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

Description:Hard gelatin capsules number 1, body and lid yellow. The contents of capsules are micro granules of a spherical shape, white or white with a light yellow hue of color.

Pharmacotherapeutic group:alpha1-blocker

ATX: & nbsp

G.04.C.A.02 Tamsulosin

Pharmacodynamics:

Tamsulosis is a specific blocker postsynaptic α1-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 - adrenergic receptors tamsulosin leads to a decrease in tone smooth musculature prostate, bladder neck and prostatic part of the urethra and improve urine outflow. Simultaneously decrease as symptoms emptying, and the symptoms of filling, due to the increased tone of smooth muscles and detrusor gipsekstivnostyo with benign hyperplasia prostate cancer. Ability tamsulosin impact on α1A-subtype of adrenergic receptors is 20 times greater than its ability to interact with α1 AT 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 blood pressure (BP) in patients with arterial hypertension, or in patients with normal blood pressure.

Pharmacokinetics:

Bioavailability of the drug is about 100%. After oral administration tamsulosin quickly and almost completely absorbed in the digestive tract: with a single intake of 0.4 mg of the drug - the maximum concentration of tamsulosin in the blood plasma is achieved after 6 hours. In a state of equilibrium concentration (after 5 days of course-taking), the maximum concentration of tamsulosin in the blood plasma at 60- 70% higher than after a single dose. Binding to plasma proteins - 99%.The volume of distribution is 0.2 l / kg; The drug is not affected by the effect of the first passage and slowly metabolized in the liver with the formation of pharmacologically active metabolites, also having a high selectivity to α1A adrenoreceptors. Most of the tamsulosin is present in the blood in unchanged form. The drug and its metabolites are excreted by the kidneys, while about 9% of the drug is excreted in an unchanged form. The half-life for a single dose is 10-12 hours.

Indications:

Treatment of dysuric disorders in benign hyperplasia

of the glands.

Contraindications:

Hypersensitivity to tamsulosin or any other component of the drug.

Orthostatic hypotension (including in the anamnesis).

Heavy hepatic failure.

Age under 18 years (due to lack of clinical data). The drug is not used in women.

Carefully:severe renal failure (creatinine clearance less than 10 ml / min).

Pregnancy and lactation:

The drug Tamsulon 0.4 mg in capsules is intended for use only in males.

Dosing and Administration:

Adults over 18 years, as well as elderly patients

Inside, after breakfast, washing down with water, take 1 capsule (0.4 mg) 1 time per day. Capsule is not recommended to chew, as this can affect the release rate of the drug.

In patients with impaired liver and kidney function With renal failure, as well as with mild to moderate hepatic insufficiency is not required dose adjustment.

Side effects:

Undesirable reactions are listed below for organs and systems with the frequency of their occurrence. Classification of the incidence of adverse events (WHO): very often> 1/10: often from> 1/100 to <1/10: infrequently from> 1/1000 to <1/100; rarely from> 1/10000 to <1/1000; very rarely from <1/10000, including individual messages.

Disorders from the cardiovascular system: infrequent heartbeat, orthostatic hypotension.

Disorders from the gastrointestinal tract: infrequently - constipation, diarrhea, nausea, vomiting; frequency unknown - dry mouth.

Disorders from the metabolism and nutrition: infrequently, asthenia.

Impaired nervous system: often - dizziness (1.3%); infrequently - a headache; rarely - faint.

Disorders from the reproductive system: often - violations of ejaculation (including, retrograde ejaculation, ejaculatory failure); very rarely - priapism.

Disturbances from the respiratory system, chest and mediastinal organs: infrequently - rhinitis; frequency unknown - epistaxis.

Disturbances from the skin and subcutaneous tissue: infrequently - a rash, itching, hives; rarely angioedema; very rarely - Stevens-Johnson syndrome; frequency is unknown - multiforms uniting exudate erythema.

The cases of intraoperative instability of the iris of the eye (narrow-pupil syndrome) are described in surgery for cataract and glaucoma in patients taking tamsulosin.

In addition to the side effects,

described above, when using gamsulosin, 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 the reception of tamsulozn.

Overdose:

There were no cases of acute drug overdose. Symptoms: it is theoretically possible the occurrence of orthostatic hypotension.

Treatment: Carry out cardiotropic therapy. If symptoms persist, replace vasoconstrictive solutions or vasoconstrictors. To prevent further absorption of tamsulosin, gastric lavage is possible, activated carbon or osmotic laxative.

Interaction:In the appointment of gamsulosin together with atenolol, epalapril or theophylline no interactions were found. With the simultaneous use of tamsulosin with cimetidine, a slight increase in the concentration of gamsulosin in the blood plasma was observed, and with furosemide a decrease in concentration, but this does not require a change in the dose of gamlosulosin, since the drug concentration remains within the normal range. Diazepam, iropraiolol, trichloromstiazide, chloromadia. amitriptylmn, diclofenac, glibenclamide, simvastatin and warfarin do not change the content of the free tamsulose fraction in human blood plasma in vitro. In its turn, tamsulosin also does not change free fractions of diazepam, propranolol, trichloromethiazide and chloromadinone.

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

The simultaneous use of tamsulosin with strong inhibitors of isofermsite CYP3A4 can lead to an increase in the concentration of tamsulosin. Simultaneous use with ketoconazole (strong inhibitor of isofermsite CYP3A4) led to an increase in the area under the pharmacokinetic curve "concentration-time" (AUC) and the maximum concentration (Stach) of tamsulosin in 2.8 and 2.2 times, respectively.

Tamsulosin hydrochloride should not be used in combination with strong inhibitors of isoenzyme CYP3A4 in patients with a metabolic disorder of isofermsite CYP2D6. The drug should be used with caution in combination with strong and moderate inhibitors of the isoenzyme CYP3A4.

Simultaneous use of tamsulosin and paroxetine, a strong inhibitor of isoenzyme CYP2D6. led to an increase in the maximum concentration (Stach) and the area under the pharmacokinetic curve "concentration-time" (AUC) tamsulosin in 1.3 and 1.6 times, respectively, but this the increase is clinically insignificant. Simultaneous use of other antagonists α1-adrenoreceptor can lead to a decrease in blood pressure.

Special instructions:

As with other α1-adrenergic blockers,when treated with Tamsulon®, in some cases, a decrease in blood pressure may occur, which can sometimes lead to a fainting condition. At the first signs of orthostatic hypotension (dizziness, weakness), the patient should sit or lie down and remain in this position until then. until these symptoms disappear.

Before starting therapy with Tamsulon®, the patient should be examined to exclude the presence of other diseases that can cause the same symptoms as benign prostatic hyperplasia. Before the beginning of treatment and regularly during therapy, a digital rectal examination should be performed and, if required, determination of prostatic specific antigen (PSA).

Treatment with Tamsulon® for patients with severe renal insufficiency (creatinine clearance <10 ml / min) requires caution, because Research in this category of patients was conducted. In some patients taking or previously taking tamsulosin hydrochloride, during the surgery for cataract and glaucoma, there was a development of intraoperative iris of the iris (narrow pupil syndrome) syndrome,which can lead to complications during surgery or in the postoperative period. The expediency of the abolition of tamsulosin hydrochloride therapy for 1 to 2 weeks before the surgery but for cataracts or glaucoma has not yet 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 hydrochloride 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 the operation of intraoperative iris of the eye.

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

Studies on the effect of the drug on the ability to drive vehicles and mechanisms were not conducted. Patients should be aware that dizziness may occur when taking the drug. During the treatment period, care must be taken when driving vehicles and other occupationspotentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Capsules of prolonged action 0.4 mg.

10 capsules per contour cell packaging made of polyvinylchloride film and aluminum foil printed lacquered. For 1, 3 or 9 contour cell packs, together with instructions for medical use, are put in a cardboard box or in a pack of cardboard.

For 10, 30 or 90 capsules in polymeric bottles materials for medicines. Sealed with a plastic lid, with or without first opening.

On the bottles stick labels from writing paper or label or self-adhesive label.

1 bottle together with instructions for use put a pack of cardboard in a pack.

On a pack put marking by a typographical method.

Packaging:(10) - packings, cellular, outline (1) - packs, cardboard
(10) - packings, cellular, outline (3) - packs, cardboard
(10) - packings, cellular planimetric (9) - packs cardboard
(10) - polymer bottles (1) - packs of cardboard
(30) - polymer bottles (1) - packs cardboard
(90) - polymer bottles (1) - packs cardboard

Storage conditions:In dry, protected from light and out of reach of children at a temperature of no higher than 25 ° C.

Shelf life:

2 years: Do not use after the expiry date stated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-000859

Date of registration:15.06.2011

The owner of the registration certificate:FARM-SYNTHESIS, CJSC FARM-SYNTHESIS, CJSC Russia

Manufacturer: & nbsp

FARMPROJECT, CJSC Russia

Information update date: & nbsp30.08.2015

Illustrated instructions

Instructions

Tamsulon® (Tamsulon®)