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medicalmeds.eu Medicines Angiotensin-converting enzyme inhibitor (APF inhibitor). Lizinoton

Lizinoton

Препарат Лизинотон. Actavis Ltd. (Актавис Лтд.) Швейцария


Producer: Actavis Ltd. (Aktavis Ltd.) Switzerland

Code of automatic telephone exchange: C09AA03

Release form: Firm dosage forms. Tablets.

Indications to use: Acute myocardial infarction. Chronic heart failure. Arterial hypertension.


General characteristics. Structure:

Lizinoton of 5 mg 
Active agent: Lisinopril dihydrate of the corresponding 5 mg of lisinopril
Excipients: Mannitolum, calcium hydrophosphate dihydrate, starch corn prezhelatinizirovanny, sodium of a kroskarmeloz, magnesium stearate.

Lizinoton of 10 mg 
Active agent: Lisinopril dihydrate of the corresponding 10 mg of lisinopril Mannitolum, calcium hydrophosphate dihydrate, starch corn prezhelatinizirovanny, sodium of a kroskarmeloz, magnesium stearate, pigmental mix PV-24823 Pink (E 172).

Lizinoton of 20 mg
Active agent: Lisinopril dihydrate of the corresponding 20 mg of lisinopril.
Excipients: Mannitolum, calcium hydrophosphate dihydrate, starch corn prezhelatinizirovanny, sodium of a kroskarmeloz, magnesium stearate, pigmental mix PV-24824 Pink (E 172).
Description. Round, biconvex tablets with a notch. Tablets with a dosage of 5 mg - white color, 10 mg - light pink color, 20 mg - pink color.




Pharmacological properties:

Pharmacodynamics. APF inhibitor, reduces formation of II angiotensin of angiotensin I. Decrease in content of angiotensin II leads to direct reduction of allocation of Aldosteronum. Reduces degradation of bradikinin and increases synthesis of prostaglandins. Reduces the general peripheric vascular resistance, the arterial pressure (AP), preloading, pressure in pulmonary capillaries, causes increase in minute volume of blood and increase in tolerance of a myocardium to loadings in patients with chronic heart failure. Expands arteries more than veins. Some effects are explained by influence on fabric a system renin-angiotenzinovye. At prolonged use the hypertrophy of a myocardium and walls of arteries of resistive type decreases. Improves blood supply of an ischemic myocardium.

APF inhibitors extend life expectancy at patients with chronic heart failure, slow down progressing of dysfunction of a left ventricle at the patients who had a myocardial infarction without clinical displays of heart failure. The anti-hypertensive effect begins approximately in 6 hours and remains within 24 hours.

Duration of effect depends also on dose size. The beginning of action - in 1 h. The maximum effect is defined in 6-7 hours. At arterial hypertension the effect is noted in the first days after an initiation of treatment, stable action develops in 1-2 months.

At sharp drug withdrawal did not observe the expressed increase in the ABP.

In addition to decrease in the ABP lisinopril reduces an albuminuria. At patients with a hyperglycemia contributes to normalization of function of the damaged glomerular endothelium.

Lisinopril does not influence concentration of glucose in blood at patients with a diabetes mellitus and does not lead to increase of cases of a hypoglycemia.

Pharmacokinetics. Absorption. After administration of drug inside lisinopril is soaked up from digestive tract. Meal does not influence drug absorption. Absorption averages 30%, bioavailability - 29%.

Distribution. Does not contact proteins of plasma. The maximum concentration in plasma (90 ng/ml) is reached in 7 hours. Permeability through a blood-brain and placental barrier low.

Metabolism. Lisinopril does not biotransformirutsya in an organism.

Removal. It is removed by kidneys in not changed look. The elimination half-life makes 12 hours.


Indications to use:

Arterial hypertension (including symptomatic), a chronic circulatory unefficiency, early treatment of an acute myocardial infarction at patients with a stable hemodynamics (as a part of a combination therapy).


Route of administration and doses:

Inside. At arterial hypertension the patient who is not receiving other antihypertensives appoint 5 mg of 1 times a day. In the absence of effect the dose is raised by each 2-3 days on 5 mg to an average therapeutic dose of 20-40 mg/days (increase in a dose usually does not lead over 40 mg/days to a further lowering of arterial pressure). The full effect develops usually in 2-4 weeks from an initiation of treatment. At insufficient clinical effect the drug combination with other antihypertensives is possible.

If the patient received preliminary treatment by diuretics, then reception of such drugs needs to be stopped in 2-3 days prior to Lizinoton's use. If it is impracticable, then the initial dose of lisinopril should not exceed 5 mg a day. In this case after reception of the first dose medical control within several hours (the maximum of action is reached approximately in 6 hours) as there can be an expressed decrease in the ABP is recommended.

At heart failure - begin with 2.5 mg once, with the subsequent increase in a dose by 2.5 mg in 3-5 days.

At elderly more expressed long hypotensive action is often observed that it is connected with reduction of speed of removal of lisinopril (it is recommended to begin treatment with 2.5 mg/days).

At a chronic renal failure cumulation comes at decrease in filtering less than 50 ml/min. (the dose has to be reduced twice, at clearance of creatinine less than 10 ml/min. are required to reduce a dose by 75%).

At persistent arterial hypertension the long maintenance therapy on 10-15 mg/days is shown, at heart failure - on 7.5-10 mg/days.


Features of use:

Extra care at appointment as the patient with a bilateral stenosis of renal arteries or a stenosis of an artery of the only kidney is required (increase in concentration of urea and creatinine in blood), the patient with coronary heart disease or a cerebrovascular disease is possible, with a dekompensirovanny chronic circulatory unefficiency (arterial hypotension, a myocardial infarction, a stroke are possible). At patients with a chronic circulatory unefficiency the arising arterial hypotension can lead to deterioration in function of kidneys.

At use of the medicines reducing arterial pressure for patients at extensive surgical intervention or during anesthesia lisinopril can block formation of angiotensin II, secondary in relation to compensatory allocation of a renin.

Safety and efficiency of use of lisinopril for children is not established.

Before an initiation of treatment it is necessary to offset loss of liquid and salts.

Use during pregnancy is contraindicated, except for cases when it is impossible to apply other lekarstvenna of means or they are inefficient (the patient has to be informed on potential risk for a fruit).

With care patients should appoint drug: sangionevrotichesky hypostasis in the anamnesis against the background of therapy by APF inhibitors, with a hereditary or idiopathic Quincke's disease, with an aortal stenosis, with cerebrovascular diseases (including with insufficiency of cerebral circulation, with coronary heart disease, with coronary insufficiency, with serious autoimmune general diseases of connecting fabric (including - with a system lupus erythematosus, a scleroderma), with oppression of a marrowy hemopoiesis, with a diabetes mellitus, with a hyperpotassemia, with a bilateral stenosis of renal arteries, with a stenosis of an artery of the only kidney, at patients is after transplantation of kidneys, with a renal failure, to the patients who are on a diet with sodium restriction at the states which are followed by decrease in volume of the circulating blood (including at diarrhea, a rvotaa), to people of advanced age, aged up to 18 years (safety and efficiency of use are not studied).


Side effects:

From cardiovascular system: decrease in the ABP, arrhythmia, a stethalgia, is rare - orthostatic hypotension, tachycardia.

From a nervous system: dizziness, a headache, increased fatigue, drowsiness, twitching of muscles of extremities and lips, is rare - an adynamy, lability of mood, confusion of consciousness.

From the alimentary system: nausea, dyspepsia, a loss of appetite, taste change, an abdominal pain, diarrhea, dryness in a mouth

From bodies of a hemopoiesis: leukopenia, thrombocytopenia, neutropenia, agranulocytosis, anemia (decrease in hemoglobin, erythrocytopenia).

Allergic reactions: Quincke's disease, skin rashes, itch.

Laboratory indicators: hyperpotassemia, hyperuricemia; seldom - increase in activity of "hepatic" transaminases, a hyperbilirubinemia.

Others: Sukhoi cough, decrease in a potentiality; seldom - an acute renal failure, an arthralgia, a mialgiya, fever, hypostasis (language, lips, extremities), disturbance of development of kidneys of a fruit.


Interaction with other medicines:

Slows down removal of drugs of lithium.

Non-steroidal anti-inflammatory drugs, estrogen, adrenostimulyator reduce hypotensive effect of drug.

At simultaneous use with kaliysberegayushchy diuretics and drugs of potassium the hyperpotassemia is possible.

The combined use with β-adrenoblockers, blockers of slow calcium channels, diuretics and other hypotensive medicines increases expressiveness of hypotensive action.

Antacids and Colestyraminum reduce absorption in digestive tract.


Contraindications:

Hypersensitivity to lisinopril or other APF inhibitors, a Quincke's disease in the anamnesis, including from use of APF inhibitors, age up to 18 years.

With care: the expressed renal failures, a bilateral stenosis of renal arteries or a stenosis of an artery of the only kidney with the progressing azotemia, a state after transplantation of a kidney, a renal failure, an azotemia, a hyperpotassemia, a stenosis of the mouth of an aorta

Use at pregnancy and in the period of a lactation
 Use of lisinopril during pregnancy is contraindicated. At pregnancy establishment administration of drug needs to be stopped as soon as possible. Reception of APF inhibitors in II and the III trimester of pregnancy makes an adverse effect on a fruit (the expressed decrease in the ABP, a renal failure, a hyperpotassemia, a skull hypoplasia, pre-natal death are possible). There are no data on negative impacts of drug on a fruit in case of use during the I trimester. For newborns and babies who underwent pre-natal influence of APF inhibitors it is recommended to conduct careful observation for early detection of the expressed decrease in the ABP, an oliguria, a hyperpotassemia.

For treatment by drug it is necessary to cancel breastfeeding.


Overdose:

Symptoms (arise at reception of a single dose of 50 mg) - dryness in a mouth, drowsiness, an urination delay, locks, concern, an acrimony.
Treatment: gastric lavage, purpose of symptomatic medicines. The specific antidote does not exist. The hemodialysis is inefficient.


Storage conditions:

At a temperature not above 25 °C. To store in the place, unavailable to children! Period of validity 3 years. Drug should not be used after the expiry date specified on packaging.


Issue conditions:

According to the recipe


Packaging:

On 10 or on 14 tablets in the blister from PVC / aluminum foil.
On 3 blisters on 10 tablets or on 2 blisters on 14 tablets in a cardboard pack.



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