Expiration date: 04/2025

Release form and composition: 

Capsules modified release hard gelatin size ?1, with transparent body and cap of dark blue color contents of capsules - micropellets almost white.

One capsule contains: tamsulosin hydrochloride 400 mcg

Excipients: copolymer of methacrylic acid with ethyl acrylate (1: 1) 30% dispersion, microcrystalline cellulose, dibutilsebaktat, polysorbate 80, colloidal silicon dioxide, talc.

The composition of the capsule shell: azorubin, dye Patent Blue V (Patent bue V), gelatin.

10 pieces. - Blisters (3) - packs cardboard.

10 pieces. - Blisters (9) - packs cardboard.

10 pieces. - Blisters (10) - packs cardboard.

Pharmachologic effect:

Blocker apha1-adrenergic receptors. Selectively and competitively blocks postsynaptic adrenoceptors apha1A- located in the smooth muscle of the prostate, bladder neck and prostatic urethra and apha1D-adrenergic receptors located predominantly in the body of the bladder. This leads to a reduction in smooth muscle tone of the prostate, bladder neck and prostatic urethra and detrusor improve function. This reduces the symptoms of obstruction and irritation associated with benign prostatic hyperplasia. Typically, the therapeutic effect develops within 2 weeks after receiving the drug, although some patients marked reduction of symptoms after the first dose.

The ability to influence the tamsulosin apha1A-adrenoceptors 20 times greater than its ability to interact with apha1B-adrenoceptors are located in vascular smooth muscle. Due to such a high selectivity of the drug does not cause any clinically significant reduction in systemic blood pressure both in hypertensive patients and in patients with normal baseline BP.

Pharmacokinetics:

Suction

After oral tamsulosin is rapidly and almost completely absorbed from the gastrointestinal tract. The bioavailability of the drug - about 100%.

After a single oral administration at a dose of 400 mg Cmax of the active substance in plasma is reached after 6 hours.

Distribution

In the equilibrium state (after 5 days course doses) Cmax value of the active substance in plasma at 60-70% higher than the Cmax after a single dose.

Binding to plasma proteins - 99%. Tamsulosin has a slight Vd - about 0.2 l / kg.

Metabolism

Tamsulosin is not subject to first-pass effect and is slowly biotransformed in the liver with the formation of pharmacologically active metabolites that retain high selectivity to apha1A-adrenoceptor. Most of the active substance is present in blood in an unmodified form.

breeding

Tamsulosin excreted by the kidneys, 9% of the dose is excreted unchanged.

T1 / 2 with single dose of tamsulosin -10 hours after multiple dose -13 h, the final T1 / 2 - 22 hours.

Indications:

• Treatment of functional disorders in benign prostatic hyperplasia.
  

Dosage and administration:

The drug is administered orally at a dose of 400 mg (1 capsule.) / Day.

Capsules are taken after the first meal, drinking plenty of water. The capsule is not recommended to chew.

Side effects:

CNS: rarely - headache, dizziness, fatigue, sleep disturbance (insomnia or drowsiness).

On the part of the reproductive system: rarely - retrograde ejaculation, decreased libido.

From the digestive system: rarely - nausea, vomiting, constipation or diarrhea.

Cardio-vascular system: in rare cases - orthostatic hypotension, tachycardia, palpitations, chest pain.

Allergic reactions: in some cases - skin rash, itching, angioedema.

Other: rarely - back pain, rhinitis.

Contraindications:

• Hypersensitivity to the drug.
  

To apply caution in patients with chronic renal insufficiency (creatinine clearance less than 10 ml / min), hypotension (including orthostatic), severe hepatic insufficiency.

Special instructions:

Caution should be used tamsulosin in patients with a predisposition to orthostatic hypotension. At the first signs of orthostatic hypotension (dizziness, weakness), the patient should sit or lay.

Before the start of the drug is necessary to verify the diagnosis.

Effects on ability to drive vehicles and management mechanisms

During treatment, the patient should be careful when driving and occupation of other potentially hazardous activities that require high concentration and psychomotor speed reactions.

Overdose:

There were no cases of acute drug overdose.

Symptoms: theoretically may cause acute hypotension.

Treatment: kardiotropnyh therapy. If the symptoms persist, you should enter obemozameschayuschie solutions or vasoconstrictor drugs. To prevent further absorption of tamsulosin may gastric lavage, activated charcoal or osmotic laxative.

Drug Interactions:

With simultaneous application of cimetidine increases the concentration of tamsulosin in plasma, furosemide - decreases (significant clinical importance has not).

Diclofenac and indirect anticoagulants increase the number of clearance rate of tamsulosin.

Concomitant use of tamsulosin with other apha1-blockers may lead to a marked strengthening of the hypotensive effect.

Conditions and terms:

Special storage conditions are required. Keep out of the reach of children. Shelf life - 2 years.