Lisinopril tablets 10 mg, 30 pcs. (lisinopril)

Release form

tablets

Pharmacological action

An 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 aldosterone excretion. 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 exercise tolerance in patients with chronic heart failure. Expands arteries to a greater extent than veins. Some effects are attributed to exposure to the renin-angiotensin-aldosterone system (RAAS).

With prolonged use, hypertrophy of the myocardium and walls of the arteries 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 after acute myocardial infarction without clinical manifestations of heart failure. The onset of action of the drug is after 1 hour, the maximum antihypertensive effect is achieved after 6-7 hours and lasts for 24 hours.

The duration of the effect also depends on the size of the dose taken. With arterial hypertension, the effect is observed in the first days after the start of treatment, a stable effect develops after 1-2 months. therapy. With a sharp abolition of lisinopril, there was no marked increase in blood pressure.

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

Pharmacokinetics

Absorption.

After oral administration, lisinopril is absorbed from the gastrointestinal tract (GIT) by an average of 25%, but absorption can vary from 6 to 60%. Bioavailability is 29%. The maximum plasma concentration (Cmax) is reached after 7 hours. Eating does not affect the absorption of lisinopril.

distribution.

Lisinopril is slightly bound to plasma proteins. Permeability through the blood-brain and placental barrier is low. Metabolism. Lisinopril is not biotransformed in the body.

Withdrawal.

Excreted by the kidneys unchanged. The half-life (T1 / 2) is 12.6 hours. The clearance of lisinopril is 50 ml / min. A decrease in the serum concentration of lisinopril occurs in two phases. The main part of lisinopril is excreted during the initial alpha phase (effective T1 / 2-12 hours), followed by the terminal distant beta phase (about 30 hours).

Pharmacokinetics in selected patient groups

In patients with heart failure, the absorption and clearance of lisinopril are reduced, bioavailability is 16%.

In patients with renal failure (creatinine clearance (CC) less than 30 ml / min), the concentration of lisinopril is several times higher than the concentration in the blood plasma of healthy volunteers, and there is an increase in the time to reach Cmax in blood plasma and an increase in T1 / 2.

In elderly patients, the concentration of the drug in the blood plasma and the area under the concentration-time curve is 2 times higher, than in young patients.

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

In elderly patients, the concentration of lisinopril in the blood is increased by an average of 60%.

Indications

Arterial hypertension (in monotherapy or in combination with other antihypertensive drugs).

Chronic heart failure (as part of combination therapy).

Early treatment of acute myocardial infarction (in the first 24 hours with stable hemodynamic parameters to maintain these parameters and prevent left ventricular dysfunction and heart failure).

Diabetic nephropathy (decreased 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 or other ACE inhibitors, history of angioedema, including the use of ACE inhibitors, hereditary Quincke edema, age under 18 years (efficacy and safety have not been established).

Caution: severe renal impairment, bilateral renal artery stenosis or stenosis of a single kidney artery with progressive azotemia, condition after kidney transplantation, renal failure, azotemia, hyperkalemia, stenosis of the aortic orifice, hypertrophic obstructive cardiomyopathy, primary hyperaldosteronism, cerebrovascular disease ), coronary heart disease, coronary insufficiency, autoimmune systemic diseases of the connective tissue (including scleroderma, sys dark lupus erythematosus) suppression of bone marrow hematopoiesis diet with sodium restriction: hypovolemic conditions (including as a result of diarrhea, vomiting) old age.

Use during pregnancy and lactation

The use of lisinopril during pregnancy is contraindicated. When pregnancy is established, the drug should be discontinued as soon as possible. Acceptance of ACE inhibitors in the II and III trimester of pregnancy has an adverse effect on the fetus (a pronounced decrease in blood pressure, renal failure, hyperkalemia, skull hypoplasia, intrauterine death are possible). There are no data on the negative effects of the drug on the fetus if used during the first trimester. For newborns and infants who underwent intrauterine exposure to ACE inhibitors, it is recommended to conduct careful monitoring to timely detect a pronounced decrease in blood pressure, oliguria, hyperkalemia.

Lisinopril crosses the placenta. There is no data on the penetration of lisinopril into breast milk. For the period of treatment with the drug, it is necessary to cancel breastfeeding.

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 marked 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 large doses of diuretics, hyponatremia, or impaired renal function. In such patients, treatment with Lisinopril should be started under the strict supervision of a physician (with caution, select a dose of the drug and diuretics).

Similar rules should be followed when prescribing patients with coronary heart disease, cerebrovascular insufficiency, in which a sharp decrease in blood pressure can lead to myocardial infarction or stroke.

Transient hypotensive reaction is not a contraindication for taking the next dose of the drug.

When using Lisinopril in some patients with chronic heart failure, but with normal or low blood pressure, a decrease in blood pressure may occur, which is usually not a reason for stopping treatment.

Before starting treatment with Lisinopril, if possible, normalize the concentration of sodium and / or replenish the lost volume of fluid, carefully monitor the effect of the initial dose of Lisinopril on the patient.

In case of renal artery stenosis (especially with bilateral stenosis, or in the presence of a single kidney artery stenosis), as well as circulatory failure due to lack of sodium and / or fluid, the use of Lisinopril can lead to impaired renal function, acute renal failure, which usually 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 conjunction with intravenous administration or with the use of therapeutic transdermal systems of nitroglycerin.

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, therefore, special care is required when determining the dose.

Since the potential risk of agranulocytosis cannot be ruled out, periodic monitoring of the blood picture is required. When using the drug in dialysis with a polyacryl-nitrile membrane, anaphylactic shock can occur, therefore, it is recommended that either a different type of membrane for dialysis, or the appointment of other antihypertensive agents.

Influence on the ability to drive vehicles and mechanisms

There is no data on the effect of lisinopril on the ability to drive vehicles and mechanisms used in therapeutic doses, however, it should be borne in mind that dizziness may occur, therefore caution should be exercised.

Composition of

1 tablet contains:

active substance:

lisinopril dihydrate (lisinopril) - 10.92 mg (10.00 mg)

excipients:

starch pregelatinized 12.00 mg,

starch 40 mg

calcium hydrogen phosphate (anhydrous) 84.88 mg,

mannitol 70.00 mg,

magnesium stearate 2.20 mg.

Dosage and administration

Inside, regardless of food intake. With arterial hypertension, patients not receiving other antihypertensive drugs are prescribed 5 mg once a day. In the absence of 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 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 after 2-4 weeks from the start of treatment, which should be considered when increasing the dose. With insufficient clinical effect, it is possible to combine the drug with other antihypertensive drugs.

If the patient received preliminary treatment with diuretics, then the administration of such drugs must be stopped 2-3 days before the start of Lisinopril. 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 achieved after about 6 hours), since a marked 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 enhanced medical supervision (blood pressure control, renal function, serum potassium concentration). A maintenance dose, continuing strict medical supervision, should be determined depending on the dynamics of blood pressure.

In case of renal failure, due to the fact that lisinopril is excreted through the kidneys, the initial dose should be determined depending on the creatinine clearance, then, in accordance with the reaction, a maintenance dose should be established under conditions of frequent monitoring of renal function, potassium, sodium in blood serum.

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

In chronic heart failure - start with 2.5 mg once a day, followed by a 2.5 mg dose increase in 3-5 days to the usual, maintenance daily dose of 5-20 mg. The dose should not exceed 20 mg per day.

In elderly people, a more pronounced long-term hypotensive effect is often observed, which is associated with a decrease in the rate of lysinopril excretion (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 after 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 mmHg or lower), a lower dose of 2.5 mg should be prescribed. In the event of a decrease in blood pressure (systolic blood pressure below or equal to 100 mm Hg), a daily dose of 5 mg can, if necessary, be temporarily reduced to 2.5 mg. In the case of a 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 may, if necessary, be increased 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.

Side effects

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

On the part of the immune system: (0.1%) angioedema (face, lips, tongue, larynx or epiglottis, upper and lower extremities).

From the cardiovascular system: a marked decrease in blood pressure, orthostatic hypotension, impaired renal function, heart rhythm disturbance, heart palpitations.

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

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

Laboratory indicators: hyperkalemia, azotemia, hyperuricemia, hyperbilirubinemia, increased activity of “liver” enzymes, especially if there is 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 marked decrease in blood pressure.

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

From the skin: urticaria, sweating, pruritus, alopecia.

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

On the part of the immune system: a syndrome that includes an acceleration of the erythrocyte sedimentation rate (ESR), arthralgia and the appearance of antinuclear antibodies.

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

Other: myalgia, fever, impaired fetal development.

Drug Interactions

Lisinopril reduces potassium excretion from the body when treated with diuretics.

Special care is required while using the drug with:

potassium-sparing diuretics (spironolactone, triamteren, amiloride), potassium, sodium chloride substitutes containing potassium (increases the risk of hyperkalemia, especially with impaired renal function), therefore, they can be prescribed together only on the basis of an individual decision of the attending physician with regular monitoring of serum potassium levels and renal function.

May be used together with caution:

with diuretics: with the additional administration of a diuretic to a patient taking Lisinopril, as a rule, an additive antihypertensive effect occurs - a risk of a marked decrease in blood pressure

with other antihypertensive drugs (additive effect) srdlcytosis with non-allergic drugs and other .), estrogens, and also adrenostimulants - a decrease in the antihypertensive effect of lisinopril

with lithium (lithium excretion may decrease, therefore, regular olirovat serum lithium concentration)

with antacids and colestyramine - reduce absorption in the gastrointestinal tract.

Alcohol enhances the effect of the drug.

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 fluids, control of blood pressure, electrolyte balance and normalization of the latter.

Lisinopril can be removed from the body via hemodialysis.

Storage conditions

In a dry, dark place and out of reach of children, at a temperature not exceeding 25 ° C.

Term hodnosty

3 years

active substance

Lisinopril

Terms leave through pharmacies

In retseptu

lekarstvennaja form

tablets

Ozon, Russia



Lisinopril tablets 10 mg, 30 pcs. (lisinopril) florida in pharmacy online. Cheap price, instruction, side effects, dosage. Lisinopril tablets 10 mg, 30 pcs. - Sale. PayPal accept. Free shipping florida. Fast international shipping.