FOKUSIN

Active material: Tamsulozin
When ATH: G04CA02
CCF: Preparation, used in violation of urination, associated with benign prostatic hyperplasia. Alpha₁-adrenoblokator
Codes ICD-10 (testimony): N40
When CSF: 28.01.02.01
Manufacturer: ZENTIVA a.s. (Czech Republic)

Pharmaceutical form, composition and packaging

Modified release capsule hard gelatin, size №1, with transparent body and cap of dark blue color; contents of capsules – micropellets almost white.

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

Ingredients of the capsule shell: azoruʙin, dye patent blue V (Patent blue V), gelatin.

10 PC. – blisters (3) – packs cardboard.
10 PC. – blisters (9) – packs cardboard.
10 PC. – blisters (10) – packs cardboard.

Pharmacological action

Блокатор a₁-adrenoreceptorov. Selectively and competitively blocks postsynaptic α_1A– adrenoreceptory, located in the smooth muscle of the prostate, bladder neck and prostatic urethra, and α_1D-adrenoreceptory, predominantly located in the body of the bladder. This reduces the tone of smooth muscles of the prostate, bladder neck and prostatic urethra and improve the function of the detrusor. This reduces the symptoms of obstruction and irritation, associated with benign prostatic hyperplasia. Usually, the therapeutic effect develops after 2 weeks after the start of dosing, although in some patients the decrease in symptoms is observed after the first dose.

The ability to influence the α tamsulosin_1A-adrenergic receptors in the 20 times greater than its ability to interact with the α_1B-adrenoreceptor, which are located in vascular smooth muscle. With such a high selectivity drug does not cause any clinically significant reduction in systemic blood pressure in patients with hypertension, and in patients with normal baseline BP.

Pharmacokinetics

Absorption

After oral tamsulosin rapidly and almost completely absorbed from the gastrointestinal tract. Bioavailability – about 100%.

After receiving a single oral dose of the drug 400 µg C_max of active substance in plasma achieved through 6 no.

Distribution

In the equilibrium state (through 5 day course taking) C values_max the active substance in blood plasma 60-70% higher, than C_max after a single dose of the drug.

Plasma protein binding – 99%. Tamsulosin has a slight V_d – about 0.2 l / kg.

Metabolism

Tamsulosin is not exposed to the effect of “first pass” and slowly biotransformed in the liver to pharmacologically active metabolites, maintain a high selectivity for the α_1A-adrenoceptor. Most of the active substance present in the blood in an unmodified form.

Deduction

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

T_1/2 tamsulosin in single dose -10 no, after multiple dose -13 no, final T_1/2 – 22 no.

Testimony

- Treatment of functional disorders in benign prostatic hyperplasia.

Dosage regimen

The drug is administered orally at a dose 400 g (1 caps.) per day.

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

Side effect

CNS: rarely – headache, dizziness, asthenia, sleep disturbance (drowsiness or insomnia).

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 a few cases – orthostatic hypotension, tachycardia, heartbeat, chest pain.

Allergic reactions: in some cases – skin rash, itch, angioedema.

Other: rarely – backache, rhinitis.

Contraindications

- Hypersensitivity to the drug.

FROM caution used in chronic renal failure (CC less than 10 ml / min), hypotension (incl. orthostatic), severe hepatic insufficiency.

Cautions

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, require high concentration and speed of psychomotor reactions.

Overdose

There were no cases of acute overdose.

Symptoms: theoretically possible occurrence of acute hypotension.

Treatment: spend cardiotropic therapy. If symptoms persist, enter obemozameschayuschie solutions or vasoconstrictor drugs. To prevent further absorption of tamsulosin possible gastric lavage, administration of activated charcoal or osmotic laxative.

Drug Interactions

With simultaneous application of cimetidine increases the concentration of tamsulosin in plasma, furosemid – decreases (significant clinical value has).

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

Concomitant use of tamsulosin with other α₁-blockers can lead to a marked increased hypotensive effect.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

No special storage conditions requires. Keep out of the reach of children. Shelf life – 2 year.