TANIZ-K

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: KRKA d.d. (Slovenia)

Pharmaceutical form, composition and packaging

Capsules of the prolonged action hard gelatin, size №2, with a corps of Orange and olive green cap with the inscription “TSL 0.4”, body and lid on top marked stripe black; contents of capsules – pellets of white or nearly white.

Excipients: microcrystalline cellulose, Copolymer of methacrylic and ètakrilovoj acid (1:1) (variance 30% (c) emulsifiers: polysorbate-80, sodium lauryl), triэtiltsitrat, talc, Purified water.

The composition of the shell capsules: iron oxide red dye (E172), Titanium dioxide (E171), dye iron oxide yellow (E172), gelatin.
The composition of the capsule caps: Indigo Carmine FDS&C Blue 2 (E132), , dye iron oxide black (E172), Titanium dioxide (E171), dye iron oxide yellow (E172), gelatin.
Ink composition: shellac glaze – 47.5% (22% jeterificirovanno), dye iron oxide black (E172), propylene glycol.

10 PC. – blisters (1) – packs cardboard.
10 PC. – blisters (2) – packs cardboard.
10 PC. – blisters (3) – packs cardboard.
10 PC. – blisters (6) – packs cardboard.
10 PC. – blisters (9) – packs cardboard.
10 PC. – blisters (20) – packs cardboard.

Pharmacological action

Preparation, used in violation of urination, associated with benign prostatic hyperplasia. Alpha₁-adrenoblokator.

Tamsulosin selectively and competitively blocks postsynaptic α_1A-adrenoreceptory, located in the smooth muscle of the prostate, bladder neck and prostatic urethra. 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 (DGPŽ). 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. This dosage form provides prolonged and slow release of tamsulosin. Bioavailability – about 100%.

Immediately after ingestion decreases the absorption of tamsulosin. Uniformity of absorption increases, if a patient takes medication every day after the same meal.

After receiving a single oral dose of the drug 400 g (After a hearty meal) FROM_max tamsulosin in plasma achieved through 6 no. In the equilibrium state (through 5 day course taking) values with_max tamsulosin in blood plasma 60-70% higher, than with_max after a single dose of the drug.

Distribution

Plasma protein binding – 90%. Tamsulosin has a slight V_d (about 0.2 l / kg).

Metabolism

Tamsulosin is practically not subjected 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. None of the metabolites is more active, than starting material – tamsulozin. Most of the active substance present in the blood in an unmodified form. When liver failure dose not required.

Deduction

Tamsulosin and its metabolites are primarily excreted by the kidneys, with approximately 9% the dose is excreted unchanged in.

T_1/2 tamsulosin in single dose – 10 no (When administered after meals), after multiple dose – 13 no, final T_1/2 – 22 no.

Testimony

- Benign prostatic hyperplasia (treatment of dysuric disorders).

Dosage regimen

Inside, After the first meal, drinking plenty of water. Drug taking in sitting or standing. The capsule should not crush and chew.

Assign 400 g (1 capsule)/d.

Side effect

Part of the central and peripheral nervous system: often – dizziness; infrequently – headache; rarely – fainting, asthenia, sleep disturbance (drowsiness or insomnia).

With the genitourinary system: infrequently – retrograde ejaculation; rarely – priapism, decreased libido.

From the digestive system: infrequently – nausea, vomiting, constipation or diarrhea.

Cardio-vascular system: infrequently – tachycardia, palpitation, orthostatic hypotension; rarely – chest pain.

Allergic reactions: infrequently – skin rash, hives; rarely – itching, angioedema.

Other: infrequently – rhinitis; rarely – backache.

Contraindications

-orthostatic hypotension in history;

- Severe hepatic impairment;

-hypersensitivity to tamsulozinu or to other components of the drug.

FROM caution should designate product in severe renal failure (CC less than 10 ml / min), tk. safety has not been proven.

Pregnancy and lactation

Tamsulosin is intended only for men.

Cautions

Tamsulosin should be used with caution in patients with a predisposition to orthostatic hypotension. At the first signs of orthostatic hypotension (dizziness or weakness), the patient should be planted or position “lying” until symptoms disappear.

Before beginning drug therapy, the patient must be examined in order, to exclude the presence of other diseases, that can cause the same symptoms, as BPH. Before treatment and regularly during therapy should be performed digital rectal examination and, if necessary, determination of prostate specific antigen.

In patients with renal insufficiency (CC less than 10 ml / min) the drug should be used with caution (safety has not been proven).

Effects on ability to drive vehicles and management mechanisms

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

Overdose

Cases of acute overdose have not been described.

Symptoms: marked reduction in blood pressure, sometimes accompanied by fainting, compensatory tachycardia.

Treatment: symptomatic therapy. The patient should immediately translate into horizontal position. If there is no effect, you should enter obemozameshhajushhie solutions or sossoudossoujiwate drugs. It was necessary to monitor kidney function. Dialysis nyeeffyektivyen (protein binding – 90%). To prevent further absorption of the drug it is advisable to gastric lavage, reception activated carbon and osmotic laxatives (sodium sulfate).

Drug Interactions

There were no interactions with the concomitant use of tamsulosin and atenolol, Enalapril, nifedipine or theophylline.

Simultaneous application of cimetidine increases the level of tamsulosin in plasma. Furosemide reduces the level of tamsulosin in plasma. In both cases, however, these levels remain within therapeutically active concentrations and dose should not be changed.

Diclofenac and indirect combined (warfarin) slightly increase the speed out tamsulosin.

In in vitro studies have not been found at the level of interaction with the hepatic metabolism of amitriptyline, salbutamol, glibenclamide and finasteride.

Concomitant use of tamsulosin with other α₁-blockers and other drugs, lower blood pressure, It can lead to a marked increased hypotensive effect.

The concentration of tamsulosin in plasma did not change in the presence of diazepam, trihlormetiazida or simvastatin. Also tamsulosin did not change the concentration of diazepam, propranolol, trichlormethiazide and chlormadinone.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children at or above 25 ° C. Shelf life - 2.5 year.