Omsulozin

General characteristics. Structure:

Active agent: tamsulozina hydrochloride of 400 mkg.

Description. Solid gelatin capsules No. 2 with the orange case and a brown lid, with the printed black R ink on a lid and "TSN 400" on the case, contents of capsules white or almost white granules.

Pharmacological properties:

Pharmacodynamics. Omsulozin selectively and competitively blocks the postsynaptic alfa1a-adrenoceptors which are in smooth muscles of a prostate, a neck of a bladder and a prostatic part of an urethra and also the α-1D-adrenoretseptor which are preferential in a bladder body.
It leads to decrease in a tone of smooth muscles of a prostate, neck of a bladder, a prostatic part of an urethra and improvement of function of a detruzor owing to what the symptoms of obstruction and irritation connected with a benign hyperplasia of a prostate decrease. The therapeutic effect usually develops in 2 weeks after the beginning of administration of drug though at some patients reduction of expressiveness of symptoms is noted after reception of the first dose.
Ability of a tamsulozin to influence alfa1a-adrenoceptors by 20 times surpasses its ability to interact with alfa1v-adrenoceptors which are located in unstriated muscles of vessels. Thanks to such high selectivity drug does not cause clinically significant decrease in the system arterial pressure (AP) both in patients with arterial hypertension, and in patients with the normal initial ABP.

Pharmacokinetics. After intake тамсулозин it is quickly and almost completely absorbed in a GIT. Bioavailability of drug about 100%. After a single dose in 0,4 mg the maximum concentration of drug in plasma is reached in 6 h. In a condition of equilibrium concentration (in 5 days of course reception) the maximum concentration of a tamsulozin in a blood plasma is 60-70% higher, than after a single dose of drug. Linkng with proteins of plasma of 99%. The volume of distribution makes 0,2 l/kg. Drug is not subject to "effect of the first passing" and is slowly metabolized in a liver with formation pharmacological of the active metabolites having high selectivity to alfa1a-adrenoceptors. The most part of a tamsulozin is present at blood in not changed look. Drug and its metabolites are removed by kidneys, about 9% are allocated in not changed look. The elimination half-life at a single dose makes 10-12 hours.

Indications to use:

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

Route of administration and doses:

Drug is accepted on 1 capsule (400 mkg) a day after the first meal, washing down with enough water. The capsule is not recommended to be chewed as it can exert impact on the speed of release of a tamsulozin.

Features of use:

Omsulozin 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.
The drug dose decline is not required from patients with a renal failure.
During treatment it is necessary to be careful during the driving 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 - dizziness, a headache, an adynamy, a sleep disorder (drowsiness or sleeplessness), a retrograde ejaculation, decrease a libido, a dorsodynia, rhinitis, nausea, vomiting, a lock, 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:

At simultaneous use of Omsulozin with Cimetidinum some increase in concentration of a tamsulozin in a blood plasma, and with furosemide - decrease in concentration is noted, however, it does not demand change of a dose of Omsulozin.
Diclofenac and warfarin can increase the speed of elimination of a tamsulozin several. Co-administration of Omsulozin with other alfa1-adrenoblockers can lead to the expressed strengthening of hypotensive effect.

Contraindications:

Hypersensitivity to 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 of drug were not noted.
Symptoms: developing of acute hypotension is possible.
Treatment: kardiotropny therapy. If symptoms remain, it is necessary to administer objemozameshchayushy solutions or the vasoconstrictive drugs. For prevention of further absorption of drug the gastric lavage, reception of absorbent carbon or osmotic laxative is possible.

Storage conditions:

To store in the dry place at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity 2 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Capsules of the prolonged action of 400 mkg. 10 capsules in the blister from aluminum foil and PVC/PVdH: 1, 3, 10 blisters in a cardboard pack with the application instruction.