Tamsulozin-Tev

General characteristics. Structure:

Active agent of a tamsulozin a hydrochloride of 0,400 mg, in terms of тамсулозин 0,367 mg;
excipients: cellulose microcrystallic (101), methacrylic acid and ethyl acrylate copolymer (1:1), triethyl citrate, talc, water *, sodium hydroxide/Acidum hydrochloricum;
pellet cover: methacrylic acid and ethyl acrylate copolymer (1:1), talc, triethyl citrate, water *;
capsule: dye ferrous oxide red, titanium dioxide, dye ferrous oxide yellow, gelatin, indigo carmine (FD&C Blue 2), dye ferrous oxide black;
paint for the press on the capsule: % Glaze-47,5 varnish, propylene glycol, dye ferrous oxide black.
* - water as solvent, is removed in the course of production

Description:
Solid gelatin capsules with the orange case and a green lid. On both ends of the capsule - a black ring. On the capsule - a black text of "TSL 0.4". Contents of capsules - white or almost white pellets.

Pharmacological properties:

Tamsulozin selectively and competitively blocks postsynaptic alfa1a-the adrenoceptors which are in smooth muscles of a prostate, a neck of a bladder and a prostatic part of an urethra and also the alfa1d-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, a prostatic part of an urethra, improves urine outflow, reduces symptoms of obstruction and irritation of urinary tract at a benign hyperplasia of a prostate.

Ability of a tamsulozin to influence alfa1a-adrenoceptors by 20 times surpasses its ability to interact with the alfa1a-adrenoceptors located in smooth muscles of vessels. Thanks to such high selectivity, drug does not cause any clinically significant system lowering of arterial pressure (ABP) both in patients with arterial hypertension, and in patients with the normal initial ABP. As a rule, the therapeutic effect is reached in 2 weeks after the beginning of administration of drug.

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 in Cmax of active agent in plasma it is reached in 6 h.

Right after meal absorption of a tamsulozin decreases. Uniformity of absorption increases if the patient accepts drug every day after the same meal.

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.

Distribution:
Linkng with proteins of plasma - 99%. Tamsulozin has the insignificant volume of distribution (about 0.2 l/kg).

Metabolism:
Tamsulozin is exposed to effect of "the first passing" a little and biotransformirutsya slowly in a liver with formation pharmacological of less active metabolites keeping high selectivity to alfa1a-adrenoceptors the Most part of active agent is present at blood in not changed look. At a liver failure dose adjustment is not required.

Removal:
Tamsulozin and his metabolites are generally removed by kidneys, and about 9% the state are removed in not changed look. T1/2 of a tamsulozin at a single dose - 10 h, after multiple dose - 13 h final time of semi-removal - 22 h. Dose adjustment of a tamsulozin in the presence of diseases of kidneys is not required.

Indications to use:

Treatment of functional symptoms of the benign hyperplasia of a prostate (BHP).

Route of administration and doses:

Inside, on 1 capsule (0,4 mg) at the same time after food once a day. The capsule needs to be swallowed entirely, in a sitting position or standing, not cracking and without chewing as it can break gradual release of active ingredient.

Features of use:

At the first symptoms of orthostatic hypotension (dizziness, weakness) it is necessary to sit down or lay down before disappearance of the specified symptoms.

Prior to treatment tamsuloziny it is necessary to conduct examination of the patient for an exception of other diseases which can cause the same symptoms as a benign hyperplasia of a prostate. Prior to treatment by drug and during therapy it is regularly necessary to conduct examination of a prostate and, if necessary, definition of the prostatic specific antigen (PSA). Due to a possibility of complications during operational treatment of a cataract, patients are not recommended to appoint treatment tamsuloziny with a cataract if carrying out operation is planned.

At reception of a tamsulozin drowsiness, deterioration in sight, dizziness and faints therefore drug should be used with care in operating time to drivers of vehicles and people whose profession demands the increased concentration of attention are possible.

Side effects:

Frequency of side reactions: often (> 1%, <10%), infrequently (> 0,1%, <1%), it is rare (> 0 01% <0,1%), are very rare (<0,01%).
From a nervous system: often - dizziness, infrequently - a headache, is rare - a syncope; sleep disorder (drowsiness or sleeplessness);
From cardiovascular system: infrequently - tachycardia, orthostatic hypotension; thorax pain;
From a respiratory organs: infrequently - rhinitis.
From the alimentary system: infrequently - a lock, a diarrhea, nausea, vomiting.
From skin and integuments: infrequently - rash, an itch, urticaria; seldom - a Quincke's disease.
From urinogenital system: infrequently - a retrograde ejaculation, it is very rare - a priapism; decrease in a libido;
Others: sometimes - an adynamy, a dorsodynia, a syndrome of a small pupil during operation for a cataract.

Interaction with other medicines:

Interaction at a concomitant use of a tamsulozin was not noted with atenololy, enalapril, nifedipine or theophylline. At a concomitant use with Cimetidinum concentration of a tamsulozin in a blood plasma increases, and at a concomitant use of a tamsulozin with furosemide - decreases. However dose adjustment is not required as concentration of a tamsulozin remains in the therapeutic range.

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

Interaction of a tamsulozin with amitriptyline, salbutamol, glibenclamide and finasteridy in the researches in vitro is not revealed. At a concomitant use with tamsuloziny diclofenac or warfarin increase in speed of elimination of a tamsulozin is possible.

At a concomitant use of a tamsulozin with the medicines reducing arterial pressure including others alfa1 - adrenoblockers and anesthetics, strengthening of hypotensive effect is possible.

Contraindications:

• Hypersensitivity to a tamsulozin to a hydrochloride or other components of drug;
• Orthostatic hypotension (including in the anamnesis);
• Heavy liver failure.

With care:
Heavy renal failure (decrease in clearance of creatinine is lower than 10 ml/min.).

Overdose:

Cases of overdose are not described, acute hypotension is theoretically possible. Treatment: in case of overdose it is recommended to transfer the patient to horizontal position and to hold the events directed to maintenance of function of cardiovascular system (recovery of arterial pressure and heart rate); gastric lavage, administration of absorbent carbon and osmotic purgatives, such, as sodium sulfate.

In the absence of effect it is necessary to enter the substances increasing the volume of the circulating blood, and if necessary, vasoconstrictors. It is necessary to carry out observation of function of kidneys and to hold the events directed to its maintenance. Dialysis is a little effective at overdose of a tamsulozin as drug substantially contacts proteins of a blood plasma.

Storage conditions:

Period of validity: 3 years. Not to apply after a period of validity. At a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Capsules with the modified release.
On 10 capsules in the blister from PVC/PE/PVDH / aluminum foil.
On 1 or 3 blisters together with the application instruction in a cardboard pack.