Penester coated pills 5mg N30
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Active ingredients
Finasteride
Release form
Pills
Composition
Active ingredient: Finasteride (Finasteride) Active ingredient concentration (mg): 5
Pharmacological effect
Finasteride is a synthetic 4-azasteroid compound. It is a specific competitive inhibitor of 5-alpha reductase type II - an intracellular enzyme that converts testosterone into an active androgen - dihydrotestosterone (DHT). With benign prostatic hyperplasia (BPH), its increase depends on the conversion of testosterone to DHT in the prostate. Finasteride highly effective reduces the concentration of DHT in both blood plasma and prostate tissue. Suppression of DHT formation is accompanied by a decrease in the size of the prostate gland, an increase in the maximum speed of urination and a decrease in the severity of symptoms associated with prostatic hyperplasia. Finasteride has no affinity for androgen receptors. According to the results of a clinical study (PLESS) in which patients with moderately or significantly pronounced symptoms participated BPH and an enlarged prostate gland, finasteride reduced the incidence of acute urinary retention from 7/100 to 3/100 in 4 years th period and frequency of need for surgery (transurethral resection of the prostate (TURP) or prostatectomy) - 10/100 to 5/100. These changes were also associated with an improvement in the symptoms of BPH (a decrease of 2 points on the quasi-AUA symptom scale), a sustained decrease in the volume of the prostate gland by about 20% and a steady increase in the speed of urine flow. The MTOPS (Medical Therapy Of Prostate Symptoms) study ranged from 4 to 6 years, in which 3,047 men with symptoms of BPH were randomly assigned to the groups receiving: finasteride at a dose of 5 mg / day; doxazosin in a dose of 4 mg / day or 8 mg / day; a combination of finasteride at a dose of 5 mg / day and doxazosin at a dose of 4 mg / day or 8 mg / day; or placebo. Treatment resulted in a significant reduction in the risk of clinical progression of BPH, which was 34% (p = 0.002), 39% (less than 0.001) and 67% (less than 0.001) compared to placebo when compared with finasteride. In most cases, the progression of BPH (274 out of 351) was manifested by exacerbation of the symptoms of BPH by more than 4 on the International Prostate Symptom Score (IPSS), while among patients who received finasteride, the risk of exacerbation of the symptoms, assessed by a point indicator, was reduced by 30% (95 % CI: 6-48%), among those receiving doxazosin - by 46% (95% CI: 25-60%), and among those receiving combination therapy - by 64% (95% CI: 48-75 %) relative to the placebo group.Among patients receiving finasteride, the risk of acute urinary retention was reduced by 67% (p = 0.011), in the group receiving doxazosin by 31% (p = 0.296), and in the group receiving combined therapy by 79% (p = 0.001 ) relative to the placebo group. A significant difference from placebo was observed only in groups of patients receiving finasteride and combination therapy.
Pharmacokinetics
Absorption of Cmax of finasteride in the blood plasma is reached approximately 2 hours after ingestion. Absorption of finasteride from the gastrointestinal tract is completed within 6-8 hours after ingestion. The oral bioavailability of finasteride is approximately 80% of the intravenous reference dose and does not depend on food intake. Distribution Binding to plasma proteins is approximately 93%. Plasma clearance is about 165 ml / min, Vd - 76 l. With long-term therapy, there is a slow accumulation of finasteride in small quantities. With the daily intake of finasteride orally at a dose of 5 mg, its minimum equilibrium plasma concentration reaches 8-10 ng / ml and remains stable over time. In patients who received the drug for 7-10 days, finasteride was detected in the cerebrospinal fluid. When taking the drug in a dose of 5 mg / day, finasteride is found in insignificant amounts in the seminal fluid. Metabolism and elimination of T1 / 2 finasteride is on average 6 hours. metabolites (unchanged finasteride is practically not excreted by the kidneys); 57% through the intestines. In this study, 2 metabolites of finasteride were identified, which have an insignificant inhibitory effect on 5-alpha reductase compared to finasteride. Pharmacokinetics in special clinical situations In elderly people, the elimination rate of finasteride is somewhat reduced. With age, T1 / 2 increases: in men 18-60 years old, the average T1 / 2 is 6 hours, and in men older than 70 years - 8 hours. These changes have no clinical significance, and, consequently, reducing the dose of the drug in older men does not required. In patients with chronic renal failure (CC from 9 to 55 ml / min), the distribution of 14C-labeled finasteride with a single dose did not differ from that in healthy volunteers.The binding of finasteride to plasma proteins also did not differ in patients with impaired renal function. In renal failure, part of the metabolites of finasteride, which is normally excreted by the kidneys, is excreted through the intestines. This is manifested by an increase in the number of metabolites of finasteride in the feces with a corresponding decrease in their concentration in the urine. In patients with renal failure who do not need hemodialysis, dose adjustment of finasteride is not required.
Indications
Benign prostatic hyperplasia (to reduce the size of the prostate gland, increase the maximum rate of outflow of urine and reduce the symptoms associated with hyperplasia; reduce the risk of acute urinary retention and the associated likelihood of surgical intervention).
Contraindications
Hypersensitivity, obstruction of the urinary tract, malignant tumor of the prostate.
Precautionary measures
Do not exceed the recommended dose. With caution, the drug should be prescribed to patients with a large amount of residual urine and / or a significantly reduced urination rate, patients with liver failure, as well as elderly patients.
Use during pregnancy and lactation
Use of the drug Penester is contraindicated in pregnancy and women of childbearing age. In connection with the ability of inhibitors of 5-alpha reductase type II to suppress the conversion of testosterone to dihydrotestosterone, these funds, including finasteride, when used in pregnant women, can cause abnormalities in the development of the external genital organs in a male fetus. Finasteride is not indicated for use in women. There is no data on the excretion of finasteride with breast milk. Small amounts of finasteride were found in the semen of patients who received finasteride at a dose of 5 mg / day. Although clinical data on the effects of finasteride on the male fetus are not available, women of childbearing age should avoid contact with the seminal fluid of men taking finasterid. Women of childbearing age and pregnant women should avoid contact with damaged finasteride pills, because the ability of the drug to suppress the conversion of testosterone to dihydrotestosterone can cause a violation of the development of the genital organs in the male fetus.
Dosage and administration
The drug is administered orally 5 mg 1 time per day, regardless of the meal. The duration of therapy to assess its effectiveness should be at least 6 months. In approximately 50% of patients, the disappearance of clinical symptoms occurred during treatment for 12 months.
Side effects
On the part of the reproductive system: gynecomastia, breast tenderness, impotence, decreased libido and decreased volume of ejaculate. Other: allergic reactions.
Overdose
Patients received finasteride once in doses up to 400 mg, with repeated administration of the drug in doses up to 80 mg / day for 3 months, no adverse reactions were observed. Overdosing finasteride does not require special treatment.
Interaction with other drugs
No clinically significant interaction with other drugs was detected. Finasteride is metabolized mainly with the participation of the cytochrome P450 isoenzyme CYP3A4, without having a significant effect on the function of this system. Although the risk of influence of finasteride on the pharmacokinetics of other drugs is estimated to be low, there is a likelihood that CYP3A4 isoenzyme inhibitors or inducers of cytochrome P450 will affect plasma plasma concentration of finasteride. However, given the available safety data, it seems unlikely that an increase in the concentration of finasteride associated with the concomitant use of such inhibitors will be of clinical significance. There were no clinically significant interactions with the combined use of finasteride with propranolol, digoxin, glibenclamide, warfarin, theophylline and phenazone.
special instructions
General indications In order to avoid obstructive complications, it is necessary to carefully monitor patients with a large volume of residual urine and / or significantly difficulty urinating. Consideration should be given to the possibility of a need for surgery. Effect on PSA content and diagnosis of prostate cancer Until now, the clinical benefits of using Penester in patients with prostate cancer have not been proven. In controlled clinical trials in patients with BPH and elevated PSA concentrations in plasma, PSA levels and prostate biopsy studies were monitored.It was found that the use of finasteride does not appear to alter the frequency of prostate cancer detection and does not affect its incidence in patients taking finasteride or placebo. Before starting treatment and periodically during Penester therapy, it is recommended to perform a rectal study diagnostic methods for prostate cancer. Determination of PSA in the blood plasma is also used to detect prostate cancer. In general, the initial concentration of PSA above 10 ng / ml indicates the need for further examination of the patient and biopsy. When determining the concentration of PSA in the range of 4-10 ng / ml, further examination of the patient is necessary. In men with BPH, normal PSA values do not exclude prostate cancer, regardless of treatment with Penester. The initial PSA concentration below 4 ng / ml also does not exclude prostate cancer. The Penester preparation causes a decrease in serum PSA concentration by approximately 50% in patients with BPH, even in the presence of prostate cancer. This fact must be taken into account when assessing the PSA content in patients with BPH who are receiving treatment with Penester, since A decrease in PSA concentration does not exclude the presence of concomitant prostate cancer. This decrease is expected for any range of PSA concentrations, although it may differ in specific patients. Analysis of PSA values in more than 3,000 patients in a 4-year double-blind, placebo-controlled PLESS study confirmed that PSA should be doubled for those taking finasteride for 6 months or more to compare them with normal values of this indicator in patients not receiving drug treatment. This correction preserves the sensitivity and specificity of the PSA assay and the possibility of detecting prostate cancer. Any continuing increase in PSA concentration in patients receiving treatment with Penester requires careful examination to determine the cause, which may be in non-compliance with the drug intake. The drug Penester does not significantly reduce the percentage of free PSA (ratio of free PSA to total).This indicator remains constant even under the influence of taking the drug. If the percentage of free PSA is used to diagnose prostate cancer, correction of the values of this indicator is not necessary. Breast cancer in men During clinical trials, as well as during the post-marketing period, breast cancer was observed in men taking Finasteride. Doctors should instruct their patients to immediately report any changes in breast tissue, such as the appearance of seals, pain, gynecomastia, or nipple discharge. The effect on the ability to drive vehicles and control mechanisms. not reported.