Pharmacological properties

Pharmacodynamics. the mechanism of action of a tamsulozin is caused by selection competitive linking with postsynaptic α1-адренорецепторами, in particular with subtypes α1a and α1d that leads to decrease in a tone of unstriated muscles of a prostate, a neck of a bladder, a prostatic part of an urethra and improvement of discharge of urine.

expressiveness of symptoms of obstruction and the irritation connected with a benign hyperplasia of a prostate At the same time decreases. Drug does not cause clinically significant decrease in the system ABP in patients with the normal initial ABP.

Therapeutic effect usually develops in 2 weeks after the beginning of administration of medicament though reduction of expressiveness of symptoms of a disease perhaps after reception of the first doses.

Pharmacokinetics. Absorption. Tamsulozin quickly and almost is completely soaked up in intestines. Absorption slows down if medicament is used after a meal. Uniform release of active ingredient can be reached if always to accept tamsulozin after a breakfast. The linear kinetics is inherent to Tamsulozin. Peak levels in blood plasma are reached approximately in 6 h after reception of a single dose of a tamsulozin after a meal. The equilibrium state is reached for the 5th day of use, at the same time by the C _max in blood plasma on ⅔ above, than after reception of a single dose. Though such data are established only for elderly people, it is possible to expect similar result for patients of younger age.

both after reception of a single dose, and after repeated use.

Distribution. Linking with proteins of blood plasma — 99%. The volume of distribution is insignificant (about 0.2 l/kg of body weight).

Metabolism. Tamsulozin is not subject to effect of the first passing and is slowly metabolized in a liver with formation pharmacological of the active metabolites keeping high selectivity to α ₁ - to adrenoceptors. The most part of active agent is present at blood in not changed look.

Removal. Tamsulozin and his metabolites are removed mainly with urine, and about 9% of a dose are removed in not changed look.

T _½ tamsulozina at patients makes about 10 h at use after a meal and 13 h — in an equilibrium state.

Indication

Treatment of functional disturbances from the lower urinary tract in a benign hyperplasia of a prostate.

Use

Recommended dose for adults — 1 capsule daily, after a breakfast or after the first reception of food. whole should swallow of the capsule, sitting or standing. the capsule cannot be chewed, broken as it will interfere with the modified release of active ingredient.

to Patients of advanced age does not need dose adjustment. However it must be kept in mind that at geriatric patients the risk of orthostatic hypotension is increased.

to Patients with a renal failure does not need dose adjustment.

to Patients with a liver failure moderate and moderate severity does not need dose adjustment (see CONTRAINDICATIONS).

Contraindication

• Hypersensitivity to a tamsulozin to a hydrochloride, including the medicamentous induced Quincke's disease, or to any of excipients; orthostatic hypotension in the anamnesis; profound liver failure.

Side reactions are classified by

by bodies and systems and frequency of emergence: often (1/100, 1/10); infrequently (1/1000, 1/100); seldom (1/10,000, 1/1000); very seldom (1/10,000), it is unknown (it is impossible to estimate according to available data).

Nervous system: often — dizziness; infrequently — a headache; seldom — a syncope (syncope).

Organ of sight: seldom — misting of sight *, disturbance zreniya*.

Cardiovascular system: infrequently — orthostatic hypotension, heart consciousness (palpitation).

Respiratory system: infrequently — rhinitis; it is unknown — nasal krovotecheniye*.

Reproductive system: often — disturbance of an ejaculation, including a retrograde ejaculation and nedostatochnos ejaculations; very seldom — a priapism.

Digestive tract: infrequently — a constipation, diarrhea, nausea, vomiting; it is unknown — dryness in a mouth.

Skin, hypodermic cellulose: infrequently — an itching, rash, urticaria; seldom — a Quincke's disease; very seldom — Stephens's syndrome — Johnson; it is unknown — a multiformny erythema *, exfoliative dermatit*.

General disturbances: infrequently — an asthenia. * it Were noted by

p during the post-registration period of use of a tamsulozin.

Krom of above-mentioned side reactions, spontaneous messages about cases of fibrillation of auricles, tachycardias, arrhythmias, dispnoe came to the post-registration period. As about the specified cases it was reported spontaneously, the frequency of reactions and their communication with tamsuloziny cannot be authentically determined.

by

As well as at reception of other blockers of α-adrenoceptors, drowsiness, dryness in a mouth, hypostases can be observed.

by

described cases of intraoperative instability of an iris of the eye of an eye (the option of a syndrome of a narrow pupil known as IFIS) during operation for a cataract and glaucoma at patients, accepting tamsulozin a long time.

Special instructions

As well as at use of other blockers α1-адренорецепторов, in some cases at use of a tamsulid the decrease hell is possible

that can sometimes lead to a loss of consciousness. at emergence of the first symptoms of orthostatic hypotension (dizziness, weakness) the patient has to accept horizontal position before disappearance of the above-stated symptoms.

Before beginning the Tamsulid medicament treatment, it is necessary to undergo medical examination for the purpose of detection of other associated diseases which can cause the same symptoms as a benign hyperplasia of a prostate. Before an initiation of treatment it is necessary to perform rectal examination of a prostate both if necessary before and regularly during treatment to control the level of prostate-specific antigen (PSA).

needs to Appoint by

medicament to patients with a severe form of a renal failure (clearance of creatinine of 10 ml/min.) with extra care in view of lack of sufficient clinical experience.

to

it was Occasionally reported about development of a Quincke's disease after use of a tamsulozin. In that case treatment it is necessary to stop and control immediately a condition of the patient before disappearance of hypostasis, tamsulozin it is not necessary to accept repeatedly.

At some patients who accepted or is accepted tamsulozin, during surgical intervention concerning removal of a cataract and glaucoma the instability of an iris of the eye of an eye (syndrome of an atonic pupil (IFIS), option of a syndrome of a miotic pupil) connected with blockade α ₁ - adrenoceptors was noted. IFIS increases risk of development of eye complications in time or after such operation.

As a rule, for 1–2 weeks before carrying out operation for removal of a cataract and glaucoma the treatment tamsuloziny is recommended to stop

. However the expediency and terms of the termination of treatment tamsuloziny are definitely not established now. About a syndrome of an atonic pupil it was reported also at patients at whom stopped use of a tamsulozin before performing surgery for a long time.

is not recommended to Begin therapy of a tamsulozin with a hydrochloride to patients to whom operation for a cataract or glaucoma is planned. At a preparation for surgery the surgeons-ophthalmologists have to know whether the patient tamsulozin for the purpose of prevention of the possible complications connected with IFIS accepted (or accepts).

Tamsulozin is intensively metabolized, mainly, by CYP 3A4 and CYP 2D6. A hydrochloride it is not necessary to appoint Tamsulozin in a combination with strong CYP inhibitors 3A4 (for example ketokonazoly) to patients with low metabolism of CYP 2D6.

Tamsulozin's

a hydrochloride should be applied with care in combination with strong (for example ketokonazol) and moderate CYP inhibitors 3A4 (for example erythromycin) (see INTERACTIONS).

to

It was reported about cases of allergic reactions on tamsulozin at patients with existence in the anamnesis of an allergy to streptocides. It is necessary to be careful at use of a tamsulozin of a hydrochloride for patients at whom the allergy to streptocides was noted earlier.

should take the Drug on doctor's orders.

Use during pregnancy and feeding by a breast. Tamsulid is not shown for use for women.

Fertility. During clinical trials of a tamsulozin during the short and long time, disturbances of an ejaculation were noted. Cases of disturbance of an ejaculation, a retrograde ejaculation and an insufficient ejaculation were noted during the post-registration period.

Children. Drug is not appointed to children. Safety and efficiency of a tamsulozin at children are aged younger than 18 years did not estimate.

Ability to influence speed of response at control of vehicles or work with mechanisms. Researches of influence of medicament on ability to run vehicles or to work with mechanisms were not conducted. However patients have to be warned about possibility of dizziness.

Interaction

Research of interaction was conducted only at adults. at simultaneous use of a tamsulozin of a hydrochloride with atenolol, enalapril, nifedipine or theophylline of medicinal interaction it was not noted. the combined use with Cimetidinum raises, and with furosemide — reduces concentration of a tamsulozin in blood plasma, but as these levels remain within norm, in special dose adjustment of a tamsulozin there is no need.

In the researches in vitro diazepam, propranolol, trikhlormetiazid, chlormadinon, amitriptyline, diclofenac, glibenclamide, simvastatin and warfarin do not influence free fraction of a tamsulozin in blood plasma of the person. In this way tamsulozin does not change the level of free fractions of diazepam, propranolol, a trikhlormetiazid and chlormadinon in blood plasma of the person. However diclofenac and warfarin can accelerate elimination of a tamsulozin from blood plasma.

In the researches in vitro did not reveal interaction at the level of hepatic metabolism with participation of microsomal fractions in a liver (the system of enzymatic metabolism with P450 cytochrome participation was indicative) concerning amitriptyline, salbutamol, glibenclamide and a finasterid. However diclofenac and warfarin can accelerate elimination of a tamsulozin from blood plasma.

to increase in influence of a tamsulozin of a hydrochloride. The combined use with ketokonazoly (the known strong CYP inhibitor 3A4) led to increase With _max and AUC to 2.2 and 2.8 respectively.

a hydrochloride should be applied with care in a combination with strong (for example ketokonazoly, itrakonazoly, vorikonazoly, klaritromitsiny, indinaviry, nelfinaviry, ritonaviry, sakvinaviry) and moderated (for example erythromycin) CYP inhibitors 3A4. And patients with low metabolism of CYP 2D6 of a tamsulozin should not appoint a hydrochloride in combination with strong CYP inhibitors 3A4.

to increase With _max and AUC to 1.3 and 1.6 respectively, but it is not clinically significant.

risk of strengthening of hypotensive effect at use of a tamsulozin along with medicaments which can lower the arterial blood pressure, including anesthetics, phosphodiesterase-5 inhibitors, other blockers α ₁ - adrenoceptors Exists.

Research in vitro with microsomal fractions of a liver were not shown by interactions with amitriptyline, salbutamol, glibenclamide and finasteridy.

Overdose

Symptoms. the overdose of a tamsulozin of a hydrochloride can cause acute and heavy hypotensive effects and also vomiting and diarrhea. heavy hypotensive effects were observed at various extents of overdose.

Treatment. In case of sharp decrease in the ABP owing to overdose it is necessary to carry out the maintenance therapy directed to restoration of normal function of a cardiovascular system (for example the patient has to accept horizontal position). If this measure is inefficient, to carry out infusional therapy and to appoint angiotonic means. It is necessary to monitor function of kidneys and to carry out the general maintenance therapy. Owing to high extent of linking of a tamsulozin with proteins of blood plasma carrying out a hemodialysis is inexpedient.

to prevent absorption, cause vomiting. At overdose of a significant amount of medicament the patient needs to wash out a stomach using activated carbon and low-osmotic depletive, such as sodium sulfate.

Storage conditions

In original packing at a temperature not above 25 °C.