Focusin, 0.4 mg 90 pcs.

Tamsulosin selectively and competitively blocks postsynaptic a1A-adrenoreceptors located in the smooth muscles of the prostate, bladder neck and prostatic part of the urethra as well as a1D-adrenoreceptors mainly located in the bladder body.

This results in decrease of tone of smooth muscles of the prostate, bladder neck and prostatic part of the urethra and improvement of detrusor function. This decreases symptoms of obstruction and irritation associated with benign prostatic hyperplasia.

Therapeutic effect usually develops within 2 weeks after the start of therapy, although some patients have less symptoms after the first dose.

The ability of tamsulosin to affect a1A-adrenoreceptors is 20 times greater than its ability to interact with a1B-adrenoreceptors which are located in vascular smooth muscle. Due to this high selectivity, the drug does not cause any clinically significant reduction in systemic arterial blood pressure (BP) both in patients with arterial hypertension and in patients with normal baseline BP.

Pharmacokinetics

Intake

After oral administration, tamsulosin is rapidly and almost completely absorbed from the GI tract. The bioavailability of the drug is about 100%. After a single oral dose of 400 mcg the Cmax of the active substance in plasma is reached after 6 hours.

Distribution

In equilibrium state (after 5 days of therapy) the Cmax( of active substance in plasma is 60-70% higher than Cmax after a single dose of the preparation. Binding to plasma proteins is 99%. Tamsulosin has low volume of distribution (approximately 0.2 l/kg).

Metabolism

Tamsulosin does not undergo “first pass” effect and is slowly biotransformed in the liver to form pharmacologically active metabolites with high selectivity for a1-adrenoreceptors. Most of the active substance is present in the blood unchanged.

Tamsulosin is excreted by the kidneys; 9% of the dose is excreted unchanged.
Tamsulosin T1/2 at single administration is 10 h; after multiple administration – 13 h; final elimination half-life – 22 h.

Indications

Treatment of functional disorders in benign prostatic hyperplasia.

Active ingredient

How to take, the dosage

Focusin is administered orally in a dose of 400 mcg (1 capsule) per day.

The capsules are taken after the first meal with plenty of water.

The capsule should not be chewed.

Interaction

Cimetidine increases plasma concentrations, furosemide decreases them (no significant clinical relevance).

Diclofenac and indirect anticoagulants slightly increase the excretion rate of tamsulosin.

The concomitant use of tamsulosin with other alpha1-adrenoblockers may lead to markedly increased hypotensive effect.

Special Instructions

Tamsulosin should be used with caution in patients with a predisposition to orthostatic hypotension. At the first signs of orthostatic hypotension (dizziness, weakness) the patient should be seated or laid down.

The diagnosis must be verified before starting to use the drug.

At the time of treatment, caution should be exercised when driving motor vehicles and engaging in other potentially hazardous activities requiring increased concentration and rapid psychomotor reactions.

Contraindications

Hypersensitivity to the components of the drug.

With caution: chronic renal failure (decreased creatinine clearance below 10 ml/min), arterial hypotension (including orthostatic), severe hepatic failure.

Side effects

Rarely – headache, dizziness, asthenia, sleep disturbance (drowsiness or insomnia), retrograde ejaculation, decreased libido, back pain, rhinitis, nausea, vomiting, constipation or diarrhea.

In single cases, orthostatic hypotension, tachycardia, palpitations, chest pain.

In extremely rare cases – hypersensitivity reactions (skin rash, itching, angioedema).

Overdose

No cases of acute overdose of the drug have been reported.

Symptoms: acute hypotension is theoretically possible.

Treatment: cardiotropic therapy is carried out. If symptoms persist, replacement solutions or vasoconstrictors should be administered.

In order to prevent further absorption of tamsulosin, gastric lavage, or administration of activated charcoal or osmotic laxatives may be indicated.

Similarities