Lisinopril-Teva pills 20mg, 30pcs

Composition

Tablets

Active ingredient:

lisinopril dihydrate 20 mg;

Auxiliary substances:

milk sugar (lactose);

MCC;

starch 1500 (pregelatinized);

aerosil (colloidal silicon dioxide);

talc;

magnesium stearate.

Pharmacological action

Pharmacodynamics .

 Angiotensin-converting enzyme (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 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 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 chronic heart failure (CHF), slow the progression of left ventricular dysfunction in patients who have had an acute myocardial infarction without clinical manifestations of heart failure. The onset of action of the drug is in 1 hour, the maximum antihypertensive effect is achieved in 6-7 hours and persists for 24 hours. The duration of the effect also depends on the amount of the dose taken. With arterial hypertension, the effect is noted in the first days after the start of treatment, a stable effect develops after 1-2 months of therapy. When lisinopril was abruptly discontinued, there was no significant increase in blood pressure.

Lisinopril reduces albuminuria. It 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, lisinopril is absorbed from the gastrointestinal tract (GI) by an average of 25%, but absorption can vary from 6 to 60%. Bioavailability is 29%. The maximum concentration in blood plasma (Cmax) is reached after 7 hours. Food intake does not affect the absorption of lisinopril.

Distribution.

 Lisinopril is slightly bound to plasma proteins. 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 (T 1/2) is 12.6 h. The clearance of lisinopril is 50 ml/min. The decrease in serum lisinopril concentration occurs in two phases. The majority of lisinopril is eliminated during the initial alpha phase (effective T 1/2-12 hours), followed by the terminal long-term beta phase (about 30 hours).

Indications

• Diabetic nephropathy (reduction of albuminuria in patients with type 1 diabetes mellitus with normal blood pressure, and patients with type 2 diabetes mellitus with arterial hypertension).
• 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).
• 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).

Contraindications

• Hypersensitivity.
• Angioedema in the anamnesis, including against the background of the use of ACE inhibitors.
• Hereditary angioedema or idiopathic angioedema.
• Age up to 18 years (efficacy and safety have not been established).
• Lactase deficiency, lactose intolerance, glucose-galactose malabsorption syndrome.

With cautionSevere renal dysfunction, bilateral renal artery stenosis or stenosis of the artery of a single kidney with progressive azotemia, condition after kidney transplantation, azotemia, hyperkalemia, aortic stenosis, hypertrophic obstructive cardiopathy, primary hyperaldosteronism, arterial hypotension, cerebrovascular diseases (including cerebrovascular insufficiency), coronary heart disease, coronary insufficiency, autoimmune systemic diseases connective tissue disorders (including scleroderma, systemic lupus erythematosus); inhibition of bone marrow hematopoiesis; diet with restriction of table salt; hypovolemic conditions (including as a result of diarrhea, vomiting); elderly age, hemodialysis using high-flow dialysis membranes with high permeability (AN69®).

Side effects

From the cardiovascular system: often-a marked decrease in blood pressure, orthostatic hypotension; rarely-chest pain, tachycardia, bradycardia, aggravation of symptoms of chronic heart failure, violation of atrioventricular conduction, myocardial infarction.

From the central nervous system: often-paresthesia, mood lability, confusion, drowsiness, convulsive twitching of the muscles of the limbs and lips, rarely-asthenic syndrome.

From the hematopoietic organs: rarely-leukopenia, neutropenia, agranulocytosis, thrombocytopenia, with long – term treatment-anemia (decreased hemoglobin, hematocrit, erythropenia).

From the respiratory system: rarely-shortness of breath, bronchospasm.

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

From the skin: rarely-urticaria, pruritus, increased sweating, alopecia, photosensitization.

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

Laboratory parameters: often-hyperkalemia, hyponatremia; rarely-hyperbilirubinemia, increased activity of “liver” enzymes, hypercreatininemia, increased urea and creatinine concentrations.

Allergic reactions: rarely-angioedema of the face, limbs, lips, tongue, epiglottis and / or larynx, skin rashes, pruritus, fever, false positive results of the antinuclear antibody test, increased erythrocyte sedimentation rate (ESR), eosinophilia, leukocytosis. In rare cases-intestinal angioedema.

Other: arthralgia/arthritis, vasculitis, myalgia.

Interaction

Concomitant use of the drug with potassium-sparing diuretics (spironolactone, triamterene, amiloride), potassium preparations, salt substitutes containing potassium, cyclosporine increases the risk of hyperkalemia, especially with impaired renal function, so they can be used together only with regular monitoring of the content of potassium ions in the blood serum and kidney function.

The combined use of lisinopril with beta-blockers, slow calcium channel blockers (BMCC), diuretics, tricyclic antidepressants/antipsychotics and other antihypertensive agents increases the severity of the hypotensive effect.

Lisinopril slows down the elimination of lithium preparations. Therefore, when used together, it is necessary to regularly monitor the concentration of lithium in the blood serum.

Antacids and colestyramine reduce the absorption of lisinopril in the gastrointestinal tract.

When combined with insulin and hypoglycemic agents for oral use, there is a possible risk of hypoglycemia. Nonsteroidal anti-inflammatory drugs (NSAIDs) (including selective cyclooxygenase-2 (COX-2) inhibitors), estrogens, and adrenomimetics reduce the hypotensive 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.

When combined with selective serotonin reuptake inhibitors, it can lead to severe hyponatremia.

Combined use with allopurinol, procainamide, cytostatics can lead to leukopenia.

How to take it, course of use and dosage

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

With arterial hypertension, patients who do not receive other antihypertensive drugs are prescribed 5 mg 1 time a day. In the absence of an 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 the dose over 40 mg / day usually does not lead to a further decrease in blood pressure). 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 start of treatment, which should be taken into account when increasing the dose. If the clinical effect is insufficient, the drug can be combined with other antihypertensive agents.

If the patient has received prior treatment with diuretics, then the use of such drugs should be stopped 2-3 days before the start of the use of Lisinopril. If this is not possible, then the initial dose of Lisinopril should not exceed 5 mg per day.In this case, after taking the first dose, medical monitoring is recommended for several hours (the maximum effect is reached in about 6 hours), since a pronounced decrease in blood pressure may occur.

In case of renovascular hypertension or other conditions with increased activity of the renin-angiotensin-aldosterone system, it is also advisable to prescribe a low initial dose of 5 mg per day, under increased medical supervision (control of blood pressure, kidney function, and serum potassium ions). 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 by the kidneys, the initial dose should be determined depending on creatinine clearance. Further, the selection of doses should be made depending on individual reactions with regular monitoring of renal function, potassium and sodium in the blood serum.

Creatinine clearance, ml / min Initial dose, mg / day 30-70 5-10 10-30 5 (including patients undergoing hemodialysis)

With persistent arterial hypertension, long-term maintenance therapy of 10-15 mg/day is indicated.

In chronic heart failure: the initial dose is 2.5 mg per day, with a gradual increase in 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 – 5 mg, then 5 mg every other day,10 mg in two days and then 10 mg once a day. The course of treatment is at least 6 weeks.

In case of a long-term marked decrease in blood pressure (systolic blood pressure less than 90 mm Hg for more than 1 hour), treatment with the drug should be discontinued.

Diabetic nephropathy: in patients with type 2 diabetes mellitus,10 mg of Lisinopril is used once a day. The dose can be increased, if necessary, to 20 mg once a day in order to achieve diastolic blood pressure values below 75 mm Hg in the “sitting” position. In patients with type 1 diabetes, the dose is the same, in order to achieve diastolic blood pressure values below 90 mm Hg in the “sitting” position.

Overdose

Symptoms (occur when taking a single dose of 50 mg): marked decrease in blood pressure, dryness of the oral mucosa, drowsiness, urinary retention, constipation, anxiety, increased irritability.

Treatment: there is no specific antidote. Symptomatic therapy. Gastric lavage, use of enterosorbents and laxatives. Intravenous use of 0.9% sodium chloride solution is indicated. In the case of treatment-resistant bradycardia, an artificial pacemaker should be used. It is necessary to monitor blood pressure, water and electrolyte balance indicators. Hemodialysis is effective.

Special instructions

Symptomatic hypotension

Most often, a marked decrease in blood pressure occurs with a decrease in the volume of circulating blood (BCC) caused by diuretic therapy, a decrease in table salt in food, dialysis, diarrhea or vomiting. In patients with chronic heart failure with simultaneous renal failure or without it, a pronounced decrease in blood pressure is possible.

Under strict medical supervision, Lisinopril should be used in patients with coronary heart disease, cerebrovascular insufficiency, in which a sharp decrease in blood pressure can lead to myocardial infarction or stroke. 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, but with normal or reduced blood pressure, may experience a decrease in blood pressure, which is usually not a reason to stop treatment.

Before starting treatment with the drug, if possible, the sodium content should be normalized and/or the BCC should be replenished, and the effect of the initial dose of Lisinopril on the patient should be carefully monitored.

In the case of renal artery stenosis (especially with bilateral stenosis or in the presence of stenosis of the artery of a single kidney), as well as with circulatory failure due to a lack of sodium ions and/or fluid, the use of Lisinopril can lead to impaired renal function, acute renal failure, which usually turns out to be irreversible even after discontinuation of the drug.

In acute myocardial infarction

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

Surgical intervention/General anesthesia

With extensive surgical interventions, as well as with the use of other agents that cause a decrease in blood pressure, Lisinopril, blocking the formation of angiotensin II, can cause a pronounced unpredictable decrease in blood pressure.

In elderly patients, the same dose leads to a higher concentration of the drug in the blood, so special care is required when determining the dose.

Since the potential risk of agranulocytosis cannot be excluded, periodic monitoring of the blood picture is required. When using the drug in a dialysis setting with polyacrylonitrile membranes, anaphylactic shock may occur, so either a different type of dialysis membrane or the appointment of other antihypertensive agents is recommended.

Influence on the ability to drive vehicles and mechanisms

There are no data on the effect of Lisinopril on the ability to drive vehicles and mechanisms used in therapeutic doses, but it should be borne in mind that at the beginning of treatment, hypotension may develop, which may affect the ability to drive vehicles and work with potentially dangerous mechanisms, as well as dizziness and drowsiness, so caution should be exercised.

Storage conditions

 In a dark place, at a temperature not exceeding 25 °C.

Shelf life

2 years

Active ingredient

Lisinopril

Conditions of release from pharmacies

By prescription

Dosage form

Tablets