Sonizin

General characteristics. Structure:

Active ingredient: One capsule contains 0,400 mg of a tamsulozin of a hydrochloride.

Excipients:
Capsule contents: calcium stearate; triethyl citrate; talc; the copolymer of methacrylic acid and ethyl acrylate (1:1) containing also polysorbate 80 and sodium lauryl sulfate; cellulose microcrystallic.
Solid gelatin capsule:
Upper part:
ferrous oxide yellow (C.I. 77492 E172); titanium dioxide (C.I. 77891 E171); ferrous oxide black (C.I. 77499 E172); ferrous oxide red (C.I. 77491 E172); gelatin.
Lower part:
ferrous oxide red (C.I. 77491 E172); ferrous oxide black (C.I. 77499 E172); ferrous oxide yellow (C.I. 77492 E172); titanium dioxide (C.I. 77891 E171); gelatin.

Pharmacological properties:

Pharmacodynamics. Tamsulozin selectively and competitively blocks postsynaptic α1A-адренорецепторы, being in smooth muscles of a prostate, a neck of a bladder and a prostatic part of an urethra, and also α1D-адренорецепторы, preferential being in a bladder body. It leads to decrease in a tone of smooth muscles of a prostate, neck of a bladder and a prostatic part of an urethra and improvement of function of a detruzor. At the expense of it the symptoms of obstruction and irritation connected with a benign hyperplasia of a prostate decrease. As a rule, the therapeutic effect develops in 2 weeks after the beginning of administration of drug though at a number of patients reduction of expressiveness of symptoms is noted after reception of the first dose. Ability of a tamsulozin to influence on α1А-адренорецепторы by 20 times surpasses its ability to interact with α1В-адренорецепторами which are located in unstriated muscles of vessels. Thanks to such high selectivity drug does not cause any clinically significant decrease in the system arterial pressure (AP) both in patients with arterial hypertension, and in patients with the normal initial ABP.

Pharmacokinetics. Absorption. After intake тамсулозин it is quickly and almost completely absorbed from digestive tract. Bioavailability of drug - about 100%. After a single dose of drug inside in a dose of 400 mkg of Cmax of active agent in plasma it is reached in 6 h.

Distribution. In an equilibrium state (in 5 days of course reception) Cmax values of active agent in a blood plasma are 60-70% higher, than Cmax after a single dose of drug. Linkng with proteins of plasma - 99%. Tamsulozin has the insignificant volume of distribution (about 0.2 l/kg).

Metabolism. Tamsulozin is not exposed to effect of "the first passing" and biotransformirutsya slowly in a liver with formation pharmacological of the active metabolites keeping high selectivity to α1А-адренорецепторам. The most part of active agent is present at blood in not changed look.

Removal. Tamsulozin is brought by kidneys, 9% of a dose are removed in not changed look. T1/2 of a tamsulozin at a single dose of-10 h, after multiple dose of-13 h, final time of semi-removal - 22 h.

Indications to use:

Treatment of the dysuric frustration caused by a benign hyperplasia of a prostate.

Route of administration and doses:

Inside, after food, on 1 capsule a day, at the same time days, washing down with enough water. It is not necessary neither to break the capsule on a part, nor to chew since at the same time the prolonged release of active ingredient is broken.

Features of use:

It is similar to others α1-адреноблокаторам тамсулозин can cause decrease in the ABP, in rare instances causing a syncope. At the first symptoms of orthostatic hypotension (dizziness, weakness) it is necessary to seat or lay the patient before disappearance of symptoms.

Tamsuloziny preliminary survey of the patient for the purpose of an exception of any other disease proceeding with the same symptoms as well as a benign hyperplasia of a prostate has to precede treatment. Rectal manual inspection of a prostate and measurement of level of a specific antigen of a prostate (PSA) which later, during treatment regularly repeat have to precede treatment preliminary.

During treatment it is necessary to abstain from occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Seldom - a headache, dizziness, an adynamy, sleep disorders (drowsiness or sleeplessness), a retrograde ejaculation, decrease a libido, a dorsodynia, rhinitis; in isolated cases - orthostatic hypotension, tachycardia, heartbeat, thorax pain.

From digestive organs: in rare instances - nausea, vomiting, locks or diarrhea. In extremely exceptional cases of reaction of hypersensitivity - skin rash, an itch, a Quincke's disease.

Interaction with other medicines:

Cimetidinum increases concentration of a tamsulozin in plasma, furosemide reduces (essential clinical value has no, change of a dosage is not required).

Diclofenac and indirect anticoagulants strengthen removal of a tamsulozin.

Diazepam, propranolol, трихлорметиазид, хлормадинон, amitriptyline, diclofenac, glibenclamide, симвастатин and warfarin do not change free fraction of a tamsulozin in plasma of the person of in vitro. In turn тамсулозин does not change free fractions of diazepam, propranolol, a trikhlormetiazid and hlormadinon.

In the researches in vitro interaction at the level of hepatic metabolism with amitriptilipy, salbutamol, glibenclamide and finasteridy was not revealed.

Other alfa1-adrenoblockers, acetylcholinesterase inhibitors, alprostadit, anesthetics, diuretics, a levodopa, antidepressants, beta adrenoblockers, blockers of "slow" calcium channels, nitrates and ethanol can increase expressiveness of hypotensive effect of a tamsulozin.

Contraindications:

Hypersensitivity to a tamsulozin to a hydrochloride or any other component of drug.

With care: a chronic renal failure (decrease in clearance of creatinine is lower than 10 ml/min.), arterial hypotension (including orthostatic), a heavy liver failure.

Overdose:

Cases of acute overdose are not described.

Symptoms: developing of acute hypotension, compensatory tachycardia is theoretically possible.

Treatment: the patient should be laid to recover arterial pressure and to normalize heart rate. Carry out kardiotropny therapy. It is necessary to monitor function of kidneys and to apply the general maintenance therapy.

If symptoms remain, it is necessary to administer objemozameshchayushchy solutions, the vasoconstrictive drugs. For prevention of further absorption of a tamsulozin the gastric lavage, reception of absorbent carbon or osmotic laxative is possible. Dialysis is not effective as it тамсулозин strongly contacts proteins of a blood plasma.

Storage conditions:

To store in original packaging at a temperature of 15 - 30 °C, in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Capsules with the modified release of 0,4 mg.

10 capsules in the blister from a film of PVH/PVDH and aluminum foil. 1 (one) or 3 (three) blisters in a cardboard pack with the application instruction.