Indapamid

General characteristics. Structure:

Active ingredient: 2,5 mg of an indapamid.

Excipients: sugar milk (lactose), starch corn, polyvinylpirrolidone (povidone), sodium lauryl sulfate, calcium октадеканоат (stearate); capsule No. 3: gelatin, water, sodium lauryl sulfate, нипагин, нипазол; dyes: a lid — titanium dioxide (Е 171), an azoruby (Е 122), yellow "sunset" (Е 110); the case — titanium dioxide (Е 171).

Diuretic drug of hypotensive action.

Pharmacological properties:

Pharmacodynamics. An antihypertensive, tiazidopodobny diuretic with moderated on force and action, long on duration, derivative benzamides. Reduces a tone of smooth muscles of arteries, reduces the general peripheric resistance of vessels. Has moderate saluretichesky and diuretic effects which are connected with blockade of a reabsorption of ions of sodium, chlorine, hydrogen, and to a lesser extent potassium ions in proximal tubules and a cortical segment of a distal tubule of nephron. Vasodilating effects and decrease in the general peripheric resistance of vessels have the following mechanisms in the basis: decrease in reactivity of a vascular wall to noradrenaline to angiotensin II; increase in synthesis of prostaglandins having vasodilating activity; oppression of current of calcium in smooth muscle cells of vessels. Promotes reduction of a hypertrophy of a left ventricle of heart. In therapeutic doses does not influence lipidic and carbohydrate exchanges (including at patients with the accompanying diabetes mellitus).

The anti-hypertensive effect develops at the end of the first / the beginning of the second week at constant administration of drug and remains within 24 hours against the background of a single dose.

Pharmacokinetics. After intake it is quickly and completely soaked up from digestive tract. The Bidostupnost — high (93%). Meal slows down speed a little, but does not influence completeness of absorption. The maximum concentration in blood is reached in 1-2 hours. Equilibrium concentration is reached in 7 days of regular reception.

Drug for 70-80% contacts proteins of a blood plasma. Has the high volume of distribution, passes through gistogematichesky (including placental) barriers, gets into breast milk. It is metabolized in a liver. The elimination half-life of an indapamid averages 14-18 hours. It is brought out of an organism by kidneys (to 80%) preferential in the form of metabolites, through intestines — 20%. At patients with a renal failure the pharmacokinetics does not change. Does not kumulirut.

Indications to use:

Arterial hypertension.

Route of administration and doses:

Inside, irrespective of meal, washing down with enough liquid. It is preferable to accept drug in the morning. The dose makes 2.5 mg (1 capsule) a day.

If in 4-8 weeks of treatment  the desirable therapeutic effect is not reached, the dose of drug is not recommended to be raised (the risk of emergence of side effects without strengthening of anti-hypertensive effect increases).  Instead it is recommended to include other anti-hypertensive drug which is not diuretic in the scheme of drug treatment.

In case of an initiation of treatment two anti-hypertensive drugs, the dose remains to Indapamida-Verta equal 2.5 mg once in the morning.

Features of use:

At very prolonged use or at reception of an indapamid in big dosages electrolytic disturbances, such as a hyponatremia, a hypopotassemia, a gipokhloremichesky alkalosis can develop. These disturbances are more often observed at patients with chronic heart failure (II-IV ф.к. on NYHA), diseases of kidneys and cirrhosis, at vomiting and diarrhea, and also at the persons which are on an electrolyte-deficient diet. Co-administration of an indapamid with cardiac glycosides and corticosteroids increases risk of emergence of a hypopotassemia. Besides, release of magnesium with urine can increase that can lead to a hypomagnesiemia. Emergence of orthostatic hypotension which can be provoked by alcohol intake, barbiturates, narcotic drugs and a concomitant use of other antihypertensives is possible. At the patients accepting cardiac glycosides, purgatives against the background of a hyper aldosteronism, and also at elderly people careful control of content of potassium and creatinine is shown.

The most careful control is shown at patients with cirrhosis, coronary heart disease, chronic heart failure. Patients with the increased QT interval on the electrocardiogram also treat group of the increased risk (inborn or developed against the background of any pathological process).

The first measurement of potassium concentration in blood should be taken within 1 week of treatment.
The hypercalcemia against the background of reception of an indapamid can be a consequence of earlier not diagnosed hyperparathyreosis.

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

Considerable dehydration can lead to development of an acute renal failure (decrease in glomerular filtering). Patients need to offset loss of liquid and in an initiation of treatment carefully to control function of kidneys.

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

It is necessary for patients with arterial hypertension and a hyponatremia (owing to reception of diuretics) in 3 days prior to reception of inhibitors of an angiotensin-converting enzyme to stop reception of diuretics (if necessary reception of diuretics can be resumed a bit later), or by it appoint initial low doses of inhibitors enzyme angiotensin-prevrashchyushchego.

Side effects:

- From a metabolism: a hypopotassemia, a hyponatremia, a gipokhloremichesky alkalosis, increase in an urea nitrogen in a blood plasma, a giperkreatininemiya, a glucosuria, a hypercalcemia
- From digestive tract: a lock or diarrhea, feeling of discomfort in a stomach, nausea, vomiting, anorexia, dryness in a mouth
- From the central nervous system: dizziness, nervousness, headache, drowsiness, increased fatigue, general weakness, sleeplessness, depression, indisposition, spasm of muscles, tension, irritability, alarm
- From sense bodys: conjunctivitis, vision disorder
- From respiratory system: rhinitis, cough, pharyngitis, sinusitis
- From cardiovascular system: orthostatic hypotension, arrhythmia, heartbeat, changes of the electrocardiogram characteristic of a hypopotassemia
- From an urinary system: nocturia, polyuria, increase in frequency of development of infections
- Allergic reactions: skin rash, itch, small tortoiseshell, hemorrhagic vasculitis
- Other: grippopodobny syndrome, thorax pain, dorsodynia, decrease in a libido and potentiality, rhinorrhea, perspiration, decrease in body weight, paresthesia, pancreatitis, aggravation of a system lupus erythematosus.

Interaction with other medicines:

At simultaneous use of an indapamid with drugs of lithium increase in concentration of lithium in a blood plasma is possible.

Astemizol, erythromycin (at in introduction), pentamidine, сультоприд, Vincaminum, the antiarrhytmic drugs Ia (quinidine, Disopyramidum) and the III class (Amiodaronum, бретилиум, соталол) increase probability of emergence of disturbances of a cordial rhythm as torsades de pointes (ventricular tachycardia like "pirouette").

Non-steroidal anti-inflammatory drugs, glucocorticosteroids, тетракоактид, sympathomimetics reduce hypotensive action, Baclofenum — increases.

Saluretics, cardiac glycosides, glyuko-and mineralokortikosteroida, тетракозактид, Amphotericinum In (at in introduction), purgatives increase risk of development of a hypopotassemia.

At simultaneous use with cardiac glycosides the probability of development of digitalis intoxication, with calcium drugs — hypercalcemias, with Metforminum — possibly aggravation of lactic acidosis increases.

The combination with kaliysberegayushchy diuretics can be effective at some category of patients, however, at the same time the probability of development hypo - and hyperpotassemias, especially at patients with a diabetes mellitus and a renal failure completely is not excluded.

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

Contrast yodosoderzhashchy means in high doses increase risk of development of renal failures (organism dehydration). Before use of contrast yodosoderzhashchy means by the patient it is necessary to recover liquid loss.

Tricyclic  antidepressants and antipsychotic drugs strengthen hypotensive action and increase risk of development of orthostatic hypotension.

Cyclosporine increases risk of development of a giperkreatininemiya.

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).

Strengthens the neuromuscular transmission blockade developing under the influence of not depolarizing muscle relaxants.

Contraindications:

 Hypersensitivity to an indapamid, other derivatives of sulfonamide or other components of drug, a decompensation of function of kidneys (anury) and/or a liver (including with encephalopathy), a hypopotassemia, a concomitant use of the drugs extending QT interval, pregnancy, the lactation period, age up to 18 years (efficiency and safety are not established).

With care: a diabetes mellitus in a decompensation stage, the giperurekimiya (which is especially followed by gout and an uratny nephrolithiasis).

Overdose:

- Symptoms: nausea, vomiting, weakness, dysfunction of digestive tract, water and electrolytic disturbances, lowering of arterial pressure, dizziness, drowsiness, confusion of consciousness, respiratory depression; at the patient with an abnormal liver function development of a hepatic coma is possible.

- Treatment: a gastric lavage and/or purpose of absorbent carbon with the subsequent recovery of normal 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: 2 years. Not to use after the term specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Capsules on 2,5 mg. On 10 capsules in a blister strip packaging or on 30 capsules in bank of polymeric. 3 blister strip packagings or one bank together with the application instruction in a pack from a cardboard.