TULOZIN

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: EGIS PHARMACEUTICALS Plc (Hungary)

Pharmaceutical form, composition and packaging

Modified release capsule hard gelatin, self-closing, with a transparent body and an opaque green cap green; contents of capsules – white pellets, odorless or almost odorless.

Excipients: microcrystalline cellulose, a copolymer of methacrylic acid and ethyl acrylate (1:1) (in shape 30% aqueous dispersion solution), calcium stearate.

Structure shell pellets: a copolymer of methacrylic acid and ethyl acrylate (1:1) (in shape 30% aqueous dispersion solution), talc, triэtiltsitrat, Tween 80 (polysorbate 80).

The composition of the shell capsules: housing – indigokarmin, quinoline yellow, Titanium dioxide, gelatin; cap – indigokarmin, quinoline yellow, gelatin.

10 PC. – blisters (1) – packs cardboard.
10 PC. – blisters (3) – packs cardboard.

Pharmacological action

Alpha₁-adrenoblokator. Tulozin 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 Tulozina_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 a single oral dose C_max of active substance in plasma achieved through 6 no.

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

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.

Distribution

Plasma protein binding – 99%. 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. Most of the active substance present in the blood in an unmodified form.

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, after multiple dose – 13 no, final T_1/2 – 22 no.

Pharmacokinetics in special clinical situations

When liver failure clarify the dose is not required.

If the kidney function dose not specify required.

Testimony

- Treatment of the functional symptoms of benign prostatic hyperplasia.

Dosage regimen

Tulozin taken orally at a dose of 400 g (1 caps. / day).

Capsules taken after the first meal, drinking plenty of water. The capsule should not crush and chew.

Side effect

CNS: 1-10% – dizziness, drowsiness or insomnia; 0.1-1% – headache.

From the digestive system: 0.1-1% – nausea, vomiting, diarrhea or constipation.

On the part of the reproductive system: 0.1-1% – retrograde ejaculation, decreased libido; < 0.01% – priapism.

Cardio vascular system: 0.01-0.1% – orthostatic hypotension, tachycardia, palpitation, chest pain, swoon.

Allergic reactions: 0.01-0.1% – skin rash, itch, hives, angioedema.

Other: 0.1-1% – reduced visual acuity, rhinitis, asthenia, backache.

Contraindications

- Hypersensitivity to the drug.

FROM caution It should be used in patients with chronic renal failure (CC < 10 ml / min), hypotension (in t. no. orthostatic), severe hepatic insufficiency.

Cautions

Tamsulosin should be used with caution in patients, prone to orthostatic hypotension, tk. and in case of reception other alpha₁-adrenoblokatorov, in some patients during treatment may decrease blood pressure, sometimes leading to fainting. At the first signs of orthostatic hypotension (dizziness or weakness) the patient should sit or lay until symptoms.

Before starting therapy with, the patient must be examined in order to exclude the presence of other diseases, which can cause similar symptoms, as well as benign prostatic hyperplasia. Before you start treatment and regularly during therapy should be performed digital rectal examination and, if required, determination of prostate specific antigen (PSA).

Patients with severe renal insufficiency (CC < 10 ml / min) Tulozin should be used with caution, tk. safety of the drug in these patients has not been studied.

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: theoretically possible occurrence of acute hypotension.

Treatment: the patient should be put, to restore blood pressure and normalize heart rate. Spend cardiotropic therapy. It should monitor renal function and to apply general supportive 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. Dialysis is not effective, as tamsulosin binds strongly to plasma proteins.

Drug Interactions

The simultaneous use of cimetidine increases the concentration of tamsulosin in blood plasma, furosemide reduces its concentration in blood plasma. However, in both cases the content of tamsulosin remains within a therapeutically active concentrations and correction dose is not required.

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

Concomitant use with other alpha tamsulosin₁-blockers and other drugs, lower blood pressure, It can lead to a marked increased hypotensive effect.

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

The concentration of tamsulosin in plasma did not change in the presence of diazepam, trixlormetiazida, amitriptyline, diclofenac, glibenclamide, simvastatin or warfarin.

Tamsulosin does not alter 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 below 25 ° C. Shelf life – 15 Months.