Lisinopril pills 10mg, 30pcs

Composition

Active ingredient:

lisinopril dihydrate;

Auxiliary substances:

milk sugar (lactose),

microcrystalline cellulose,

starch 1500 (gelatinized),

aerosil (colloidal silicon dioxide),

talc,

magnesium stearate

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 a combination therapy for the treatment of patients taking digitalis and/or diuretics);
• Early treatment of acute myocardial infarction (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 insulin-dependent patients with normal blood pressure and non-insulin-dependent patients with arterial hypertension).

Contraindications

Hypersensitivity to lisinopril or other ACE inhibitors, a history of angioedema, including from the use of ACE inhibitors, hereditary angioedema, age up to 18 years (efficacy and safety have not been established).

With caution:  severe renal dysfunction, bilateral renal artery stenosis or stenosis of the artery of a single kidney with progressive azotemia, condition after kidney transplantation, renal failure, azotemia, hyperkalemia, aortic stenosis, hypertrophic obstructive cardiomipathy, primary hyperaldosteronism, arterial hypotension, cerebrovascular diseases (including cerebrovascular insufficiency), coronary heart disease, coronary insufficiency, autoimmune systemic diseases of connective tissue (including scleroderma, systemic lupus erythematosus); suppression of bone marrow hematopoiesis; diet with sodium restriction: hypovolemic conditions (including as a result of diarrhea, vomiting); elderly age.

Side Effects

Are Common:  dizziness, headache (5-6% of patients), weakness, diarrhea, dry cough (3%), nausea, vomiting, orthostatic hypotension, skin rash, chest pain (1-3%).

Immune system disorders: (0.1%) angioedema (face, lips, tongue, larynx or epiglottis, upper and lower extremities).

From the cardiovascular system:  marked decrease in blood pressure, orthostatic hypotension, impaired renal function, cardiac arrhythmias, rapid heartbeat.

From the central nervous system:  increased fatigue, drowsiness, convulsive twitching of the muscles of the limbs and lips.

From the hematopoietic system:  possible leukopenia, neutropenia, agranulocytosis, thrombocytopenia, with prolonged treatment-a slight decrease in the concentration of hemoglobin and hematocrit, erythrocytopenia.

Laboratory parameters:  hyperkalemia, azotemia, hyperuricemia, hyperbilirubinemia, increased activity of “liver” enzymes, especially in the presence of a history of kidney disease, diabetes mellitus and renovascular hypertension.

Rarely

From the cardiovascular system:  palpitations; tachycardia; myocardial infarction; cerebrovascular stroke in patients with an increased risk of the disease, due to a pronounced decrease in blood pressure.

From the digestive tract:  dry mouth, anorexia, dyspepsia, taste changes, abdominal pain, pancreatitis, hepatocellular or cholestatic jaundice, hepatitis.

From the side of the skin:  urticaria, increased sweating, pruritus, alopecia.

From the urinary system:  impaired renal function, oliguria, anuria, acute renal failure, uremia, proteinuria.

From the immune system:  a syndrome that includes accelerated erythrocyte sedimentation rate (ESR), arthralgia, and the appearance of antinuclear antibodies.

From the central nervous system:  asthenic syndrome, mood lability, confusion, decreased potency.

Other services:  myalgia, fever, impaired fetal development.

Interaction

Lisinopril reduces the elimination of potassium from the body when treated with diuretics. Extreme care is required during simultaneous use of the drug:

• potassium-sparing diuretics (spironolactone, triamterene, amiloride), potassium, salt substitutes containing potassium (increased risk of hyperkalemia, especially when impaired renal function), so they can be shared only be assigned based on individual decisions of the attending physician of the regular monitoring of the level of potassium in the blood serum and renal function.

Caution can be applied together:

• with diuretics: in additional use of a diuretic to a patient receiving lisinopril, usually in additive antihypertensive effect of risk expressed lower AD;
• with other antihypertensive agents (additive effect);
• and non-steroidal anti-inflammatory drugs (Indometacin, etc. ), estrogens, as well as agonists – reduction of the antihypertensive effect of lisinopril;
• with lithium (lithium allocation can be reduced, therefore, you should regularly monitor the concentration of lithium in blood serum);
• with antacids and kolestiraminom – reduce absorption in the gastrointestinal tract.

Alcohol increases the effect of the drug.

How to take it, course of use and dosage

Inside, regardless of food intake. 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 Lisinopril use. If this is not feasible, 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 2.5-5 mg per day, under increased medical supervision (control of blood pressure, renal function, and serum potassium concentration). The maintenance dose, while continuing strict medical monitoring, should be determined depending on the dynamics of blood pressure. In case of renal insufficiency, due to the fact that lisinopril is excreted through the kidneys, the initial dose should be determined depending on creatinine clearance, then, in accordance with the reaction, a maintenance dose should be established in conditions of frequent monitoring of renal function, serum potassium and sodium levels.

With persistent arterial hypertension, long-term maintenance therapy of 10-15 mg/day is indicated. In case of chronic heart failure-start with 2.5 mg once a day, followed by an increase in the dose by 2.5 mg in 3-5 days to the usual, maintenance daily dose of 5-20 mg. The dose should not exceed 20 mg per day.

Elderly people often have a more pronounced long-term hypotensive 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). Acute myocardial infarction (as part of combination therapy) 

On the first day – 5 mg orally, then 5 mg every other day,10 mg in two days and then 10 mg once a day. 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 mm Hg or lower), a lower dose of 2.5 mg should be prescribed. If blood pressure decreases (systolic blood pressure is less than or equal to 100 mm Hg), the daily dose of 5 mg can be temporarily reduced to 2.5 mg, if necessary. 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.

Diabetic nephropathy In patients with non-insulin-dependent 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 a sitting position. In patients with insulin-dependent diabetes mellitus, the dosage is the same, in order to achieve diastolic blood pressure values below 90 mm Hg in a sitting position.

Overdose

Symptoms (occur when taking a single dose of 50 mg or higher):

marked decrease in blood pressure; dry mouth, drowsiness, urinary retention, constipation, anxiety, increased irritability.

Treatment:

symptomatic therapy, intravenous fluid use, control of blood pressure, water-electrolyte balance and normalization of the latter. Lisinopril can be removed from the body by hemodialysis.

Special instructions

Symptomatic hypotension

Most often, a marked decrease in blood pressure occurs with a decrease in fluid volume caused by diuretic therapy, a decrease in the amount of 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. 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 with Lisinopril should be started under strict medical supervision (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.

A transient hypotensive reaction 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 low blood pressure, may experience a decrease in blood pressure, which is usually not a reason to stop treatment.

Before starting treatment with Lisinopril, if possible, the sodium concentration should be normalized and / or the lost volume of fluid 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 and/or fluid, the use of Lisinopril can also lead to impaired renal function, acute renal failure, which usually turns out to be irreversible 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 drugs 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 polyacrylonitrile membrane dialysis setting, anaphylactic shock may occur, so either a different type of dialysis membrane is recommended, or other antihypertensive agents are prescribed.

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 dizziness may occur, so caution should be exercised.

Composition

Tablet Form of production

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