Tamsulosin - instructions for use, dose, side effects, contraindications

Tamsulosin hydrochloride substitution-pellets 0,2% - 200,0 mg [active substance-. tamsulosin hydrochloride 0.4 mg; Excipients: sugar spheres (sucrose - 99%, hypromellose - 1%) - 190.0 mg, methacrylic acid copolymer - 4.8 mg, ethyl cellulose - 4.0 mg, polyethylene glycol - 0.8 mg].

Capsules hard gelatinous-, titanium dioxide 1.0%, iron oxide yellow (iron oxide) 0.27%, blue patented dye 0.015%, gelatin 100%.

Description:Capsules hard gelatinous № 3 green. The contents of the capsules are white or almost white in color.

Pharmacotherapeutic group:ss-adrenoblocker.

ATX: & nbsp

G.04.C.A.02 Tamsulosin

Pharmacodynamics:

Tamsulosin is a specific blocker of postsynaptic si-adrenergic receptors located in the smooth muscles of the prostate gland, the neck of the bladder and the prostatic part of the urethra. Blockade α1 adrenoreceptor tamsulosin leads to a decrease in the tone of the smooth muscles of the prostate gland, the neck of the bladder and the prostatic part of the urethra and improve the urine flow.At the same time, the symptoms of filling and emptying caused by the increased tone of smooth muscles and detrusor hyperacia in the benign prostatic hyperplasia decrease. The ability of tamsulosin to act on the α1A subtype of adrenoceptors is 20 times greater than its ability to interact with am subtype of adrenoreceptors, which are located in the smooth muscles of blood vessels. Due to its high selectivity tamsulosin does not cause a clinically significant decrease in systemic arterial pressure (BP) in both patients with arterial hypertension and in patients with normal initial BP.

Pharmacokinetics:

Suction

Tamsulosin is well absorbed in the intestine and has almost 100% bioavailability. Absorption of tamsulosin somewhat slows down after eating. The same level of absorption can be achieved if the patient takes the drug every time after a normal breakfast. Tamsulosin characterized by linear kinetics. After a single dose of the drug inside at a dose of 0.4 mg, its maximum concentration in the blood plasma is reached after 6 hours.After repeated intake of the drug in a daily dose of 0.4 mg, the equilibrium concentration is reached by the 5th day, while its value is 2/3 higher than the value of this parameter after a single dose of the drug.

Distribution

Binding to blood plasma proteins - 99%, the distribution of small (about 0.2 l / kg).

Metabolism

Tamsulosin is slowly metabolized in the liver with the formation of less active metabolites. Most of the tamsulosin is present in plasma in unchanged form.

In experimental studies, the ability of tamsulosin to induce insignificantly the activity of microsomal liver enzymes has been revealed. With a slight and moderate degree of hepatic insufficiency, there is no need for correction of the dosing regimen.

Excretion

Tamsulosin and its metabolites are excreted mainly by the kidneys, with approximately 9 % of the dose is excreted unchanged.

Half-life with a single admission of 0.4 mg of tamsulosin after meals is 10 hours, after repeated intake - 13 hours.

With renal failure, no dose reduction is required. If the patient has severe renal failure (creatinine clearance 10 ms / min), tamsulosin should be administered with caution.

Indications:

Treatment of dysuric disorders in benign prostatic hyperplasia.

Contraindications:

- hypersensitivity to tamsulosin or other components of the drug;

- orthostatic hypotension (including in the anamnesis);

- severe hepatic impairment;

- glucose-galactose malabsorption;

- deficiency of sugar / isomaltase;

- intolerance to fructose;

- children's age till 18 years.

Carefully:

- severe renal failure (creatinine clearance less than 10 ml / min);

- arterial hypotension.

Pregnancy and lactation:

The drug is intended for use only in males.

Dosing and Administration:

Capsules of tamsulosin should be taken after breakfast, without chewing, squeezed with enough water. The drug is taken 1 capsule (0.4 mg) once a day.

Side effects:

The incidence of adverse events is classified according to the recommendations

World Health Organization:

very often:> 1/10 (> 10%);

often: from 1/100 to 1/10 (> 1% and <10%);

infrequently: from 1/1000 to 1/100 (> 0.1% and <1%);

rarely: from 1/10000 to 1/1000 (> 0.01% and <0.1%);

very rarely: <1/10000 (<0.01%), including individual events;

frequency is unknown.

From the cardiovascular system:

infrequent-palpitation, orthostatic hypotension;

frequency unknown - atrial fibrillation, arrhythmia, tachycardia, dyspnea.

From the gastrointestinal tract: infrequently - constipation, diarrhea, nausea, vomiting.

From the nervous system: often - dizziness; infrequently - a headache; rarely - faint.

On the part of the reproductive system: often - violations of ejaculation; very rarely - priapism.

On the part of the respiratory, thorax and mediastinal organs: sometimes it is rhinitis.

From the skin and subcutaneous tissue: infrequently - a rash, itching, hives; rarely - angioedema; very rarely - Stevens-Johnson syndrome;

frequency unknown - erythema multiforme, exfoliative edema.

General condition disorders: infrequently, asthenia.

Other:

infrequently - asthenia;

frequency unknown - intraoperative iris of the eye (narrow pupil syndrome) during surgery but for cataract and glaucoma, epistaxis.

Overdose:

There are no reports of acute drug overdose.

The most likely symptoms

Pronounced decrease in arterial pressure and compensatory tachycardia.

Treatment

Symptomatic. Arterial pressure and heart rate can be restored when the patient takes a horizontal position.In the absence of effect, it is possible to use agents that increase the volume of circulating blood, and, if necessary, vasoconstrictors. It is necessary to monitor kidney function. Conducting hemodialysis is inadvisable, since tamsulosin largely binds to blood plasma proteins. To prevent further absorption of the drug, it is advisable to wash the stomach, taking activated charcoal or osmotic laxative, for example sodium sulfate.

Interaction:

When tamsulosin was prescribed together with agenolol, enalapril, nifedipine and theophyllium, no drug interaction was found.

With the simultaneous use of tamsulosin with cimetidine, a slight increase in the concentration of tamsulosin in the blood plasma was noted, with furosemide a decrease in concentration, but this requires a dose adjustment, since the concentration of tamsulosin remains within the normal range.

Diazepam, propranolol, trichloromethiazide, chloromadinone, amitriptyline, diclofenac, glibenclamide, simvastatin and warfarin do not change the free fraction of tamsulosin in human plasma in vitro. In its turn, tamsulosin also does not change free fractions of diazepam, nrpra-nanolol, trichloromethiazide and chloromadinone.

Diclofenac and warfarin can increase the rate of excretion of tamsulosin.

In studies in vitro no interaction was found at the level of hepatic metabolism with amitriptyline, salbutamol, glibenclamide, and finasteride. Simultaneous administration of tamsulosin with strong inhibitors of isoenzyme CYP3A4 can lead to an increase in the concentration of tamsulosin. Simultaneous administration with kostokonazol (strong inhibitor of isoenzyme CYP3A4) led to an increase in the area under the pharmacokinetic curve (AUC) and the maximum concentration (C_max) of tamsulosin in 2.8 and 2.2 times, respectively.

Tamsulosin should be given in combination with strong inhibitors of the isoenzyme CYP3A4 in patients with a metabolic isoenzyme disorder CYP2D6. The drug should be used with caution in combination with strong and moderate inhibitors of the isoenzyme CYP3A4.

Simultaneous administration of tamsulosin and paroxetine, a strong inhibitor of isoenzyme CYP2D6, led to an increase in C_max and AUC tamsulosin in 1.3 and 1.6 times, respectively, but this increase is clinically insignificant.The simultaneous use of tamsulosin with other α1-blockers can lead to a decrease in blood pressure.

Special instructions:

As with the use of other α1 adrenoblockers, in the treatment of tamsulosin in some cases, there may be a decrease in blood pressure, which sometimes can lead to a fainting condition. At the first signs of orthostatic hypotension (dizziness, weakness), the patient must sit or lie down and remain in this position until the signs disappear.

Before the appointment of tamsulosin therapy, it is necessary to exclude the presence of other diseases in the patient, which can cause the same symptoms as benign prostatic hyperplasia.

Before the start of treatment and regularly during therapy, a digital rectal examination and, if necessary, the definition of a prostatic specific antigen (PSA) should be performed.

Treatment with tamsulosin in patients with severe renal insufficiency (creatinine clearance less than 10 ml / min) requires caution, studies in this category of patients were not conducted.

In some patients who have or have previously taken tamsulosin, during the operation of operations for cataracts or glaucoma may develop a syndrome of intraoperative instability of the iris (narrow pupil's syndrome), which can lead to complications during surgery or in the postoperative period. The feasibility of abolishing tamsulosin therapy for
1-2 weeks before surgery for cataracts or glaucoma is not proven. Cases of intraoperative iris of the iris occurred in patients who stopped taking the drug and at an earlier time before the operation. It is not recommended to begin therapy with tamsulosin in patients who are scheduled for surgery for cataract or glaucoma. During the preoperative examination of the patients, the surgeon and the ophthalmologist must consider whether the patient is taking or taking the patient tamsulosin. This is necessary to prepare for the possibility of development during the operation of intraoperative iris of the eye.

If angioedema develops, the drug should be discontinued immediately. Re-administration of tamsulosin is contraindicated.

With renal failure, as well as with mild and moderate hepatic insufficiency, nc requires correction of the dosing regimen.

Effect on the ability to drive transp. cf. and fur:

Studies on the effects of tamsulosin on the ability to manage vehicles and mechanisms have not been conducted. But, given the possibility of dizziness, care must be taken when driving a car and engaging in other potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Capsules with sustained release of 0.4 mg.

10, 15 or 20 capsules in a contour cell box made of a polyvinylchloride film and aluminum foil.

30, 60 or 90 capsules in a can of high-density polyethylene.

1, 3 or 6 contour cell packs of 10 capsules, 2, 4 or 6 out-of-round cell packs of 15 capsules, 3 out-of-round packagings but 20 capsules or one can, together with instructions for medical use in a pack of cardboard.

Packaging:(10) - packings, cellular, outline (1) - packs, cardboard
(10) - packings, cellular, outline (3) - packs, cardboard
(10) - packings, cell planimetric (6) - packs cardboard
(15) - packings, cellular, outline (2) - packs, cardboard
(15) - packings cellular planimetric (4) - packs cardboard
(15) - packings, cellular, outline (6) - packs, cardboard
(20) - packings, cellular, outline (3) - packs, cardboard
(30) - polyethylene cans (1) - packs of cardboard
(60) - polyethylene cans (1) - packs cardboard
(90) - polyethylene cans (1) - packs cardboard

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use but expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002820

Date of registration:14.01.2015

The owner of the registration certificate:VERTEKS, AO VERTEKS, AO Russia

Manufacturer: & nbsp

VERTEKS, AO Russia

Information update date: & nbsp30.08.2015

Illustrated instructions

Instructions

Tamsulosin (Tamsulosin)