Diroton - instructions for use, reviews, analogs and formulations (tablets 2.5 mg, 5 mg, 10 mg and 20 mg, KO-Diroton in combination with a diuretic) drug for the treatment of arterial hypertension and pressure reduction in adults, children and of pregnancy

In this article, you can read the instructions for using the drug Diroton. Comments of visitors of the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Diroton in their practice are presented. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Diroton in the presence of existing structural analogues.Use to treat hypertension and reduce blood pressure in adults, children, as well as during pregnancy and lactation.

Diroton - an ACE inhibitor, reduces the formation of angiotensin 2 from angiotensin 1. Reducing angiotensin 2 leads to a direct decrease in the release of aldosterone. Reduces the degradation of bradykinin and increases the synthesis of prostaglandins. Reduces OPSS, AD, preload, pressure in the pulmonary capillaries, causes an increase in the minute volume of blood and increased tolerance of the myocardium to loads in patients with chronic heart failure. Expands arteries more than veins. Some effects are explained by the effect on tissue renin-angiotensin systems. With prolonged use, myocardial hypertrophy and the walls of arteries of resistive type decrease. Improves the blood supply of the ischemic myocardium.

ACE inhibitors prolong life expectancy in patients with chronic heart failure, slow the progression of left ventricular dysfunction in patients who underwent myocardial infarction without clinical manifestations of heart failure.

The beginning of the drug - after 1 hour, reaches a maximum after 6-7 hours and persists for 24 hours. The duration of the effect also depends on the amount of the dose taken. With arterial hypertension, the effect is observed in the first days after the start of treatment, stable action develops after 1-2 months. With a sharp withdrawal of the drug, no pronounced increase in blood pressure was observed.

Diroton reduces albuminuria. In patients with hyperglycemia contributes to the normalization of the function of the damaged glomerular endothelium. 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.

Hydrochlorothiazide

A thiazide diuretic whose diuretic effect is associated with a disruption of the reabsorption of sodium, chlorine, potassium, magnesium, water in the distal nephron; delays the excretion of calcium ions, uric acid. Has antihypertensive properties; the hypotensive effect develops due to the expansion of arterioles. Virtually no effect on normal blood pressure.

The diuretic effect develops after 1-2 hours, reaches a maximum after 4 hours and persists for 6-12 hours.Antihypertensive effect occurs in 3-4 days, but it may take 3-4 weeks to achieve the optimal therapeutic effect.

Lizinopril and hydrochlorothiazide, if used simultaneously, have an additive antihypertensive effect.

Composition

Lysinopril dihydrate + excipients.

Lizinopril dihydrate + Hydrochlorothiazide + excipients (KO-Diroton).

Pharmacokinetics

Lizinopril weakly binds to blood plasma proteins. Permeability through the blood-brain barrier (BBB) ​​and the placental barrier is low. Lizinopril is not metabolized. Excreted by the kidneys unchanged.

Indications

• 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);
• acute myocardial infarction (within the first 24 hours with stable hemodynamic parameters to maintain these parameters and prevention of left ventricular dysfunction and heart failure);
• Diabetic nephropathy (to reduce albuminuria in patients with insulin-dependent diabetes mellitus whennormal blood pressure and in patients with non-insulin-dependent diabetes mellitus with arterial hypertension).

Forms of release

Tablets of 2.5 mg, 5 mg, 10 mg and 20 mg.

Tablets 10 mg and 20 mg (KO-Diroton).

Instructions for use and dosage

The drug is taken orally once a day, for all indications, regardless of food intake, preferably at the same time of day.

With essential hypertension, patients who do not receive other antihypertensive drugs are prescribed 10 mg once a day. The usual daily maintenance dose is 20 mg. The maximum daily dose is 40 mg.

The full effect usually develops in 2-4 weeks from the start of treatment, which should be taken into account when increasing the dose. With insufficient clinical effect, it is possible to combine the drug with other antihypertensive drugs.

If the patient received prior treatment with diuretics, then their reception should be discontinued 2-3 days before the application of Diroton. If it is impossible to cancel diuretics, then the initial dose of Diroton should not exceed 5 mg per day. In this case, after taking the first dose, medical supervision is recommended for several hours (maximum effect is achieved after about 6 hours), because can develop a marked decrease in blood pressure.

In case of renovascular hypertension or other conditions with increased activity of RAAS, it is also advisable to prescribe a lower initial dose of 2.5-5 mg per day under enhanced medical control (control of blood pressure, kidney function, potassium concentration in blood serum). The maintenance dose should be determined depending on the dynamics of blood pressure.

In chronic heart failure, the initial dose is 2.5 mg once a day, which can be gradually increased 3-5 days before the usual, maintaining a daily dose of 5-20 mg. The dose should not exceed the maximum daily dose of 20 mg. When used simultaneously with diuretics, the dose of a diuretic should be reduced, if possible. Before starting treatment with Diroton and later, during treatment should regularly monitor blood pressure, kidney function, the content of potassium and sodium in the blood in order to avoid the development of arterial hypotension and related impaired renal function.

In acute myocardial infarction (as part of a combination therapy), 5 mg are prescribed on the first day, 5 mg again on the second day, 10 mg on the third day, and a 10 mg maintenance dose, 10 times a day.In patients with acute myocardial infarction, the drug should be used for at least 6 weeks. With low systolic blood pressure (less than 120 mm Hg), treatment starts with a low dose (2.5 mg per day). In the case of development of arterial hypotension, when systolic blood pressure is less than 100 mm Hg. The maintenance dose is reduced to 5 mg per day, if necessary, it is possible to temporarily administer 2.5 mg per day. In the case of a long pronounced decrease in blood pressure (systolic blood pressure below 90 mm Hg for more than 1 hour), discontinue treatment with the drug.

With diabetic nephropathy in patients with insulin-dependent diabetes mellitus, Diroton is used at a dose of 10 mg once a day. If necessary, the dose can be increased to 20 mg once a day in order to achieve diastolic blood pressure values ​​below 75 mm Hg. Art. in the sitting position. Patients with non-insulin-dependent diabetes mellitus are prescribed the drug in the same dose, in order to achieve diastolic blood pressure values ​​below 90 mm Hg. in the sitting position.

Side effect

• marked decrease in blood pressure;
• chest pain;
• orthostatic hypotension;
• tachycardia;
• bradycardia;
• the onset of symptoms of heart failure;
• violation of AV-conduction;
• myocardial infarction;
• nausea, vomiting;
• stomach ache;
• dry mouth;
• diarrhea;
• dyspepsia;
• anorexia;
• a taste disorder;
• hives;
• increased sweating;
• photosensitization;
• itching;
• hair loss;
• mood lability;
• violation of concentration of attention;
• paresthesia;
• increased fatigue;
• drowsiness;
• convulsive twitching of the muscles of the limbs and lips;
• asthenic syndrome;
• confusion of consciousness;
• dry cough;
• bronchospasm;
• leukopenia, thrombocytopenia, neutropenia, agranulocytosis, anemia (decrease in hemoglobin, hematocrit, erythrocytopenia), agranulocytosis;
• angioedema, swelling of the face, limbs, lips, tongue, epiglottis and / or larynx;
• vasculitis;
• increased ESR;
• impaired renal function;
• acute renal insufficiency;
• decreased potency;
• arthritis;
• myalgia;
• fever;
• exacerbation of gout.

Contraindications

• idiopathic angioedema in the anamnesis (including with the use of ACE inhibitors);
• hereditary angioedema;
• age under 18 years (effectiveness and safety not established);
• increased sensitivity to lisinopril or other ACE inhibitors.

Application in pregnancy and lactation

The use of Diroton in pregnancy is contraindicated. Lizinopril penetrates the placental barrier. When establishing a pregnancy, the drug should be stopped as soon as possible. Admission of ACE inhibitors in the 2nd and 3rd trimester of pregnancy has an adverse effect on the fetus (there may be a marked decrease in blood pressure, renal failure, hyperkalemia, skull hypoplasia, fetal death). Data on the negative effects of the drug on the fetus in the case of application in the first trimester is not available. For newborns and infants who have undergone intrauterine exposure to ACE inhibitors, it is recommended that careful monitoring be established to detect a marked decrease in blood pressure, oliguria, and hyperkalemia in a timely manner.

There is no data on the penetration of lisinopril into breast milk. If it is necessary to prescribe the drug during lactation, breastfeeding should be discontinued.

special instructions

Most often, a marked decrease in blood pressure occurs with a decrease in fluid volume caused by diuretic therapy, a decrease in salt content in food, dialysis, diarrhea, or vomiting. In chronic heart failure with simultaneous renal failure or without it, a marked decrease in blood pressure is possible.The most pronounced decrease in blood pressure is detected in patients with a severe stage of chronic heart failure, as a result of the use of diuretics in high doses, hyponatremia or impaired renal function. In such patients, treatment with Diroton should be started under the strict supervision of a doctor (with care to select a dose of the drug and diuretics).

Similar rules should be adhered to when appointing Diroton to patients with IHD, cerebrovascular insufficiency, in which a sharp decrease in blood pressure can lead to myocardial infarction or stroke.

Transient hypotensive reaction is not a contraindication for taking the next dose of the drug.

Prior to treatment, Diroton should, if possible, normalize the sodium concentration and / or make up for lost volume of fluid, carefully monitor the effect of the initial dose of Diroton on the patient's blood pressure.

Treatment of symptomatic arterial hypotension consists of providing bed rest and, if necessary, with / in the administration of fluid (infusion of physiological solution). Transient arterial hypotension is not a contraindication for treatment with the drug Diroton, however, it may be necessary to temporarily cancel it, or reduce the dose.

Treatment with Diroton is contraindicated in case of cardiogenic shock and with acute myocardial infarction, if the appointment of a vasodilator can significantly worsen hemodynamic parameters, for example, when systolic blood pressure does not exceed 100 mm Hg. Art.

In patients with acute myocardial infarction, a decrease in renal function (creatinine concentration in the blood plasma greater than 177 μmol / L and / or proteinuria more than 500 mg / 24 h) is a contraindication for the use of the drug Diroton. In case of development of renal failure during treatment with lisinopril (the creatinine concentration in the blood plasma is more than 265 μmol / l or twice as high as the baseline level), the doctor should decide whether to stop treatment.

With bilateral renal artery stenosis and renal artery stenosis of a single kidney, as well as with hyponatremia and / or a decrease in bcc or circulatory failure, arterial hypotension caused by taking the drug Diroton may lead to a decrease in kidney function followed by the development of reversible (after discontinuation of the drug) acute renal failure . A small temporary increase in the concentration of urea in the blood and creatinine can be observed in cases of impaired renal function, especially against a background of simultaneous treatment with diuretics.Caution and monitoring of renal function are required in cases of significant decrease in kidney function (QC less than 30 ml / min).

Angioedema of the face, extremities, lips, tongue, epiglottis and / or larynx was rarely seen in patients treated with ACE inhibitors, including Diroton, which may occur during any treatment period. In this case, treatment with Diroton should be stopped as soon as possible and for the patient to establish an observation until the symptoms regress completely. In cases where there was only edema of the face and lips, the condition usually passes without treatment, however, it is possible to prescribe antihistamines. Angioedema with edema of the larynx can be fatal. When the tongue, epiglottis or larynx are covered, airway obstruction can occur, therefore, appropriate therapy should be performed immediately (0.3-0.5 ml epinephrine (adrenaline) solution 1: 1000 subcutaneously, administration of glucocorticosteroids, antihistamines) and / or measures to ensure airway patency. Patients who have had a history of angioedema, not associated with previous treatment with ACE inhibitors, may have an increased risk of developing it during treatment with an ACE inhibitor.

Anaphylactic reaction was noted in patients on hemodialysis using high-flow dialysis membranes (AN69), which simultaneously take Diroton. In such cases, one should consider the possibility of using another type of membrane for dialysis or another antihypertensive agent.

In some cases of desensitization against arthropod allergens, treatment with ACE inhibitors was accompanied by hypersensitivity reactions. This can be avoided by interrupting the administration of ACE inhibitors.

In patients with extensive surgical intervention or during general anesthesia, ACE inhibitors (in particular, lisinopril) can block the formation of angiotensin 2. The decrease in blood pressure associated with this mechanism of action is corrected by an increase in BCC. Before surgery (including dentistry), an anesthesiologist must be warned about the use of Diroton.

The use of recommended doses of the drug in elderly patients can be accompanied by an increase in the concentration of lisinopril in the blood, so the selection of a dose requires special attention and is carried out depending on the function of the kidneys and blood pressure of the patient.However, in elderly and young patients, the antihypertensive effect of Diroton is equally pronounced.

With the use of ACE inhibitors, there was a cough (dry, prolonged, which disappears after discontinuation of ACE inhibitor treatment). With a differential diagnosis of cough, one must also consider the cough caused by the use of ACE inhibitors.

In some cases, hyperkalemia was noted. Risk factors for the development of hyperkalemia include renal failure, diabetes mellitus, the use of potassium drugs or drugs that cause an increase in potassium in the blood (eg, heparin), especially in patients with impaired renal function.

During the treatment with the drug, regular monitoring of the potassium ions, glucose, urea, lipids in the blood plasma is necessary.

During the period of treatment it is not recommended to drink alcoholic beverages. alcohol increases the hypotensive effect of the drug.

Care should be taken when performing physical exercises, in hot weather (the risk of dehydration and excessive blood pressure lowering due to a decrease in BCC).

Because the potential risk of agranulocytosis can not be ruled out, periodic monitoring of the blood picture is required.

Impact on the ability to drive vehicles and manage mechanisms

When there are side effects from the central nervous system, it is not recommended to drive vehicles, as well as perform work associated with increased risk.

Drug Interactions

With simultaneous use 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. Therefore, joint appointment is possible only on the basis of an individual decision of the doctor with regular monitoring of potassium content in the blood serum and kidney function.

With simultaneous use with beta-blockers, slow calcium channel blockers, diuretics and other antihypertensive drugs, there is an increase in the hypotensive effect of the drug.

With the simultaneous use of ACE inhibitors and preparations of gold (sodium aurotyomalate) intravenously, a symptom complex including facial flushing, nausea, vomiting and arterial hypotension is described.

With simultaneous use with vasodilators, barbiturates, phenothiazines, tricyclic antidepressants, ethanol (alcohol), the hypotensive effect of the drug is enhanced.

When used simultaneously with non-steroidal anti-inflammatory drugs (including selective inhibitors of COX-2), estrogens, as well as adrenomimetics, the antihypertensive effect of lisinopril decreases.

With simultaneous use with lithium preparations, lithium removal from the body slows down (increased cardiotoxic and neurotoxic action of lithium).

With simultaneous use with antacids and colestyramin, absorption in the digestive tract decreases.

The drug enhances the neurotoxicity of salicylates, weakens the effect of hypoglycemic agents for oral administration, norepinephrine, epinephrine and antidotal drugs, increases the effects (including side effects) of cardiac glycosides, the action of peripheral muscle relaxants, reduces the excretion of quinidine.

Reduces the effect of oral contraceptives.

With the simultaneous administration of methyldopa, the risk of hemolysis increases.

Analogues of the drug Diroton

Structural analogs for the active substance:

• Dapril;
• Diropress;
• Irumed;
• Lysacard;
• Lizigamma;
• Lysinopril;
• Lysinopril dihydrate;
• Lysinoton;
• Lisonorm;
• Lysoril;
• Listril;
• Liten;
• Assigned;
• Rileys-Sanovel;
• Sinopril.

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