Акрипамид®

General characteristics. Structure:

Active ingredient: 2,5 mg of an indapamid.

Excipients: lactose (sugar milk), potato starch, povidone, sodium lauryl sulfate, talc, magnesium stearate.

Structure of a cover: gipromelloz (gidroksipropilmetiltsellyuloz), macrogoal (polyethyleneglycol 6000), glitse-rol (glycerin), titanium dioxide, talc.

Antihypertensive (diuretic, vazodilatator).

Pharmacological properties:

Pharmacodynamics. On pharmacological properties it is close to thiazide diuretics (disturbance of a reabsorption of ions of sodium in a cortical segment of a Henle's loop). Increases removal with urine of ions of sodium and chlorine and to a lesser extent potassium ions and magnesium. 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 plasma (triglycerides, lipoproteins of high and low 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 synthesis of PgE2 and PgI2 prostacyclin, reduces products of free and stable oxygen radicals. At appointment in high doses does not influence degree of a lowering of arterial pressure, despite increase in a diuresis. After multiple dose the therapeutic effect is noted in 1-2 weeks, reaches a maximum to 8-12 weeks and remains up to 8 weeks; after reception of a single dose the maximum effect is noted in 24 h.

Pharmacokinetics. After intake it is quickly and completely soaked up from digestive tract. Bioavailability — high (93%). Meal slows down speed a little, but does not influence final amount of the soaked-up drug. The maximum concentration in blood is reached in 1-2 hours. The maximum concentration after intake in a dose of 5 mg makes 260 ¡ú/l. At repeated methods of fluctuation of concentration of drug in plasma in an interval between receptions of two doses decrease. Equilibrium concentration is reached in 7 days of regular reception. Drug for 70-80% contacts proteins of a blood plasma. Contacts also elastin of unstriated muscles of a vascular wall. 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 indapamin averages 14 hours. It is brought out of an organism by kidneys (to 70%) preferential in the form of metabolites, through intestines — 20-23%. 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 daily dose makes 1 tablet (2,5 mg). If in 4-8 weeks of therapy 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 case of an initiation of treatment two anti-hypertensive means, Akripamid's dose remains equal 2,5 mg once in the morning.

Features of use:

At the patients accepting cardiac glycosides, laxative medicines against the background of a hyper aldosteronism, and also at elderly people careful control of maintenance of potassium ions and creatinine is shown.

Against the background of reception of a praparat of Akripamid® it is necessary to control systematically concentration of potassium ions, sodium, magnesium in plasma (electrolytic disturbances can develop), рН, concentration of glucose, uric acid and residual nitrogen. The most careful control is shown at patients with cirrhosis (especially with hypostases or ascites — the risk of development of the metabolic alkalosis strengthening displays of hepatic encephalopathy is high), by coronary heart disease, chronic heart failure, and also at elderly people. Patients with the increased Q-T interval on an ECG also treat group of the increased risk (inborn or developed against the background of any pathological process).

The first measurement of concentration of potassium ions in blood should be taken within 1 week of treatment.

The hypercalcemia against the background of administration of drug of Akripamid® 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.

Акрипамид® 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 the angiotensin-converting enzyme (ACE) to stop reception of diuretics (if necessary reception of diuretics can be resumed a bit later) or by it appoint initial low doses of APF inhibitors.

Can aggravate a current of a system lupus erythematosus.

Efficiency and safety at children are not established

Side effects:

From cardiovascular system: orthostatic hypotension, arrhythmia, heartbeat.

From a nervous system: headache, dizziness, nervousness, adynamy, drowsiness, вертиго, sleeplessness, depression, increased fatigue, indisposition, spasm of muscles, tension, irritability, uneasiness.

From the alimentary system: a lock or diarrhea, dyspepsia (including nausea, vomiting), anorexia, dryness in a mouth, abdominal pain, hepatic encephalopathy (against the background of a liver failure), pancreatitis.

From urinogenital system: nocturia, polyuria.  

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

Allergic reactions: skin itch, spotty and papular rash, small tortoiseshell, hemorrhagic vasculitis.

From bodies of a hemopoiesis: thrombocytopenia, leukopenia, agranulocytosis, aplasia of a bone brain, hemolitic anemia.

Laboratory indicators: hypercalcemia, hyperuricemia, hypochloraemia, hypopotassemia, hyponatremia, hyperglycemia, increase in an urea nitrogen of blood, giperkreatininemiya, glucosuria.

Others: aggravation of a system lupus erythematosus.

Interaction with other medicines:

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

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

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.

Saluretics (loopback, thiazide), cardiac glycosides, glucocorticosteroids and mineralokortikosteroida, тетракозактид, Amphotericinum In (at intravenous administration), laxative medicines increase risk of development of a hypopotassemia.

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

Astemizol, erythromycin (at intravenous administration), pentamidine, сультоприд, терфенадин, Vincaminum, antiarrhytmic Ia medicines of a class (quinidine, Disopyramidum) and the III class (Amiodaronum, a bretylium tosylate, соталол) can lead to development of arrhythmia in the pirouette type due to sinergidny influence (lengthening) on Q-T interval duration.

Non-steroidal anti-inflammatory drugs, glucocorticosteroids, тетракозактид, adrenostimulya-Torahs 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.

APF inhibitors increase risk of development of arterial hypertension and/or acute renal failure (especially at the available renal artery stenosis).

Imipraminovy (tricyclic) antidepressants and antipsychotic medicines (neuroleptics) strengthen hypotensive action and increase risk of development of orthostatic hypotension.

Cyclosporine increases risk of development of a giperkreatininemiya.

Contraindications:

Hypersensitivity to drug and other derivatives of sulfonamide, an anury, the expressed liver failure (including with encephalopathy) and/or a renal failure, a hypopotassemia, a concomitant use of the drugs extending QT interval, pregnancy, the lactation period, children's age up to 18 years (efficiency and safety are not established). Lactose intolerance, galactosemia, syndrome of disturbance of absorption of a glucose/galactose.

With care. Disturbances of water and electrolytic exchange, a liver and/or renal failure, lengthening of an interval of QT, the hyperuricemia (which is especially shown gout or an uratny nefrourolitiaz), a hyperparathyreosis.

Overdose:

Symptoms: nausea, vomiting, weakness, arterial hypotension, dizziness, drowsiness, confusion of consciousness, respiratory depression, dysfunction of digestive tract; at patients with an abnormal liver function development of a hepatic coma is possible.

Treatment: gastric lavage and/or purpose of absorbent carbon, correction 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. Not to apply after a period of validity. A period of validity - 4 years.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated, 2,5 mg. On 10 tablets in a blister strip packaging. 1, 2 or 3 blister strip packagings together with the application instruction place in a pack from a cardboard.