The Urorek (Urorec)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceSilodosinSilodosin
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  • The Urorek
    capsules inwards 
    RECORDATA Ireland Co., Ltd.     Ireland
    • Dosage form: & nbspcapsules
    Composition:Aactive substance: silodosin

    4 mg or 8 mg.

    Excipients:

    Mannitol 132.4 mg (264.8 mg), starch

    pregelatinized (starch

    1500 ™) 9 mg (18 mg), starch

    pregelatinized (starch

    PCS ™ PC-10) 26 mg (52 mg), sodium

    lauryl sulfate 1.8 mg (3.6 mg), magnesium

    stearate 1.8 mg (3.6 mg).


    Composition of gelatin capsule:

    gelatin 47.434 mg (98.0 mg), titanium

    dioxide 0.48 mg (2.0 mg), dye

    iron oxide yellow (E-172)

    0.086 mg (only for 4 mg).

    Description:Hard gelatin capsules of yellow color of size 3 (for a dosage of 4 mg).
    Hard gelatin capsules of white color, size 0 (for a dosage of 8 mg).
    The contents of capsules are amorphous or fine crystalline powder from white to light yellow color.
    Pharmacotherapeutic group:treatment of benign prostatic hyperplasia
    ATX: & nbsp

    C.02.C.A   Alpha-blockers

    G.04.C.A.04   Silodosin

    Pharmacodynamics:

    Mechanism of action

    Silodosin, highly selective competitive antagonist alpha1A-adrenergic receptors, which in mostly located in thegland, in the tissues of the bottom and neck bladder, capsule presentand prostatic parts of the urethra. Blockade of alpha1A-adrenergic receptors reduces the tone of smooth muscles in these tissues, which leads to an improvement in outflow of urine from the bladder.

    Simultaneously, the symptoms of obstruction and irritation decrease, associated with benign hyperplasia of the prostate.

    In studies in vitro It was It was shown that the affinity of silodosin to alphaiA-adrenoceptors 162 times exceeds its ability interact with α1β-adreno-receptors that are located in smooth muscles of blood vessels. Thanks high selectivity silodosin not causes clinically significant lowering blood pressure (BP) in patients with baseline normal blood pressure.

    Pharmacokinetics:Cilodozine is well absorbed after Poral reception, absorption is proportional to the dose. Absolute bioavailability is about 32 %. Food reduces the maximum concentration (Cmax) about 30%, increasing the time to reach maximum concentration (Tmax) up to 1 hour and provides minimal impact 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 are 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, binding to plasma proteins is 96.6%. Silodosin is metabolized by glucuronation (involving UGT2B7), with the participation of alcohol dehydrogenase and aldehyde dehydrogenase, oxidative pathways, mainly involving CYP3A4. The main active metabolite in the plasma is carbamoyl-glucuronide (KMD-3213G) reaches a plasma concentration 4 times greater than itself silodosin. 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 kidney and 54,9 % through the intestines.

    The clearance of silodosin is about 0.28 l / h / kg. Silodosin excreted mainly in the form of metabolites and in a very small number in unchanged in the urine.

    Final half-life T1 / 2 silodosin and glucuronide

    is 11 hours and 18 hours respectively.

    Pharmacokinetics in various patient groups

    Elderly patients: pharmacokinetics silodosin and metabolites essentially does not depend on age. The clearance of silodosin does not change in patients older than 75 years.

    Application in children: Application silodosin was not evaluated in patients younger than 18 years.

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    Repeatable:

    The recommended dose is 8 mg once, concurrently with food intake, preferably in one and the other same time of day. Required swallow the capsule whole, it is advisable to drink a glass of water.

    Patients with impaired function kidney:

    In patients with mild renal disease insufficiency (creatinine clearancefor> 50- <80 ml / min) dose adjustment not required. For the treatment of patients with renal insufficiency moderate severity (ground clearance creatinine> 30 to <50 mL / min) it is recommended to take an initial dose of 4 mg per day during the first week, with a good individual tolerance, the dose can be increased to 8 mg per day. The use of the drug for patients with severe renal insufficiency (creatinine clearance <30 ml / min) is not recommended.

    Patients with impaired liver function:

    For patients with mild hepatic impairment and with moderate hepatic insufficiency gravity correction is not required. Due to lack of data, the use of the drug for patients with severe hepatic impairment is not recommended Elderly patients:

    For the elderly, dose adjustment is not required.

    Application in children: The corresponding use of the drug Urerek in pediatric practice according to indications for use was not.

    Side effects:

    The following are undesirable The adverse reactions noted in all clinical trials and during the international post marketing experience applications for which there is a causal relationship, according to the classification MedDRA at compliance with organ damage and systems of organs and 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 can not be determined from the available data).

    Immune system disorders

    Very rarely: allergic reactions: angioedema, edema of the face, tongue and throat *.

    Disorders of the psyche Infrequent: decreased libido. Disturbances from the nervous system

    Often: dizziness, rarely: loss of consciousness *, frequency unknown: syncope.

    Heart Disease Infrequent: tachycardia *, rarely: feeling of palpitations *. Vascular disturbances Often: orthostatic hypotension, infrequently: lowering of arterial pressure *.

    Violations with hand respiratory system, chest and mediastinal organs

    Often: nasal congestion. Disorders from the gastrointestinal tract

    Often: diarrhea, infrequently: nausea, dry mouth.

    Disorders from the hepatobiliary system

    Infrequently: deviation from the norm of indicators of liver function *. Disturbances from the skin and subcutaneous tissue

    Infrequently: rash *, skin itch *, hives *, medicinal dermatitis *.

    Violations of the genitals and mammary gland

    Often: retrograde ejaculation, anejaculation, infrequently: erectile disfunction.

    Injury, poisoning and complications of procedures

    frequency is unknown: intraoperative syndrome of "flabby" iris during operationsovarian cataract.

    * - side effects recorded spontaneously in the international post-marketing experience (the frequency of occurrence was calculated based on the occurrence of events in clinical trials I-IV phases and noninterventional studies).

    Orthostatic hypotension: the frequency of orthostatic hypotension in placebo-controlled clinical trials was 1.2% in the group receiving silodosin and 1.0% in the group, taking placebo.

    Orthostatic hypotension can sometimes cause fainting.

    Intraoperative syndrome of flabby iris (ISDR) It was reported on the development of the ISDR during surgery to remove cataracts.

    If any of the listed side effects aggravated or you notice any other side effects not listed in the instructions, report about this doctor.

    Overdose:Silodosin was evaluated at a dose of up to 48 mg / day in healthy men.

    A dose-dependent adverse reaction was postural hypotension. With recent ingestion, initiation of vomiting or gastric lavage is possible. If an overdose of the drug Urerek led to hypotension, it is necessary to carry out measures to support the cardiovascular system of the patient. It is unlikely that dialysis will yield significant results, since silodosin actively binds to the blood protein (96.6%).

    Interaction:

    Silodosin is an active metabolitemainly, through CYP3A4, alcohol-dehydrogenase and UGT2B7. Silodosin is also substrate for P-glycoprotein. Substances that inhibit or induce these enzymes and carriers can affect the concentration of silodosin and its active metabolite in plasma. Alpha blockers

    Sufficient information on the safety of co-administration of silodosin and other alpha-blockers no. Therefore, simultaneous admission other

    antagonists of alpha-adrenergic receptors is not recommended.

    Inhibitors of CYP3A4 In the study of the interaction, a 3.7-fold increase in the maximum concentration silodosin in plasma and a 3.1-fold increase in the effect of silodosin (i.e., AUC) with simultaneous administration strong inhibitor of CYP3A4 (ketoconazole 400 mg). Simultaneous application with powerful inhibitors of CYP3A4 (such as ketoconazole, itraconazole and ritonavir) Not recommended.

    When co-administration of silodosin and a moderate inhibitor of CYP3A4, for example diltiazem, an approximately 30% increase in silodosin AUC was observed, but there were no effects on the Stach values ​​and half-life. This change is not clinically important, dose adjustment is not required.

    Inhibitors of phosphodiesterase (PDE), type 5

    Between silodosin and the maximum dose of sildenafil or tadalafil, only a minimal pharmacodynamic mutualityact. In a placebo-controlled study, 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 diastolic blood pressure, which was assessed when an orthostatic test was performed (pulse difference between lying and standing). In patients older than 65 years, the mean decrease at different times was between 5 and 15 mm Hg. (systolic) and between 0 and 10 mm Hg. (diastolic). The positive results of orthostatic tests were only slightly more frequent during joint medication, however, symptomatic orthostasis or dizziness was not documented. The condition of patients concurrently receiving PDE-5 inhibitors and the drug should be monitored for the possible development of adverse reactions.

    Hypotensive drugs In accordance with the clinical research program, many patients received concomitant therapy with antihypertensive drugs (mainly agents acting on the renin-angiotensin system, beta-blockers, calcium antagonists and diuretics) without increasing the frequency of orthostatic hypotension.Nevertheless, 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

    With simultaneous administration of silodosin 8 mg once daily, no significant effect on the plateau of the concentrations of digoxin, the substrate of P-glycoprotein, was observed. Correction of the dose is not required.



    Special instructions:As with the use of other alpha1-blockers in the treatment with silodosin, a decrease in blood pressure may be observed, orthostatic hypotension. Patients with orthostatic hypotension in anamnesis are not recommended to take silodosin.

    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.

    Since benign prostatic hyperplasia and prostate cancer have similar symptoms and can develop together, patients with suspected benign prostatic hyperplasia before prescribing the drug need an examination to exclude a malignant tumor of the prostate.

    Finger rectal examination and, if necessary, the definition of a prostatic specific antigen (PSA) should be performed before the start of treatment and at regular intervals after it.

    Treatment with silodosin can lead to a decrease in the amount of seminal fluid released during orgasm, which can temporarily affect male fertility. This effect disappears after discontinuing silodosin.

    In patients taking or taking alpha1-adrenergic blockers, an intraoperative syndrome of "flabby" iris (ICD) may occur during surgery for cataracts, which can lead to complications during surgery. Patients who are scheduled for cataract surgery, it is not recommended to begin treatment with silodosin. It is recommended that treatment with alpha 1 blockers be discontinued 1-2 weeks before such surgery, but the benefits and duration of cessation prior to cataract surgery have not yet been established.

    In the preliminary assessment before surgery, surgeons and ophthalmologists should consider - take or take silodosin patients who have planned this operation, for taking appropriate measures to maintain and control the ISDR.

    There have been no studies of the effect of silodosin on the ability to drive vehicles and equipment. Patients should be informed of possible manifestations of symptoms associated with orthostatic hypotension (eg, dizziness), and in the case of of refraining from driving and other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.


    Form release / dosage:

    Capsules of 4 mg and 8 mg. For 5 or 10 capsules in a PVC / PVDC solar cell loop and aluminum foil. According to 1, 2, 3, 5, 9, 10 contour cell packs together with instructions for use in a cardboard bundle

    Packaging: For 5 or 10 capsules in a PVC / PVDC solar cell loop and aluminum foil. According to 1, 2, 3, 5, 9, 10 contour cell packs together with instructions for use in a cardboard bundle
    Storage conditions:In dry, dark place at a temperature of not more than 30C.
    Keep out of the reach of children.
    Shelf life:3 years. Do not use at the expiration date indicated on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LSR-005971/10
    Date of registration:25.06.2010
    The owner of the registration certificate:RECORDATA Ireland Co., Ltd.RECORDATA Ireland Co., Ltd. Ireland
    Manufacturer: & nbsp
    Information update date: & nbsp08.07.2014
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