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

Excipients: hypromellose (hydroxypropylmethylcellulose) 75 mg, silicon dioxide colloid 1.2 mg, lactose monohydrate 12 mg, magnesium stearate 2.4 mg, microcrystalline cellulose 149 mg;

film sheath: Opadrai II yellow 7 mg, including: [polyvinyl alcohol 2,8 mg, macrogol (polyethylene glycol) 1.414 mg, talc 1.036 mg, titanium dioxide 1.645 mg, iron oxide dye yellow 0.105 mg].

Description:

The tablets are round biconvex, covered with a film coat of yellow color. On the cross-section - the core is almost white.

Pharmacotherapeutic group:Alpha-blocker

ATX: & nbsp

G.04.C.A.02 Tamsulosin

Pharmacodynamics:

Tamsulosin is a specific competitive blocker of postsynaptic α1-adrenoceptors, especially α_1Aand α₁_D subtypes responsible for relaxing the smooth muscles of the prostate gland, the neck of the bladder and the prostatic part of the urethra. Tamsulosin at a dosage of 0.4 mg increases the maximum rate of urination, and also reduces the tone of the smooth muscles of the prostate and urethra, improving the outflow of urine and, thus, reducing the symptoms of emptying and filling the bladder. Tamsulosin also reduces the severity of filling symptoms, in the development of which an important role is played by detrusor hyperactivity.

With prolonged therapy, the effects on the symptoms of filling and emptying remain, reducing the risk of acute urinary retention and the need for prompt intervention.

Typically, the therapeutic effect develops 2 weeks after the start of the drug, although in a number of patients, the decrease in the severity of symptoms is noted after the first dose. The ability of tamsulosin to affect α_1A the adrenergic receptor subtype is 20 times greater than its ability to interact with the subtype of adrenoreceptors that are located in the smooth muscle of the vessels. Due to this high selectivity, the drug does not cause any clinically significant decrease in systemic blood pressure (BP) in patients with arterial hypertension or in patients with normal blood pressure.

When tamsulosin was used in a daily dose of 0.4 mg, no clinically significant reduction in blood pressure was noted.

Pharmacokinetics:

Suction: Tamsulosin Bacter, a sustained-release tablet coated with a coat 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 pharmacokinetics. After a single oral administration of 0.4 mg of Tamsulosin Bacteur, the maximum concentration of tamsulosin in plasma (C_max) is achieved on average in 6 hours. In the equilibrium state, which is reached by the 4th day of administration, the concentration of tamsulosin in plasma (C_ss) reaches its highest value in 4-6 hours, either on an empty stomach or after a meal. The maximum plasma concentration increases from about 6 ng / ml after the first dose to 11 ng / ml in the equilibrium state. The lowest concentration of tamsulosin in plasma is 40% of the maximum plasma concentration in the fasting and after meals.There are significant individual differences among patients with regard to the concentration of the drug in the plasma after a single dose and repeated administration.

Distribution: The connection with plasma proteins is about 99%, the volume of distribution is small (about 0.2 l / kg).

Metabolism: tamsulosin does not undergo the "first pass" effect and is slowly biotransformed in the liver to form pharmacologically active metabolites that retain high selectivity to α_1A-adrenergic receptors. Most of the tamsulosin is present in plasma in unchanged form. The ability of tamsulosin to induce the activity of microsomal liver enzymes is practically absent (experimental data). With minor and moderate hepatic insufficiency, there is no need for correction of the dosing regimen.

Excretion: tamsulosin and its metabolites are mainly derived kidneys, with approximately 9% of the drug released in unchanged form.

The half-life of the drug (T_1/2) with a single admission of 0.4 mg after a meal is 10 hours, with repeated admission - 13 hours, the final half-life is 22 hours.When renal failure is not required to reduce the dose, if the patient has severe renal failure (creatinine clearance (CC) less than 10 ml / min), the appointment of tamsulosin should be done with caution.

Indications:

Treatment of dysuric disorders in benign prostatic hyperplasia.

Contraindications:

- Hypersensitivity to tamsulosin or any other component of the drug;

- Orthostatic hypotension (including in the anamnesis);

severe hepatic impairment;

- children's age till 18 years;

- Lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

Carefully:

Severe renal failure (creatinine clearance less than 10 ml / min), arterial hypotension.

Pregnancy and lactation:

The drug Tamsulosin Bacter is intended for use only in males.

Dosing and Administration:

Inside, 1 tablet (0.4 mg) 1 time per day, regardless of food intake. Duration of use is not limited, the drug is prescribed in the form of continuous therapy.

The tablet should be taken in its entirety, it can not be chewed, since this can affect the release rate of the drug.

The withdrawal syndrome is absent.

Side effects:

The incidence of side effects developing with tamsulosin is classified according to the recommendations of the World Health Organization: very often (≥1 / 10 cases); often (≥1 / 100, <1/10 cases); infrequently (≥1 / 1000, <1/100 cases); rarely (≥1 / 10000, <1/1000 cases); very rarely (<1/10000 cases); frequency is unknown - according to available data, it was not possible to establish the frequency of occurrence.

Impaired nervous system:

often - dizziness;

infrequently - headache;

rarely - fainting, sleep disturbance (drowsiness or insomnia).

Disorders from the side of the organ of vision:

frequency unknown - intraoperative instability of the iris of the eye (narrow pupil syndrome) during surgery for cataracts, glaucoma.

Heart Disease:

infrequently - a feeling of palpitations;

rarely chest pain.

Vascular disorders:

infrequently - Orthostatic hypotension.

Disturbances from the respiratory system, organs of the thorax and mediastinum:

infrequently - rhinitis;

frequency unknown - nose bleed.

Disorders from the gastrointestinal tract:

infrequently - constipation, diarrhea, nausea, vomiting.

Disturbances from the skin and subcutaneous tissues:

infrequently - a rash, itching, hives;

rarely - angioedema;

rarely - Stevens-Johnson syndrome;

frequency unknown - erythema multiforme, exfoliative edema.

Violations of the genitals and breast. Congenital, hereditary and genetic disorders:

often - violation of ejaculation (including retrograde ejaculation, ejaculatory failure);

rarely - decreased libido, priapism.

General disorders and disorders at the site of administration:

infrequently - asthenia.

Other:

infrequently - backache.

In addition to the side effects described above, with tamsulosin, atrial fibrillation, arrhythmia, tachycardia and dyspnea were observed. Due to the fact that the data were obtained by the method of spontaneous messages in the period after registration, it is difficult to determine the frequency and cause-and-effect relationship of these phenomena with tamsulosin.

If any of the side effects indicated in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:

There are no reports of cases of acute overdose with tamsulosin.

Symptoms: lowering of arterial pressure, compensatory tachycardia. Treatment is symptomatic. Arterial blood pressure and heart rate can be restored when patients are taken to 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. It is unlikely that dialysis will be effective, since tamsulosin intensively binds to plasma proteins.

To prevent further absorption of the drug, it is advisable to wash the stomach, taking activated charcoal and osmotic laxatives.

Interaction:

When prescribing tamsulosin along with atenolol, enalapril, nifedipine or theophylline interactions were not found.

When used simultaneously with cimetidine there was a slight increase in the concentration of tamsulosin in the blood plasma, with furosemide - a decrease in concentration, however, this does not require a change in the dose of Tamsulosin Bacteur, since the drug concentration 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 the free fractions diazepam, propranolol, trichloromethiazide and chloromadinone.

In studies in vitro There was no interaction at the level of hepatic metabolism with amitriptyline, salbutamol, glibenclamide and finasteride. Diclofenac and warfarin can increase the rate of excretion of tamsulosin.

The simultaneous use of tamsulosin with strong isoenzyme inhibitors CYP3A4 can lead to an increase in the concentration of tamsulosin. Simultaneous application with ketoconazole (strong inhibitor of isoenzyme CYP3A4) led to an increase in the area under the pharmacokinetic curve "concentration-time" (AUC) and the maximum concentration (C_m_Oh) of tamsulosin in 2.8 and 2.2 times, respectively. Tamsulosin Do not administer in combination with strong inhibitors of 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, strong inhibitor of isoenzyme CYP2D6 led to an increase in C_m_Oh and AUC tamsulosin in 1.3 and 1.6 times, respectively, but this increase is clinically insignificant.

Simultaneous assignment of other α1-adrenoreceptor blockers can lead to an antihypertensive effect.

Special instructions:

As with the use of other α1adrenoblockers, 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 starting therapy with Tamsulosin Bucket, the patient should be examined to exclude the presence of other diseases that 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.

In some patients, with surgical interventions for cataracts or glaucoma on the background of taking the drug, the development of intraoperative irrosis syndrome (a narrow pupil syndrome) may occur, which can lead to complications during surgery or in the postoperative period. The feasibility of canceling tamsulosin therapy 1-2 weeks before surgery for cataracts or glaucoma has not been 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 cataracts 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 intraoperative instability of the iris of the eye.

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

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.

With renal failure, as well as with mild or moderate hepatic insufficiency, correction of the dosing regimen is not required. There are reports of cases of development of prolonged erection and priapism against the background of therapy with alpha-1-adrenergic blockers. If the erection persists for up to 4 hours, you should immediately seek medical help. If priapism therapy has not been carried out immediately, it can lead to damage to the tissues of the penis and an irreversible loss of potency.

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

Data on the negative impact on the ability to drive vehicles and engage in potentially hazardous activities are not available. Nevertheless, in connection with the possibility of dizziness, to elucidate the individual reaction of the patient, it is necessary to refrain from occupations requiring increased concentration and speed of psychomotor reactions, including driving.

Form release / dosage:

Tablets with prolonged release, film-coated, 0.4 mg.

Packaging:

10 tablets per contour cell packaging made of polyvinyl chloride film, PVC / PCTFE film or aluminum multilayer foil and aluminum lacquered aluminum foil.

For 1, 3 contour squares, together with instructions for use, are placed in a pack of cardboard.

Storage conditions:

At a temperature of no higher than 25 ° C in the manufacturer's packaging.

Keep out of the reach of children.

Terms of leave from pharmacies:On prescription

Registration number:LP-004253

Date of registration:19.04.2017

Expiration Date:19.04.2022

The owner of the registration certificate:Bakter, OOOBakter, OOO Russia

Manufacturer: & nbsp

CANONFARMA PRODUCTION, CJSC Russia

Information update date: & nbsp11.05.2017

Illustrated instructions

Instructions

Tamsulosin Bacher (Tamsulosin Bacter)