Properties
What is it?
Composition Physical and chemical properties: Opaque, hard gelatin capsules with an orange body and a black cap, filled with white granules; Composition: 1 capsule contains: Tamsulosin hydrochloride _ 0.4 mg. Excipients: Hypromellose, purified talc, sodium lauryl sulfate, ethylcellulose, Eudragit L30D, polyethylene glycol, sucrose, corn starch, methylparaben, propylparaben, coloring titanium dioxide (E 171). Capsule shell composition: Sodium lauryl sulfate, methylparaben, propylparaben, gelatin, purified water, colorants: Ponceau 4R (E 124), Brilliant Blue (E 133), Sunset Yellow (E 110), titanium dioxide (E 171). Pharmacological properties Tamsulosin hydrochloride is an alpha1A-adrenoreceptor blocker and is intended for symptomatic treatment of benign prostatic hyperplasia. It selectively blocks postsynaptic alpha1A-adrenoreceptors of the smooth muscles of the prostate gland, bladder neck, and prostatic urethra, resulting in reduced smooth muscle tone, improved urine flow, and enhanced voiding. Simultaneously, it reduces the symptoms of obstruction (emptying) and irritation (filling) associated with benign prostatic hyperplasia. The therapeutic effect is observed approximately 2 weeks after the start of treatment. Tamsulosin has a less pronounced ability to block alpha1B-adrenoreceptors of smooth muscles, therefore its effect on systemic arterial blood pressure is insignificant in patients with both arterial hypertension and normal blood pressure. Pharmacokinetics Absorption: After oral administration, tamsulosin is rapidly and almost completely absorbed from the gastrointestinal tract. When 400 mcg of Salover is taken once, the Cmax of tamsulosin in blood plasma is reached 6 hours after administration. The bioavailability of the preparation is approximately 100%. After food intake, the absorption of Salover decreases. When the preparation is taken at the same time as a meal, its absorption level is equalized. Upon reaching steady-state concentrations (after a 5-day course), the Cmax of tamsulosin in blood plasma is 60-70% higher than after a single dose of the preparation. Distribution: 99% is bound to plasma proteins. Vd is 0.2 L/kg. Metabolism and excretion: Tamsulosin is slowly metabolized in the liver, forming pharmacologically less active metabolites that retain high selectivity for alpha1A-adrenoreceptors. Most of the active substance circulates in the blood unchanged. Salover and its metabolites are mainly excreted by the kidneys, of which 9% of tamsulosin is excreted unchanged. After a single dose, T1/2 is 10-12 hours, and the terminal T1/2 is 22 hours. Indications Symptomatic treatment of benign prostatic hyperplasia, characterized by frequent and difficult urination, especially at night, intermittent urine flow, and incomplete bladder emptying. Dosage and administration Salover is taken orally 0.4 mg (1 capsule) once a day, in the morning, half an hour after a meal, with a sufficient amount of water. Chewing the capsule is not recommended. Side effects Genitourinary system: rarely – retrograde ejaculation; Cardiovascular system: in isolated cases – orthostatic hypotension, tachycardia, palpitations, chest pain; Digestive system: rarely – nausea, vomiting, diarrhea or constipation; Central nervous system: rarely – headache, dizziness, asthenia, sleep disturbances (drowsiness or insomnia); Allergic reactions: in isolated cases – rash, itching, angioneurotic edema; Other: rarely – back pain, rhinitis. Contraindications Hypersensitivity to the preparation and its components; severe hepatic insufficiency; arterial hypotension (including orthostatic hypotension). Special instructions Tamsulosin should be used with caution in patients prone to orthostatic hypotension, as, like with other alpha1-adrenoblockers, blood pressure decreases, leading to syncope. In case of the first signs of orthostatic hypotension (dizziness and weakness), the patient should sit or lie down. Rectal digital examination is mandatory before starting treatment and regularly during therapy. Prostate-specific antigen (PSA) should be determined if necessary. It is prescribed with caution in chronic renal failure (creatinine clearance less than 10 ml/min), as its safety in this category of patients has not been studied. Effect of the preparation on the ability to drive vehicles and operate machinery: During the treatment period, caution should be exercised when driving vehicles and performing other potentially hazardous activities that require concentration and speed of psychomotor reactions. Overdose Acute cases of overdose have not been described. Symptoms: acute arterial hypotension may develop. Treatment: symptomatic therapy. Restoration of normal arterial blood pressure and heart rate rhythm is possible if the patient is placed in a horizontal position. If necessary, blood-filling agents and vasoconstrictor drugs should be administered. To prevent further absorption of tamsulosin, gastric lavage and administration of activated charcoal, osmotic laxative (sodium sulfate) are recommended. Kidney function should be monitored. Dialysis is unlikely to be effective, as tamsulosin is extensively bound to plasma proteins. Drug interactions No interaction of tamsulosin with atenolol, enalapril, nifedipine, or theophylline has been found during their simultaneous administration. When taken with cimetidine, an increase in tamsulosin concentration in blood plasma is observed; with furosemide combination – a decrease in concentration, however, dose adjustment of Salover is not required. Diclofenac and indirect anticoagulants slightly increase the elimination rate of tamsulosin. Diazepam, propranolol, trichlormethiazide, chlormadinone, amitriptyline, diclofenac, glibenclamide, simvastatin, and warfarin do not change the free fraction of tamsulosin in blood plasma in vitro. In turn, tamsulosin does not change the free fractions of diazepam, propranolol, trichlormethiazide, and chlormadinone. Simultaneous use of Salover and other alpha1-adrenoblockers may enhance the hypotensive effect. Storage conditions and shelf life Store at a temperature not exceeding 25°C, in a dry place, protected from children. Shelf life: 2 years. The preparation should not be used after the expiry date indicated on the packaging. Dispensing from pharmacy Prescription only.
