Фокусин®

General characteristics. Structure:

Active ingredient: Tamsulozina hydrochloride of 0,4 mg
Auxiliary veshchestva:30% dispersion of methacrylic acid-copolymer of an etakrilat (1:1), cellulose microcrystallic, дибутилсебакат, polysorbate 80, silicon dioxide colloid, talc.
Capsule cover: azoruby, dye Patent of blue V (Patent blue V), gelatin.

DESCRIPTION
Solid gelatin capsules No. 1. Case and lid: dark blue color, transparent.
Contents of capsules: almost white micropellets.

Pharmacological properties:

Pharmacodynamics. Tamsulozin selectively and competitively blocks the postsynaptic a1a-adrenoceptors which are in smooth muscles of a prostate, a neck of a bladder and a prostatic part of an urethra and also the a1d-adrenoceptors which are preferential 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 a1a-adrenoceptors by 20 times surpasses its ability to interact with a1v-adrenoceptors 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 a GIT. 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 (active agent in a blood plasma is 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 a1a-adrenoceptors. 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 - 10 h, after multiple dose of-13 h, final time of semi-removal - 22 h.

Indications to use:

Treatment of functional symptoms at a benign hyperplasia of a prostate.

Route of administration and doses:

Drug is appointed on 400 mkg (1 capsule) a day.
Capsules accept after the first meal, washing down with enough water. The capsule is not recommended to be chewed.

Features of use:

Tamsulozin it is necessary to apply with care at patients with predisposition to orthostatic hypotension. At the first symptoms of orthostatic hypotension (dizziness, weakness) of the patient it is necessary to seat or lay.
Before use of drug it is necessary to verify the diagnosis.
During treatment it is necessary to be careful at control of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Seldom - a headache, dizziness, an adynamy, a sleep disorder (drowsiness or sleeplessness), a retrograde ejaculation, decrease a libido, a dorsodynia, rhinitis, nausea, vomiting, a lock or diarrhea.
In isolated cases - orthostatic hypotension, tachycardia, heartbeat, thorax pain.
In extremely exceptional cases - hypersensitivity reactions (skin rash, an itch, a Quincke's disease).

Interaction with other medicines:

Cimetidinum increases concentration in plasma, furosemide - reduces (essential clinical value has no). Diclofenac and indirect anticoagulants increase the speed of removal of a tamsulozin a little.
Simultaneous use of a tamsulozin with other alfa1-adrenoblockers can lead to the expressed strengthening of hypotensive effect.

Contraindications:

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

Overdose:

Cases of acute overdose of drug are noted.
Symptoms: developing of acute hypotension is theoretically possible.
Treatment: carry out kardiotropny therapy. If symptoms remain, it is necessary to administer objemozameshchayushchy solutions or the vasoconstrictive drugs. For prevention of further absorption of a tamsulozin the gastric lavage, reception of absorbent carbon or osmotic laxative is possible.

Storage conditions:

Does not demand special storage conditions. 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 capsules in the blister from PVH/PVDH/AI. On 3, 9 or 10 blisters are placed in a cardboard pack together with the application instruction.