Composition, form of production and packaging
Capsules hard gelatinous, yellow, size 3; the contents of the capsules are amorphous or fine crystalline powder from white to light yellow.
1 caps.
silodosin 4 mg
Auxiliary substances: mannitol - 132.4 mg, pregelatinized starch (starch 1500 в„ў ) - 9 mg, pregelatinized starch (PCS в„ў PC-10 starch) - 26 mg, sodium lauryl sulfate - 1.8 mg, magnesium stearate - 1.8 mg.
The composition of the gelatin capsule: gelatin - 47.434 mg, titanium dioxide - 0.48 mg, iron-oxide oxide yellow (E172) - 0.086 mg.
5 pieces. - packings of cellular contour (1) - packs cardboard.
5 pieces. - packings cellular planimetric (2) - packs cardboard.
5 pieces. - packings cellular planimetric (3) - packs cardboard.
5 pieces. - packings cellular planimetric (5) - packs cardboard.
5 pieces. - packings cellular planimetric (9) - packs cardboard.
5 pieces. - packings cellular planimetric (10) - packs cardboard.
10 pieces. - packings of cellular contour (1) - packs cardboard.
10 pieces. - packings cellular planimetric (2) - packs cardboard.
10 pieces. - packings cellular planimetric (3) - packs cardboard.
10 pieces. - packings cellular planimetric (5) - packs cardboard.
10 pieces. - packings cellular planimetric (9) - packs cardboard.
10 pieces. - packings cellular planimetric (10) - packs cardboard.
Capsules hard gelatinous, white, size в„–0; the contents of the capsules are amorphous or fine crystalline powder from white to light yellow.
1 caps.
silodosin 8 mg
Auxiliary substances: mannitol - 264.8 mg, pregelatinized starch (starch 1500 в„ў ) - 18 mg, pregelatinized starch (PCS в„ў PC-10 starch) - 52 mg, sodium lauryl sulfate - 3.6 mg, magnesium stearate - 3.6 mg.
The composition of the gelatin capsule: gelatin - 98 mg, titanium dioxide - 2 mg.
5 pieces. - packings of cellular contour (1) - packs cardboard.
5 pieces. - packings cellular planimetric (2) - packs cardboard.
5 pieces. - packings cellular planimetric (3) - packs cardboard.
5 pieces. - packings cellular planimetric (5) - packs cardboard.
5 pieces. - packings cellular planimetric (9) - packs cardboard.
5 pieces. - packings cellular planimetric (10) - packs cardboard.
10 pieces. - packings of cellular contour (1) - packs cardboard.
10 pieces. - packings cellular planimetric (2) - packs cardboard.
10 pieces. - packings cellular planimetric (3) - packs cardboard.
10 pieces. - packings cellular planimetric (5) - packs cardboard.
10 pieces. - packings cellular planimetric (9) - packs cardboard.
10 pieces. - packings cellular planimetric (10) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
PHARMACHOLOGIC EFFECT
Highly selective competitive antagonist? 1A- adrenoreceptors. Blocks postsynaptic? 1A- adrenoreceptors, located in the smooth muscles of the prostate gland, the neck of the bladder and the prostatic part of the urethra. Reduces the tone of the smooth musculature of the prostate gland, the neck of the bladder and the prostatic part of the urethra, improving the outflow of urine. Simultaneously, the symptoms of obstruction and irritation associated with benign prostatic hyperplasia decrease.
The affinity of silodosin to? 1A- adrenoreceptors located in the bladder, 162 times greater than its ability to interact with? 1B- adrenoreceptors, which are located in the smooth muscles of the vessels. Due to the high selectivity, silodosin does not cause a clinically significant decrease in blood pressure in patients with initially normal blood pressure.
PHARMACOKINETICS
Suction and distribution
When ingestion, silodosin is well absorbed. Absolute bioavailability is 32%. Eating reduces Cmax by about 30%, increasing the time to reach Cmax for about 1 h and has minimal effect on the AUC. C max 87 В± 51 ng / ml, T max - 2.5 h, the average concentration in urine is 433 В± 286 ng В· h / ml.
V d of silodosin is 0.81 l / kg. Silodosin binds to plasma proteins by 96.6%.
Metabolism and excretion
Silodosin is metabolized by glucuronation (involving UGT2B7), involving alcohol dehydrogenase and aldehyde dehydrogenase, oxidative pathways, mainly involving CYP 3A4. The main active metabolite in plasma carbamoylglucuronide (KMD-3213G) reaches a plasma concentration 4 times greater than silodosin itself.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 intestine. The clearance of silodosin is about 23.1 l / h. Silodosin is excreted mainly in the form of metabolites and in a very small amount in unchanged form with urine. T 1/2 of silodosin and carbamoyl - glucuronide is 11 hours and 18 hours, respectively.
Pharmacokinetics in specific patient groups
The pharmacokinetics of silodosin and metabolites were not significantly dependent on age. The clearance of silodosin did not change in patients older than 75 years.
In patients with moderate impairment of liver function (7-9 on the Child-Pugh scale), the pharmacokinetics of silodosin do not change significantly. Patients with severe hepatic insufficiency did not study the pharmacokinetics of silodosin.
For patients with moderate renal insufficiency, no dose reduction was required. For patients with severe renal failure, silodosin is not recommended.
INDICATIONS
benign prostatic hyperplasia.
DOSING MODE
The recommended dose is 8 mg 1 time / day, simultaneously with food intake, preferably at the same time of day. It is necessary to swallow the whole capsule, preferably with a glass of water.
In the treatment of patients with moderate renal insufficiency (KK? 30- <50 ml / min), it is recommended to take the drug at a dose of 4 mg / day during the first week, then with a good individual tolerance it can be increased the dose to 8 mg / day.
In patients with severe renal insufficiency, silodosin is not recommended.
SIDE EFFECT
Undesirable reactions with frequency indication are given below: 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), the frequency is unknown (the available data do not allow to determine the frequency).
From the side of the central nervous system: often - dizziness; the frequency is unknown - syncope.
From the cardiovascular system: often - orthostatic hypotension.
From the respiratory system: often - nasal congestion.
On the part of the digestive system: often - diarrhea; infrequently - nausea, dry mouth.
On the part of the reproductive system: very often - retrograde ejaculation, anejaculation; infrequently - decreased libido, erectile dysfunction.
Other: frequency unknown - intraoperative syndrome of flabby iris during operations for cataracts.
CONTRAINDICATIONS
- renal failure of severe degree (CK <30 ml / min);
- severe hepatic insufficiency (not enough clinical data);
- children and adolescence under 18;
- Hypersensitivity to the active substance or any of the auxiliary components or their intolerance.
With caution should be used for renal failure of mild to moderate severity (QC from 30 to 50 ml / min).
PREGNANCY AND LACTATION
Silodosin is for men only.
APPLICATION FOR FUNCTIONS OF THE LIVER
In the treatment of patients with moderate renal insufficiency (KK? 30- <50 ml / min), it is recommended to take the drug at a dose of 4 mg / day during the first week, then, with good individual tolerance, it is possible to increase the dose to 8 mg / day.
With renal insufficiency of severe degree (CK <30 ml / min), the appointment of silodosin is contraindicated.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
The drug is contraindicated in patients with severe hepatic impairment (not enough clinical data).
APPLICATION FOR CHILDREN
Contraindicated use of the drug in children and adolescents under the age of 18 years.
SPECIAL INSTRUCTIONS
As with the use of other alpha 1- adrenoblockers in the treatment with silodosin, a decrease in blood pressure may be observed, 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.
Since benign prostatic hyperplasia and prostate tumors have similar symptoms and can develop together, patients with suspected benign prostatic hyperplasia before prescribing the drug need an examination to exclude prostate tumors.
Treatment with Urerek reduces the amount of seminal fluid that can be released, which can affect male fertility. This effect disappears after discontinuation of the drug Urerek.
In patients taking or taking alpha- 1- adrenoblockers, a cirrhotic syndrome may occur during surgery for cataracts, which can lead to complications during surgery. It is necessary to stop treatment with alpha 1- adrenergic blockers 1-2 weeks before such an operation. Patients who are prescribed an operation for cataract, it is not recommended to start treatment with Urerek.
Impact on the ability to drive vehicles and manage mechanisms
There have been no studies of the impact on the ability to drive vehicles and equipment. However, patients should be informed of the possibility of symptoms associated with orthostatic hypotension (for example, dizziness), and also warn that one should refrain from controlling vehicles and equipment until the patient's individual tolerability of Urerek is determined.
OVERDOSE
Symptoms: marked decrease in blood pressure, compensatory tachycardia.
Treatment: gastric lavage, reception of activated carbon or osmotic laxative, symptomatic therapy aimed at increasing BCC, vasoconstrictive drugs. Control of kidney function. Dialysis is ineffective due to intensive binding of the drug to plasma proteins.
DRUG INTERACTION
It is not recommended to combine with other alpha-blockers due to possible potentiation of the action.
The combined use of inhibitors of the isoenzyme CYP3A4 (ketoconazole, clarithromycin, itraconazole, ritonavir) is not recommended, because increases the concentration of silodosin in plasma.
Inhibitors of PDE5 (sildenafil, tadalafil), when combined, can increase the risk of dizziness.
Hypotensive drugs (beta adrenoblockers, calcium antagonists, drugs acting on RAAS, diuretics), when combined, can enhance orthostatic hypotension.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored in a dry, protected from light, out of reach of children at a temperature of no higher than 30 В° C. Shelf life - 2 years.
