Glansin

General characteristics. Structure:

Active ingredient: 0,2 mg or 0,4 mg of a tamsulozin in the form of a hydrochloride.

Excipients: sugar krupka (sucrose, starch syrup), ethyl cellulose, methacrylic acid copolymer, macrogoal 6000.

Capsule cover: gelatin, water, dye ferrous oxide red, dye ferrous oxide yellow, titanium dioxide, sodium lauryl sulfate.

Ink for drawing a text on a cover of capsules: alcohol *; isopropanol *; butanol *; propylene glycol *; polysorbate 80 *; shellac *; titanium dioxide. * Are removed during production.

Pharmacological properties:

Pharmacodynamics. Tamsulozin is a specific blocker postsynaptic α1-адренорецепторов, being in smooth muscles of a prostate, a neck of a bladder and a prostatic part of an urethra. Blockade α1-адренорецепторов tamsuloziny 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 outflow of urine. At the same time both emptying symptoms, and the filling symptoms caused by the raised tone of smooth muscles and a detruzorny hyperactivity at a benign hyperplasia of a prostate decrease.

Ability of a tamsulozin to influence on α1A-подтип adrenoceptors by 20 times surpasses its ability to interact with α1B-подтипом adrenoceptors which are located in unstriated muscles of vessels. Thanks to the high selectivity, drug does not cause clinically significant decrease in the system ABP both in patients with arterial hypertension, and in patients with the normal initial ABP.

Pharmacokinetics. Tamsulozin is well soaked up in intestines and nearly 100% have bioavailability.

Absorption of a tamsulozin is a little slowed down after meal. Identical level of absorption can be reached if the patient every time accepts drug after a usual breakfast. Tamsulozin is characterized by linear kinetics. After a single dose in 0,4 mg of Tmax in plasma makes 6 h. After multiple dose in 0,4 mg in day of Css it is reached by 5th day, at the same time its value is approximately 2/3 higher than value of this parameter after reception of a single dose. Linkng with proteins of plasma — 99%. Vd is insignificant and makes about 0,2 l/kg.

Tamsulozin is slowly metabolized in a liver with formation of less active metabolites. Бóльшая a part of a tamsulozin is present at a blood plasma in not changed look. Tamsulozin and his metabolites are removed with urine, at the same time about 9% of drug are allocated in not changed look. Drug T1/2 at a single dose of 0,4 mg after food makes 10 h, at multiple dose — 13 h.

At insignificant and moderate degree of a liver failure correction of the mode of dosing is not required.

At a renal failure the dose decline, in the presence is not required from the patient of a heavy renal failure (creatinine Cl less than 10 ml/min.) it is necessary to appoint тамсулозин with care.

Indications to use:

Treatment of dysuric frustration at a benign hyperplasia of a prostate.

Route of administration and doses:

Inside, swallowing entirely, not chewing, without crushing (since it can exert impact on the speed of release of a tamsulozin).

On 0,4 mg (1 капс.) 1 time a day after the first meal (the time interval between administration of drug has to make 24 h). At insignificant and moderate abnormal liver functions, and also at renal failures dose adjustment is not required.

At intolerance of a dose of 0,4 mg appoint a dose on 0,2 mg/days. In case of lack of therapeutic effect after use of drug in a dose of 0,4 mg during 2–4 weeks it is possible to increase a dose to 0,8 mg/days.

If administration of drug in a dose of 0,2 or 0,4 mg was interrupted on 2 weeks (for any reason), then treatment should be begun again with the same dosage. If administration of drug in a dose of 0,8 mg was interrupted on 2 weeks (for any reason), then treatment should be begun again with a dosage in 0,4 mg/days.

Duration of use is not limited, drug is appointed in the form of continuous therapy.

Features of use:

Use at pregnancy and feeding by a breast. There are no data.

With care it is necessary to appoint drug at a renal failure of heavy degree (creatinine Cl less than 10 ml/min.), as well as when using others α1-адреноблокаторов. Drug should be used with care at patients with predisposition to orthostatic hypotension. At the first symptoms of orthostatic hypotension (dizziness, weakness) the patient has to sit down or lay down and remain in this situation until above-mentioned signs do not disappear. Before use of drug it is necessary to verify the diagnosis and to exclude existence of other diseases which can cause similar symptoms.

Before the beginning and regularly during therapy manual rectal inspection and if necessary definition of the DOG has to be carried out.

It is reasonable to stop administration of drug for 1–2 weeks before cataract surgery (against the background of administration of drug possibly development of a syndrome of intraoperative instability of an iris of the eye of an eye that the surgeon needs to consider by preoperative training of the patient and carrying out operation).

Influence on ability to manage vehicles and mechanisms. During treatment it is necessary to be careful at control of vehicles and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions since drug can cause dizziness and other side effects which can influence the specified abilities.

Side effects:

Gradation of frequency of development of side effects: very often —> 1/10; often — from> 1/100 to <1/10; sometimes — from> 1/1000 to <1/100; seldom — from> 1/10 000 to <1/1000; very seldom, in isolated cases — from <1/10000.

From CCC: in isolated cases — orthostatic hypotension, a heart consciousness, tachycardia.

From TsNS: seldom — dizziness; in isolated cases — a headache, an adynamy.

From reproductive system: seldom — a retrograde ejaculation.

From the alimentary system: seldom — nausea, vomiting, diarrhea, a lock.

Allergic reactions: in isolated cases — skin rash, an itch, a Quincke's disease (including a Quincke's edema).

From a respiratory organs: seldom — rhinitis.

From organs of sight: very seldom — a vision disorder; in isolated cases — intraoperative instability of an iris of the eye of an eye (a syndrome of a narrow pupil) at operation for a cataract at patients that increases risk of complications in time and after operation.

Interaction with other medicines:

At simultaneous use with Cimetidinum some increase in concentration of a tamsulozin in a blood plasma, with furosemide — decrease in concentration is noted, however it does not demand change of a dose of a tamsulozin as concentration of drug remains within normal range.

Diclofenac and warfarin can increase the speed of removal of a tamsulozin several.

Simultaneous use of a tamsulozin with other antagonists α1-адренорецепторами can lead to decrease in the ABP.

At a concomitant use with atenololy, enalapril, nifedipine medicinal interaction was revealed not.

Diazepam, propranolol, трихлорметиазид, хлормадинон, amitriptyline, diclofenac, glibenclamide, симвастатин and warfarin do not change free fraction of a tamsulozin in in vitro plasma. Tamsulozin does not change free fractions of diazepam, propranolol, a trikhlormetiazid and hlormadinon.

In the researches in vitro interaction at the level of hepatic metabolism with amitriptyline, salbutamol, glibenclamide and finasteridy was not revealed.

Contraindications:

- hypersensitivity to a tamsulozin or any other component of drug;

- orthostatic hypotension (including in the anamnesis);

- the expressed liver failure;

- children's age up to 18 years.

With care: heavy renal failure (creatinine Cl less than 10 ml/min.).

Overdose:

Cases of acute overdose of drug are noted. Symptoms: developing of acute arterial hypotension and compensatory tachycardia is theoretically possible.

Treatment: symptomatic — giving to the patient of horizontal position, if necessary — administration of objemozameshchayushchy solutions or vasoconstrictive drugs. For prevention of further absorption of a tamsulozin the gastric lavage, purpose of absorbent carbon or osmotic laxative is possible. It is necessary to control function of kidneys. It is improbable that dialysis will be effective since it тамсулозин is in active communication with proteins of plasma.

Storage conditions:

To store in the dry, protected from light place, at a temperature from 8 °C to 25 °C. To store in the place, unavailable to children. A period of validity - 4 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Capsules with the modified release, 0,2 mg, 0,4 mg. For drugstores: on 10 капс. in It is scarlet/is scarlet the blister and/or in ПВДХ/ПВХ/Ал the blister. On 1, 3 or 10 blisters on 10 (No. 10), 30 (No. 30) or 100 (No. 100) капс. in a cardboard pack. On 1 or 3 blisters on 10 or 30 (No. 10 or No. 30) капс. in a cardboard pack with perforation (the oval openings protected by a film from PVC from the inside of a cardboard pack).

For hospitals: on 100, 500 or 1000 капс. in a package from PVC, the package is placed in bank from PEVP.