TULOZIN

General characteristics. Structure:

Active ingredient: 0,4 mg of active agent of a tamsulozin of a hydrochloride, excipients: cellulose microcrystallic, calcium stearate, copolymer of methacrylic acid and ethyl acrylate (in the form of 30% of aqueous dispersive solution), the Twin 80 (Polisorbat 80), triethyl citrate, talc a capsule Cover: indigo carmine, quinolinic yellow, titanium dioxide, gelatin

Description: The solid gelatin capsules which are self-closed with the transparent basis of green color (a code of color: 13009) and opaque cover of green color (code of color: 17026). Pellets of almost white color, inodorous or almost inodorous.

Pharmacological properties:

Pharmacodynamics. Tamsulozin selectively and competitively blocks the postsynaptic a1A-adrenoceptors which are in smooth muscles of a prostate, a neck of a bladder and a prostatic part of an urethra and also the a1D-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 and a prostatic part of an urethra and improvement of function of a detruzor. At the expense of it the symptoms of obstruction and irritation connected with a benign hyperplasia of a prostate decrease. As a rule, the therapeutic effect develops in 2 weeks after the beginning of administration of drug though at a number of patients reduction of expressiveness of symptoms is noted after reception of the first dose. Ability of a tamsulozin to influence a1A-adrenoceptors by 20 times surpasses its ability to interact with a1B-adrenoceptors which are located in unstriated muscles of vessels. Thanks to such high selectivity drug does not cause any clinically significant decrease in the system arterial pressure (AP) both in patients with arterial hypertension, and in patients with the normal initial ABP.

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 practically not exposed to effect of "the first passing" and biotransformirutsya slowly in a liver with formation pharmacological of the active metabolites keeping high selectivity to a1A-adrenoceptors. Any of metabolites is not more active, than initial substance. The most part of active agent is present at blood in not changed look. At a liver failure specification of a dose is not required. Removal: Tamsulozin and his metabolites are generally removed by kidneys, and about 9% of a dose are removed in not changed look. T1/2 of a tamsulozin at a single dose is 10 h, after multiple dose - 13 h, final time of semi-removal - 22 h. At a renal failure the dose of drug is not required to be specified.

Indications to use:

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

Route of administration and doses:

Inside, after food. On 400 mkg (1 capsule) a day. Capsules accept after the first meal, washing down with enough water. The capsule should not be broken and chewed

Features of use:

Tamsulozin it is necessary to apply with care at patients with predisposition to orthostatic hypotension as and in case of reception of others alfa-1 blockers, at some patients during a course of treatment arterial pressure can decrease that can sometimes lead to an unconscious state. At emergence of the first symptoms of orthostatic hypotension (dizziness or weakness) of the patient it is necessary to seat or lay before disappearance of symptoms. 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. At patients with the expressed renal failure (clearance of creatinine less than 10 ml/min.) it is necessary to use drug with care since this group of patients was not investigated.

Side effects:

The most often found side effects (1-10%): dizziness, drowsiness or sleeplessness Rare (0,1-1%): headache, decrease in visual acuity, rhinitis, nausea, vomiting, diarrhea or lock, retrograde ejaculation, adynamy, decrease in a libido, dorsodynia. Extremely rare (0,01-0,1%): orthostatic hypotension, tachycardia, the strengthened heartbeat, thorax pain, faints, hypersensitivity reactions (skin rash, an itch, a small tortoiseshell, a Quincke's disease). Single (<0,01%): priapism.

Interaction with other medicines:

Simultaneous use of Cimetidinum increases the level of a tamsulozin in a blood plasma; furosemide reduces its level in a blood plasma. However in both cases these levels remain within therapeutic active levels and the dosage should not be changed. Diclofenac and indirect anticoagulants increase the speed of removal of a tamsulozin a little. Simultaneous use of a tamsulozin with other alfa1-adrenoblockers and other drugs reducing arterial pressure can lead to the expressed strengthening of hypotensive effect. Interaction at simultaneous use of a tamsulozin with atenololy, enalapril, nifedipine or theophylline is not revealed. Concentration of a tamsulozin in a blood plasma did not change in the presence of diazepam, a trikhlormetiazid, amitriptyline, diclofenac, glibenclamide, a simvastatin or warfarin. Also тамсулозин did not change concentration of diazepam, propranolol, a trikhlormetiazid and a hlormadinon.

Contraindications:

Hypersensitivity to a tamsulozin to a hydrochloride or any other component of drug. With care: a chronic renal failure (decrease in clearance of creatinine is lower than 10 ml/min.), arterial hypotension (including orthostatic), a heavy liver failure.

Overdose:

Cases of acute overdose are not described.

Symptoms: developing of acute hypotension is theoretically possible.

Treatment: the patient should be laid to recover arterial pressure and to normalize heart rate. Carry out kardiotropny therapy. It is necessary to monitor function of kidneys and to apply the general maintenance therapy. If symptoms remain, it is necessary to administer objemozameshchayushchy solutions or the vasoconstrictive drugs. For prevention of further absorption of a tamsulozin the gastric lavage, reception of absorbent carbon or osmotic laxative is possible. Dialysis is not effective as it тамсулозин strongly contacts proteins of a blood plasma

Storage conditions:

Period of storage of 15 months. Not to use after the expiry date specified on packaging. To store at a temperature below 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Capsules with the modified release of 0,4 mg. On 10 capsules in the blister from PVH/PVDH/al.folga. 1 or 3 blisters together with the instruction on a medical use in a cardboard pack.