Urorek capsules 8mg №10×3

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Urorek 8mg capsules in box No. 10×3
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Urorek 4 mg: yellow hard gelatin capsules, size 3. Urorek 8 mg: white hard gelatin capsules, size 0. Main active ingredient Silodosin Release formCapsules of 4 mg and 8 mg. 10 capsules in a blister pack of PVC / PVDC and aluminum foil. 1, 2 or 3 blister packs along with instructions for use in a cardboard box. Dosage 8 mg Pharmacodynamics Mechanism of action Silodosin, a highly selective competitive antagonist of alpha1A-adrenergic receptors, which are mainly located in the prostate gland, in the tissues of the fundus and neck of the bladder, the prostate capsule and the prostatic part of the urethra. Blockade of alpha1A-adrenergic receptors reduces the tone of smooth muscles in these tissues, which leads to an improvement in the outflow of urine from the bladder. At the same time, the symptoms of obstruction and irritation associated with benign prostatic hyperplasia are reduced. In an in vitro study, it was shown that the affinity for alpha1A-adrenergic receptors located in the bladder is 162 times greater than its ability to interact with alpha1B-adrenergic receptors, which are located in vascular smooth muscle. Due to its high selectivity, it does not cause a clinically significant decrease in blood pressure (BP) in patients with initially normal blood pressure. Pharmacokinetics Silodosin is well absorbed after oral administration, absorption is dose proportional. Absolute bioavailability is 32%. Food reduces the maximum concentration (Cmax) by about 30%, increasing the time to reach the maximum concentration (tmax) to about 1 hour and has a minimal effect on the area under the concentration-time curve (AUC). After oral administration of 8 mg once a day immediately after breakfast for 7 days, the following pharmacokinetic parameters were noted: Cmax 87 ± 51 ng / ml (sd), tmax – 2.5 hours (range 1.0 – 3.0), AUC – 433±286 ng·h/ml. The volume of distribution of silodosin is 0.81 l/kg. Silodosin binds to plasma proteins by 96.6%. Silodosin is metabolized via glucuronidation (involving UGT2B7), alcohol dehydnogenase and aldehyde dehydrogenase, oxidative pathways, mainly CYP3A4. The main active metabolite in plasma, carbamoylglucuronide (KMD-3213G), reaches plasma concentrations 4 times greater than silodosin itself. The binding of silodosin glucuronide to plasma proteins is 91%. Silodosin does not have the potential to induce or inhibit cytochrome P450 isoenzymes. 33.5% of silodosin is excreted through the kidneys and 54.9% through the intestines. The clearance of silodosin is about 0.28 l/h/kg. Silodosin is excreted mainly as metabolites and in very small amounts unchanged in the urine. The terminal half-life of T1 / 2 of silodosin and glucuronide is 11 hours and 18 hours, respectively. Pharmacokinetics in different groups of patients Elderly patients: the pharmacokinetics of silodosin and metabolites do not significantly depend on age. The clearance of silodosin did not change in patients over 75 years of age. Use in children: The use of silodosin has not been evaluated in patients under 18 years of age. Patients with hepatic impairment: in patients with moderate hepatic impairment (Child-Pugh score 7-9), the pharmacokinetics of silodosin does not change significantly. The pharmacokinetics of silodosin have not been studied in patients with severe hepatic impairment. Patients with impaired renal function: for patients with mild renal insufficiency (creatinine clearance ? 50 – ? 80 ml / min), dose adjustment is not required. For patients with moderate renal insufficiency (creatinine clearance ? 30 – ? 50 ml / min), a low initial dose of 4 mg is recommended. For patients with severe renal insufficiency (creatinine clearance < 30 ml / min), the appointment of silodosin is not recommended. Indications for use Treatment of signs and symptoms of benign prostatic hyperplasia (BPH) in adults. Route of administration and doses The recommended dose is 8 mg once, simultaneously with meals, preferably at the same time of day. The capsule should be swallowed whole, preferably with a glass of water. For special patient groups, we recommend taking one Urorec 4mg capsule daily (see below). Patients with impaired renal function Dose adjustment for elderly patients and patients with mild renal insufficiency (creatinine clearance ? 50 - ? 80 ml / min) is not required. For the treatment of patients with moderate renal insufficiency (creatinine clearance ? 30 - ? 50 ml / min), it is recommended to take an initial dose of 4 mg per day during the first week, with good individual tolerance, then you can increase the dose to 8 mg per day. Not recommended for use in patients with acute renal failure (creatinine clearance < 30 ml/min). Patients with impaired liver function No dose adjustment is required for patients with mild to moderate hepatic insufficiency. Due to the lack of data, the use of this drug in patients with acute liver failure is not recommended. Elderly patients Dose adjustment is not required for the elderly. Use in children There has been no appropriate use of the drug Urorek in pediatric practice according to indications for use. Use during pregnancy and lactation Pregnancy and breastfeeding Silodosin is contraindicated during pregnancy and breastfeeding. Fertility Ejaculation with reduced or no seminal fluid has been observed in clinical studies. This is due to the pharmacodynamic properties of silodosin. Before starting treatment, the patient should be informed that this effect may occur, temporarily affecting male fertility. Precautions Intraoperative flabby iris syndrome (ISDR) Intraoperative iris flaccid syndrome may occur during cataract surgery in patients taking or have taken alpha1-blockers during cataract surgery, which can lead to complications during surgery. Patients who are scheduled for cataract surgery are not recommended to start treatment with silodosin. Discontinuation of alpha1-blocker treatment 1–2 weeks prior to such surgery is recommended, but the benefits and duration of discontinuation of therapy prior to cataract surgery have not yet been established. In a pre-operative assessment, surgeons and ophthalmologists should take into account whether patients who are scheduled for this operation have taken or are taking silodosin in order to take appropriate measures for the management and control of ISDR. Orthostatic effect As with the use of other alpha1-blockers in the treatment with silodosin, there may be a decrease in blood pressure, orthostatic hypotension. Silodosin is not recommended for patients with a history of orthostatic hypotension. At the first signs of orthostatic hypotension (dizziness, weakness), the patient should sit or lie down and remain in this position until the symptoms of orthostatic hypotension disappear. Renal insufficiency It is not recommended to use this drug for the treatment of patients with acute renal insufficiency (creatinine clearance < 30 ml / min) (see sections "Dosage and Administration", "Pharmacokinetics"). Hepatic insufficiency Due to the lack of data, the use of this drug in patients with acute hepatic insufficiency is not recommended (see sections "Method of administration and dosage", "Pharmacokinetics"). Prostate carcinoma Since BPH and prostate cancer have similar symptoms and may develop together, patients with suspected BPH should be screened to exclude prostate cancer before prescribing the drug. A digital rectal examination and, if necessary, determination of prostate specific antigen (PSA) should be performed before starting treatment and at regular intervals thereafter. Treatment with Urorek leads to a decrease in the amount of seminal fluid released, which can affect male fertility. This effect disappears after discontinuation of the drug (see section "Side Effects"). Interaction with other drugs Silodosin is extensively metabolized, mainly through CYP3A4, alcohol dehydrogenase and UGT2B7. Silodosin is also a substrate for P-glycoprotein. Substances that inhibit or induce these enzymes and transporters may affect the plasma concentrations of silodosin and its active metabolite. Alpha-blockers There is no sufficient information on the safety of co-administration of silodosin and other alpha-blockers. Therefore, the simultaneous use of other alpha-adrenergic antagonists is not recommended. Inhibitors of CYP3A4 In an interaction study, a 3.7-fold increase in maximum plasma concentration of silodosin and a 3.1-fold increase in silodosin exposure (i.e. AUC) were found with simultaneous administration of a potent inhibitor of CYP3A4 (ketonazole 400 mg). Co-administration with potent CYP3A4 inhibitors (such as ketonazole, itraconazole and ritonavir) is not recommended. When silodosin was co-administered with a moderate CYP3A4 inhibitor such as diltiazem, an approximately 30% increase in silodosin AUC was observed, but there was no effect on Cmax and half-life. This change is not clinically important and dose adjustment is not required. Phosphodiesterase (PDE) type 5 inhibitors Only a minimal pharmacodynamic interaction was observed between silodosin and the maximum dose of sildenafil or tadalafil. In a placebo-controlled study in 24 people aged 45-78 years who received silodosin, concomitant administration of sildenafil 100 mg or tadalafil 20 mg caused a clinically insignificant mean decrease in systolic or blood pressure, which was assessed during an orthostatic test (the difference in heart rate lying and standing ). In patients older than 65 years, the average decrease at various time points was between 5 and 15 mm Hg. Art. (systolic) and between 0 and 10 mm Hg. (diastolic). Positive orthostatic test results were only slightly more frequent during co-administration of drugs, however, symptomatic orthostasis or dizziness was not recorded. The condition of patients simultaneously receiving a PDE-5 inhibitor and the drug should be monitored for the possible development of adverse reactions. Antihypertensive drugs In accordance with the clinical study program, many patients received concomitant therapy with antihypertensive drugs (mainly drugs that act on the reninangiotensin system, beta-blockers, calcium antagonists and diuretics) without increasing the incidence of orthostatic hypotension. However, it is necessary to take precautions while using the drug with antihypertensive drugs. The condition of patients should be monitored for the possible development of adverse reactions. Digoxin Co-administration of silodosin 8 mg once daily showed no significant effect on the plateau of digoxin, a P-glycoprotein substrate. Dose adjustment is not required. Contraindications - Hypersensitivity to the active substance or any of the auxiliary components or their intolerance. - Children under 18 years of age. - Severe renal failure (creatinine clearance less than 30 ml/min). - Severe liver failure (not enough clinical data). Composition One capsule contains: Active ingredient: silodosin 4 mg or 8 mg. Excipients: mannitol (E421), pregelatinized starch (1500™ starch), pregelatinized starch (PCS™ PC-10 starch). sodium lauryl sulfate (E 487), magnesium stearate (E 470). The composition of the gelatin capsule: gelatin, titanium dioxide (E171), iron dye yellow oxide (E-172). The last component is present only at a dosage of 4 mg. Overdose Silodosin has been evaluated at doses up to 48 mg/day in healthy males. The dose-dependent adverse reaction was postural hypotension. With a recent intake, initiation of vomiting or gastric lavage is possible. If an overdose of the drug has led to hypotension, it is necessary to take measures to support the patient's cardiovascular system. It is unlikely that dialysis will give significant results, since silodosin is actively associated with blood protein (96.6%). Adverse reactions are listed below, noted in all clinical studies and throughout the international post-marketing experience of use, for which there is a causal relationship, according to the MedDRA classification according to the damage to organs and organ systems and the frequency of development: very often (? 1/10) , often (from ? 1/100 to < 1/10), infrequently (from ? 1/1000 to < 1/100), rarely (from ? 1/10,000 to < 1/1000), very rarely (from < 1 /10 000), the frequency is unknown (the frequency cannot be determined from the available data). Immune system disorders Very rare: allergic reactions: angioedema of the face, tongue and larynx*. Psychiatric disorders Uncommon: decreased libido. Nervous system disorders Common: dizziness; rare: loss of consciousness*, fainting. Cardiac disorders Uncommon: tachycardia*; rare: palpitations*. Vascular disorders Common: Orthostatic hypotension; Uncommon: Decreased blood pressure*. Respiratory, thoracic and mediastinal disorders Common: Nasal congestion. Gastrointestinal disorders Common: diarrhea Uncommon: nausea, dry mouth. Hepatobiliary system disorders Uncommon: Abnormal liver function tests*. Skin and subcutaneous tissue disorders Uncommon: rash*, pruritus*, urticaria*, drug dermatitis*. Violations of the genital organs and breast Very often: retrograde ejaculation (ejection of semen not into the urethra, but into the bladder, after orgasm, semen is excreted in the urine during urination, this condition is harmless to the body and disappears after stopping the use of silodazine), anejaculation (lack of sperm release with orgasm preservation), infrequently: erectile dysfunction. Injury, poisoning, and procedural complications Not known: Intraoperative flabby iris syndrome during cataract surgery. * - Side effects recorded spontaneously during international post-marketing experience of use (the frequency of occurrence of events was calculated based on the occurrence during phases I-IV clinical trials and non-interventional studies). Orthostatic Hypotension: The incidence of orthostatic hypotension in placebo-controlled studies was 1.2% in the silodosin group and 1.0% in the placebo group. Orthostatic hypotension can sometimes cause fainting. Intraoperative flabby iris syndrome (ISDR): ISDR has been reported during cataract surgery. If any of the side effects listed in the instructions get worse, or if you notice any other side effects not listed in the instructions, tell your doctor. Storage conditionsKeep in a place protected from light at a temperature not exceeding 25°C. Keep out of the reach of children. 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