Tulosin - instructions for use, dose, side effects, contraindications

microcrystalline cellulose, calcium stearate, methacrylic acid copolymer and ethyl acrylate (in the form of a 30% aqueous dispersion solution), Tween 80 (Polysorbate 80), triethyl citrate, talc.

Capsule shell: indigo carmine, quinoline yellow, titanium dioxide, gelatin.

Description:Hard gelatin capsules are self-closing, with a transparent base of green color (color code: 13009) and an opaque lid of a green color (color code: 17026). Pellets are almost white, odorless or almost odorless.

Pharmacotherapeutic group:alpha 1-blocker

ATX: & nbsp

G.04.C.A.02 Tamsulosin

Pharmacodynamics:

Tamsulosin selectively and competitively blocks postsynaptic α1A-adrenoreceptors, located in the smooth muscles of the prostate gland, the neck of the bladder and the prostatic part of the urethra, and α1D -adrenoreceptors, mainly located in the body of the bladder. This leads to a decrease in the tone of the smooth muscles of the prostate gland, the neck of the bladder and the prostatic part of the urethra and improve detrusor function.This reduces the symptoms of obstruction and irritation associated with benign prostatic hyperplasia. Typically, the therapeutic effect develops 2 weeks after the start of the drug, although in a number of patients, the decrease in the severity of symptoms is noted after the first dose. The ability of tamsulosin to affect α1A -adrenoceptors is 20 times greater than its ability to interact with α1B -adrenoceptors, which are located in the smooth muscles of the vessels. Due to this high selectivity, the drug does not cause any clinically significant decrease in systemic blood pressure (BP) in both patients with arterial hypertension and in patients with normal initial BP.

Pharmacokinetics:

Suction:

After oral administration tamsulosin quickly and almost completely absorbed from the digestive tract. Bioavailability of the drug is about 100%.

After a single dose of the drug inside C_max the active substance in the plasma is reached after 6 hours.

Immediately after eating, the absorption of tamsulosin decreases. Uniformity of absorption increases if the patient takes the drug every day after the same meal.

In the equilibrium state (after 5 days of course intake), the value of Stax of the active substance in blood plasma is 60-70% higher than Cmax after a single dose of the drug.

Distribution:

Binding to plasma proteins - 99%. Tamsulosin has a small volume of distribution (approximately 0.2 l / kg).

Metabolism:

Tamsulosin is practically not exposed to the effect of "first passage" and is slowly biotransformed in the liver with the formation of pharmacologically active metabolites that retain high selectivity for α1A-adrenergic receptors. None of the metabolites is more active than the original substance. Most of the active substance is present in the blood in unchanged form.

With hepatic failure, a dose adjustment is not required.

Excretion:

Tamsulosin and its metabolites are mainly excreted by the kidneys, with approximately 9% of the dose being excreted unchanged.

T1/2 tamsulosin with a single admission - 10 hours, after repeated intake of -13 hours, the final half-life - 22 hours.

If the kidney function is not regulated, the dose of the drug should not be specified.

Indications:

Treatment of functional symptoms of benign prostatic hyperplasia (BPH).

Contraindications:Hypersensitivity to tamsulosin hydrochloride or any other component of the drug.

Carefully:chronic renal failure (lower creatinine clearance below 10 ml / min), arterial hypotension (including orthostatic), severe hepatic impairment.

Dosing and Administration:

Inside, after eating.

400 mcg (1 capsule) per day.

Capsules are taken after the first meal, with plenty of water. Capsule should not be broken and chewed.

Side effects:

The most common side effects are P-10%): dizziness, drowsiness, or insomnia

Rare (0.1-1%): headache, decreased visual acuity, rhinitis, nausea, vomiting, diarrhea or constipation, retrograde ejaculation, asthenia, decreased libido, back pain.

Extremely rare (0.01-0.1%): Orthostatic hypotension, tachycardia, heart palpitations, chest pain, syncope, hypersensitivity reactions (skin rash, itching, urticaria, angioedema).

Overdose:

Cases of acute overdose are not described.

Symptoms: it is theoretically possible the emergence of acute hypotension.

Treatment: the patient should be laid to restore blood pressure and normalize the heart rate. Carried out cardiotropic therapy. It is necessary to monitor the function of the kidneys and apply general supportive therapy.

If symptoms persist, replace vasoconstrictive solutions or vasoconstrictors. To prevent further absorption of tamsulosin, it is possible to wash the stomach, taking activated charcoal or osmotic laxative. Dialysis is not effective, because tamsulosin strongly binds to blood plasma proteins.

Interaction:

Simultaneous use of cimetidine increases the level of tamsulosin in blood plasma; furosemide reduces its level in blood plasma. However, in both cases, these levels remain within the therapeutically active levels and dosage should not be changed.

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

The simultaneous use of tamsulosin with other alpha-adrenoblockers and other drugs that reduce blood pressure can lead to a marked increase in the hypotensive effect.

No interaction was found with simultaneous use of tamsulosin with atenolol, enalapril, nifedipine, or theophylline.

The concentration of tamsulosin in the blood plasma did not change in the presence of diazepam, trichloromethiazide, amitriptyline, diclofenac, glibenclamide, simvastatin or warfarin. Also tamsulosin did not change the concentration of diazepam, propranolol, trichloromethiazide and chloromadinone.

Special instructions:

Tamsulosin should be used with caution in patients with a predisposition to orthostatic hypotension, as in the case of taking other alpha-1 blockers, some patients may lose blood pressure during the course of treatment, which can sometimes lead to a fainting condition. When the first signs of orthostatic hypotension (dizziness or weakness) appear, the patient should be seated or laid until the symptoms disappear.

Before starting therapy with the drug, the patient should be examined to exclude the presence of other diseases that can cause the same symptoms as benign prostatic hyperplasia. Before the start of treatment and regularly during therapy, a digital rectal examination and, if required, the determination of a specific prostate antigen (PSA).

In patients with severe renal insufficiency (creatinine clearance less than 10 ml / min), the drug should be used with caution. this group of patients has not been investigated.

Effect on the ability to drive transp. cf. and fur:

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Capsules with a modified release of 0.4 mg. For 10 capsules in a blister of PVC / PVDC / al.foil. 1 or 3 blisters together with instructions for medical use in a cardboard bundle.

Packaging:(10) - blisters (1) - packs of cardboard
(10) - blisters (3) - packs cardboard

Storage conditions:Store below 25 ° C. Keep out of the reach of children.

Shelf life:5 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-001934/07

Date of registration:06.08.2007

The owner of the registration certificate:EGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary

Manufacturer: & nbsp

EGIS Pharmaceutical Plant, ZAO Hungary

Representation: & nbspEGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary

Information update date: & nbsp31.08.2015

Illustrated instructions

Instructions

Tulosin® (Tulosin®)