Diroton, tablets 20 mg 28 pcs

Diroton is an ACE inhibitor and reduces angiotensin II formation from angiotensin I. Reduction of angiotensin II leads to a direct reduction of aldosterone release. Reduces bradykinin degradation and increases prostaglandin synthesis.

Limits OPPS, BP, preload, pulmonary capillary pressure, causes an increase in the minute blood volume and increases myocardial tolerance to exercise in patients with chronic heart failure. Dilates arteries more than veins.

Some effects are explained by the effect on tissue renin-angiotensin systems. Long-term use reduces myocardial hypertrophy and resistive arterial wall hypertrophy. It improves the blood supply to the ischemic myocardium.

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

The onset of action of the drug is in 1 hour, reaches a maximum in 6-7 hours and lasts for 24 hours. The duration of the effect also depends on the dose taken. In case of arterial hypertension, the effect is noted in the first days after the start of treatment, the stable effect develops after 1-2 months. When the drug is abruptly withdrawn, no pronounced increase in BP was observed.

Diroton reduces albuminuria. In patients with hyperglycemia it normalizes the function of the damaged glomerular endothelium. It does not affect the blood glucose concentration in patients with diabetes mellitus and does not lead to increased incidence of hypoglycemia.

Indications

Heart failure, Myocardial infarction, Hypertension (high blood pressure), Diabetic nephropathy, Cardialgia (heart pain)

Arterial hypertension (as monotherapy or in combination with other antihypertensive drugs);

Chronic heart failure (as part of combination therapy to treat patients taking foxglove drugs and/or diuretics);

Acute myocardial infarction (in the first 24 h with stable hemodynamic parameters to maintain these parameters and prevent left ventricular dysfunction and heart failure);

Diabetic nephropathy (to reduce albuminuria in patients with insulin-dependent diabetes with normal BP and in patients with insulin-independent diabetes with arterial hypertension).

Active ingredient

Lisinopril

Composition

1 tablet contains lisinopril 20 mg.

How to take, the dosage

The drug is taken orally once a day, in the morning hours, for all indications, before or after meals, always at about the same time of the day.

In patients with essential hypertension who are not receiving other antihypertensive agents, 10 mg once daily is prescribed. 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 beginning of treatment, which should be taken into account when increasing the dose. If the clinical effect is insufficient, it is possible to combine the drug with other hypotensive agents.

If the patient has received prior treatment with diuretics, their intake should be stopped 2-3 days before the start of Diroton. If diuretics cannot be stopped, the initial dose of Diroton should not exceed 5 mg/ In this case, a physician’s control for several hours after the first dose is recommended (maximum action is reached after about 6 hours), because a pronounced decrease in BP may develop.

In renovascular hypertension or other conditions with increased activity of renin-angiotensin-aldosterone system it is also reasonable to prescribe lower initial dose – 2.5-5 mg per day under increased medical control (BP control, renal function, serum potassium concentration). The maintenance dose should be determined depending on the dynamics of BP.

In patients with renal impairment, because lisinopril is excreted by the kidneys, the initial dose should be determined according to creatinine clearance, then the maintenance dose should be established according to the response with frequent monitoring of renal function, serum potassium and sodium concentrations.

In chronic heart failure, the initial dose is 2.5 mg once daily, which can be increased to the usual maintenance daily dose of 5-20 mg. The daily dose should not exceed 20 mg.

In acute myocardial infarction (as part of combination therapy), 5 mg is prescribed the first day, then 5 mg every other day, 10 mg every other day, and then 10 mg once daily. In patients with acute myocardial infarction, the drug should be used for at least 6 weeks. At the beginning of treatment or within the first 3 days after acute myocardial infarction in patients with low systolic BP (

In diabetic nephropathy in patients with insulin-dependent diabetes mellitus, Diroton is used in a dose of 10 mg once daily. If necessary, the dose can be increased to 20 mg once daily in order to achieve diastolic BP values below 75 mmHg in sitting position. In patients with insulin-independent diabetes mellitus the drug is administered in same dose with aim to reach values of diastolic BP lower than 90 mmHg in sitting position.

Interaction

The simultaneous use of Diroton with potassium-saving diuretics (spironolactone, triamterene, amiloride), potassium preparations, salt substitutes containing potassium increases the risk of hyperkalemia, especially in patients with impaired renal function. That is why combined use is possible only on the base of individual decision of a physician with regular control of serum potassium and renal function.

When used concomitantly with beta-adrenoblockers, slow calcium channel blockers, diuretics and other hypotensive agents the hypotensive effect of the drug is increased.

When concomitant use of ACE inhibitors and gold drugs (sodium aurothiomalate) by IV, a symptom complex including facial hyperemia, nausea, vomiting and arterial hypotension has been described.

Concomitant use with vasodilators, barbiturates, phenothiazines, tricyclic antidepressants, and ethanol increases the hypotensive effect of the drug.

When Diroton is used concomitantly with NSAIDs (including COX-2 selective inhibitors), estrogens, and adrenomimetics, the antihypertensive effect of lisinopril decreases.

When used concomitantly with lithium preparations, excretion of lithium from the body is delayed (increase of the cardiotoxic and neurotoxic effects of lithium).

Concomitant use with antacids and colestiramine reduces absorption in the gastrointestinal tract.

Diroton increases neurotoxicity of salicylates, reduces the effect of hypoglycemic oral agents, norepinephrine, epinephrine and antipodagric agents, increases the effects (including side effects) of cardiac glycosides, effects of peripheral myorelaxants, reduces excretion of quinidine.

Decreases the effect of oral contraceptives.

The simultaneous use of methyldopa increases the risk of hemolysis.

Special Instructions

A pronounced decrease in BP most often occurs with a decrease in fluid volume caused by diuretic therapy, salt reduction, dialysis, diarrhea, or vomiting. In chronic heart failure with or without concomitant renal failure, a marked decrease in BP may occur. More often a significant BP reduction is detected in patients with a severe stage of chronic heart failure, as a consequence of using high dose diuretics, hyponatremia or impaired renal function. In such patients Diroton treatment should be started under the strict control of a physician (select the dosage of the drug and diuretics with caution).

Similar rules should be followed when prescribing Diroton to patients with CHD, cerebrovascular insufficiency, in whom a sharp decrease in BP may lead to myocardial infarction or stroke.

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

Diroton may decrease BP in some patients with chronic heart failure but with normal or decreased BP, which is usually not a reason to discontinue treatment.

Before treatment with Diroton, if possible, normalize sodium concentration and/or replenish lost fluid volume, carefully monitor the effect of the initial dose of Diroton on the patient’s BP.

In case of renal artery stenosis (especially in bilateral stenosis or in the presence of artery stenosis of the only kidney), as well as in circulatory failure due to lack of sodium and/or fluid, use of Diroton may lead to impaired renal function, acute renal failure, which is usually irreversible after drug withdrawal.

In acute myocardial infarction the use of standard therapy (thrombolytics, acetylsalicylic acid, beta-adrenoblockers) is indicated. It is possible to use Diroton together with IV administration or with the use of therapeutic transdermal nitroglycerin systems.

In major surgical interventions, as well as in the use of other drugs that cause BP reduction, lisinopril, by blocking angiotensin II formation, may cause a significant unpredictable decrease in BP.

In elderly patients, the use of standard doses leads to higher blood concentrations of the drug, so extra caution is required in determining the dose, although no differences in the antihypertensive effect of Diroton have been found in elderly and young patients.

Because the potential risk of agranulocytosis cannot be excluded, periodic monitoring of blood counts is required.

Anaphylactic shock may occur when the drug is used in dialysis with a polyacrylonitrile membrane, so either a different type of dialysis membrane or the administration of other antihypertensive agents is recommended.

There are no data on the effect of lisinopril on the ability to drive and operate vehicles, but it should be taken into account that dizziness may occur, so caution should be exercised.

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Contraindications

An history of angioedema (including when using ACE inhibitors); hereditary Quincke’s edema; age under 18 years (effectiveness and safety not established); hypersensitivity to lisinopril or other ACE inhibitors; pregnancy and lactation.

With caution: In severe renal dysfunction, bilateral renal artery stenosis or artery stenosis of the single kidney with progressive azotemia, condition after renal transplantation, renal failure, azotemia, hyperkalemia, aortic estuary stenosis, hypertrophic obstructive cardiomyopathy, primary hyperaldosteronism, arterial hypotension, cerebrovascular disease (incl.cerebrovascular diseases (including insufficiency of cerebral circulation), coronary artery disease, autoimmune systemic connective tissue diseases (including scleroderma, systemic lupus erythematosus), inhibition of medullar hemopoiesis, hypovolemic conditions (including those caused by diarrhea, vomiting), patients on sodium-restricted diet, elderly patients.

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Side effects

The most common side effects are dizziness, headache (5-6%), weakness, diarrhea, dry cough (3%), nausea, vomiting, orthostatic hypotension, skin rash, chest pain (1-3%).

The frequency of other adverse reactions is less than 1%.

Cardiovascular system: significant decrease in BP, chest pain; rarely – orthostatic hypotension, tachycardia, bradycardia, appearance of symptoms of heart failure, AV conduction failure, myocardial infarction.

Digestive system disorders: nausea, vomiting, abdominal pain, dry mouth, diarrhea, dyspepsia, anorexia, taste disorders, pancreatitis, hepatitis (hepatocellular and cholestatic), jaundice (hepatocellular or cholestatic), hyperbilirubinemia, increased liver transaminase activity.

Skin disorders: urticaria, increased sweating, photosensitization, skin itching, hair loss.

CNS disorders: mood lability, concentration disorders, paraesthesia, fatigue, somnolence, convulsive twitching of limbs and lips; rarely – asthenic syndrome and mental confusion.

Respiratory system: dyspnea, dry cough, bronchospasm, apnea.

Hematopoietic system disorders: leukopenia, thrombocytopenia, neutropenia, agranulocytosis, anemia (decrease in hemoglobin concentration, hematocrit, erythrocytopenia), with long-term treatment a slight decrease in hemoglobin and hematocrit may occur, in some cases – agranulocytosis.

Allergic reactions: angioedema of the face, extremities, lips, tongue, epiglottis and/or larynx, intestinal angioedema, vasculitis, positive reactions to antinuclear antibodies, increased CRP, eosinophilia; in very rare cases – interstitial angioedema (edema of the interstitial lung tissue without transudate exit into the alveolar lumen).

Urogenital system disorders: uremia, oliguria, anuria, renal dysfunction, acute renal failure, decreased potency.

Laboratory measures: hyperkalemia and/or hypokalemia, hyponatremia, hypomagnesemia, hypochloremia, hypercalcemia, hyperuricemia, increased concentration of urea and creatinine in plasma, hypercholesterolemia, hypertriglyceridemia, reduced glucose tolerance.

Other: arthralgia, arthritis, myalgia, fever, exacerbation of gout.

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Overdose

Symptoms: pronounced BP decrease.

Treatment: if necessary, symptomatic therapy (IV fluid administration, control and normalization of BP, water-electrolyte balance). Lisinopril may be eliminated from the body by dialysis.

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Similarities

Diroton, Lisinopril, Lisinopril Stada, Lisinopril-Teva, Lisinopril-ALSI