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Active ingredients
Lisinopril
Release form
Pills
Composition
Lisinopril (in the form of dihydrate) 20 mg; excipients: mannitol, calcium phosphate dihydrate, corn starch, pregelatinized corn starch, iron dye yellow oxide (e172), iron dye red oxide (e172), colloidal silicon dioxide, magnesium stearate.
Pharmacological effect
ACE inhibitor. Antihypertensive drug. The mechanism of action is associated with the inhibition of ACE activity, which leads to the suppression of the formation of angiotensin II from angiotensin I and to a direct decrease in the release of aldosterone. Reduces the degradation of bradykinin and increases prostaglandin synthesis .; Reduces the OPSS, blood pressure, preload, pressure in the pulmonary capillaries, causes an increase in the minute volume of blood and increased tolerance to stress in patients with chronic heart failure. Lisinopril has a vasodilating effect, while expanding the arteries to a greater extent than the veins. Some effects are attributed to effects on tissue renin-angiotensin systems. Improves blood supply to ischemic myocardium. With prolonged use, hypertrophy of the myocardium and the walls of resistive arteries is reduced .; The use of ACE inhibitors in patients with chronic heart failure leads to an increase in life expectancy; in patients after myocardial infarction, without clinical manifestations of heart failure, to slow the progression of left ventricular dysfunction .; The onset of action is noted 1 hour after taking the drug, the maximum effect is noted after 6-7 hours, the duration of action is 24 hours. With hypertension, the effect is noted in the first days after the start of treatment, a stable action develops after 1-2 months .; With a sharp withdrawal of the drug was not observed a pronounced increase in blood pressure. In addition to reducing blood pressure, lisinopril reduces albuminuria. In patients with hyperglycemia, it helps normalize the function of the damaged glomerular endothelium. Lisinopril does not affect the concentration of glucose in the blood plasma in patients with diabetes mellitus and does not lead to an increase in the incidence of hypoglycemia.
Pharmacokinetics
Absorption; After taking the drug inside about 25% of lisinopril is absorbed from the gastrointestinal tract.Eating does not affect the absorption of lisinopril. Absorption averages 30%. Bioavailability - 29%. Cmax in plasma is reached after approximately 6-8 h; Distribution; Poorly bound to plasma proteins. Lisinopril weakly penetrates the BBB through the placental barrier .; Withdrawal; T1 / 2 - 12 h. Lisinopril is not metabolized and is excreted unchanged in the urine.
Indications
- arterial hypertension (as monotherapy or in combination with other antihypertensive drugs); - chronic heart failure (as part of combination therapy for the treatment of patients taking digitalis and / or diuretics); - early treatment of acute myocardial infarction (as part of combination therapy in the first 24 hours in patients with stable hemodynamic parameters, to maintain these indicators and prevent left ventricular dysfunction and heart failure); - diabetic nephropathy (to reduce albuminuria in insulin-dependent patients with normal blood pressure and insulin-independent patients with arterial hypertension).
Contraindications
- angioedema in history (including with the use of ACE inhibitors); - hereditary angioedema or idiopathic edema; - pregnancy; - lactation period (breastfeeding); - age up to 18 years (efficacy and safety have not been established); - hypersensitivity to lisinopril and other ACE inhibitors; The drug should be prescribed with caution in aortic stenosis, cerebrovascular diseases (including cerebral circulatory insufficiency), coronary artery disease, coronary insufficiency, severe autoimmune systemic connective tissue diseases (including SLE, scleroderma), in case of bone marrow inhibition, sugar diabetes, hyperkalemia, bilateral renal artery stenosis, single kidney artery stenosis, with a condition after kidney transplantation, renal failure, azotemia, primary hyperaldosteronism , arterial hypotension, bone marrow hypoplasia, hypertrophic obstructive cardiomyopathy, arterial hypotension, on the background of a salt-restricted diet, conditions accompanied by a decrease in BCC (including diarrhea, vomiting), elderly patients.
Use during pregnancy and lactation
The use of Irumed during pregnancy and lactation (breastfeeding) is contraindicated .; Lisinopril penetrates the placental barrier. If pregnancy occurs, Irumed treatment should be stopped immediately. Acceptance of ACE inhibitors in the II and III trimesters of pregnancy can cause death of the fetus and newborn. Newborns may develop hypoplasia of the skull, oligohydramnios, deformation of the bones of the skull and face, hypoplasia of the lungs, impaired development of the kidneys. For newborns and infants whose mothers were taking ACE inhibitors during pregnancy, it is recommended that careful monitoring be carried out in order to timely detect a pronounced decrease in blood pressure, oliguria, hyperkalemia .; No data on the penetration of lisinopril into breast milk. During the period of treatment with Irumed it is necessary to cancel breastfeeding.
Dosage and administration
The drug is prescribed inside. Eating does not affect absorption, so the drug can be taken before, during or after a meal. Frequency of administration is 1 time per day (approximately at the same time) .; In the treatment of essential hypertension, it is recommended to prescribe an initial dose of 10 mg. Maintenance dose is 20 mg / day. The maximum daily dose is 40 mg. For the full development of the effect, a 2-4 week course of drug treatment may be required (this should be taken into account when increasing the dose). If the use of the drug in the maximum dose does not cause a sufficient therapeutic effect, then the additional prescription of another antihypertensive agent is possible .; Patients taking diuretics should be discontinued with diuretics 2-3 days before starting Irumed. For patients in whom it is impossible to discontinue diuretic therapy, Irumed is prescribed in an initial dose of 5 mg / day. In case of renovascular hypertension or other conditions with increased function of the renin-angiotensin-aldosterone system, Irumed is prescribed in the initial dose of 2.5-5 mg / day under the control of blood pressure, kidney function, and serum potassium concentration. Maintenance dose is set depending on blood pressure .; In patients with renal failure and patients on hemodialysis, the initial dose is determined depending on the CC. Maintenance dose is determined depending on blood pressure (under the control of kidney function, the level of potassium and sodium in the blood) .; In chronic heart failure, lisinopril may be used simultaneously with diuretics and / or cardiac glycosides. If possible, the dose of diuretic should be reduced before starting lisinopril.The initial dose is 2.5 mg 1 time / day, then it is gradually increased (by 2.5 mg in 3-5 days) to 5-10 mg / day. The maximum dose is 20 mg / day; In acute myocardial infarction (as part of combination therapy, in the first 24 hours, patients with stable hemodynamic parameters) in the first 24 hours, 5 mg are prescribed, then 5 mg every other day, 10 mg - after two days, and then 10 mg 1 time / day. In patients with acute myocardial infarction, the drug is used for 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), the drug is prescribed at a dose of 2.5 mg. In case of arterial hypotension (systolic blood pressure less than or equal to 100 mm Hg), the daily dose of 5 mg can be temporarily reduced to 2.5 mg. In the case of longer arterial hypotension (systolic blood pressure below 90 mm Hg for more than 1 hour), Irumed should be stopped; In diabetic nephropathy in patients with diabetes mellitus type 1 (insulin-dependent) Irumed prescribed in a dose of 10 mg 1 time / day. If necessary, the dose can be increased to 20 mg / day in order to achieve diastolic blood pressure values below 75 mm Hg. in a sitting position. In patients with type 2 diabetes mellitus (insulin-independent), the dose is the same in order to achieve diastolic blood pressure values below 90 mm Hg. in a sitting position.
Side effects
Most often: dizziness, headache, fatigue, diarrhea, dry cough, nausea .; Since the cardiovascular system: marked reduction in blood pressure, chest pain; rarely - orthostatic hypotension, tachycardia, bradycardia, worsening symptoms of heart failure, impaired AV conduction, myocardial infarction .; On the part of the central nervous system and peripheral nervous system: mood lability, confusion, paresthesias, drowsiness, jerky muscles of the limbs and lips; rarely, asthenic syndrome .; On the part of the digestive system: dry mouth, anorexia, dyspepsia, change in taste, abdominal pain, pancreatitis, hepatocellular or cholestatic, jaundice, hepatitis, increased activity of hepatic transaminases, hyperbilirubinemia .; On the part of the respiratory system: dyspnea, bronchospasm .; Dermatological reactions: increased sweating, pruritus, alopecia, photosensitization .; From the side of blood-forming organs: leukopenia, thrombocytopenia, neutropenia, agranulocytosis, anemia (decrease in hematocrit, hemoglobin, erythrocytopenia) .; Metabolism: hyperkalemia, hyponatremia, hyperuricemia,increased creatinine levels in the blood .; On the part of the urinary system: renal dysfunction, oliguria, anuria, uremia, proteinemia .; Allergic reactions: urticaria, angioedema of the face, extremities, lips, tongue, epiglottis and / or larynx, skin rash, pruritus, fever, positive antinuclear antibody test results, increased ESR, eosinophilia, leukocytosis; in some cases, interstitial angioedema .; Other: arthralgia / arthritis, myalgia, vasculitis, decreased potency.
Overdose
Symptoms: marked reduction in blood pressure, dry mouth, drowsiness, urinary retention, constipation, anxiety, irritability .; Treatment: conducting symptomatic therapy, in / in the introduction of saline and, if necessary, the use of vasopressor agents under the control of blood pressure and water-electrolyte balance. Perhaps the use of hemodialysis.
Interaction with other drugs
With simultaneous use of Irumed with potassium-sparing diuretics (spironolactone, triamterene, amiloride), potassium preparations, salt substitutes containing potassium, the risk of hyperkalemia increases, especially in patients with impaired renal function .; With simultaneous use of Irumed with diuretics there is a pronounced decrease in blood pressure .; With simultaneous use of Irumed with other antihypertensive drugs, an additive effect is noted .; With the simultaneous use of Irumed with NSAIDs, estrogens, adrenostimulants, the antihypertensive effect of lisinopril is reduced. The simultaneous use of Irumed with lithium slows down the elimination of lithium from the body .; With simultaneous use of Irumed with antacids and colestyramine, absorption of lisinopril from the gastrointestinal tract is reduced .; Ethanol enhances the effect of the drug.
special instructions
It should be borne in mind that a pronounced decrease in blood pressure occurs with a decrease in the volume of fluid caused by diuretic therapy, with a decrease in salt in food, during dialysis and in patients with diarrhea or vomiting. In patients with chronic heart failure with simultaneous renal failure or without it, the development of symptomatic arterial hypotension, which was more often detected in patients with severe heart failure, as a result of the use of large doses of diuretic, hyponatremia or impaired renal function, is possible. In such patients, treatment should begin under the strict supervision of a physician (carefully select the dose of the drug and diuretics).Similar tactics should be followed when prescribing Irumed to patients with coronary artery disease, cerebrovascular insufficiency, in which a sharp decrease in blood pressure can lead to a myocardial infarction or stroke .; In the case of the development of a pronounced decrease in blood pressure, the patient should be given a horizontal position and, if necessary, in / in to enter a 0.9% solution of sodium chloride. Transient hypotensive reaction is not a contraindication for taking the next dose of the drug .; When using Irumed in some patients with chronic heart failure, but with normal or lowered blood pressure, there may be a decrease in blood pressure, which is usually not a reason to stop treatment. If arterial hypotension becomes symptomatic, it is necessary to decrease the dose of the drug or to stop treatment with Irumed .; In acute myocardial infarction, the use of standard therapy (thrombolytics, acetylsalicylic acid, beta-blockers) is indicated. Irumed can be used in conjunction with iv administration or with the use of nitroglycerin transdermal systems .; Irumed should not be prescribed to patients with acute myocardial infarction who have a risk of further marked deterioration of hemodynamic parameters after the use of vasodilators: patients with systolic blood pressure of 100 mm Hg. or lower, or with cardiogenic shock .; In patients with chronic heart failure, a pronounced decrease in blood pressure after the start of treatment with ACE inhibitors can lead to a further deterioration in renal function. Cases of the development of acute renal failure. In patients with bilateral renal artery stenosis or arterial stenosis of a single kidney who received ACE inhibitors, there was an increase in serum urea and creatinine, usually reversible after stopping treatment (it was more common in patients with renal insufficiency) .; Lisinopril is not prescribed for acute myocardial infarction in patients with severe impaired renal function with a serum creatinine content of more than 177 mmol / l or with proteinuria more than 500 mg / day. If renal dysfunction develops on the background of the use of the drug (the content of serum creatinine is more than 265 mmol / l or an increase of 2 times, compared to the rate before treatment), assess the need for continued Irumed therapy. Patients taking ACE inhibitors, including lisinopril, rarely developed angioedema of the face, extremities, lips, tongue, epiglottis, and / or larynx, and its development is possible at any time during treatment.In this case, treatment with Irumed should be stopped as soon as possible and the patient should be monitored until the symptoms are fully regressed. However, in cases where edema occurs only on the face and lips and the condition most often normalizes without treatment, antihistamine medications may be prescribed .; If angioedema spreads to the tongue, epiglottis or larynx, the airway obstruction can be fatal, therefore, appropriate therapy should be carried out immediately (0.3-0.5 ml of 1: 1000 solution of epinephrine s / c) and / or measures to ensure the airway. It was noted that angioedema developed more frequently in patients of the Negroid race who took ACE inhibitors more often than in patients of other races. Patients with a history of already having angioedema, not associated with previous treatment with ACE inhibitors, may have an increased risk of developing it during Irumed treatment .; In patients taking ACE inhibitors, during desensitization to hymenoptera poison (wasps, bees, ants), it is extremely rare that anaphylactoid reaction can develop. This can be avoided if you temporarily discontinue treatment with an ACE inhibitor before each desensitization .; It should be borne in mind that patients taking ACE inhibitors and are on hemodialysis using high-permeable dialysis membranes (for example, AN69) may develop an anaphylactic reaction. In such cases, it is necessary to consider the possibility of using a different type of membrane for dialysis or another antihypertensive drug .; When using ACE inhibitors, cough is noted (dry, long-lasting, which disappears after stopping treatment with an ACE inhibitor). In the differential diagnosis of cough, cough caused by the use of an ACE inhibitor should also be considered .; When using drugs that reduce blood pressure in patients with extensive surgery or during general anesthesia, lisinopril can block the formation of angiotensin II, secondary to compensatory release of renin. A pronounced decrease in blood pressure, which is considered a consequence of this mechanism, can be eliminated by increasing the BCC. Before surgery (including dental surgery), the surgeon / anesthetist should be informed about the use of an ACE inhibitor .; In some cases, hyperkalemia was observed.Risk factors for the development of hyperkalemia include renal failure, diabetes mellitus and the simultaneous use of potassium-sparing diuretics (spironolactone, triamterene or amiloride), potassium preparations, or potassium-containing salt substitutes, especially in patients with impaired renal function. If necessary, the use of these combinations should regularly monitor the level of potassium in the serum .; In patients who are at risk of developing symptomatic hypotension (on a low-salt or salt-free diet) with / without hyponatremia, as well as in patients who received high doses of diuretics, these conditions must be compensated for (loss of fluid and salt). It is necessary to control the effect of the initial dose of Irumed on the value of blood pressure .; Influence on the ability to drive motor vehicles and control mechanisms; There is no data on the effect of Irumed used in therapeutic doses on the ability to drive vehicles and mechanisms, but it must be taken into account that dizziness may occur. Therefore, during the period of treatment, patients should be careful when driving and work that requires high concentration of attention and speed of psychomotor reactions.