Tamsulosin

Chemical name

(-)-(R)-5-[2-[[2-(О-Этоксифен��кси)этил]амино]пропил ]-2-метоксибензолсульф онамид (as hydrochloride)

Gross

C20-H28-N2-O5-S

Characteristics

White crystals. Poor soluble in water and methanol, little soluble in glacial acetic acid and ethanol, practically insoluble in ether.

Of drugs

The drugs-antidizuricescoe, альфа-адренолитическ��е. Yes blocks postsinapticalkie альфа_1А-адренорецепт��ры smooth muscles prostate cancer, uterine bladder and prostaticescoy part of the urethra. A block альфа_1А-адренорецепт��ры 20 times greater than the effect on the �льфа_1B-адренорецепто��ы smooth muscles receptacles (impact on the system AD �езначительно).Снижае�� tone smooth muscles prostate cancer, uterine bladder prostaticescoy part of the urethra, improves urine flow, reduces symptoms of obstruction and irritation urinary tract in good prostate hyperplasia �елезы.Терапевтически й effect has two Ned.posle intake of almost completely absorbed from the gastrointestinal (absorption of more than 90%). Away increases bioavailability and value C_max, reduces the time of C_max. C_max achieved in 4-5 hours (to prandial), or 6-7 hours (to the reception with their food). Equilibrium concentration determined by the 6th day admission course, its peak value by 60 to 70% higher than C_max after a single reception inside. Linking plasma proteins (mostly with альфа_1-гликопротеино��) is 94-99%, distributed by the blood and fluid vnekletocna (volume of 0.2 l / kg). Biotransformiroetsa slowly in the liver, with the participation of zitohroma R450 with the formation of active metabolites (retain selectivity to Alfa_1a-adrainoretseptoram) plasma circulates mainly in unaltered form. T_1/2 9-13 h in healthy volunteers, 14 and 15 h, in patients for the treatment. Report the news is in the form of metabolites kongugatov with glukuronova and sulphuric acids (10% in unaltered) partly-Fekaliami.wvedenie tamsulosine samzam and Female rats in doses of 43 mg / kg / day and 52 mg / kg / day, respectively, does not result in the increased frequency of tumours, with the exception of a moderate statistically meaningful increase in the frequency fibroadenoma breast cancer in female rats at doses more than 5.4 mg / Kg.otsenka potential carcinogenicity in mice with a dose of 127 mg / kg / day (males) and 158 mg / kg / day (females) did not reveal a meaningful increase in the frequency of tumors in males, while females, within two years of receiving the highest dose of 45 mg / kg / day and 158 mg / kg / day, found a statistically significant increase in the frequency of fibroadenoma and adenocartinoma breast. The highest doses used to assess the carcinogenicity in mice, AUC values in animals 8 times more than any person in the employment rate 0.8 �г/сут.Зарегистрирова��ные cases of tumours mammary glands of female rodents are secondary, and should be connected to the �амсулозин-индуцирова нной �иперпролактинемией.Н е revealed mutagenna activity in a number of in vitro assays and in Vivo.v studies in male rats receiving tamsulosin occasionally or repeatedly in the dose of 300 mg / kg / day (AUC value in rats 50 times greater than any, observed in humans to the reception dose 0.8 mg / kg) found significant declines in fertility, perhaps as a consequence of the change in the composition of semen or violation ejaculate. The effects were reversible. improvements have been 3 days after receiving a single dose and four weeks after receiving multiple (full recovery at 9 weeks). When multiple doses admission 10 and 100 mg / kg / day (at 1 / 5, and 16 of the suspected AUC values in a person) adverse effects fertility is not Nabludalosi.u female rats showed significant declines in fertility in one or more imposing R-izomera or racemic mixtures tamsulosine in the dose of 300 mg / kg / sut. Lower fertility after a single dose, it was due to an abnormal sperm. In repeated a racemic mixture in dose of 10 or 100 mg / kg / day of the negative impact on the fertility of female rats have been detected.

Indications

Functional symptoms, including mocheotdelenia violation, and sound hyperplasia prostate gland.

Contraindications

Hypersensitivity, ortostatical gipotenzia in history expressed liver and / or kidney failure.

Side-Effects

From the nervous system and sensory organs : 5-20%, dizziness, headache, fatigue; Less than 5% сонливость/бессонниц��.Со the circulatory system and blood (blood, gemostaz) : less than 5% ortostatical Gipotenzia.so the urogenital system : retrogradnaya Path (8.4%); less than 5% reduction Libido.prochie : 5-20% pain in the back, myalgia, diarrhea; less than 5% pain in the chest, nausea.

Patient interaction

The combined application with the others. альфа_1-адреноблокато��ами could increase gipotenzivnogo effect. Zimetidin increases and decreases furosemide concentration in the blood, diclofenak warfarin and increase speed breeding.

Overdosing

Symptoms : acute possible Gipotenzia.lechenie : making sick bed of a plazmozameshchath solutions or sossoudossoujiwath products; for the upper-stomach scene, reception activated charcoal or osmotic slabitelnogo.

Precautions

Before treatment to verify the diagnosis (to exclude carcinoma of prostate cancer). Be wary when using propensity to Orthostatic Hypotension, expressed human liver and Cl creatinine below 10 ml / min. When signs Orthostatic hypotension (dizziness, weakness) to the patient or bring Ulojiti.s use caution during the drivers of vehicles and people profession involve heightened concentration.

Dosing and Administration

Inside (after breakfast, squeezed enough water), to 0.4 mg / sut.

Directory → Wegetotropona funds → Adrainoliticaskie funds → Альфа-адреноблокатор�� → Tamsulosin