Tamzelin

General characteristics. Structure:

Active agent: a tamsulozina a hydrochloride of a pellet of 0,15% - 267 mg containing a tamsulozin a hydrochloride - 0,4 mg Excipients of pellets: Sucrose - 143,36 mg, starch - 95,58 mg, ethyl cellulose - 3,74 mg, a gipromelloza - 2,56 mg, K-30 povidone - 1,5 mg, коповидон (пласдон S-630) - 2,54 mg, gipromelloza phthalate - 10,4 mg, cetyl alcohol - 1,0 mg, diethyl phthalate - 0,35 mg, talc - 5,47 mg Structure of a gelatin capsule: Gelatin - 62,306465 mg the Cover Dyes: Diamond black - 0,0065 mg Blue patent - 0,00715 mg Quinolinic yellow - 0,00871 mg Ferrous oxide yellow - 0,071175 mg of Titanium dioxide - 1,3 mg the Basis Dyes: Titanium dioxide - 1,3 mg.

Pharmacological properties:

Selectively and competitively blocks the postsynaptic alfa1a-adrenoceptors which are in smooth muscles of a prostate gland, a neck of a bladder and a prostatic part of an urethra. Reduces a tone of smooth muscles of a prostate, neck of a bladder and a prostatic part of an urethra, improving urine outflow. At the same time the symptoms of obstruction and irritation of urinary tract connected with a benign hyperplasia of a prostate decrease. The therapeutic effect occurs in 2 weeks after an initiation of treatment. Tropism to the alfa1a-adrenoceptors located in a bladder by 20 times surpasses its ability to interact with alfa1b-adrenoceptors which are located in unstriated muscles of vessels. Thanks to such high selectivity does not cause any clinically significant decrease in system arterial pressure both in patients with arterial hypertension, and in patients with normal initial arterial pressure. 

Pharmacokinetics. Absorption high (more than 90%). The maximum concentration in plasma after a single dose in 0,4 mg is reached in 6 h. Communication with proteins of plasma of 94-99%. The volume of distribution is insignificant – 0,2 l/kg. It is slowly metabolized in a liver with formation pharmacological of active metabolites. The most part is present at blood in not changed look. It is removed by kidneys (4-9% in not changed look). An elimination half-life – 10-12 h.

Indications to use:

Benign hyperplasia of a prostate (treatment of dysuric frustration).

Route of administration and doses:

Inside, on 0,4 mg/days, washing down with enough water. Capsules accept entirely, without chewing, after the first meal.

Features of use:

As well as when using other alfa1-adrenoblockers, at treatment by drug the lowering of arterial pressure which can sometimes lead to an unconscious state in some cases can be observed. At the first symptoms of orthostatic hypotension (dizziness, weakness) the patient has to sit down or lay down and remain in this situation until signs do not disappear.
Before beginning therapy with drug, the patient has to be inspected to exclude existence of other diseases which can cause the same symptoms, as well as a benign hyperplasia of a prostate. Before an initiation of treatment and regularly during therapy manual rectal inspection and if it is required, definition of a specific antigen of a prostate (PSA) has to be carried out.
With a renal failure of change of the mode of dosing it is not required from patients.
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:

Headache, dizziness, adynamy, sleep disorders (drowsiness or sleeplessness), retrograde ejaculation, decrease libido, priapism, dorsodynia, rhinitis; orthostatic hypotension, syncope, tachycardia, heart consciousness, thorax pain; nausea, vomiting, lock or diarrhea; allergic reactions (skin rash, itch, small tortoiseshell, Quincke's disease).

Interaction with other medicines:

At simultaneous use of drug with Cimetidinum increase in concentration of a tamsulozin in a blood plasma is noted, and with furosemide - decreases.
Diclofenac and indirect anticoagulants increase the speed of removal of a tamsulozin a little.
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 also 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 amitriptyline, 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.

Contraindications:

Hypersensitivity to a tamsulozin or other component of drug.
Age up to 18 years.
Drug is not used at women. 
Use at pregnancy -

Overdose:

Symptoms: the expressed lowering of arterial pressure, tachycardia.
Treatment: a gastric lavage, reception of absorbent carbon or osmotic laxative (sulfate sodium), symptomatic therapy (the horizontal position of the patient, medicines increasing the volume of tsirkuliruyemy blood, vasoconstrictive medicines),
control of function of kidneys. Dialysis is ineffective (intensively contacts proteins of plasma).

Storage conditions:

In the dry, protected from light place at a temperature not above 30 °C. To store in the places unavailable to children. 
Period of validity 2 years. Not to use after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Capsules of the prolonged action of 0.4 mg; packaging planimetric cell 10, pack cardboard 1.