Expiration date: 05/2025

Structure and Composition:

Capsules modified release. One capsule contains:

Tamsulosin hydrochloride 0.4 mg

Excipients:

Capsule contents: Calcium stearate, triethyl citrate talc copolymer of ethyl acrylate and methacrylic acid (1: 1) containing also polysorbate 80 and sodium lauryl sulfate MCC

hard gelatin capsule

upper part - iron oxide yellow (C.I. 77492 E172) titanium dioxide (C.I. 77891 E171), iron oxide black (C.I. 77499 E172), iron oxide red (C.I. 77491 E172) Gelatin

lower part - iron oxide red (C.I. 77491 E172), iron oxide black (C.I. 77499 E172) iron oxide yellow (C.I. 77492 E172) titanium dioxide (C.I. 77891 E171) Gelatin

in blister 10 pcs. In the paper cartons 1 or 3 blisters.

Description pharmaceutical form:

Hard gelatin capsule size 2 ? cap opaque brown opaque body, brown and yellow. The contents of capsules - pellets of white or nearly white.

Pharmacokinetics:

Suction

After oral tamsulosin is rapidly and almost completely absorbed from the gastrointestinal tract. The bioavailability of the drug - about 100%.

After a single oral administration at a dose of 400 mg Cmax of the active substance in plasma is reached after 6 hours.

Distribution

In the equilibrium state (after 5 days course doses) Cmax values ??of active substance in plasma at 60-70% higher than the Cmax after a single dose.

Binding to plasma proteins - 99%. Tamsulosin has a slight volume of distribution (about 0.2 l / kg).

Metabolism

Tamsulosin is not subject to the effect of "first pass" and slowly biotransformed in the liver with the formation of pharmacologically active metabolites that retain high selectivity to & alphalA-adrenoceptor. Most of the active substance is present in the blood in an unmodified form.

breeding

Tamsulosin excreted by the kidneys, 9% of the dose is excreted unchanged.

T1 / 2 with single dose of tamsulosin - 10 hours, after multiple dose - 13 hours, the final T1 / 2 - 22 hours.

Description of the pharmacological actions:

Tamsulosin selectively and competitively blocks postsynaptic & alpha1A-adrenoceptors located in the smooth muscle of the prostate, bladder neck and prostatic urethra and adrenoceptors & alpha1D-, preferably located in the body of the bladder. This leads to a reduction in smooth muscle tone of the prostate, bladder neck and prostatic urethra and detrusor improve function. This reduces the symptoms of obstruction and irritation associated with benign prostatic hyperplasia. Typically, the therapeutic effect develops after 2 weeks after starting the drug, although in some patients the decrease of symptoms is observed after the first dose.

The ability to influence the tamsulosin & alpha1A-adrenoceptors 20 times greater than its ability to interact with & alpha1B-adrenoceptors are located in vascular smooth muscle. Due to such a high selectivity of the drug does not cause any clinically significant reduction in systemic blood pressure both in hypertensive patients and in patients with normal baseline BP.

Indications:

Treatment dizuricheskih disorders caused by benign prostatic hyperplasia.

Contraindications:

Hypersensitivity to tamsulosin hydrochloride or any other component of the formulation.

Carefully:

• chronic renal failure (Cl creatinine decrease <10 ml / min)
  
• hypotension (including orthostatic)
  
• severe hepatic impairment.
  

Side effect:

Rarely - headache, dizziness, fatigue, sleep disturbances (insomnia or drowsiness), retrograde ejaculation, decreased libido, pain, back pain, rhinitis and in rare cases - orthostatic hypotension, tachycardia, palpitations, chest pain.

Co of the digestive system: rarely - nausea, vomiting, constipation or diarrhea, rarely - hypersensitivity reactions (rash, pruritus, angioedema).

Drug Interactions:

Cimetidine increases the concentration of tamsulosin in plasma furosemide - reduces the (substantial clinical significance has not, change the dosing is not required).

Diclofenac and indirect anticoagulants increases the excretion of tamsulosin.

Diazepam, propranolol, trichloromethiazide, chlormadinone, amitriptyline, diclofenac, glibenclamide, simvastatin and warfarin does not alter tamsulosin free fraction in human plasma in vitro. In turn, does not change the tamsulosin free fractions of diazepam, propranolol, trichlormethiazide and chlormadinone.

In in vitro studies found no interaction at the level of hepatic metabolism with amitriptyline, salbutamol, glibenclamide and finasteride.

Other & alpha1-blockers, acetylcholinesterase inhibitors, alprostadil, anesthetics, diuretics, levodopa, antidepressants, beta-blockers, blockers "slow" calcium channel blockers, nitrates and ethanol - can exacerbate the severity of the hypotensive effect of tamsulosin.

Dosage and administration:

Inside, after eating, 1 caps. per day, in one and the same time of day, drinking plenty of water. The capsule should neither apart crush or grind, as wherein the broken sustained release of the active substance.

Overdose:

Cases of acute overdose have not been described.

Symptoms: theoretically possible occurrence of acute hypotension, compensatory tachycardia.

Treatment: The patient should be put to restore blood pressure and normalization of heart rate. Spend kardiotropnyh therapy. It is necessary to monitor renal function and to apply the general supportive therapy.

If the symptoms persist, you should enter obemozameschayuschie solutions vasoconstrictor drugs. To prevent further absorption of tamsulosin may gastric lavage, activated charcoal or osmotic laxative. Dialysis is not effective as tamsulosin binds strongly to plasma proteins.

Special instructions:

Like other & alpha1-blockers, tamsulosin can cause a decrease in blood pressure, rarely causing faint. At the first signs of orthostatic hypotension (dizziness, weakness), you must sit down or put the patient until symptoms disappear.

Treatment with tamsulosin must be preceded by a preliminary examination of the patient in order to exclude any other disease, flowing with the same symptoms as benign prostatic hyperplasia. Treatment should be preceded by a pre-digital rectal examination of the prostate and measuring the level of prostate specific antigen (PSA), which later in the course of treatment is repeated regularly.

In the period of treatment should refrain from activities potentially hazardous activities that require high concentration and psychomotor speed reactions.

Storage conditions:

In its original packaging.