Lisinopril. 20 mg. 30 tablets
Lisinopril. 20 mg. 30 tablets
Indications for the treatment of essential and renovascular hypertension alone or in combination with other antihypertensives;
Treatment of heart failure in addition to cardiac glycosides and diuretics;
Prevention of left ventricular dysfunction and heart failure and improve survival in patients with acute myocardial infarction and stable hemodynamics in the first 24 hours.
Dosage and method of administration
Food does not affect absorption of the drug and thus may be used before,. during or after meals. Individual daily dose of the product is taken off.
Treatment of essential and renovascular hypertension:
The recommended starting dose is 10 mg (one tablet of 10 mg) once daily. An unsatisfactory therapeutic effect the dose may be increased to 20 mg. The maximum daily dose should not exceed 40 to 80 mg.
In patients with renovascular hypertension, the initial dosage should be lower - 2,5 mg - 5 mg, and gradually increasing the effective.
In hypertensive patients receiving diuretic treatment, the risk of symptomatic hypotension is greater, so special attention is required when initiating treatment with lisinopril. The diuretic should be discontinued two to three days prior to beginning therapy with lisinopril. If the diuretic can not be discontinued, therapy with lisinopril should be initiated with a low dose - 2,5 mg per day.
Treatment of heart failure:
The initial dose is 2,5 mg, which can then be increased to 5 mg - 20 mg once daily, depending on: the therapeutic response and tolerability.
In acute myocardial infarction in stable hemodynamics in the first 24 hours
The initial dose is 5 mg, followed by 5 mg after 24 hours. The dose may be increased to 10 mg on January 48 ~ hours. Treatment with lisinopril 10 mg a day goes b weeks.
In patients with myocardial infarction and a lower systolic blood pressure (120 mmHg or lower) treatment should be started at a dose of 2,5 mg for 3 days. If hypotension (systolic blood pressure less than 100 mmHg) a daily dose of 5 mg may be temporarily reduced to 2,5 mg. In the event naprolongirana hypotension (systolic pressure below 90 mmHg for more than one hour) lisinopril should be discontinued. During therapy with lisinopril patients should receive the recommended standard therapy with thrombolytics, aspirin and beta-blockers. Lisinopril is compatible with nitrates, intravenous or transdermal.
Patients with renal impairment
The dosage of lisinopril in patients with impaired renal function determined by creatinine clearance.
In high risk patients. eg patients with salt depletion, with volume depletion due to vomiting, diarrhea and more., with malignant hypertension with severe heart failure, patients with ischemic heart disease or cerebrovascular disease, the effect of the initial dose should be carefully monitored.
There are no specific studies on the effectiveness and safety of lisinopril for children and is therefore not recommended for use in children.
Known hypersensitivity to the active substance or excipients of the tablet;
Known hypersensitivity to other ACE inhibitors;
hereditary / idiopathic angioneurotic edema, and patients with a history of angioedema with previous treatment with an ACE inhibitor;
Haemodynamically significant aortic stenosis, or hypertrophic cardiomyopathy;
Patients with bilateral renal artery stenosis or stenosis of the artery to a solitary kidney.
Patients with unstable hemodynamics after acute myocardial infarction;
Simultaneous use of lisinopril and high-flux membranes of poliakrilnitrilnatriy-2-metilalilsulfonat (eg AN 96) in the emergency dialysis;
Patients with creatinine> 220 mmol / l;
Special warnings and special precautions for use
During treatment with lisinopril careful monitoring is required in patients with severe heart failure whose renal function depends on the activity of the renin-angiotensin-aldosterone system. Treatment of these patients with ACE inhibitors, including lisinopril, may lead to oliguria, progressive azotemia and rarely to acute renal failure.
In patients with underlying kidney disease are at higher risk of renal impairment (creatinine level increase in plasma) to acute renal failure. "ACE inhibitors can cause agranulocytosis. The risk of agranulocytosis or neutropenia was higher in patients with collagen (systemic lupus erythematosus, scleroderma) in patients receiving immunosuppressive therapy, particularly if there is concomitant kidney dysfunction. During treatment with lisinopril need regular blood counts.
Treatment with Lisinopril hypotension as an adverse drug reaction is rare. Careful monitoring is required for patients receiving diuretic therapy, located on dialysis, diarrhea or vomiting during surgery or general anesthesia, as they lisinopril can cause a marked hypotensive effect.
Patients at high risk of hypotension (ischemic heart disease, cerebrovascular disease), in which a sharp drop in blood pressure can lead to heart attack or serious ischemic attack, treatment with lisinopril should be initiated in hospital conditions, under strict medical supervision.
In patients with acute myocardial infarction should not take lisinopril treatment if evidence of renal dysfunction, serum creatinine above 177 pmol / i, and / or proteinuria exceeding 500 mg/24 hours. Upon the occurrence of renal dysfunction treatment with lisinopril should be discontinued.
In patients treated with ACE inhibitors, including. Lisinopril may, rarely, be seen angioneurotic edema, which is swelling in the face, extremities, lips, tongue, larynx and / or pharynx. In these cases, treatment with lisinopril sheet should be discontinued immediately and the patient should be monitored until disappearance of the edema. If swelling affects only the face and lips do not need special treatment. Where there is involvement of the pharynx and / or larynx, which can be fatal due to airway obstruction, recommended the introduction of subcutaneous epinephrine solution of 1/1000 (0,3 ml - 0,5 ml). Contraindicated reappointment of drugs from the group of ACE inhibitors in patients with a history of edema Quincke.
Risk of severe anaphylactic reactions in patients with desensitization (specific immunotherapy) against insect venom and LDL-apheresis with dekstransulfat.
In patients on hemodialysis with high-flux membranes (polyacrylonitrile) and concomitant therapy with lisinopril can be observed anaphylactic reaction (swelling of the tongue and lips, dyspnea, hypotension).
During treatment with lisinopril require periodic monitoring of liver function tests. When deviations in them lisinopril treatment should be stopped.
During treatment with lisinopril to monitoring levels of potassium ions. By increasing their levels Herceptin treatment should be stopped.
During treatment with lisinopril should be monitored serum electrolytes, blood count, serum creatinine and urea, especially at the beginning of treatment and at risk patients (with renal disease, collagen, etc..) And concomitant immunosuppressants, cytostatics, allopurinol, procainamide.
"In the event of cough during treatment with lisinopril should be a differential diagnosis in terms of its origin. Persistent nonproductive cough may be associated with the use of lisinopril.
When co-administration of lisinopril with diuretics or other antihypertensive agents may occur enhancing the hypotensive effect;
Concomitant administration of lisinopril and products containing potassium or potassium-sparing diuretics may lead to increased plasma potassium;
therapeutic and adverse effects of lisinopril can be increased by neuroleptics, tricyclic antidepressants or lithium salts when administered concomitantly.
Indomethacin and other NSAIDs may diminish the therapeutic effect of lisinopril when co-administered.
Co-administration of lisinopril allopurinol, cytostatic, immunosuppressive agents, systemic corticosteroids, procainamide an increased risk of leucopenia.
Co-administration of lisinopril with oral antidiabetic agents (sulfonylureas, biguanides) and insulin potentiate hypoglycaemic effect.
Pregnancy and lactation
Like all other ACE inhibitors, lisinopril when administered in II and III trimester of pregnancy can cause fetal harm. Lesions consist of hypotension, neonatal skull hypoplasia, anuria, reversible or irreversible renal failure and death. For these reasons, its use is contraindicated in pregnancy.
Due to lack of sufficient clinical data on the excretion of lisinopril in human milk and its safety for infants is not recommended its use during lactation.
EFFECTS ON ABILITY TO DRIVE AND USE MACHINES
Lisinopril can adversely affect psychosomatic status as occasionally cause dizziness and vertigo in individual patients. Caution should be monitored for these symptoms when treated with lisinopril and their appearance does not engage in activities requiring alertness.
Tolerability of lisinopril in general is good.
The most commonly reported adverse reactions (broken down by system organ class) are:
Body as a Whole / 1810 /
Asthenia, fatigue. Cardiovascular / 1010 /
Hypotensive reactions, orthostatic hypotension, palpitations, tachycardia, cardiac arrhythmias, angina pectoris, myocardial infarction, cerebrovascular accidents.
Gastrointestinal / 0600 /
More often they occur anorexia, dry mouth, altered taste, abdominal pain, nausea, vomiting, diarrhea, dyspepsia, hepatic dysfunction, hepatitis, pancreatitis, ileus, constipation. Treatment with ACE inhibitors has been associated with rare syndrome that begins with cholestatic jaundice that may progress to hepatic necrosis with fatal outcome. The mechanism of this syndrome is unknown. If jaundice or changes in liver function tests, treatment with lisinopril should be discontinued.
Musculoskeletal / 0200 /
Registered Isolated cases of muscle cramps.
In the central nervous system and psyche / 0410, 0500 /
More common were headache and dizziness. In rare cases, possible sleep disorders, depression, paresthesia, decreased libido, vertigo. By respiratory / 1100 /
More common are cough, upper respiratory tract in rare cases - nasal congestion, symptoms similar to "cold", bronchospasm, dyspnea, pharyngeal pain, angioneurotic edema covering upper respiratory tract.
Leather / 0100 /
Possible allergic reactions such as urticaria, pruritus, angioneurotic edema covering the face and lips. In isolated cases, serious skin reactions such as pemphigus, exfoliative dermatitis, erythema multiforme syndrome, Stevens-Johnson syndrome and toxic epidermal necrolysis. Skin changes may be accompanied by fever, myalgia, arthralgia, vasculitis, eosinophilia, leukocytosis or elevated titer of ANA. In suspected serious skin reactions required consultation and discontinuation of lisinopril. There have been isolated cases of psoriasis, skin changes, photosensitivity, diaphoresis, alopecia, oniholizis, exacerbation of Raynaud's disease.
Urogenital / 1300.1410 /
Can be seen isolated cases of impotence, oliguria / anuria, acute renal insufficiency.
Changes in laboratory values
Decreased hemoglobin, hematocrit, leukocytes and platelets isolated cases of agranulocytosis or pancytopenia, hemolytic anemia, hyponatremia, hyperkalemia, increased serum creatinine and urea, proteinuria, increased bilirubin, increase in liver transaminases.
No evidence of accidental overdose lisinopril.
In a single dose, repeated exceeding therapeutic, may be seen marked hypotension and asthenia. They can be corrected by infusion of normal saline. Lisinopril can be removed by hemodialysis.
ATC - code S09AA03
Drugs acting on the renin-angiotensin system, ACE - inhibitors alone
Lisinopril is a synthetic peptide derivative that treats nonsulfhydryl ACE inhibitor for oral administration. He is a long-acting angiotensin-converting enzyme. (ACE), which makes it effective when administered once daily. It appears to inhibit ACE (peptidyl dipeptidase) for 36 hours demonstrated in humans and experimental animals. ACE inhibition causes a reduction of the production of angiotensin II, resulting in decreased peripheral vascular resistance and secretion of aldosterone. Like other ACE inhibitors, lisinopril causes lowering of sodium ions and increased potassium. Potassium level can be increased to 0,1 mEq / L in most cases, individual patients (up 4%), this increase can be up to 0,5 mEq / L.
Antihypertensive effect of lisinopril can be determined by its ability to affect adrenergic receptors indirectly. Like other ACE inhibitors, it can reduce the membrane permeability of sodium level kidney tubules. Also, perhaps it affects bradykinin and other kinins as it has structural similarity to kininase, an enzyme involved in the breakdown of bradykinin. Thus bradykinin accumulates, which has expressed vasodilatory and decreasing adhesion and platelet aggregation activity.
Reducing the levels of angiotensin II lisinopril in heart failure leads to the elimination of compensatory venous and arterial vasospasm, resulting in improved hemodynamics.
Positive hemodynamic changes in heart failure are as follows: a decrease in peripheral vascular resistance, decrease in blood pressure and filling pressures of the left and right ventricle, reducing lung congestion, reducing telediastolniya telesistolniya volume and left ventricular fraction increases left ventricular ejection, improved tissue perfusion, increased stroke volume and cardiac output.
Neurohormonal and metabolic changes under the influence of lisinopril include decreased levels of norepinephrine, vasopressin, aldosterone, and increased levels of potassium.
Increasing the amount of bradykinin in turn, leads to the release of large amounts of nitric oxide (N0) associated with endothelial vasodilator.
Following oral administration of lisinopril is absorbed relatively slowly and incompletely. Approximately 25% to 30% of the single dose is absorbed, but there are significant individual differences between patients. Thus, in patients with heart failure absorption is lower and can be only 15% of the dose. The drug is absorbed into its active form, so there is no need to make it active in the liver. Food does not significantly affect the volume of his rezorbtsiya.Pri patients with heart failure class II - IV, NYHA absolute bioavailability of the drug is 16%.
After administration of a single oral dose maximum plasma concentration (Cmax) was observed between b - 7 hours. Some shifting of time of onset of the peak maximum plasma concentration was observed in patients with acute myocardial infarction. No evidence of binding of lisinopril plasma proteins, except angiotensin-converting enzim.V small quantities cross the blood brain barrier, which will znachenie.Samo in experimental clinical studies found that lisinopril crosses the placental barrier and is excreted in breast milk.
In multiple-dose half-life time (half-life) of lisinopril is approximately 12 to 13 hours.
Lisinopril is not metabolized and is excreted unchanged.
Excretion is primarily by the kidneys unchanged, only with significantly impaired renal function (in the volume of glomerular filtration rate of less than 30ml/min) establishes clinically significant changes in its excretion.