Indapamid

General characteristics. Structure:

Active agent: индапамид 2,5 mg;

excipients: potato starch, кросповидон (коллидон S-M or коллидон S), lactose (sugar milk), magnesium stearate, povidone (коллидон 30), talc, cellulose microcrystallic; structure of a film cover: hypro rod (hydroxypropyl cellulose), gipromelloz (gidroksipropilmetiltsellyuloz), коповидон (коллидон UA-64), talc, titanium dioxide.

Description: Round, biconvex tablets, film coated white or almost white color. On cross section — white color.

Pharmacological properties:

Pharmacodynamics. Indapamid treats derivatives of sulfonamide and on pharmacological properties is close to thiazide diuretics.

Has moderate saluretichesky and diuretic effects which are caused by inhibition of a reabsorption of ions of sodium, chlorine and to a lesser extent potassium ions and magnesium in proximal tubules of kidneys and in a cortical segment of a distal tubule of nephron.

Indapamid reduces a tone of smooth muscles of arteries and has vasodilating effect, reduces the general peripheric resistance of vessels. These effects are mediated by decrease in reactivity of a vascular wall to noradrenaline and angiotensin II; increase in synthesis of E2 prostaglandin having vasodilating activity; oppression of current of calcium in smooth muscle cells of vessels.

Indapamid promotes reduction of a hypertrophy of a left ventricle of heart. Has anti-hypertensive effect in the doses which do not have the expressed diuretic effect. In therapeutic doses does not influence lipidic and carbohydrate metabolism (including at patients with the accompanying diabetes mellitus).

At systematic reception the therapeutic effect of an indapamid develops in 1–2 weeks, reaches a maximum by 8–12 week and remains up to 8 weeks. After reception of a single dose the maximum effect is noted in 24 hours.

Pharmacokinetics. Indapamid after intake is quickly and completely soaked up in digestive tract. Meal slows down drug absorption speed a little, but does not influence amount of the soaked-up substance. Communication with proteins of a blood plasma — 71–79%. Contacts also elastin of unstriated muscles of a vascular wall. Has the high volume of distribution, passes through gistogematichesky barriers (including through placental). Time of achievement of the maximum concentration in blood makes 1–2 h Indapamid is metabolized in a liver to inactive metabolites (about 5-7% of the accepted dose of drug are removed by kidneys in not changed look). The elimination half-life of an indapamid averages 16 hours. Drug is removed from an organism by kidneys (60–70%) and through intestines (20–23%) in the form of inactive metabolites. At patients with a renal failure pharmacokinetic parameters of drug do not change.

Indications to use:

Arterial hypertension.

Route of administration and doses:

It is appointed inside, irrespective of meal, more preferably in the morning. Indapamid it is necessary to accept without chewing, washing down with enough liquid.

At arterial hypertension индапамид it is appointed in a dose — 2,5 mg of 1 times a day. Increase in a dose of drug does not lead to strengthening of anti-hypertensive action.

Features of use:

During therapy by Indapamid it is necessary to control systematically in blood concentration of ions of sodium, magnesium (as electrolytic disturbances can develop), glucose, uric acid and residual nitrogen, level рН blood.

Careful control of maintenance of potassium ions and creatinine in blood is shown to the patients accepting against the background of Indapamid's use cardiac glycosides, purgatives, to patients with a hyper aldosteronism, and also elderly people.

The first measurement of concentration of potassium ions in blood should be performed within the first week of treatment.

The most careful control is shown to patients with cirrhosis (especially with hypostases or with ascites) because of risk of development of the metabolic alkalosis worsening the course of hepatic encephalopathy with coronary heart disease, chronic heart failure, and also the patient of advanced age. To group of the increased risk patients with lengthening of an interval With> T on the electrocardiogram also treat (inborn or developed against the background of any pathological process). The hypercalcemia against the background of Indapamid's reception can be a consequence of earlier not diagnosed hyperparathyreosis.

At some patients the combination of an indapamiad with kaliysberegayushchy diuretics can be effective, however at the same time the possibility of development hypo - or hyperpotassemias, especially at patients with a diabetes mellitus and a renal failure is not excluded.

At patients with a diabetes mellitus it is necessary to control concentration of glucose in blood, especially in the presence of a hypopotassemia.

Considerable dehydration can against the background of therapy by Indapamid can lead to development of an acute renal failure (owing to reduction in the rate of glomerular filtering). Patients need to compensate OTsK in an initiation of treatment and to carefully control function of kidneys.

Derivatives of sulfonamides can aggravate a current of a system lupus erythematosus (it is necessary to consider at Indapamid's appointment).

Indapamid can yield positive takes when carrying out a drug test.

Efficiency and safety at children up to 18 years is not established.

Influence on ability to driving of motor transport and to control of mechanisms
In an initiation of treatment Indapamid it is necessary to refrain from driving of motor transport and occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions as development of dizziness is possible.

Side effects:

From cardiovascular system: orthostatic hypotension, arrhythmia, heartbeat, changes on the ECG characteristic of a hypopotassemia.

From a digestive tract: a loss of appetite, dryness in a mouth, nausea, vomiting, an abdominal pain, diarrhea or a lock; seldom — pancreatitis. At patients with a liver failure development of hepatic encephalopathy is possible.

From the central nervous system: dizziness, headache, hyperexcitability, sleep disorders, depression, increased fatigue, indisposition, adynamy, tension, irritability, uneasiness, paresthesias, spasms of muscles.

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

From urinogenital system: infections, nocturia, polyuria.

From bodies of a hemopoiesis: hemorrhagic vasculitis, thrombocytopenia, leukopenia, agranulocytosis, marrow aplasia, hemolitic anemia.

Allergic reactions: skin itch, spotty and papular rash, small tortoiseshell. From laboratory indicators: hypercalcemia, hyperuricemia, hypochloraemia, hyponatremia, hyperglycemia, hypopotassemia, increase in concentration of an urea nitrogen of blood, giperkreatininemiya, glucosuria. Other: aggravation of a system lupus erythematosus.

Interaction with other medicines:

At simultaneous use индапамид leads to increase in concentration of ions of lithium in a blood plasma (due to decrease in its removal by kidneys).

When using along with iodinated contrast means in high doses Indapamid increases risk of development of renal failures (due to decrease in the volume of the circulating blood (VCB)). Before use of iodinated contrast agents by the patient it is necessary to make correction of OTsK.

Indapamid reduces effect of indirect anticoagulants (derivative coumarin or an indandion) due to increase in concentration of blood-coagulation factors (as a result of reduction of OTsK). Indapamid strengthens action of not depolarizing muscle relaxants. The risk of development of a hypopotassemia increases at simultaneous use of an indapamid with diuretics ("loopback", thiazide), cardiac glycosides, glucocorticosteroids, mineralokortikoida, tetrakozaktidy, Amphotericinum In (intravenously), purgatives.

At a concomitant use of an indapamid with cardiac glycosides the probability of development of digitalis intoxication increases; with calcium drugs — hypercalcemias; with Metforminum — aggravation of lactic acidosis.

Astemizol, erythromycin (intravenously), pentamidine, сультоприд, терфенадин, Vincaminum, antiarrhytmic medicines 1A of a class (quinidine, Disopyramidum) and the III class (Amiodaronum, a bretylium tosylate) can increase risk of development of arrhythmia like "pirouette" due to lengthening of an interval FROM.

Non-steroidal anti-inflammatory drugs, glucocorticosteroids, тетракозактид, adrenostimulyator reduce hypotensive effect of an indapamid, Baclofenum — strengthens.

Inhibitors of an angiotensin-converting enzyme at simultaneous use with indapamidy increase risk of development of orthostatic hypotension and/or acute renal failure (especially in the presence of a renal artery stenosis).

Imipraminovy (tricyclic) antidepressants and antipsychotic means (neuroleptics) strengthen hypotensive action of an indapamid and increase probability of developing of orthostatic hypotension. Cyclosporine increases risk of development of a giperkreatininemiya.

Contraindications:

- hypersensitivity to an indapamid, other derivatives of sulfonamide or to other components of drug;
- renal failure (anury stage);
- hepatic encephalopathy or liver failure of heavy degree;
- hypopotassemia;
- lactose intolerance, deficit of lactase or glyukozo-galaktazny malabsorption;
- age up to 18 years (efficiency and safety are not established);
- pregnancy;
- lactation period.

With care
Renal failures and/or a liver, a diabetes mellitus in a stage of a decompensation, disturbance of water and electrolytic balance, the hyperuricemia (which is especially followed by gout and an uratny nephrolithiasis), a hyperparathyreosis; to patients with the extended interval (^Т on an ECG or receiving therapy as a result of which lengthening of an interval is possible With> T (астемизол, erythromycin (intravenously), pentamidine, сультоприд, терфенадин, Vincaminum, antiarrhytmic medicines 1A of a class (quinidine, Disopyramidum) and the III class (Amiodaronum, a bretylium tosylate).

Pregnancy and period of a lactation
Reception of an indapamid at pregnancy is not recommended. Use of drug can become the reason of fetoplacental ischemia with risk of delay of fetation. It is not recommended to use drug in the period of a lactation (индапамид gets into breast milk).

Overdose:

Symptoms: are connected with disturbance of water and electrolytic balance - nausea, vomiting, the expressed lowering of arterial pressure, dizziness, spasms, drowsiness, confusion of consciousness, a polyuria or the oliguria giving anuries (owing to a hypovolemia).

Treatment: a gastric lavage, purpose of absorbent carbon with the subsequent recovery of water and electrolytic balance, symptomatic therapy. There is no specific antidote.

Storage conditions:

List B. In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity: 3 years. Not to apply after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated on 2,5 mg. On 10 or 30 tablets in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished. On 1, 2, 3, 4 blister strip packagings on 10 tablets or on 1, 2, 3 blister strip packagings on 30 tablets together with the application instruction place in a pack from a cardboard for a retail container.