Lisinopril of Grindeks

General characteristics. Structure:

Active ingredient: 10 mg or 20 mg of lisinopril.

Excipients: starch prezhelatinizirovanny, starch corn, calcium hydrophosphate anhydrous, Mannitolum, silicon dioxide colloid anhydrous, magnesium stearate.

Antihypertensive.

Pharmacological properties:

Pharmacodynamics. Inhibits APF, prevents transition of angiotensin I to angiotensin II, increases concentration of endogenous vazodilatiruyushchy PG. Arginine-vasopressin and эндотелина−1, having vasopressor properties reduces education. Lowers OPSS, system the ABP, an afterload on a myocardium, pressure in pulmonary capillaries.

Increases cordial emission and tolerance of a myocardium to loading at patients with heart failure. Increases (for the second time) activity of a renin of a blood plasma. Action is shown in 1 h, increases during 6–7 h, continues to 24 h.

The hypotensive effect reaches optimum values at repeated appointment within several weeks. The renin-angiotenzinovuyu inhibits fabric system of heart, prevents development of a hypertrophy of a myocardium and dilatation of a left ventricle or promotes their involution (cardioprotective action).

Reduces number of cases of sudden death, reduces probability of development of a repeated myocardial infarction, disturbances of a coronary blood-groove and developing of ischemia of a myocardium. According to the research ATLAS at patients with chronic heart failure use of lisinopril in high doses (35 mg), in comparison with its use in low doses (5 mg), reduced the combined indicator: the general mortality + all reasons of hospitalization for 12%, hospitalization number — for 13%, hospitalization number concerning a decompensation of heart failure — for 24%.

Results of the research CALM (a combination therapy kandesartany and lisinopril) showed big expressiveness of nefroprotektivny and hypotensive effects in group of the patients receiving the combined treatment in 24 weeks.

Pharmacokinetics. After intake about 25% (6–60%) are soaked up. Meal does not exert impact on absorption.

Badly contacts proteins of plasma (6–10%). It does not biotransformirutsya and excreted by kidneys in not changed look, the elimination half-life makes 12 h. Clinically significant changes of pharmacokinetic parameters demanding correction of the mode of dosing are observed at reduction of glomerular filtering less than 30 ml/min. (Cmax in plasma increases, the elimination half-life and time of action is extended).

Elderly patients have a concentration in plasma and AUC increase twice. Is removed at a hemodialysis. At introduction to rats slightly passes through GEB, does not kumulirut in fabrics at repeated use, it is found in breast milk and a placenta (but not in fruit fabrics).

Indications to use:

Arterial hypertension (mono - and a combination therapy), including renovascular; chronic heart failure (as a part of a combination therapy for treatment of the patients accepting drugs of a foxglove and/or diuretics); an acute myocardial infarction (in the first 24 h with stable indicators of a hemodynamics for maintenance of these indicators, and also for prevention of dysfunction of the left heart camera and heart failure); a diabetic nephropathy (for decrease in an albuminuria at insulin-dependent patients with the normal ABP and insulinonezavisimy patients with arterial hypertension).

Route of administration and doses:

Inside, 1 time a day in the morning, irrespective of meal, preferably at the same time.
Essential hypertensia: an initial dose - 10 mg/days, a maintenance dose - 20 mg/days. The maximum daily dose - 40 mg. For full development of effect 2-4 weeks can be required that should be considered at increase in a dose. If use of drug in the maximum dose does not cause sufficient therapeutic effect, then perhaps additional appointment other hypotensive HP.
At the patients receiving previously diuretics it is necessary to cancel them in 2-3 days prior to drug use. At impossibility of cancellation of diuretics the initial dose of lisinopril has to make no more than 5 mg/days.
Renovascular hypertensia or other states with a superactivity of RAAS: an initial dose - 2.5-5 mg/days under control of the ABP, function of kidneys, potassium concentrations in blood serum. The maintenance dose is established depending on size ABP.
At HPN the dose is defined depending on KK: at KK of 30-70 ml/min. - 5-10 mg/days, at KK - 10-30 ml/min. - 2.5-5 mg/days, less than 10 ml/min., including the patients who are on a hemodialysis - 2.5 mg/days. The maintenance dose is defined depending on the ABP (under control of function of kidneys, concentration of K+ and Na + in blood).
HSN (along with diuretics and/or cardiac glycosides): an initial dose - 2.5 mg/days, with gradual increase on 2.5 mg in 3-5 days to 5-10 mg/days. The maximum daily dose - 20 mg. Whenever possible the dose of diuretic should be reduced prior to lisinopril reception.
Acute myocardial infarction (as a part of a combination therapy in the first 24 h with stable indicators of a hemodynamics): in the first 24 h - 5 mg, then 5 mg in 1 days, 10 mg in two days and then on 10 mg of 1 times a day. A course of treatment - not less than 6 weeks.
In an initiation of treatment or within the first 3 days after an acute myocardial infarction at patients with the low systolic ABP (120 mm hg or below) appoint a smaller dose - 2.5 mg. In case of decrease in the ABP (systolic the ABP is lower or 100 mm hg are equal) the daily dose in 5 mg if necessary is temporarily reduced to 2.5 mg. In case of the long expressed decrease in the ABP (systolic the ABP is lower than 90 mm hg more than 1 h) treatment by drug is stopped.
Diabetic nephropathy: an initial dose - 10 mg/days which is raised if necessary to 20 mg/days for the purpose of achievement of values of the diastolic ABP by lower than 75 mm hg in situation "sitting" for patients with a diabetes mellitus 2 types and lower than 90 mm hg in situation "sitting" at patsiyentovsakharny diabetes of 1 type.

Features of use:

Treatment is carried out under regular medical control. Prior to treatment it is necessary to correct water and electrolytic balance. During treatment monitoring of the ABP, level of protein and potassium in plasma, an urea nitrogen, creatinine, function of kidneys, a picture of blood, body weight and observance of a diet is necessary. Care is necessary during operative measures (including dental), especially when using the general anesthetics having hypotensive effect. It is necessary to avoid carrying out a hemodialysis through high-performance membranes from a poliakrilonitrilmetaallilsulfat (for example AN69), haemo filterings or LNP-afereza (development of an anaphylaxis or anaphylactoid reactions is possible).

Contraindicated at pregnancy.

Category of action on a fruit on FDA — C (the I trimester).

Category of action on a fruit on FDA — D (II and III trimesters).

For the period of treatment it is necessary to stop breastfeeding.

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 an ischemic heart disease or a cerebrovascular disease is possible, from dekompensirovanny HSN (arterial hypotension, a myocardial infarction, a stroke are possible).

At patients with HSN the arising arterial hypotension can lead to deterioration in function of kidneys. The expressed decrease in the ABP against the background of treatment most often arises at decrease in OTsK caused by therapy by diuretics, restriction of consumption of table salt, dialysis, diarrhea or vomiting.

Treatment by lisinopril at an acute myocardial infarction is carried out against the background of standard therapy (trombolitik, ASK, beta adrenoblockers). Let's combine with in/in administration of nitroglycerine or with nitroglycerine TTS.

At use of HP, the reducing ABP, 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. Before surgical intervention (including dental surgery) it is necessary to inform the surgeon/anaesthesiologist on APF inhibitor use.

On the basis of results of epidemiological researches it is supposed that the concomitant use of APF inhibitors and insulin, and also peroral hypoglycemic HP can lead to development of a hypoglycemia. The greatest risk of development is observed within the first weeks of a combination therapy, and also at patients with a renal failure.

Careful control of a glycemia is required from patients with a diabetes mellitus, especially during the first month of therapy by APF inhibitor. Before an initiation of treatment it is necessary to offset loss of liquid and salts. Risk factors for development of a hyperpotassemia include HPN, a diabetes mellitus and simultaneous use of kaliysberegayushchy diuretics (Spironolactonum, Triamterenum or amiloride), the drugs K+ or substitutes of salt containing K+. Periodic control of concentration of K+ in a blood plasma is recommended.

At the patients accepting APF inhibitors when performing desensitization to a gimenopter emergence of life-threatening anaphylactoid reaction is extremely rare, possible. It is necessary to stop temporarily treatment by APF inhibitor before a desensitization course. Emergence of anaphylactoid reactions at simultaneous carrying out a hemodialysis with use of high-flowing membranes is possible (including AN 69). It is necessary to consider the possibility of use of other type of a membrane for dialysis or other hypotensive HP.

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

Side effects:

From a nervous system and sense bodys: headache, dizziness, increased fatigue, consciousness disturbances, irritability, nervousness, passing disturbance of cerebral circulation, syncope, ataxy, decrease in memory, drowsiness, sleeplessness, peripheral neuropathy, paresthesia, tremor, spasms, visual disturbances (diplopia, photophobia, decrease in visual acuity), sonitus.

From cardiovascular system and blood (a hemopoiesis, a hemostasis): heartbeat, a stethalgia, the expressed decrease in the ABP, arrhythmia (atrial and ventricular tachycardia, fibrillation of auricles, bradycardia, etc.), a cardiac standstill, a myocardial infarction, orthostatic reactions, a vasculitis, oppression of marrow, a leukopenia, thrombocytopenia, anemia.

From respiratory system: dry cough, malignant tumors of lungs, a pneumorrhagia, infiltration, an embolism and a heart attack of a lung, a bronchospasm, asthma, a pleural exudate, pain at breath, bronchitis, laryngitis, sinusitis, pharyngitis, rhinitis, nasal bleeding, cold, paroxysmal postural диспноэ.

From bodies of a GIT: dryness in a mouth, dyspepsia, heartburn, nausea, vomiting, a diarrhea/lock, a meteorism, GIT spasms, an abdominal pain, a hepatotoxic (hepatitis, cholestatic jaundice, a fulminantny necrosis of a liver with possible death), gastritis, pancreatitis.

From urinogenital system: renal failure, acute renal failure, pyelonephritis, dysuria, oliguria, anury, uraemia, hypostases, weakening of a libido, impotence.

From a musculoskeletal system: arthritis, arthralgia, mialgiya, neck, spin pain.

From integuments: rash, urticaria, an alopecia, a photosensitization, a pempigus, damages and infections of skin, a toxic epidermal necrolysis, Stephens's syndrome — Johnson.

Others: reduction (increase) of body weight, fever, perspiration, allergic reactions, including Quincke's disease, development of infections, including herpes zoster, diabetes mellitus, dehydration, gout, increase in a caption of antinuclear antibodies, concentration of creatinine, urea, hyperpotassemia, hyponatremia, hyperuricemia.

Interaction with other medicines:

Contraindications:

Hypersensitivity to lisinopril or other APF inhibitors; a Quincke's disease in the anamnesis, including and from use of APF inhibitors, a hereditary Quincke's edema or idiopathic hypostasis; pregnancy, feeding by a breast, age up to 18 years (safety and efficiency of use are not defined).

Overdose:

At overdose acute arterial hypotension is observed.

Treatment: introduction of normal saline solution and other symptomatic therapy. Is removed at a hemodialysis.

Storage conditions:

In the dry, protected from light place, at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

14 tablets in the blister, on 2 blisters in cardboard packaging.