Diroton, tablets 5 mg, 56 pcs.

Diroton tablets are an ACE inhibitor.

It reduces the formation of angiotensin II from angiotensin I. Reducing angiotensin II leads to a direct reduction in the release of aldosterone . Reduces bradykinin degradation and increases prostaglandin synthesis. Reduces RPS, 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 to a greater extent 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 When the drug is abruptly withdrawn, no pronounced increase in BP was observed.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

– Arterial hypertension (as monotherapy or in combination with other antihypertensive drugs).
– Chronic heart failure (as part of combined therapy for the treatment of patients taking foxglove drugs and/or diuretics).
– Acute myocardial infarction (in the first 24 hours 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 hypertension).

Active ingredient

Composition

One tablet contains:

Lisinopril 5 mg.

Auxiliary substances:

magnesium stearate,

talc,

mannitol,

How to take, the dosage

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

Performance in essential hypertension: In patients not receiving other antihypertensive agents, 10 mg once daily is prescribed. Normal 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. In case of insufficient clinical effect, the drug may be combined with other hypotensive agents. If the patient received prior treatment with diuretics, their intake should be stopped 2-3 days before the start of Diroton. If it is impossible to cancel diuretics, the initial dose of Diroton should not exceed 5 mg/day. In this case, after taking the first dose, it is recommended that a physician monitor for several hours (the maximum effect is reached after about 6 hours), because a pronounced decrease in BP may develop.

Application in renovascular hypertension and states with increased activity of renin-angiotensin-aldosterone system: it is reasonable to administer lower initial dose – 2.5-5 mg/day under increased medical control (BP control, renal function, serum potassium concentration). The maintenance dose should be determined depending on the dynamics of BP.

Perhaps for use in chronic heart failure: The initial dose is 2.5 mg once daily, which may be increased to the usual maintenance daily dose of 5-20 mg. The daily dose should not exceed 20 mg.

Application in acute myocardial infarction: as part of combination therapy, 5 mg in 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 during the first 3 days after acute myocardial infarction in patients with low systolic blood pressure (?120 mmHg), the drug should be administered in a dose of 2.5 mg. In case of BP lowering (systolic BP ?100 mm Hg) against the background of Diroton use the daily dose of 5 mg can be temporarily reduced to 2.5 mg. In case of prolonged marked BP lowering (systolic BP

In patients with insulin-dependent diabetes mellitus Diroton is used in dose of 10 mg once daily. If necessary, the dose can be increased up to 20 mg once daily in order to achieve values of diastolic BP 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.

In view of the fact that lisinopril is excreted by the kidneys, the initial dose should be determined according to creatinine clearance, then a maintenance dose should be established according to the response, with frequent monitoring of renal function, potassium concentration and serum sodium concentration: Creatinine clearance (ml/min) Initial dose 30-70 5-10 mg 10-30 2.5-5 mg Less than 10 (including patients on hemodialysis) 2.5 mg

Interaction

With caution, Diroton should be administered simultaneously with potassium-saving diuretics (spironolactone, triamterene, amiloride), potassium, salt substitutes containing potassium, because the risk of hyperkalemia increases, especially with impaired renal function. This is why these combinations should only be prescribed on the basis of an individual decision of the physician with regular monitoring of serum potassium levels and renal function.

When used concomitantly with diuretics and other antihypertensive agents an additive antihypertensive effect develops (risk of significant BP reduction).

Concomitant use with NSAIDs (including indomethacin), estrogens, and adrenostimulants reduces the antihypertensive effect of lisinopril.

Concomitant use with lithium may decrease excretion of lithium, therefore serum lithium concentration should be monitored regularly.

Simultaneous use with antacids and colestyramine decreases gastrointestinal absorption of lisinopril.

Concomitant use of Diroton may increase the effect of ethanol (alcohol).

When used concomitantly with diuretics, lisinopril decreases potassium excretion.

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.

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

In major surgical procedures or other BP lowering medications, lisinopril, by blocking angiotensin II formation, may cause a significant, unpredictable decrease in BP.

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

In chronic heart failure with or without concomitant renal failure, marked BP decrease may occur. More often a significant BP decrease is revealed in patients with severe stage of chronic heart failure as a consequence of using high dose diuretics, hyponatremia or impaired renal function. In such patients, treatment with Diroton should be started under the strict supervision of a doctor (with caution, select the dosage of the drug and diuretics). When using Diroton in some patients with chronic heart failure, but with normal or lowered BP, a decrease in BP may be noted, which is usually not a reason for stopping the treatment. A transient hypotensive reaction is not a contraindication for the next dose of the drug.

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, the use of Diroton may lead to impaired renal function, acute renal failure, which is usually irreversible after withdrawal of the drug.

When using the drug in dialysis with a polyacrylonitrile membrane, anaphylactic shock may occur, so either another type of dialysis membrane or prescription of other antihypertensive agents is recommended.

Contraindications

– Angioneurotic edema in anamnesis (including ACE inhibitors).
– Hereditary Quincke’s edema.
– Age under 18 years (effectiveness and safety not established).
– Hypersensitivity to lisinopril or other ACE inhibitors.

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.

Overdose

Symptoms: pronounced BP decrease.

Treatment: if necessary, symptomatic therapy (intravenous fluid administration, control and normalization of BP, water-electrolyte balance).

Lisinopril may be eliminated from the body by dialysis.

Pregnancy use

The use of Diroton during pregnancy is contraindicated. Lisinopril crosses the placental barrier. If pregnancy is established, the drug should be discontinued as soon as possible.

The use of ACE inhibitors in the II and III trimesters of pregnancy has adverse effects on the fetus (marked BP decrease, renal failure, hyperkalemia, skull hypoplasia, fetal death are possible).

There are no data on the negative effects of the drug on the fetus in case of I trimester use. It is recommended that neonates and infants who have been intrauterine exposed to ACE inhibitors be closely monitored for the timely detection of marked BP decrease, oliguria, hyperkalemia.

There is no evidence of lisinopril penetration into breast milk. If it is necessary to prescribe the drug during lactation, breast-feeding should be discontinued.

Similarities