Instruction for use: Tamsulosin

Trade name of the drug – Omnic, Omnic Okas, Proflosin, Fokusin, Sonizin, Tulozin, Omsulozin, Taniz, tamsulosin, Tamsulosin Retard, Tamsulosin-Teva, Tamzelin, Tamsulosin hydrochloride, Tamsulon XPS, hypersimple, Tamsulosin, Glansin, Tamsulosin Sandoz, Tanyz Eras, Miktosin, Tamsulon, Tamsulosin OCAS, tamsulosin Canon

The Latin name of the substance Tamsulosin

Tamsulosinum (genus. Tamsulosini)

Chemical rational name: (-) - (R) -5- [2 - [[2- (O-ethoxyphenoxy) ethyl] amino] propyl] -2-methoxybenzenesulfonamide (as hydrochloride)

Gross formula C20H28N2O5S

Pharmacotherapeutic group: Alpha-blockers

Drugs affecting the metabolism of the prostate gland and correctors urodynamics

The nosological classification (ICD-10)

N40 Hyperplasia of prostate gland: Prostate adenoma; BPH; Prostatauxe; prostate Hypertrophy; Dysuric disorders caused by benign prostatic hyperplasia; Dizuricheskie disorder with benign prostatic hyperplasia; Dysuria with prostate cancer; Benign prostatic giperpalaziya; Benign prostatic hyperplasia; Benign prostatic hyperplasia stages 1 and 2; Benign prostatic hyperplasia I degree; Benign prostatic hyperplasia II degree; Benign prostatic hypertrophy; The disease of the prostate gland; Acute urinary retention related to benign prostatic hyperplasia; Benign prostatic hyperplasia stages 1 and 2 in combination with prostatitis; paradoxical ischuria

CAS code 106133-20-4

Description of Tamsulosin

Tamsulosin hydrochloride - a white crystalline powder. Poorly soluble in water and methanol, slightly soluble in glacial acetic acid and ethanol, almost insoluble in ether. The molecular weight of 444.98.

Pharmacological Properties of Tamsulosin

Pharmachologic effect - Mode of action - alpha adrenoliticheskoe, antidizuricescoe.

Selectively blocks postsynaptic alpha1-adrenergic receptors of the smooth muscles of the prostate, bladder neck and prostatic urethra. The ability to block the alpha 1-adrenergic receptors is 20 times higher as compared with the action on alfa1B-adrenoceptors in vascular smooth muscles (effect on systemic blood pressure slightly).

It lowers the tone of smooth muscles of the prostate, bladder neck, prostatic urethra, improves urine flow and reduces the symptoms of urinary tract obstruction and irritation in benign prostatic hyperplasia.

The therapeutic effect develops after 2 weeks.

Once inside almost completely absorbed from the gastrointestinal tract (absorption 90%). Food intake increases the bioavailability and the amount of Cmax, reduces the time to reach Cmax. Cmax is reached within 4-5 hours (when fasted) or 6-7 hours (when administered with food). The equilibrium concentration is established by the 6th day course taking, its peak at 60-70% higher than the Cmax after a single ingestion. Binding to plasma proteins (primarily to alpha-1-glycoprotein) amounts to 94-99%, is distributed over the volume of blood and extracellular fluid (volume of distribution - 0.2 l / kg). Slowly biotransformed in the liver, with the participation of cytochrome P450 isoenzymes (predominantly CYP3A4 and CYP2D6) with the formation of active metabolites (selectivity to retain alpha1 -adrenoceptors), it circulates in the plasma primarily in the unchanged form. T1 / 2 - 9-13 hours in healthy volunteers, 14-15 h - in the treatment of patients. Write mainly kidneys as metabolites conjugates with glucuronic and sulfuric acid (10% - unchanged), partially - with the feces.

Introduction of tamsulosin in male and female rats at doses of 43 mg / kg / day and 52 mg / kg / day, respectively, did not lead to an increase in the incidence of tumors, except for a moderate statistically significant increase in the incidence of fibroadenomas of breast cancer in female rats at doses greater than 5 4 mg / kg.

Evaluation of potential carcinogenic in mice when administered doses of 127 mg / kg / day (males) and 158 mg / kg / day (females) revealed no significant increase in the incidence of tumors in males while in females, for 2 years receiving the highest dose of 45 mg / kg / day and 158 mg / kg / day, a statistically significant increase in the incidence of fibroadenoma and breast adenocarcinomas has been detected. At the highest doses used for evaluation of carcinogenicity in mice, AUC values in animals is 8 times higher than those in humans at a dose of 0.8 mg / day.

Reported cases of occurrence of mammary tumors in female rodents are secondary, and due, apparently tamsulozinindutsirovannoy hyperprolactinemia.

There was no evidence of mutagenic activity in a series of tests in vitro and in vivo.

In studies in male rats treated with tamsulosin singly or multiply in doses of 300 mg / kg / day (AUC value in rats is 50 times higher than that observed in humans at a dose of 0.8 mg / kg) revealed a significant decrease in fertility. possibly due to changes in the composition of seminal fluid or abnormal ejaculation. The effects were reversible, improvement was observed after 3 days and a single dose at 4 weeks after the multiple administration (complete recovery was observed after 9 weeks). Repeated reception doses of 10 and 100 mg / kg / day (05.01 and 16 constitute from AUC values estimated human) negative effect on fertility was observed.

In female rats showed significant decrease in fertility in single or multiple administration of R-isomer or racemic mixture of tamsulosin in a dose of 300 mg / kg / day. Reduced fertility after a single dose was apparently due to an impaired fertilization. Repeated administration of the racemic mixture at a dose of 10 or 100 mg / kg / day negative effect on fertility is not detected in female rats.

Indications for Tamsulosin

Benign prostatic hyperplasia (treatment dizuricheskih disorders).

Contraindications for Tamsulosin

Hypersensitivity, orthostatic hypotension (including history), severe renal impairment (creatinine clearance less than 10 ml / min) and severe hepatic impairment (safety and efficacy in these patient groups is not defined).

Pregnancy and breast-feeding

Category effects on the fetus by FDA - B.

Side effect of Tamsulosin

From the nervous system and sensory organs: dizziness, headache, fatigue, drowsiness / insomnia.

Cardio-vascular system and blood (blood, hemostasis): orthostatic hypotension, syncope, palpitations, tachycardia, chest pain.

From the digestive tract: nausea, vomiting, constipation / diarrhea.

With the genitourinary system: retrograde ejaculation, decreased libido, priapism.

Allergic reactions: skin rash, pruritus, urticaria, angioedema.

Other: back pain, rhinitis.

Overdose of Tamsulosin

Symptoms can be severe hypotension.

Treatment: giving the patient lying position, the introduction of plasma-solutions or vasoconstrictor drugs; to stop the absorption - gastric lavage, activated charcoal or osmotic laxative.

Interaction

The combined use with other alpha1-blockers may lead to increased hypotensive effect (not to be used simultaneously). The use of tamsulosin and 5-phosphodiesterase inhibitors can cause symptomatic hypotension (be careful). Concomitant use of ketoconazole - a potent inhibitor of CYP3A4 isoenzyme - leads to an increase in Cmax and AUC of tamsulosin 2.2 and 2.8 times, respectively (not to be used simultaneously). Concomitant use of paroxetine - a potent inhibitor of CYP2D6 isoenzyme - leads to an increase in Cmax and AUC of tamsulosin 1.3 and 1.6 times, respectively (use with caution). In an application with cimetidine decreased clearance (26%) and increase in AUC (44%) of tamsulosin (used with caution). Furosemide lowers Cmax and AUC of tamsulosin at 11 and 12%, respectively (not clinically significant). Drug interaction studies with tamsulosin and warfarin in vitro and in vivo studies are few (be careful).

Routes of administration

Inside.

Precautions for substance Tamsulosin

Before treatment is necessary to verify the diagnosis (to rule out prostate carcinoma). Before you start treatment and regularly during therapy should be performed digital rectal examination and, if necessary, determination of prostate-specific antigen (PSA).

At the first signs of orthostatic hypotension (dizziness, weakness), the patient should sit or lay.

When surgery for cataracts in patients receiving the drug may develop iris syndrome intraoperative instability eyes (narrow pupil syndrome), it is necessary to take into account the surgeon in the preoperative patient preparation and conduct of operations.

Be wary of during the drivers of vehicles and people skills relate to the high concentration of attention.