Instruction for use: Fokusin

Trade name of the drug – Fokusin

Active substance: Tamsulosinum

Dosage Form: Modified release capsule

Composition (per tablet):

active substance:Tamsulosin hydrochloride 0.4 mg

Excipients: methacrylic acid-ethyl acrylate copolymer [1: 1] [30% dispersion] * - 74.9 (in solid form), MSC - 257.1 mg; dibutyl sebacate - 8.4 mg; polysorbate 80 - 0.5 mg; colloidal silicon dioxide - 3.7 mg; Talc - 0.3 mg

capsule shell: dye azorubin - 0.2%; patented dye blue - 0.12%; Gelatin - 100%

* For a capsule dispersion with 30% methacrylic acid and ethacrylate copolymer [1: 1] in an amount of 249.67 mg, which corresponds to 74.9 mg in the form of a solid

Description of Fokusin: Hard gelatin capsules ¹1, body and cap in dark blue, transparent.

The contents of capsules: white or almost white micropellets.

Pharmacotherapeutic group:

Alpha1-blocker [alpha-blockers]

Alpha1-blocker [Drugs affecting the metabolism of the prostate gland and correctors urodynamics]

ATX G04CA02 Tamsulosin

The nosological classification (ICD-10)

N40 Hyperplasia of prostate gland: Prostate adenoma; BPH; Prostatauxe; prostate Hypertrophy; Dysuric disorders caused by benign prostatic hyperplasia; Dizuricheskie disorder with benign prostatic hyperplasia; Dysuria with prostate cancer; Benign prostatic giperpalaziya; Benign prostatic hyperplasia; Benign prostatic hyperplasia stages 1 and 2; Benign prostatic hyperplasia I degree; Benign prostatic hyperplasia II degree; Benign prostatic hypertrophy; The disease of the prostate gland; Acute urinary retention related to benign prostatic hyperplasia; Benign prostatic hyperplasia stages 1 and 2 in combination with prostatitis; paradoxical ischuria

Pharmacological Properties of Fokusin

Pharmachologic effect - Mode of action - alpha adrenoliticheskoe.

Pharmacodynamics

Tamsulosin selectively and competitively blocks postsynaptic α1A-adrenergic receptors of smooth muscles of the prostate, bladder neck and prostatic urethra and α1D -adrenoceptors bladder that leads to a reduction in smooth muscle tone of the prostate, bladder neck and prostatic urethra improve detrusor function, and reduction of obstruction and irritation symptoms associated with benign prostatic hyperplasia.

Typically, the therapeutic effect develops after 2 weeks after starting the drug, although in some patients the decrease of symptoms is observed after the first dose.

The ability to influence the tamsulosin α1A-adrenergic receptors 20 times greater than its ability to influence the α1D-adrenergic receptors of 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, its bioavailability - almost 100%. After a single dose of the drug Fokusin® oral dose of 400 mg Cmax of the active substance in plasma is reached after 6 hours.

Distribution. After 5 days of course taking the value Cmax of the active substance in plasma at 60-70% higher than the Cmax after a single dose. Binding to plasma proteins - 99%. Vd tamsulosin insignificant (about 0.2 l / kg).

Metabolism. Tamsulosin is not subjected to the effect of the first passage slowly biotransformed in the liver with the formation of pharmacologically active metabolites that retain high selectivity to α-adrenoceptor. Most of the active substance is present in the blood in an unmodified form.

Withdrawal. 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 hours, final - 22 hours.

Indications

Treatment of functional disorders in benign prostatic hyperplasia.

Contraindications

Hypersensitivity to the drug;

orthostatic hypotension (including history);

severe hepatic impairment;

age of 18 years (effectiveness and safety have been established).

Precautions: Chronic renal failure (creatinine Cl decrease below 10 ml / min); hypotension (including orthostatic); planned cataract surgery; sharing with strong or moderately active inhibitors of isoenzyme CYP3A4 (eg, ketoconazole, voriconazole).

Side effects

The frequency of adverse reactions reported in accordance with the classification of the Medical dictionary for regulatory activities (MedDRA): very common (> 10%); frequently (≥1, <10%); rare: (≥0,1, <1%); rarely (≥0,01 <0,1%); very rare (<0.01%); Frequency unknown (to determine the frequency of occurrence of the available data it is not possible).

Immune system: very rarely - hypersensitivity reaction.

From the nervous system: often - dizziness; rarely - headache; rarely - syncope; the frequency is unknown - sleep disturbance (insomnia or drowsiness).

From a sight organ: the frequency is unknown - blurred vision, blurred vision.

From the heart: Infrequent - palpitation; the frequency is unknown - tachycardia.

On the part of the vessels: rarely - orthostatic hypotension.

The respiratory system, organs, thoracic and mediastinal disorders: rarely - rhinitis; the frequency is unknown - nosebleeds.

On the part of the digestive tract: rarely - nausea, vomiting, constipation or diarrhea.

Skin and subcutaneous tissue disorders: rare - skin rash, itching, hives; rarely - angioedema; very rarely - Stevens-Johnson syndrome; the frequency is unknown - erythema multiforme, exfoliative dermatitis.

From the genitals and breast: very rarely - priapism; the frequency is unknown - ejaculation disorders, including retrograde ejaculation, decreased libido.

General disorders and administration site at: rare - asthenic syndrome; the frequency is unknown - back pain, chest pain, dry mouth.

Interaction

Concomitant use of tamsulosin with other α1-blockers may lead to blood pressure reduction.

Diclofenac and indirect anticoagulants (warfarin), a few increase the elimination rate of tamsulosin.

Cimetidine increases the concentration of tamsulosin in plasma and furosemide reduces the (substantial clinical significance has not).

In a joint application of tamsulosin with atenolol, enalapril or theophylline signs of drug interaction were absent.

In in vitro conditions diazepam, propranolol, trichloromethiazide, chlormadinone, amitriptyline, diclofenac, glibenclamide, simvastatin and warfarin did not result in the free fraction of tamsulosin in plasma changes. Tamsulosin also had no effect on the free fractions of diazepam, propranolol, trichlormethiazide and chlormadinone.

The combined use of tamsulosin and potent inhibitors of CYP3A4 may cause increased systemic exposure of tamsulosin. Simultaneous administration of tamsulosin with ketoconazole (a potent inhibitor of the isoenzyme CYP3A4) resulted in an increase in AUC and Cmax parameters tamsulosin 2.8 and 2.2 times respectively. Tamsulosin should not be used in combination with potent inhibitors of CYP3A4 isozyme phenotype in patients with slow metabolism by isoenzyme CYP2D6.

Caution should be exercised when used in conjunction with powerful tamsulosin or moderately active inhibitors of CYP3A4 isoenzyme.

Fokusin Dosage and Administration

Inside, after the first meal, not liquid, squeezed enough water. The drug is prescribed at 400 mg (1 capsule.) / Day.

Fokusin can be administered as a monotherapy or in combination with inhibitors of 5α-reductase inhibitors (finasteride, dutasteride).

Overdose

Symptoms: marked reduction of blood pressure.

Treatment: kardiotropnyh therapy, monitoring of renal function, general supportive therapy, the introduction of obemozameschayuschih solutions or vasoconstrictor drugs. To prevent further absorption of tamsulosin may gastric lavage, activated charcoal or osmotic laxative.

SPECIAL INSTRUCTIONS of Fokusin

Before starting therapy with Fokusin® neohodimo exclude the presence of other diseases that can cause the same symptoms as benign prostatic hyperplasia. Before you start treatment and regularly during therapy should be performed examinations of the prostate (digital rectal examination, PSA determination). As with other α1-adrenoceptor antagonists in the treatment of drug Fokusin® in some cases, decrease in blood pressure may occur, which may lead to fainting.

Fokusin The drug 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 sit or lay.

With the development of angioedema, as well as other immunological reactions, such as Stevens-Johnson syndrome, use of the drug should be discontinued immediately. The patient should be kept under surveillance until the elimination of the disease state; reappointment of tamsulosin is not allowed. During surgery, cataract surgery in some patients treated with tamsulosin hydrochloride at the time of operation or in the past, there has been a development of the iris syndrome intraoperative instability eyes (narrow pupil syndrome). The occurrence of intraoperative instability syndrome iris can lead to an increased risk of complications from the organ of vision during and after surgery.

tamsulosin hydrochloride should not be used in combination with potent inhibitors of CYP3A4 isozyme phenotype in patients with slow metabolism by isoenzyme CYP2D6.

Tamsulosin is not intended for use in women.

Effects on ability to drive and engage in other potentially hazardous activities. Use caution when driving and occupations that require high concentration and speed of psychomotor reactions. In the event of dizziness should refrain from road management and other potentially hazardous activities.

Release Form

Modified release capsule, 0.4 mg. On 10 caps. in blister PVC / PVDC / A1. 3, 9 or 10 bl. in a cardboard bundle.

Manufacturer

Producer and packer (primary packaging): Zentiva sg Czech Republic. In kabelovny 130, 102 37 Prague 10, Dolní Měcholupy, Czech Republic; Zentiva AS, the Slovak Republic. Nitrianska 100 920 27 Hlohovec, Slovak Republic.

Packer (secondary (consumer) packaging) and producing quality control: Zentiva sg Czech Republic; Zentiva AS, the Slovak Republic. OJSC Pharmstandard-Leksredstva, 305022, Russia, Kursk, st. 2nd Aggregate 1a / 18.

The owner of the registration certificate. Zentiva cc, the Czech Republic, have kabelovny 130, 102 37 Prague 10, Dolní Měcholupy, Czech Republic.

Claims the quality of the drug sent to: 125009, Russia, Moscow, ul. Tverskaya, 22.

Phone: (495) 721-14-00; fax: (495) 721-14-11.

Storage conditions of Fokusin

In ordinary conditions.

Keep out of the reach of children.

Shelf life

2 years.

Do not use beyond the expiration date printed on the package.

Conditions of supply of pharmacies

On prescription.