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

1 tablet contains: active substance tamsulosin hydrochloride 0.4 mg; Excipients: cellulose microcrystalline 47.0 mg, macrogol 200.0 mg, silicon colloidal dioxide 1.3 mg, magnesium stearate 1.3 mg; shell: Fell yellow 03F32784 (Hypromellose 6cR 5.21520 mg, titanium dioxide (E 171) 1.03425 mg, macrogol-8000 0.97680 mg, iron oxide yellow dye (E172) 0.27300 mg, iron oxide red oxide (E172) 0.00075 mg ).

Description:Yellow biconvex oval tablets covered with a film sheath, engraved with "T04" on one side. On the cross-section - the core is from white to almost white.

Pharmacotherapeutic group:alpha1-blocker

ATX: & nbsp

G.04.C.A.02 Tamsulosin

Pharmacodynamics:

Tamsulosin is a specific competitive blocker for postsynaptic alpha 1-adrenergic receptors, especially alpha1 and alpha-1D-adrenergic receptors, responsible for relaxing the smooth muscles of the prostate, bladder neck and prostatic urethra. Tamsulosin increases the maximum rate of urination, reduces the tone of the smooth muscles of the prostate and urethra, improving the outflow of urine and, thus,reducing the severity of symptoms of filling and emptying, in the development of which an important role plays the detrusor's hyperactivity.

Tamsulosin reduces the symptoms of obstruction and irritation of the lower parts of the urinary tract associated with benign prostatic hyperplasia.

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

Blockers of alpha 1-adrenergic receptors can reduce blood pressure (BP) by decreasing peripheral resistance of blood vessels. Clinically significant decrease in blood pressure was not observed.

Pharmacokinetics:

Suction. After ingestion of tamsulosin in the form of long-acting tablets, 57% of the dose taken is absorbed in the intestine. Eating does not affect the degree and rate of absorption of tamsulosin. Tamsulosin characterized by linear kinetics. After a single oral administration of an empty tablet 0.4 mg maximum concentration (C_max) of tamsulosin in blood plasma is achieved after 6 hours. In the equilibrium state, which is reached by the 4th day of intake, C_max tamsulosin is achieved in 4-6 h as an empty stomach, and after eating. FROM_max tamsulosin increases from about 6 ng / ml (after a single dose) to 11 ng / ml (in the equilibrium state). The minimum concentration of tamsulosin is 40% of C_maxtamsulosin both on an empty stomach and after a meal. There are significant individual differences among patients on the concentration in the blood plasma after taking a single dose and repeated intake.

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

Metabolism. Tamsulosin is not exposed to the effect of "first passage" and is slowly metabolized in the liver with the formation of less active metabolites. Most of tamsulosin is present in the blood plasma unchanged. The ability of tamsulosin to induce the activity of microsomal liver enzymes is negligible.

With a mild and moderate degree of hepatic insufficiency, there is no need for correction of the dosing regimen.

Excretion. Tamsulosin and its metabolites are mainly excreted by the kidneys, with about 4-6% of tamsulosin excreted unchanged.

The half-life of tamsulosin in the form of long-acting tablets with a single administration and in an equilibrium state is 19 hours and 15 hours, respectively.

Indications:Treatment of dysuric disorders in benign prostatic hyperplasia.

Contraindications:

Hypersensitivity to tamsulosin and other components of the drug; orthostatic hypotension, including in history; severe hepatic impairment; children's age till 18 years.

Carefully:

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

Pregnancy and lactation:Tamsulosin-Teva is not used in women.

Dosing and Administration:

Inside, regardless of food intake. Tablets are not recommended to break or chew, as this can affect the release rate of tamsulosin.

1 tablet (0.4 mg) once a day. The duration of use is not limited, the drug Tamsulosin-Teva is used in the form of continuous therapy.

Side effects:

Side effects are classified according to the following frequency: very often - not less than 10%; often - not less than 1%, but less than 10%; infrequently - not less than 0,1%,but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01%; unknown frequency (can not be estimated from available data).

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

From the side of the organ of vision: unknown frequency - impaired vision, blurred vision.

From the cardiovascular system: infrequently - orthostatic hypotension, palpitation.

From the respiratory system: infrequently - rhinitis.

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

From the genitourinary system: often - violation of ejaculation; very rarely - priapism; unknown frequency - retrograde ejaculation, ejaculatory failure. From the skin and subcutaneous tissues: infrequently - skin rash, itching, hives; rarely - angioedema; very rarely - Stevens-Johnson syndrome; unknown frequency - erythema multiforme, exfoliative edema.

Other: infrequently - asthenia; unknown frequency - epistaxis. Postmarketing application

The cases of development of intraoperative syndrome of the unstable iris of the eye (ISNR) (narrow pupil syndrome) are described in case of operative intervention for cataract in patients taking tamsulosin.

From the cardiovascular system: unknown frequency - atrial fibrillation, arrhythmia, tachycardia.

On the part of the respiratory system, unknown frequency - shortness of breath.

Overdose:

Symptoms. An overdose of tamsulosin can be accompanied by a pronounced hypotensive effect. Cases of orthostatic hypotension were observed with varying degrees of overdose.

Treatment: symptomatic. To normalize blood pressure and heart rate, you must put the patient in a horizontal position. If this is not enough, introduce plasma-substituting solutions or vasoconstrictor drugs. It is necessary to monitor kidney function. To prevent further absorption of tamsulosin, the stomach is washed, applied Activated carbon and / or osmotic laxatives. Dialysis is ineffective.

Interaction:

With simultaneous use of tamsulosin with atenolol, enalapril, nifedipine or theophylline no interactions were found.

With simultaneous use with cimetidine, a slight increase in the concentration of tamsulosin in the blood plasma was noted, and with furosemide a decrease in the concentration of furosemide, but this does not require changes in the doses of tamsulosin,since the concentrations of tamsulosin in these cases remain 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, propranolol, trichloromethiazide and chloromadinone.

In studies in vitro no interaction was found at the level of microsomal liver enzymes with amitriptyline, salbutamol, glibenclamide, and finasteride. Diclofenac and warfarin can increase the rate of excretion of tamsulosin. Simultaneous use of tamsulosin with potent inhibitors of isoenzyme CYP3A4 may increase the effect of tamsulosin. When used simultaneously with ketoconazole (a known potent inhibitor CYP3A4) the area under the "concentration-time" curve increases (AUC) and C_max tamsulosin with a coefficient of 2.8 and 2.2, respectively. Tamsulosin Do not use simultaneously with powerful inhibitors CYP3A4 in patients with a phenotype of slow isoenzyme metabolism CYP2D6.

With the simultaneous use of tamsulosin with paroxetine (a potent inhibitor of isoenzyme CYP2D6) AUC and C_max tamsulosin increased by 1.3 and 1.6 times, respectively, but this increase was not clinically significant.

The simultaneous use of other antagonists of alpha1-adrenergic receptors may lead to a decrease in blood pressure.

Special instructions:

As with the use of other alpha1-adrenoblockers, when treated with Tamsulosin-Teva, in some cases there may be a decrease in blood pressure, which can sometimes lead to fainting. At the first signs of orthostatic hypotension (dizziness, weakness), the patient should sit or lie down and remain in this position until these symptoms disappear.

Due to the lack of data on the use of tamsulosin in patients with severe renal insufficiency (CC less than 10 ml / min), treatment of such patients should be done with caution.

During surgery for cataracts in some patients who had previously taken tamsulosin, ECRI can develop, which can increase the risk of complications from the organ of vision during and after surgery.It is considered useful to cancel tamsulosin 1-2 weeks before surgery for cataracts, but the benefits of cessation of treatment with tamsulosin have not yet been confirmed. There are reports of the development of ICPH in patients who stopped taking tamsulosin long before surgery. It is not recommended to use the drug Tamsulosin-Teva in patients who are scheduled surgical intervention for cataracts. When preparing for an operative intervention for cataracts, the surgeon must take into account the possibility of developing ECRI and have the necessary means to treat ICPH if it develops during the operation.

Before starting therapy with tamsulosin, the patient should be examined to exclude other diseases that can cause the same symptoms as benign prostatic hyperplasia. Before and during treatment, a digital rectal examination and, if necessary, a determination of the concentration of the prostatic specific antigen to exclude prostate cancer.

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

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions, due to the possibility of dizziness.

Form release / dosage:

Tablets of prolonged action, film-coated, 0.4 mg.

For 10 tablets in blisters OPA / aluminum foil / PVC.

1, 2, 3, 5, 6, 9, 10, 20 blisters with instructions for use in a cardboard bundle.

For 7 tablets in blisters OPA / aluminum foil / PVC.

2, 4, 8 blisters with instructions for use in a cardboard pack.

Packaging:(10) - blisters (1) - packs of cardboard
(10) - blisters (10) - packs of cardboard
(10) - blisters (2) - packs cardboard
(10) - blisters (20) - packs cardboard
(10) - blisters (3) - packs cardboard
(10) - blisters (5) - packs of cardboard
(10) - blisters (6) - packs cardboard
(10) - blisters (9) - packs cardboard
(7) - blisters (2) - packs cardboard
(7) - blisters (4) - packs cardboard
(7) - blisters (8) - packs cardboard

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-002615

Date of registration:05.09.2014

The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel

Manufacturer: & nbsp

TEVA Pharmaceutical Works Private, Ltd. Co. Hungary

Information update date: & nbsp30.08.2015

Illustrated instructions

Instructions

Tamsulosin-Teva (Tamsulosin-Teva)