Diroton 5mg tablets 28 (Lisinopril)
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Active substance: lisinopril dihydrate 5.44 mg, which corresponds to the content of lisinopril 5 mg.
Excipients : Magnesium stearate, talc, mannitol, corn starch, calcium hydrogen phosphate dihydrate.
Mechanism of action
Lisinopril inhibits the enzyme peptidyl peptidase (angiotensin-converting enzyme (ACE)), which catalyzes the conversion of angiotensin I to a vasoconstrictor peptide, angiotensin II. Angiotensin II also stimulates secretion aldosterone by the adrenal cortex. Inhibition of ACE leads to a decrease in the concentrations of angiotensin II, as a result of which vasopressor activity decreases and aldosterone secretion decreases. A decrease in the latter can lead to an increase in the potassium content in the blood serum.
Clinical efficacy and safety
It is believed that the mechanism by which lisinopril lowers blood pressure (BP) is primarily based on the inhibition of the renin-angiotensin-aldosterone system (RAAS), lisinopril reduces blood pressure even in patients with arterial hypertension with a low concentration of renin. ACE is identical to kininase II, an enzyme that breaks down bradykinin, which is a potent vasodilator peptide. Lisinopril prevents the degradation of bradykinin.
The onset of antihypertensive action - after 1 h. The maximum effect is observed after 6-7 hours and persists for 24 h. The duration of the effect also depends on the magnitude of the dose. With arterial hypertension, the effect is noted in the first days after the start of treatment, a stable effect develops after 1-2 months. With prolonged use, lisinopril reduces the severity of hypertrophy of the myocardium and the walls of the arteries of the resistive type. With a sharp withdrawal of lisinopril, there is no pronounced increase in blood pressure.
Chronic heart failure
The effect of lisinopril on morbidity and mortality in CHF was studied by comparing high and low doses of lisinopril (32.5 mg or 35 mg 1 fold / day and 2.5 mg or 5 mg 1 time / day) with an average follow-up period of 46 months (for surviving patients). A high dose of lisinopril provided a 12% reduction in risk on a combined Endpoint: all-cause mortality and hospitalization for all causes (p=0.002) and an 8% reduction in the risk of all-cause death and hospitalization for cardiovascular disease (p=0.036) compared to low dose. There was a reduced risk of death from all causes (8%; p=0.128) and death from cardiovascular disease (10%; p=0.073). In retrospective analysis, the number of hospitalizations due to CHF decreased by 24% (p = 0.002) in patients receiving high doses of lisinopril compared with patients receiving low doses. The overall adverse event profiles in patients receiving high or low doses of lisinopril were similar in both nature and quantity. Predicted adverse events resulting from ACE inhibition, such as arterial hypotension or impaired renal function, responded well to correction and rarely led to discontinuation of treatment. Cough was less common in patients receiving high doses of lisinopril than in patients who received low doses.
ACE inhibitors prolong life expectancy in patients with CHF, slow the progression of left ventricular dysfunction in patients who have had myocardial infarction without clinical manifestations of heart failure.
Acute myocardial infarction
Lisinopril improves the blood supply to the ischemic myocardium. Evaluation of the efficacy and safety of lisinopril (up to 10 mg / day) was carried out in patients with acute myocardial infarction (AMI). Lisinopril, administered in the first 24 hours after AMI, within 6 weeks led to a statistically significant reduction in overall mortality by 11% (2p = 0.03).
In addition to reducing blood pressure, lisinopril reduces albuminuria. In a double-blind, randomized, multicenter trial in which lisinopril was compared with a slow calcium channel blocker in patients with arterial hypertension and type 2 diabetes mellitus with the initial stage of nephropathy manifesting as microalbuminuria, taking 10-20 mg of lisinopril 1 time / day for 12 months reduced systolic / diastolic blood pressure by 13/10 mm Hg, and albumin excretion in the urine by 40%.
In patients with hyperglycemia, lisinopril helps to normalize the function of the damaged glomerular endothelium.
Lisinopril does not affect the concentration of glucose in the blood in patients with diabetes mellitus and does not lead to an increase in cases of hypoglycemia.
Indications for use
- essential and renovascular arterial hypertension (in the form of monotherapy or in combination with other antihypertensive drugs);
- chronic heart failure (as part of combination therapy);
- early treatment of acute myocardial infarction (in patients with stable hemodynamic indicators in the first 24 hours for the prevention of left ventricular dysfunction and heart failure);
- diabetic nephropathy (in order to reduce albuminuria in patients with type 1 diabetes mellitus with normal blood pressure and in patients with type 2 diabetes mellitus with arterial hypertension).
- hypersensitivity to lisinopril and other components of the drug;
- angioedema in the anamnesis (including associated with the use of ACE inhibitors);
- idiopathic angioedema;
- hereditary edema of Quincke;
- the period of breastfeeding;
- age up to 18 years (efficacy and safety have not been established);
- Simultaneous use with aliskiren and preparations containing aliskiren in patients with diabetes mellitus and / or moderate or severe renal impairment (GFR less than 60 ml / min / 1.73 m 2 surface area of the body);
- simultaneous use with angiotensin II receptor antagonists (ARA II) in patients with diabetic nephropathy;
- simultaneous use with inhibitors of neutral endopeptidase (for example, with drugs containing sacubitril) due to the high risk of developing angioedema.
With caution: aortic stenosis, hypertrophic obstructive cardiomyopathy, mitral stenosis, bilateral renal artery stenosis, single kidney artery stenosis, condition after kidney transplantation, renal failure (QC less than 30 ml / min), primary hyperaldosteronism, arterial hypotension, bone marrow depression hematopoiesis, immunosuppressive therapy, simultaneous use of allopurinol or procainamide, or a combination of these complicating factors (risk of developing neutropenia and agranulocytosis), hyponatremia (increased risk of arterial hypotension in patients on a low-salt or salt-free diet), hypovolemic conditions (including diarrhea, vomiting), systemic connective tissue diseases (including systemic lupus erythematosus, scleroderma), diabetes mellitus, gout, hyperuricemia, hyperkalemia, coronary heart disease, cerebrovascular diseases (including cerebral circulation failure), chronic heart failure, hemodialysis using high-flow dialysis membranes with high permeability (AN69) ® ), advanced age (over 65 years), simultaneous use with potassium-sparing diuretics, potassium preparations, potassium-containing substitutes for edible salt, simultaneous use with lithium preparations, burdened allergic history, simultaneous desensitization with an allergen from hymenoptera venom, simultaneous administration of low-density lipoprotein apheresis (LDL-apheresis) using dextran sulfate, use during major surgical interventions or during general anesthesia, use in patients of the Negroid race.
Dosage and Administration
The drug is taken orally 1 time / day, regardless of food intake, preferably at the same time of day.
The recommended initial dose of lisinopril for patients not taking antihypertensive drugs is 10 mg 1 time / day. In the absence of a therapeutic effect, the dose is increased every 2-3 days by 5 mg / day to an average therapeutic dose of 20-40 mg / day. Regular Support the dose is 20 mg 1 time / day. The maximum daily dose of lisinopril is 40 mg 1 time / day (in clinical studies, the maximum dose of lisinopril was 80 mg / day, but increasing the dose over 40 mg / day usually does not lead to a further decrease in blood pressure). The therapeutic effect develops after 2-4 weeks from the start of treatment, which should be taken into account when increasing the dose. With insufficient therapeutic effect, it is possible to combine lisinopril with other antihypertensive drugs.
If the patient has previously received treatment with diuretics, then their reception should be discontinued 2-3 days before the start of the use of lisinopril. If this is not possible, the initial dose of Diroton ® should not exceed 5 mg / day. After taking the first dose, it is necessary to observe a doctor for several hours, because there may be a pronounced decrease in blood pressure.
Renovascular hypertension and others conditions associated with increased RAAS activity
The recommended initial dose is 2.5-5 mg / day, while it is recommended to provide careful medical supervision of the patient, control of blood pressure, kidney function, potassium concentration in the blood serum. The maintenance dose is selected depending on the dynamics of blood pressure, and the patient should be under constant medical supervision.
Since lisinopril is excreted by the kidneys, the initial dose of diroton ® depends on the QC indicators: when QC 30-80 ml/min - 5-10 mg / day, with QC 10-30 ml/min - 2.5-5 mg/day, with QC less than 10 ml / min, incl. in patients on hemodialysis - 2.5 mg/day The maintenance dose depends on the clinical effect and is selected with regular monitoring of renal function indicators, concentration potassium and sodium in the blood serum.
Recommendations regarding doses of patients with mild to moderate hepatic insufficiency not yet developed, so the selection of doses to such patients should be carried out with caution, and should begin with the lowest possible dose.
Chronic heart failure
With CHF, the initial dose of lisinopril is 2.5 mg 1 time / day. The first intake of lisinopril should be started under close medical supervision in order to assess the effect of the drug on blood pressure. In the future, the dose of lisinopril should be gradually increased by 2.5 mg with an interval of 3-5 days to 5-10-20 mg / day. It is not recommended to exceed the maximum daily dose of lisinopril 20 mg (in clinical studies, the maximum dose of lisinopril in patients with CHF was 35 mg 1 time / day).
Before treatment with Diroton ® and further, during treatment, blood pressure, kidney function, potassium and sodium concentrations in the blood serum should be regularly monitored in order to avoid the development of arterial hypotension and associated renal dysfunction.
Early treatment of acute myocardial infarction
Starting therapy (the first 3 days of acute myocardial infarction)
In the first 24 hours after an acute myocardial infarction, 5 mg of lisinopril is prescribed once. After 24 hours (one day), 5 mg of lisinopril is prescribed once, after 48 hours (two days) - 10 mg of lisinopril once.
You can not start treatment with systolic blood pressure less than 100 mm Hg. Patients with low systolic blood pressure (≤120 mm Hg) at the beginning of treatment and during the first 3 days after acute myocardial infarction, a smaller dose of lisinopril is prescribed - 2.5 mg 1 time / day.
The maintenance dose of lisinopril is 10 mg 1 time / day. The course of treatment is at least 6 weeks. In the future, the feasibility of continuing therapy should be assessed. Patients with symptoms of heart failure are advised to continue taking lisinopril.
In the case of arterial hypotension (systolic blood pressure ≤100 mm Hg), the daily dose of lisinopril is temporarily reduced to 5 mg, if necessary - up to 2.5 mg. In the case of a prolonged pronounced decrease in blood pressure (systolic blood pressure below 90 mm Hg. for more than 1 h), the use of lisinopril should be discontinued.
The initial dose of lisinopril is 10 mg / day, which, if necessary, is increased to 20 mg / day until the target values of diastolic blood pressure are reached (diastolic blood pressure below 75 mm Hg in a sitting position in patients with type 1 diabetes mellitus and below 90 mm Hg in a sitting position in patients with type 2 diabetes mellitus).
At impaired renal function (QC less than 80 ml / min) the initial dose is determined depending on the QC (see above).
At elderly patients (over 65 years of age) the drug should be used with caution.
During treatment with lisinopril, the following adverse drug reactions (NLR) have been reported. NLR is presented in system-organ classes in accordance with the MedDRA classification and with the frequency of occurrence: very often - 1/10 of the appointments (≥10%), often - 1/100 of the appointments (≥1%, but <10%), infrequently - 1/1000 of appointments (≥0.1%, but <1%), rarely - 1/10,000 of appointments (≥0.01%, but <0.1%), very rarely less than 1/10,000 of appointments (<0.01%), frequency unknown - cannot be estimated on the basis of available data.
Within each frequency group, adverse reactions are presented in descending order of severity.
On the part of the hematopoietic system: very rarely - inhibition of bone marrow hematopoiesis, agranulocytosis, leukopenia, neutropenia, thrombocytopenia, hemolytic anemia, anemia, lymphadenopathy.
On the part of the immune system: very rarely - autoimmune disorders; frequency unknown - anaphylactic/anaphylactoid reaction.
From the endocrine system: rarely - syndrome of inadequate secretion of antidiuretic hormone.
From the side of metabolism and nutrition: very rarely - hypoglycemia.
Mental disorders: infrequently - mood changes, sleep disturbances, hallucinations; rarely - mental disorders; the frequency is unknown - depression.
From the nervous system: often - dizziness, headache; infrequently - vertigo, paresthesia, dysgeusia; rarely - confusion, drowsiness, muscle cramps, back pain, parosmia (impaired sense of smell); frequency unknown - fainting.
From the cardiovascular system: often - a pronounced decrease in blood pressure, orthostatic hypotension and related symptoms; infrequently - myocardial infarction (due to a pronounced decrease in blood pressure in high-risk groups of patients), tachycardia, heart palpitations, acute cerebral circulation disorder (due to a pronounced decrease in blood pressure in groups of patients at increased risk), Raynaud's syndrome.
From the respiratory system: often - cough; infrequently - chest pain, rhinitis; very rarely - bronchospasm, allergic alveolitis / eosinophilic pneumonia, sinusitis.
From the digestive system: often - diarrhea, vomiting; infrequently - abdominal pain, nausea, digestive disorders; rarely - dry mouth; very rarely - pancreatitis, anorexia, angioedema of the intestine.
From the liver and biliary tract: very rarely - liver failure, hepatic cell hepatitis or cholestatic, jaundice.
From the skin and subcutaneous tissues: infrequently - skin rash, skin itching; rarely - psoriasis, urticaria, alopecia, increased sensitivity / angioedema of the face, hands and feet, lips, tongue, glottis and / or larynx; very rarely - toxic epidermal necrolysis, Stevens-Johnson syndrome, erythema multiforme, pemphigus vulgaris, hyperhidrosis, pseudolymphoma of the skin *.
From the musculoskeletal system: rarely - pain in the limbs.
From the urinary system: often - impaired renal function; rarely - acute renal failure, uremia; very rarely - oliguria / anuria.
From the genitals and mammary gland: infrequently - impotence; rarely - gynecomastia, sexual dysfunction.
General disorders and disorders at the injection site: infrequently - increased fatigue, asthenia.
Laboratory and instrumental data: infrequently - an increase in the concentration of urea and creatinine in the blood serum, hyperkalemia, increased activity of liver enzymes; rarely - a decrease in hemoglobin and hematocrit, hyperbilirubinemia, hyponatremia.
* A symptom complex has been reported, which may include one or more of the following symptoms: fever, vasculitis, myalgia, arthralgia/arthritis, a positive reaction to antinuclear antibodies (AHA), an increase in the erythrocyte sedimentation rate (ESR), eosinophilia and leukocytosis, skin rash, photosensitization, or other changes in the skin.
The drug should be stored out of the reach of children at a temperature not exceeding 30 ° C.
Shelf life - 3 years. Do not use after the expiry date which is stated on the carton.
- Gedeon Richter Ltd
- Dosage form
- 5 mg
- Number of tablets
- INN Russian
- Russian title