Indapamid retard-OBL - instructions for use, dose, side effects, contraindications

Active substances:
Indapamide	1.5 mg
Excipients:
silicon dioxide colloid (aerosil)	0.9 mg
hypromellose (hydroxypropylmethylcellulose)	55.0 mg
copolyvidone (copovidone)	4.5 mg
magnesium stearate	1.8 mg
lactose monohydrate	58.2 mg
microcrystalline cellulose	58.1 mg
Weight of the core tablet	180.0 mg
Auxiliary substances for the film sheath:
hypromellose (hydroxypropylmethylcellulose)	3.5 mg
macrogol 6000 (polyethylene glycol 6000)	0.6 mg
talc	0.2 mg
titanium dioxide	0.7 mg
Weight of coated tablets	185.0 mg

Description:

The tablets covered with a film membrane of white or almost white color, round, biconcave form. On the cross-section, two layers are visible, the inner layer is white or almost white.

Pharmacotherapeutic group:Diuretics

ATX: & nbsp

C.03.B.A.11 Indapamide

Pharmacodynamics:

Hypotensive agent (diuretic, vasodilator). By pharmacological properties is close to thiazide diuretics, it disrupts the reabsorption of sodium ions in the cortical segment of the Henle loop. Increases the allocation of kidney ions of sodium and chlorine, to a lesser extent - ions of potassium and magnesium. Possessing the ability to selectively block "slow" calcium channels, increases the elasticity of the walls of the arteries, reduces the overall peripheral vascular resistance (OPSS). Helps reduce hypertrophy of the left ventricle of the heart. In therapeutic doses does not affect lipid and carbohydrate metabolism, including in patients with concomitant diabetes mellitus (DM).

Reduces the sensitivity of the vascular wall to norepinephrine and angiotensin II, stimulates the synthesis of prostaglandin (PgE2) and prostacyclin (PgI2).

With a systematic admission, the therapeutic effect of indapamide develops in 1-2 weeks, peaks at 8-12 weeks and persists for up to 8 weeks. After taking a single dose, the maximum effect is observed after 24 hours.

Pharmacokinetics:

Indapamide after oral administration is rapidly and completely absorbed from the gastrointestinal tract (GIT). Bioavailability is high, about 93%. Eating somewhat slows the rate of absorption, but does not affect the amount of absorbed substance. Time to reach the maximum concentration in the blood (T_mOh) - 12 hours after ingestion. At repeated receptions fluctuations of concentration of a preparation in a blood plasma in an interval between receptions of two doses decrease. The equilibrium concentration is established after 7 days of regular intake. The half-life (T_1/2) - 18 h, communication with blood plasma proteins - 71-79%. It also binds to the elastin of the smooth muscles of the vascular wall. Has a high volume of distribution, passes through the histohematological barriers (including placental), penetrates into breast milk.

Indapamide is metabolized in the liver to inactive metabolites. The kidneys excrete 60-80% in the form of metabolites, in unchanged form is about 5%, through the intestine - 20%. In patients with renal insufficiency, pharmacokinetics does not change.Do not cumulate.

Indications:

Arterial hypertension.

Contraindications:

Hypersensitivity to the drug and other derivatives of sulfonamide, thiazide derivatives or other components of the drug, renal failure (anuria stage), hypokalemia, marked hepatic (including encephalopathy) insufficiency, pregnancy, lactation, age under 18 (efficacy and security not established); lactose intolerance, lactase deficiency or glucose-galactose malabsorption.

Carefully:

Impaired renal and / or liver function, diabetes mellitus in decompensation, water-electrolyte balance disorders, hyperuricemia (especially accompanied by gout and urate nephrolithiasis), hyperparathyroidism; patients receiving therapy, as a result of which an extension of the QT interval is possible (astemizole, erythromycin (intravenously), pentamidine, phenothiazines (chlorpromazine, cyamemazine, levomepromazine, thioridazine, trifluoperazine), benzamides (amisulpride, sulpiride, sultopride, tiapride), butyrophenones (droperidol, haloperidol), bepridil, cisapride, difemanyl, halofantrine, misolastine, sparfloxacin, moxifloxacin, sotalol, terfenadine, wincamine, antiarrhythmic drugs of IA class (quinidine, disopyramide) and III class (amiodarone, brethil tosylate).

Pregnancy and lactation:The drug is not recommended for pregnancy. 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:

Inside, not liquid, regardless of food intake, it is preferable to apply in the morning hours, squeezed enough liquid.

The daily dose of the drug is 1 tablet (1.5 mg).

If the desired therapeutic effect is not achieved after 4-8 weeks of treatment, the dose of the drug should not be increased (an increased risk of side effects without increasing the antihypertensive effect). Instead, it is recommended that another antihypertensive drug that is not a diuretic be included in the drug regimen.

Side effects:

From the digestive tract: loss of appetite, dryness of the oral mucosa, nausea, vomiting, abdominal pain, diarrhea or constipation, pancreatitis. Patients with hepatic insufficiency may develop hepatic encephalopathy.

From the central nervous system: increased excitability, headache, dizziness, vertigo, sleep disturbances, insomnia, depression, fatigue, drowsiness, general weakness, malaise, asthenia, muscle spasms, tension, irritability, anxiety, paresthesia.

From the sense organs: conjunctivitis, impaired vision.

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

From the cardiovascular system: orthostatic hypotension, changes in the electrocardiogram (characteristic of hypokalemia), arrhythmia, palpitation.

From the urinary system: infection, nocturia, polyuria.

Allergic reactions: skin itch, rash, urticaria, Stevens-Johnson syndrome, toxic epidermal necrolysis angioedema, maculopapular rash, photosensitivity.

From the hematopoiesis: hemorrhagic vasculitis, thrombocytopenia, leukopenia, agranulocytosis, bone marrow aplasia, hemolytic anemia.

Laboratory indicators: hyperuricemia, hyperglycemia, hypokalemia, hypochloraemia, hyponatremia, hypercalcemia,increase in blood plasma concentrations of urea nitrogen, hypercreatininaemia.

Other: exacerbation of systemic lupus erythematosus.

Overdose:

Symptoms: associated with a violation of the water-electrolyte balance - nausea, vomiting, dizziness, drowsiness, confusion, respiratory depression, convulsions, inhibition, in patients with impaired liver function, the development of "hepatic" coma, polyuria or oliguria leading to anuria (due to hypovolemia ), excessive lowering of blood pressure.

Treatment: gastric lavage, the appointment of activated charcoal with the subsequent restoration of the water-electrolyte balance, symptomatic therapy. There is no specific antidote. With a significant reduction in blood pressure, the patient should be placed in the "lying" position on the back with raised legs, if necessary, correct hypovolemia (for example, intravenous infusion of 0.9% sodium chloride solution).

Interaction:

With simultaneous use with drugs, lithium causes an increase in the content of lithium ions in the blood plasma due to a decrease in its excretion by the kidneys, lithium has a nephrotoxic effect.

When applied simultaneously with iodine-containing contrast media in high doses indapamide increases the risk of developing kidney dysfunction by reducing the volume of circulating blood (BCC). Before using iodine-containing contrast agents, patients need to fill a shortage of BCC.

Indapamide reduces the effect of indirect anticoagulants (coumarin or indanedione derivatives) by increasing the concentration of clotting factors (as a result of a decrease in BCC).

Indapamide enhances the action of nondepolarizing muscle relaxants.

The risk of hypokalemia increases with simultaneous use of indapamide with diuretics ("loop", thiazide), cardiac glycosides, glucocorticosteroids, mineralocorticoids, tetracosactide, amphotericin B (intravenously), laxatives.

With the simultaneous administration of indapamide with cardiac glycosides, the likelihood of developing digitalis intoxication increases; with calcium preparations - hypercalcemia; with metformin - the risk of development of lactic acidosis increases.

Astemizole, erythromycin (intravenously), pentamidine, phenothiazines (chlorpromazine, cyamemazine, levomepromazine, thioridazine, trifluoperazine), benzamides (amisulpride, sulpiride, sultopride, tiapride), butyrophenones (droperidol, haloperidol), bepridil, cisapride, difemanyl, halofantrine, misolastine, sparfloxacin, moxifloxacin, sotalol, terfenadine, wincamine, antiarrhythmic drugs of IA class (quinidine, disopyramide) and III class (amiodarone, brethil tosylate) when combined with indapamide may cause a heart rhythm disorder of the "pirouette" type due to the prolongation of the QT interval.

Non-steroidal anti-inflammatory drugs, including selective inhibitors of cyclooxygenase-2 (COX-2), high doses of acetylsalicylic acid (3 g / day or more), glucocorticosteroids, tetracosactide, adrenostimulants reduce the antihypertensive effect of indapamide; baclofen - Strengthens.

Angiotensin converting enzyme inhibitors, when used concurrently with indapamide, increase the risk of orthostatic hypotension and / or acute renal failure (especially in the presence of renal artery stenosis).

Imipramine (tricyclic) antidepressants and antipsychotics (antipsychotics) increase antihypertensive actionindapamide and increase the likelihood of orthostatic hypotension.

Cyclosporine and tacrolimus increase the risk of hypercreatininaemia.

Special instructions:

During the treatment with the drug, the content of sodium, magnesium ions (since electrolyte disturbances can develop), glucose, uric acid and residual nitrogen, and the pH of the blood should be systematically monitored in the blood.

Patients taking cardiac glycosides against the background of the drug, laxatives, patients with hyperaldosteronism, as well as patients of advanced age, are shown regular monitoring of the content of potassium and creatinine ions in the blood.

The first measurement of the content of potassium ions in the blood should be made during the first week of treatment.

The most regular control is indicated for patients with cirrhosis of the liver (especially with edema or ascites) because of the risk of metabolic alkalosis worsening the course of hepatic encephalopathy, with coronary heart disease, chronic heart failure, and elderly patients. Patients with an increased QT interval on an electrocardiogram (congenital or developing against a background of a pathological process) are also considered to be at high risk.

Hypercalcemia on the background of taking the drug may be a consequence of previously undiagnosed hyperparathyroidism.

In some patients, a combination of the drug with potassium-sparing diuretics may be effective, but the possibility of hypo- or hyperkalemia, especially in patients with diabetes mellitus and kidney failure, is not ruled out.

Patients with diabetes should monitor the concentration of glucose in the blood, especially when there is hypokalemia.

A significant decrease in the volume of circulating blood on the background of drug therapy may lead to the development of acute renal failure due to a decrease in the rate of glomerular filtration. Patients need to compensate for the shortage of circulating blood at the beginning of treatment and monitor kidney function.

Derivatives of sulfonamides can aggravate the course of systemic lupus erythematosus.

Indapamid retard-OBL can give positive results in the conduct of doping control.

Efficacy and safety in children under 18 years of age is not established.

In patients with elevated uric acid concentration in blood plasma, the frequency of gout attacks may increase with therapy.

With the use of thiazide-like diuretics, cases of the development of photosensitivity reactions were noted. If they develop, the drug should be discontinued. Against the background of therapy with the drug, it is necessary to protect the exposed areas of the body from exposure to sunlight and artificial ultraviolet radiation.

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

At the beginning of the treatment, the drug should refrain from driving vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions, as dizziness may develop.

Form release / dosage:

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

Packaging:

For 10, 15, 20 or 30 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 1, 2, 3, 4 or 5 contour mesh packages with instructions for use are placed in a pack of cardboard.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LS-000939

Date of registration:23.09.2011 / 11.09.2012

Expiration Date:Unlimited

The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Manufacturer: & nbsp

OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Representation: & nbspOBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSCOBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSCRussia

Information update date: & nbsp02.11.2017

Illustrated instructions

Instructions

Indapamide Retard-OBL (Indapamide retard-OBL)