Indamid

General characteristics. Structure:

Active agent - индапамид (in terms of 100% substance) 2,5 mg.

Excipients: lactoses monohydrate, cellulose microcrystallic, polyvinylpirrolidone, sodium of starch glikolit, silicon dioxide colloid, calcium stearate.

Structure of a cover: gidroksipropilmetiltsellyuloza, polysorbate-80, titanium dioxide, liquid paraffin.

Pharmacological properties:

Pharmacokinetics. After intake it is quickly and completely soaked up from digestive tract. Bioavailability high - 93%. Meal slows down absorption speed a little, but does not influence amount of the soaked-up substance. The maximum concentration in a blood plasma - 1 - 2 h after intake. At repeated methods of fluctuation of concentration of drug in a blood plasma in an interval between receptions of two doses decrease. Equilibrium concentration is established in 7 days of regular reception. Elimination half-life till 18 o'clock. Communication with blood proteins - 79%. Contacts also elastin of unstriated muscles of a vascular wall. Has the high volume of distribution, passes through gistogematichesky barriers (including placental), gets into breast milk. It is metabolized in a liver. Kidneys remove 60 - 80% in the form of metabolites (in not changed look about 5% are removed), through intestines - 20%. At patients with a renal failure the pharmacokinetics does not change. Does not kumulirut.

Pharmacodynamics. Indamid - tiazidopodobny diuretic, anti-hypertensive means. Causes the moderate saluretichesky and diuretic effect connected with inhibition of a reabsorption of ions of sodium, chlorine, hydrogen and to a lesser extent, potassium ions in proximal tubules and in a cortical segment of a distal tubule of nephron.

Indamid has anti-hypertensive effect which is shown only at initially raised ABP. The hypotensive effect develops by the end of the first week, remains during 24 h against the background of a single dose.

Having ability to selectively block "slow" calcium channels, increases elasticity of walls of arteries and reduces the general peripheric vascular resistance. Promotes reduction of a hypertrophy of a left ventricle of heart. Does not influence the maintenance of lipids in a blood plasma (TG, lipoproteins of low density, lipoproteins of high density); does not influence carbohydrate metabolism (including at patients with the accompanying diabetes mellitus). Reduces sensitivity of a vascular wall to noradrenaline and angiotensin II, stimulates E2 prostaglandin synthesis, reduces products of free and stable oxygen radicals.

Indications to use:

- arterial hypertension

Route of administration and doses:

Inside, in the morning, to food on 2,5 mg (1 tablet) of 1 times a day.

The maximum daily dose - 10 mg a day in 2 receptions (in the first half of day). The maximum anti-hypertensive action develops in 7-10 days after the beginning of therapy.

Duration of a course of treatment is determined by the doctor.

Features of use:

With care apply at patients with a diabetes mellitus (control of level of glucose, especially in the presence of a hypopotassemia), at patients with instructions in the anamnesis on allergic reactions to derivatives of sulfonamides, cirrhosis (especially with hypostases or ascites – risk of development of a metabolic alkalosis is necessary), coronary heart disease, heart failure, and also at elderly people.

In the course of treatment it is necessary to control the level of electrolytes in a blood plasma (potassium, sodium, calcium).

At the patients accepting cardiac glycosides, laxative drugs against the background of a hyper aldosteronism, and also at elderly people regular control of maintenance of ions of K+ and creatinine is necessary.

Drug is not recommended to use for patients aged up to 18 years because its efficiency and safety are not established.

At administration of drug there can be dizziness and drowsiness that can reduce concentration of attention. It is not necessary to manage vehicles and to service moving mechanisms.

Side effects:

Often:

- nausea, anorexia, dryness in a mouth, feeling of discomfort or pain in epigastriums, vomiting, diarrhea, a lock.

Seldom:

- increased fatigue, general weakness, indisposition, spasm of muscles, tension, irritability, feeling of alarm;

- adynamy, nervousness, headache, dizziness, drowsiness, sleeplessness, depression;

- conjunctivitis, vision disorder;

- cough, pharyngitis, sinusitis;

- orthostatic hypotension, changes on the electrocardiogram (hypopotassemia), arrhythmia, heartbeat;

- nocturia, polyuria;

- rash, urticaria, itch, hemorrhagic vasculitis;

- thorax pain, dorsodynia, pricking in extremities;

- decrease in a potentiality, decrease in a libido;

- rhinorrhea, perspiration, decrease in body weight;

- pancreatitis;

- a hyperuricemia, a hypopotassemia, a hypochloraemia, a hyponatremia (at prolonged use or reception in high doses);

- a hypercalcuria, increase in an urea nitrogen blood plasma, a giperkreatininemiya.

Interaction with other medicines:

At simultaneous use of an indamid with drugs of lithium increase in concentration of lithium in a blood plasma is possible. With non-steroidal anti-inflammatory drugs (for system use) – decrease in hypotensive action of an indapamid is possible.

Imipraminovy (tricyclic) antidepressants and antipsychotic drugs strengthen hypotensive effect of drug and the risk of development of orthostatic hypotension increases.

At a concomitant use of an indamid with:

- saluretics, glyuko-and mineralokortikoidam, tetrakozaktidy, Amphotericinum In (in/in), purgatives the risk of development of a hypopotassemia increases;

- with cardiac glycosides - development of digitalis intoxication;

- with drugs of Sa - development of a hypercalcemia;

- with Metforminum - aggravation of lactic acidosis;

- with astemizoly, erythromycin, pentamidine, sultopridy, terfenadiny, Vincaminum, antiarrhytmic drugs 1a of a class (quinidine, Disopyramidum) and the III class (Amiodaronum, бретилиум, соталол) - development of arrhythmia as "torsades de pointes";

- with glucocorticosteroid means, tetrakozaktidy, sympathomimetics - decrease in hypotensive effect, and with Baclofenum – strengthening of its action is possible;

- with inhibitors of an angiotensin-converting enzyme - increase in risk of development of arterial hypotension and/or acute liver failure (especially at the available renal artery stenosis).

Indamid reduces effect of indirect anticoagulants (derivative coumarin or an indandion) owing to increase in concentration of factors of coagulation as a result of reduction of volume of the circulating blood and increase in their products liver (dose adjustment can be required).

Contraindications:

- hypersensitivity to an indapamid and other derivatives of sulfonamide;

- acute disorder of cerebral circulation;

- the expressed renal failures (anury);

- the expressed abnormal liver functions;

- heavy diabetes mellitus;

- heavy gout;

- hypopotassemia;

- pregnancy, period of a lactation (breastfeeding);

- children's and teenage age up to 18 years.

Overdose:

Symptoms: nausea, vomiting, weakness, dysfunctions of digestive tract, water and electrolytic disturbances, in certain cases – an excessive lowering of arterial pressure, respiratory depression. At patients with cirrhosis development of a hepatic coma is possible.

Treatment: gastric lavage, correction of introduction and electrolytic balance, symptomatic therapy. There is no specific antidote.

Storage conditions:

To store in the dry, protected from light place, at a temperature not above 30 °C. To store in the place, unavailable to children!

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging.

On 3 planimetric packagings together with the approved instruction on a medical use in the state and Russian languages place in a pack from a cardboard.

It is allowed to place planimetric packagings in boxes from a cardboard. Put the approved instructions on a medical use in each box in the state and Russian languages. The number of instructions invests in group packaging on number of packagings.