Acuteur-Sanovel - instructions for use, dose, side effects, contraindications

Indapamide belongs to the sulfonamide derivatives and is pharmacologically similar to thiazide diuretics. Has moderate saluretic and diuretic effects, which are associated with the blockade of the reabsorption of sodium, chlorine and, to a lesser extent, potassium and magnesium ions in the proximal tubules and the cortical segment of the distal tubule of the nephron. Reduces the tone of the smooth muscles of the arteries, reduces the overall peripheral resistance of the vessels. The vasodilator effects and the reduction of the overall peripheral vascular resistance are based on the following mechanisms: a decrease in the reactivity of the vascular wall to norepinephrine and angiotensin II; an increase in the synthesis of prostaglandins with vasodilating activity; suppression of calcium current in smooth muscle cells of blood vessels. Helps reduce hypertrophy of the left ventricle of the heart. Indapamide has an antihypertensive effect in doses that do not have a pronounced diuretic effect. In therapeutic doses does not affect lipid and carbohydrate metabolism (including in patients with concomitant diabetes mellitus).

The antihypertensive effect of the drug persists for 24 hours against a background of a single dose.

Pharmacokinetics:

Suction

Indapamide after oral administration is rapidly and completely absorbed in the gastrointestinal tract. Eating somewhat slows the rate of absorption of the drug, but it does not affect the amount of absorbed substance. After taking a single dose or multiple doses of the drug, the maximum concentration in the blood plasma is reached after 12 hours.

Distribution

About 79% of the drug binds to blood plasma proteins.

Metabolism

Indapamide is metabolized in the liver to inactive metabolites, only about 5-8% of the accepted dose of the drug is excreted by the kidneys unchanged.

Excretion

The drug is excreted from the body by the kidneys (70%) and through the intestine (22%) in the form of inactive metabolites. The half-life of indapamide is on average 16 hours. Equilibrium concentration is achieved after 7 days of regular intake of the drug. Repeated reception of Acuteur-Sanovel does not lead to the accumulation of indapamide in the body.

In patients with renal insufficiency, the pharmacokinetic parameters of the drug do not change.

Indications:

Arterial hypertension.

Contraindications:

- Hypersensitivity to indapamide, other derivatives of sulfonamide or other components of the drug;

- severe renal failure (anuria stage);

- hepatic encephalopathy or severe hepatic impairment;

- hypokalemia;

- lactose intolerance, galactosemia, glucose / galactose absorption disorder;

- age to 18 years (efficacy and safety not established).

Carefully:

Impaired renal and / or liver function, diabetes mellitus at the stage of decompensation, water-electrolyte balance disorders, hyperuricemia (especially accompanied by gout and urate nephrolithiasis), hyperparathyroidism, patients with an increased interval QT on an electrocardiogram or receiving a combination therapy, as a result of which it is possible to increase the interval QT (see section "Interaction with other drugs").

Pregnancy and lactation:

Taking indapamide during pregnancy is not recommended. The use of the drug may cause fetoplacental ischemia with the risk of slowing the development of the fetus.

It is not recommended to use the drug during lactation (indapamide penetrates into breast milk).

Dosing and Administration:

Dosing and Administration Inside, 1 tablet / day, without chewing, regardless of food intake, squeezed a sufficient amount of liquid. It is preferable to take the drug in the morning.

When treating patients with arterial hypertension, an increase in the dose of the drug does not lead to an increase in antihypertensive action, but enhances the diuretic effect.

Side effects:

From the cardiovascular system: arrhythmia, palpitations, changes on the ECG (manifestations of hypokalemia).

From the digestive system: sensation of dryness in the oral cavity, nausea, indigestion (including vomiting), constipation, diarrhea, anorexia, abdominal pain. Very rarely - pancreatitis.

From the nervous system: dizziness, paresthesia, headache, nervousness, asthenia, drowsiness, vertigo, insomnia, depression, fatigue, malaise, muscle spasm, tension, irritability, anxiety. Patients with hepatic impairment may develop hepatic encephalopathy (see "Contraindications").

From the respiratory system: cough, pharyngitis, sinusitis, rhinitis.

Allergic reactions: skin itching, urticaria, puncture rash; in patients predisposed to allergic reactions, there may be a manifestation of hypersensitivity, mainly dermatological reactions;

From the genitourinary system: infection, nocturia, polyuria.

Other: hemorrhagic vasculitis, exacerbation of systemic lupus erythematosus.

Laboratory indicators: hyperuricemia, hyperglycemia, hypercreatininaemia, glycosuria, decreased potassium levels and development of hypokalemia. Clinical data show that hypokalemia (potassium in plasma ≤ 3.4 mmol / L) was observed in 10% of patients and ≤ 3.2 mmol / L in 4% of patients after 4-6 weeks of treatment. After 12 weeks of therapy, the potassium level in the blood plasma was 0.23 mmol / l.

Decrease in the level of sodium in the blood plasma, accompanied by hypovolemia, dehydration of the body and orthostatic hypotension. In rare cases, the simultaneous loss of chloride ions can lead to compensatory metabolic alkalosis.

Increase in urea in the blood plasma; extremely rare - an increase in the level of calcium in the blood plasma.

Very rarely: thrombocytopenia, leukopenia, agranulocytosis, aplastic and hemolytic anemia.

Overdose:

Indapamide even in high concentrations up to 40 mg (27 times more than the therapeutic dose) has no toxic effect.

Symptoms acute poisoning with the drug, primarily associated with a violation of the water-electrolyte balance: nausea, vomiting, severe lowering of blood pressure, dizziness, convulsions, drowsiness, confusion, polyuria or oliguria, ending with anuria (due to hypovolemia).

Treatment: gastric lavage and / or the administration of activated charcoal, followed by restoration of normal water-electrolyte balance, symptomatic therapy. There is no specific antidote.

Interaction:

Unwanted combination of drugs

Lithium preparations: with the simultaneous use of indapamide with lithium preparations, an increase in the concentration of lithium in blood plasma is possible. If necessary, diuretic drugs can be used in combination with lithium preparations, but you should carefully select the dose of drugs, constantly monitoring the lithium content in blood plasma.

Preparations that do not belong to the class of antiarrhythmic drugs, causing arrhythmia of the type "pirouette" (astemizole, beprideil, erythromycin (with intravenous administration), halofantrine, pentamidine, sultopride, terfenadine, wincamine): with simultaneous use with indapamide increases the likelihood of heart rhythm disorders by type torsades de pointes (ventricular tachycardia of the "pirouette" type).

A combination of drugs that requires special attention

Nonsteroidal anti-inflammatory drugs (for systemic administration): with a significant loss of fluid may develop acute renal failure (due to reduced glomerular filtration). Patients need to compensate for fluid loss and at the beginning of treatment carefully monitor kidney function.

Other drugs that can cause hypokalemia: amphotericin B (with in / in the introduction), gluco- and mineralocorticosteroids (for systemic administration), tetracosactide, agents that stimulate intestinal motility: increased risk of hypokalemia (additive effect). It is necessary to constantly monitor the level of potassium in the blood plasma, if necessary, patients are prescribed appropriate treatment.

Baclofen: there is an increase in the hypotensive effect.Patients need to compensate for fluid loss and at the beginning of treatment carefully monitor kidney function.

Drugs of digitalis: the probability of development of digitalis intoxication increases. With the simultaneous use of thiazide diuretics and cardiac glycosides, the level of potassium in the blood plasma and ECG parameters should be carefully monitored.

Saluretics (looped, thiazide): increase the risk of hypokalemia.

Potassium-sparing diuretics (amiloride, spironolactone, triamterene): this combination of drugs is effective in some patients, but the possibility of developing hypokalemia, especially in patients with diabetes mellitus or kidney failure, is not completely excluded. It is necessary to monitor the level of potassium in the blood plasma, the parameters of the ECG and, if necessary, change the course of treatment.

Angiotensin-converting enzyme (ACE) inhibitors: a reduced plasma concentration of sodium in patients receiving ACE inhibitors increases the risk of sudden arterial hypotension and / or acute renal failure during the first week (especially with existing renal artery stenosis).In the first week of taking ACE inhibitors in patients, it is necessary to monitor the function of the kidneys (containing creatinine in the blood plasma).

Antiarrhythmic drugs that can cause arrhythmia of the "pirouette" type: drug IA (quinidine, disopyramide) and III class (amiodarone, brethil tosylate, sotalol): arrhythmia of the "pirouette" type (risk factors: hypokalemia, bradycardia and initially elongated interval QT). Care should be taken to monitor potassium levels in the blood plasma and the interval QT, changing the course of treatment if necessary.

Metformin: lactic acidosis, arising on the background of taking metformin, is often a consequence of functional renal failure caused by the action of diuretics and especially loop diuretics. Do not use metformin, if the level of creatinine exceeds 15 mg / L (135 μmol / L) in men and 12 mg / L (110 μmol / L) in women.

Contrasting iodine-containing products: in high doses increase the risk of kidney dysfunction (dehydration). Before using contrasting iodine-containing substances, patients need to restore fluid loss.

Tricyclic antidepressants and antipsychotics: increase the hypotensive effect of indapamide and increase the risk of developing orthostatic hypotension.

Salts of calcium: with the simultaneous administration of an increase in the concentration of calcium ions in the blood plasma due to a decrease in their excretion in the urine.

Cyclosporin: while simultaneous use with indapamide increases the risk of hypercreatininaemia.

Glucose and mineralocorticosteroids (for systemic administration), tetracosactide: decreased hypotensive effect (fluid retention and sodium ions as a result of the action of corticosteroids).

Indirect anticoagulants: reduction in the effect of coumarin or indanedione derivatives due to increased liver production (dose adjustment may be required).

Non-depolarizing muscle relaxants: strengthening the blockade of neuromuscular transmission.

Adrenostimulators: decreased hypotensive effect.

Special instructions:

Dysfunction of the liver

When diuretics are prescribed, patients with impaired liver function may develop hepatic encephalopathy. In this case, the drug should be immediately withdrawn.

Water-electrolyte balance

Sodium content in blood plasma: before the start of treatment it is necessary to determine the content of sodium ions in the blood plasma. Against the background of the drug, this control should be carried out continuously. All diuretics can cause hyponatremia, which sometimes leads to extremely serious consequences. Periodic monitoring of sodium content is necessary, because the initial decrease in the concentration of sodium in the blood plasma may not be accompanied by the appearance of pathological symptoms. The most thorough control of the level of sodium ions is indicated for patients with cirrhosis of the liver and elderly people (see the sections "Side effect" and "Overdose").

The content of potassium in blood plasma: with diuretic therapy, the main risk is a sharp decrease in the level of potassium in the blood plasma and the development of hypokalemia. It is necessary to avoid the risk of developing hypokalemia (<3.4 mmol / l) especially in patients of the following categories: elderly, weakened or receiving concomitant medication, patients with cirrhosis, peripheral edema or ascites, coronary heart disease, heart failure. Hypokalemia in these patients increases the toxic effect of cardiac glycosides and increases the risk of developing cardiac arrhythmias.In addition, patients with an extended QT interval on the ECG are at increased risk, but it does not matter whether this elongation is due to congenital symptoms or the presence of a pathological process. Hypokalemia, as well as bradycardia, is a condition conducive to the development of severe cardiac arrhythmias, in particular of the "pirouette" type, often leading to death. In all the cases described above, it is necessary to regularly monitor the potassium content in the blood plasma. The first control of the concentration of potassium ions in the blood should be carried out during the first week after the start of treatment. When hypokalemia occurs, appropriate treatment should be prescribed.

Calcium in the blood plasma: diuretics reduce the excretion of calcium in the urine, leading to a slight and temporary increase in the concentration of calcium in the blood plasma. Expressed hypercalcemia may be a consequence of previously not diagnosed hyperparathyroidism. It is necessary to cancel the use of diuretic drugs before the study of parathyroid function.

Other laboratory indicators

The content of glucose in the blood plasma: against the background of therapy with Acuteter-sanovel in patients with diabetes mellitus, blood glucose levels can change, especially in the presence of hypokalemia.

Uric acid: in patients with a high level of uric acid in the blood plasma against the background of therapy with the drug AcuTer-sanovel, the incidence of gout attacks may increase.

Athletes

The active substance, which is part of the drug Acuter-sanovel, can give a positive result in the conduct of doping control in athletes.

Effect on the ability to drive transp. cf. and fur:

In some cases, individual reactions associated with changes in blood pressure are possible, especially at the beginning of treatment or with the addition of other antihypertensive drugs. As a result, the ability to drive and work with mechanisms that require increased attention can be reduced.

During the treatment period, one should refrain from driving by car and engage in potentially dangerous activities that require increased concentration and speed of psychomotor reactions, as dizziness is possible, especially at the beginning of the course of treatment.

Form release / dosage:

Tablets of prolonged action, film-coated, 1.5 mg.

Packaging:

10 tablets in a blister of PVC-aluminum foil.

3 blisters are placed in a cardboard box together with instructions for use

Storage conditions:

In a dry place at a temperature of 15 to 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-001485/09

Date of registration:03.03.2009 / 24.10.2016

Expiration Date:Unlimited

The owner of the registration certificate:Sanovel Pharmaco-industrial trading companySanovel Pharmaco-industrial trading company Turkey

Manufacturer: & nbsp

SANOVEL PHARMACEUTICAL PRODUCTS IND., Inc. Turkey

Representation: & nbspSANOVEL branch of the company pharmaco-industrial trading companySANOVEL branch of the company pharmaco-industrial trading companyRussia

Information update date: & nbsp28.06.2017

Illustrated instructions

Instructions

Acuter-Sanovel (Akuter-Sanovel)