Urorec, capsules 8mg, 30pcs

Composition

Composition per capsule:

Active ingredient:  

silodosin 4 mg or 8 mg.

Auxiliary substances:  

mannitol, pregelatinized starch (starch 1500™),

pregelatinized starch (starch PCS™ PC-10),

sodium lauryl sulfate, magnesium stearate.

Composition of the gelatin capsule:

gelatin,

titanium dioxide,

iron oxide yellow dye (E-172)

Pharmacological action

Pharmacodynamics .

Mechanism of action

Silodosin, a highly selective competitive antagonist of alpha-1a adrenergic receptors, blocks postsynaptic alpha-1a adrenergic receptors located in the smooth muscle of the prostate, the bladder neck and the prostatic part of the urethra.

Reduces the smooth muscle tone of the prostate, bladder neck and prostatic part of the urethra, improving the outflow of urine. At the same time, the symptoms of obstruction and irritation associated with benign prostatic hyperplasia are reduced.

Affinity for alpha / 1a-adrenoreceptors located in the bladder is 162 times higher than its ability to interact with alpha-1b-adrenoreceptors 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 BP.

When taken orally, silodosin is well absorbed. 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).

Cmax is 87±51 mg / ml, tmax is 2.5 h, the average concentration in the urine is 433±286 ng * h/ml. The volume of distribution of silodosin is 0.81 l / kg and binds to plasma proteins by 96.6%. The binding of silodosin carbamoyl glucuronide by plasma proteins is 91%. Silodosin is metabolized by glucuronidation (involving UGT2B7), alcohol dehydrogenase and aldehyde dehydrogenase, and oxidative pathways, mainly involving CYP3A4.

The main active metabolite in plasma carbamoyl glucuronide (K. MD-3213G) reaches a plasma concentration 4 times higher than silodosin itself. Silodosin does not have the potential to induce or inhibit cytochrome P isoenzymes

450.33,5% of silodosin is excreted through the kidneys and 54.9% through the intestine. The clearance of silodosin is about 23.1 l / h. Silodosin is mainly excreted as metabolites and in very small amounts in unchanged form in the urine. T 1/2 of silodosin and carbamoyl glucuronide is 11 hours and 18 hours, respectively.

Pharmacokinetics in different groups of patients

Elderly patients: the pharmacokinetics of silodosin and its metabolites were not significantly affected by age. Silodosin clearance did not change in patients over 75 years of age. Patients with impaired liver function: In patients with moderate hepatic impairment (7-9 points on the Child-Pugh scale), the pharmacokinetics of silodosin did not significantly change. The pharmacokinetics of silodosin have not been studied in patients with severe hepatic insufficiency.

Patients with impaired renal function: No dose reduction was required for patients with moderate renal insufficiency. Silodosin is not recommended for patients with severe renal insufficiency.

Indications

Urorec is intended for the treatment of benign prostatic hyperplasia.

Use during pregnancy and lactation

Uorek is contraindicated in children under 18 years of age, pregnant women and during lactation.

Contraindications

• Hypersensitivity to the Active ingredient or any of the excipients.
• components or their intolerance.
• Children under 18 years of age.
• Severe renal insufficiency (creatinine clearance less than 30 ml / min).
• Severe hepatic insufficiency (insufficient clinical data).

Side effects

Adverse reactions with frequency are listed below: very common: >10, common: > > 1/100 to >>< 1/10, uncommon: > 1/1000 to < 1/10, uncommon: > < 1/100, rare: > 1/10 000 to < 1/100, rare: > Nervous System

Often:  dizziness.

Frequency unknown:  syncope

The cardiovascular system

Often:  orthostatic hypotension.

Respiratory system

Frequently:  nasal congestion.

Gastrointestinal Tract

Often:  diarrhea.

Infrequently:  nausea, dry mouth.

Reproductive system

Very often:  retrograde ejaculation, anejaculation

Infrequently; decreased libido, erectile dysfunction

Intraoperative cider

syndrome Frequency unknown:  

Intraoperative syndrome of “flabby” iris during cataract operations.

Interaction

Combination with other alpha-blockers is not recommended due to possible potentiation of the action.

Concomitant use of inhibitors of the CYP3A4 isoenzyme (ketoconazole, clarithromycin, itraconazole, ritonavir) is not recommended, as it increases the concentration of silodosin in plasma.

Phosphodiesterase-5 inhibitors (sildenafil, tadalafil) when used together, they may increase the risk of developing dizziness.

Antihypertensive drugs beta-blockers, calcium antagonists, drugs acting on the renin-angiotensin-aldosterone system, diuretics when used together increase orthostatic hypotension.

How to take, course of use and dosage

The recommended dose is 8 mg once, at the same time as a meal, preferably at the same time of day. It is necessary to swallow the capsule whole, preferably with a glass of water.

For the treatment of patients with moderate renal insufficiency (creatinine clearance >30 ->

Overdose

Symptoms: marked decrease in blood pressure, compensatory tachycardia.

Treatment: gastric lavage, taking activated charcoal or an osmotic laxative, symptomatic therapy aimed at increasing the volume of circulating blood (BCC), vasoconstrictor medications. Monitoring of kidney function. Dialysis is ineffective due to the intense binding of the drug to plasma proteins.

Special instructions

As with the use of other alpha-1-blockers, treatment with silodosin may experience a decrease in blood pressure, orthostatic hypotension. At the first sign 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 tumors have similar symptoms and can develop together, patients with suspected benign prostatic hyperplasia should be examined to rule out prostate tumors before prescribing the drug.

Patients taking or taking alpha-1 blockers may experience “flabby” iris syndrome during cataract surgery, which may lead to complications during surgery. It is necessary to stop treatment with alpha-1-blockers 1-2 weeks before such an operation. Patients who are scheduled for cataract surgery are not recommended to start treatment with Uorek.

Influence on the ability to drive motor vehicles and manage mechanisms: no studies have been conducted on the effect on the ability to drive vehicles and equipment. However, patients should be informed about possible manifestations of symptoms associated with orthostatic hypotension (for example, dizziness), and also warn that they should refrain from driving vehicles and equipment until the patient’s individual tolerance to Urorec is determined.

Form of production

Uorek. Capsules.

Storage conditions

The drug should be stored in a dry place, protected from light, inaccessible to children at a temperature not exceeding 30°C.

Shelf life

2 years

Active ingredient

Silodosin

Conditions of release from pharmacies

By prescription

Dosage form

Capsules

Description

For adults as directed by your doctor

Indications

Prostatic Hyperplasia