparations, it slows down the elimination of lithium from the body (increased cardiotoxic and neurotoxic effects of lithium).

When used concomitantly with antacids and colestyramine-reduced absorption in the gastrointestinal tract.

The drug increases the neurotoxicity of salicylates, weakens the effect of hypoglycemic agents for oral use, norepinephrine( norepinephrine), epinephrine (epinephrine) and anti-gouty drugs, increases the effects (including side effects) of cardiac glycosides, the effect of peripheral muscle relaxants, reduces the excretion of quinidine.

Reduces the effect of oral contraceptives. When taking methyldopa at the same time, the risk of developing hemolysis increases. Co-use with selective serotonin reuptake inhibitors may result in severe hyponatremia. Combined use with allopurinol, procainamide, cytostatics can lead to leukopenia.

With the simultaneous use of ACE inhibitors and gold preparations (sodium aurothiomalate) intravenously, a symptom complex is described, including facial hyperemia, nausea, vomiting and arterial hypotension.

How to take, course of use and dosage

Inside,1 time a day in the morning, regardless of food intake, preferably at the same time.

Essential hypertension: initial dose-10 mg / day, maintenance dose-20 mg/day, maximum daily dose-40 mg. A stable antihypertensive effect develops after 1-2 months, which should be taken into account when increasing the dose. If the use of the drug in the maximum dose does not cause a sufficient therapeutic effect, then an additional appointment of another antihypertensive agent is possible.

In patients who have previously received diuretics, they should be discontinued 2-3 days before the start of the drug. If diuretics cannot be discontinued, the initial dose of lisinopril should not exceed 5 mg / day.

Renovascular hypertension or other conditions with increased RAAS activity: the initial dose is 2.5-5 mg / day under the control of blood pressure, renal function, and serum potassium. The maintenance dose is set depending on the value of blood pressure.

In chronic renal failure (CRF), the dose is determined depending on creatinine clearance (creatinine clearance): with creatinine clearance 30-70 ml/min – 5-10 mg/day, with creatinine clearance 10-30 ml/min – 2.5 – 5 mg/day, less than 10 ml/min, including patients on hemodialysis-2.5 mg/day. The maintenance dose is determined depending on blood pressure (under the control of renal function, potassium and sodium content in the blood).

CHF (concomitantly with diuretics and / or cardiac glycosides): the initial dose is 2.5 mg / day, with a gradual increase of 2.5 mg after 3-5 days of the maintenance daily dose of 5-10 mg / day. The maximum daily dose is 20 mg. If possible, the diuretic dose should be reduced before starting lisinopril.

Elderly patients often have a more pronounced long-term antihypertensive effect, which is associated with a decrease in the rate of elimination of lisinopril (it is recommended to start treatment with 2.5 mg/day – ½ tablet of 5 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 other day, and then 10 mg once a day. The course of treatment is at least 6 weeks.

At the beginning of treatment or during the first 3 days after acute myocardial infarction, a lower dose of 2.5 mg is prescribed in patients with low systolic blood pressure (120 mm Hg or lower). If blood pressure decreases (systolic blood pressure is less than or equal to 100 mm Hg), the daily dose of 5 mg is temporarily reduced to 2.5 mg if necessary. In case of a long-term pronounced decrease in blood pressure (systolic blood pressure below 90 mm Hg for more than 1 hour), treatment with the drug is discontinued.

Diabetic nephropathy: the initial dose is 10 mg / day, which, if necessary, is increased to 20 mg / day in order to achieve diastolic blood pressure values below 75 mm Hg measured in the “sitting” position for patients with type 1 diabetes mellitus and below 90 mm Hg in the “sitting” position for patients with type 2 diabetes mellitus.

Overdose

Symptoms:

marked decrease in blood pressure, dryness of the oral mucosa, drowsiness, urinary retention, constipation, impaired water-electrolyte balance, renal failure, rapid breathing, tachycardia, palpitation, bradycardia, dizziness, anxiety, increased irritability.

Treatment:

gastric lavage, taking activated charcoal, giving the patient a horizontal position with raised legs, replenishing the volume of circulating blood-intravenously 0.9% sodium chloride solution or other plasma-substituting solutions, if necessary – vasopressors, monitoring the functions of the cardiovascular and respiratory systems, blood pressure, BCC, urea, creatinine, water and electrolyte balance. In the case of persistent bradycardia, an artificial pacemaker is used. Hemodialysis is effective.

Special instructions

A marked decrease in blood pressure most often occurs with a decrease in the volume of circulating blood caused by diuretic therapy, a decrease in the amount of salt in food, hemodialysis, diarrhea or vomiting. In patients with chronic heart failure with simultaneous renal failure or without it, a pronounced decrease in blood pressure is possible. It is more often detected in patients with severe chronic heart failure, as a result of the use of high doses of diuretics, hyponatremia or impaired renal function. In such patients, treatment should be started under the strict supervision of a doctor (with caution, select the dose of the drug and diuretics). Such rules should 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. Before starting treatment, if possible, the sodium concentration should be normalized and / or the volume of circulating blood should be replenished, and the effect of the initial dose of the drug on the patient should be carefully monitored. Treatment of symptomatic arterial hypotension consists of providing bed rest and, if necessary, intravenous fluid use (infusion of saline solution). Transient arterial hypotension is not a contraindication for treatment with Lisinopril, however, it may be necessary to temporarily cancel it, or reduce the dose.

Treatment with Lisinopril is contraindicated in cases of cardiogenic shock and acute myocardial infarction, if the appointment of a vasodilator can significantly worsen hemodynamic parameters, for example, when systolic blood pressure does not exceed 100 mm Hg In patients with acute myocardial infarction, a decrease in renal function (plasma creatinine concentration more than 177 mmol/l and / or proteinuria more than 500 mg/24 h) is a contraindication for the use of Lisinopril. If renal failure develops during treatment with lisinopril (the concentration of creatinine in the blood plasma is more than 265 mmol/l or twice the initial level), the doctor should decide whether to stop treatment.

With bilateral renal artery stenosis and renal artery stenosis of a single kidney, as well as with hyponatremia and/or decreased circulating blood volume or circulatory insufficiency, hypotension caused by taking Lisinopril can lead to a decrease in renal function, followed by the development of reversible (after discontinuation of the drug) acute renal failure. A slight temporary increase in the concentration of urea in the blood and creatinine can be observed in cases of impaired renal function, especially against the background of simultaneous treatment with diuretics. In cases of a significant decrease in renal function (creatinine clearance less than 30 ml/min), caution and monitoring of renal function is required.

Angioedema of the face, extremities, lips, tongue, epiglottis, and / or larynx has been reported rarely in patients treated with ACE inhibitors, including Lisinopril, and may occur during any period of treatment. In this case, treatment with Lisinopril should be discontinued as soon as possible and the patient should be monitored until symptoms fully regress. In cases where only the face and lips are swollen, the condition most often passes without treatment, however, antihistamines may be prescribed. Angioedema with laryngeal edema can be fatal. When the tongue, epiglottis, or larynx is affected, airway obstruction may occur, so appropriate therapy should be given immediately (0.3-0.5 ml of epinephrine (epinephrine)solution).1: 1000 subcutaneously, use of glucocorticosteroids, antihistamines) and/or measures to ensure airway patency. Patients who have a history of angioedema that is not associated with previous treatment with ACE inhibitors may have an increased risk of developing angioedema during treatment with an ACE inhibitor.

Anaphylactic reaction has also been observed in patients undergoing hemodialysis using high-flow dialysis membranes (AN69®), who are simultaneously taking lisinopril. In such cases, the possibility of using a different type of dialysis membrane or other antihypertensive agent should be considered. Anaphylactic reactions may occur during apheresis of low-density lipoproteins with dextran sulfate.

In some cases of desensitization to hymenopteran venom (wasps, bees, etc. ), treatment with ACE inhibitors was accompanied by hypersensitivity reactions. This can be avoided if you temporarily stop taking ACE inhibitors beforehand. In patients undergoing extensive surgery or undergoing general anesthesia, ACE inhibitors (in particular, lisinopril)are recommended. they can block the formation of angiotensin II. The decrease in blood pressure associated with this mechanism of action is corrected by an increase in the volume of circulating blood. Before surgery (including dentistry), the surgeon/anesthesiologist should be warned about the use of Lisinopril.

The use of recommended doses of the drug in elderly patients may be accompanied by an increase in the concentration of lisinopril in the blood, so the dose selection requires special attention and is carried out depending on the patient’s kidney function and blood pressure.

At the same time, the antihypertensive effect of Lisinopril is equally pronounced in elderly and young patients. Coughing has been reported with ACE inhibitors. The cough is dry and prolonged, which disappears after discontinuation of treatment with ACE inhibitors. In the differential diagnosis of cough, it is necessary to take into account the cough caused by the use of ACE inhibitors.

In some cases, hyperkalemia was observed. Risk factors for developing hyperkalemia include renal failure, diabetes mellitus, taking potassium supplements or drugs that cause an increase in blood potassium (for example, heparin), especially in patients with impaired renal function. During treatment with the drug, regular monitoring of potassium, glucose, urea, and lipids in the blood plasma is necessary. During the treatment period, it is not recommended to consume alcoholic beverages, as alcohol increases the antihypertensive effect of the drug. Caution should be exercised when exercising, in hot weather (the risk of dehydration and excessive blood pressure reduction due to a decrease in the volume of circulating blood).

Since the potential risk of agranulocytosis cannot be excluded, periodic monitoring of the blood picture is required. Based on the results of epidemiological studies, it is assumed that the simultaneous use of ACE inhibitors and insulin, as well as hypoglycemic agents for oral use, may lead to the development of hypoglycemia. The greatest risk of development is observed during the first weeks of combination therapy, as well as in patients with impaired renal function. In patients with diabetes mellitus, careful glycemic control is required, especially during the first month of ACE inhibitor therapy. ACE inhibitors can lead to the development of cholestatic jaundice with progression to fulminant liver necrosis, so it is necessary to stop taking the drug if the activity of “hepatic” transaminases increases and symptoms of cholestasis appear.

Effect of the drug on the ability to drive vehicles and mechanisms If there are side effects from the central nervous system, it is not recommended to drive vehicles, as well as perform work associated with an increased risk.

Form of production

Tablets

Active ingredient

Lisinopril

Conditions of release from pharmacies

By prescription

Dosage form

Tablets