Indapamid

General characteristics. Structure:

Active ingredient: 2,5 mg of an indapamid.

Excipients – microcrystallic cellulose, a pharmatoza of dcl15 (lactose for direct pressing), sodium glikolit starch, magnesium stearate, talc, a gidroksipropilmetiltsellyuloz of 15 cps, titanium dioxide, propylene glycol, dye Orange yellow (Е 110).

Pharmacological properties:

Pharmacodynamics. Antihypertensive (diuretic, vazodilatator). On pharmacological properties it is close to thiazide diuretics (disturbance of a reabsorption of Na + in a cortical segment of a Henle's loop). Increases allocation with urine of ions Na+, Cl-and to a lesser extent ions of K+ and Mg2+. 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.

The hypotensive effect develops by the end of the first week, remains during 24 h against the background of a single dose.

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. An elimination half-life - 18 h, communication with proteins of a blood plasma – 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.

Indications to use:

Arterial hypertension.

Route of administration and doses:

Pill is taken inside, without chewing. A daily dose of drug – 1 tablet (2,5 mg) a day (morning). If in 4-8 weeks of treatment do not reach desirable therapeutic effect, it is not recommended to raise a dose of drug (increase in risk of side effects without strengthening of anti-hypertensive effect). Instead it is recommended to include other anti-hypertensive drug which is not diuretic in the scheme of drug treatment.

In cases when treatment needs to be begun with reception of two drugs, Indapamid's dose remains equal 2,5 mg in the morning once in days.

Features of use:

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 shown.

Against the background of reception of an indapamid it is necessary to control systematically concentration of ions of K+, Na+, Mg2 + in a blood plasma (electrolytic disturbances can develop), pH, concentration of glucose, uric acid and residual nitrogen.

The most careful control is shown at patients with cirrhosis (especially with hypostases or ascites - risk of development of the metabolic alkalosis strengthening displays of hepatic encephalopathy), coronary heart disease, heart failure, and also at elderly people. 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 concentration of K+ in blood should be taken within the first 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 water 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 of an angiotensin-converting enzyme.

Derivatives of sulfonamides can aggravate a current of a system lupus erythematosus (it must be kept in mind at purpose of an indapamid).

Efficiency and safety at children is not established.

Side effects:

From digestive tract: nausea/anorexia, dryness in a mouth, a gastralgia, vomiting, diarrhea, a lock are possible.

From a nervous system - an adynamy, nervousness, a headache, dizziness, drowsiness, вертиго, sleeplessness, a depression; seldom – increased fatigue, the general weakness, an indisposition, a spasm of muscles, tension, irritability, alarm.

From sense bodys – konjyuktivit, a vision disorder.

From respiratory system – cough, pharyngitis, sinusitis, it is rare – rhinitis.

From cardiovascular system - orthostatic hypotension, changes on the electrocardiogram (hypopotassemia), arrhythmia, heartbeat.

From an urinary system – frequent infections, a nocturia, a polyuria.

Allergic reactions - rash, urticaria, an itch, a hemorrhagic vasculitis.

Laboratory indicators – a hyperuricemia, a hyperglycemia, a hypopotassemia, a hypochloraemia, a hyponatremia, a hypercalcemia, increase in an urea nitrogen blood plasma, a giperkreatininemiya, a glucosuria.

Others – a grippopodobny syndrome, thorax pain, a dorsodynia, infections, decrease in a potentiality, decrease a libido, a rhinorrhea, perspiration, decrease in body weight, a pricking in extremities, pancreatitis, an aggravation of a system lupus erythematosus.

Interaction with other medicines:

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

At a concomitant use with cardiac glycosides the probability of development of digitalis intoxication increases; with the drugs Ca2 + - hypercalcemias; with Metforminum – aggravation of lactic acidosis is possible.

Increases concentration of ions of Li + in a blood plasma (decrease in removal with urine), lithium has nephrotoxic effect.

Astemizol, erythromycin in/in, pentamidine, сультоприд, терфенадин, Vincaminum, the antiarrhytmic drugs Ia of a class (quinidine, Disopyramidum) and the III class (Amiodaronum, бретилиум, соталол) can lead to development of arrhythmia as "torsades de pointes".

Non-steroidal anti-inflammatory drugs, glucocorticosteroid means, тетракозактид, sympathomimetics reduce hypotensive effect, Baclofenum - strengthens.

The combination with kaliysberegayushchy diuretics can be effective at some category of patients, however, at the same time the possibility of development hypo - or 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).

Increases risk of development of renal failures when using iodinated contrast means in high doses (organism dehydration). Before use of iodinated contrast agents by the patient it is necessary to recover liquid loss.

Imipraminovy (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 drug and other derivatives of sulfonamide, an anury, the hypopotassemia expressed hepatic (including with encephalopathy) and/or a renal failure, pregnancy, the lactation period, age up to 18 years (efficiency and safety are not established); a concomitant use of the drugs extending QT interval.

With care appoint at a diabetes mellitus in a stage of a decompensation, a hyperuricemia (especially, the followed gout and an uratny nephrolithiasis).

Overdose:

Symptoms: nausea, vomiting, weakness, dysfunction 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 water and electrolytic balance, symptomatic therapy. There is no specific antidote.

Storage conditions:

List B. To store in the place protected from moisture and light, 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 date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging. 3 blister strip packagings with a leaf insert in a cardboard pack.

On 30 tablets in bank polymeric. 1 bank with a leaf insert in a cardboard pack.