Proteride
Proterid: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Prosterid
ATX code: G04CB01
Active ingredient: finasteride (Finasteride)
Producer: CJSC "PharmFirma" Sotex "(Russia)
Description and photo update: 2019-29-11
Prices in pharmacies: from 671 rubles.
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Proteride is an antiandrogenic agent used in the treatment of benign prostatic hyperplasia (BPH).
Release form and composition
The drug is produced in the form of film-coated tablets: in the form of a rounded triangle, slightly biconvex, almost white or white, almost odorless (14 pieces in a blister, in a cardboard box 1 or 2 blisters and instructions for use of Proteride).
1 tablet contains:
- active substance: finasteride - 5 mg;
- additional components: sodium carboxymethyl starch (type A), magnesium stearate, pregelatinized starch, talc, lactose monohydrate, microcrystalline cellulose;
- film shell: lactose monohydrate, hydroxypropyl cellulose, titanium dioxide (CI 77891 EEC 171), macrogol-6000, hypromellose.
Pharmacological properties
Pharmacodynamics
Finasteride is a synthetic 4-azasteroid compound that belongs to competitive and specific inhibitors of the type II isoenzyme of steroid 5-α-reductase, which is involved in the conversion of testosterone to the active androgen 5-α-dihydrotestosterone (DHT). The active substance Proterida blocks the stimulating effect of testosterone on tumor development. Inhibition of the production of the enzyme dehydrogenase is accompanied by a decrease in the size of the prostate gland, an increase in the maximum rate of urine outflow and a decrease in the severity of symptoms of urinary tract obstruction. Against the background of constant intake of the drug, a statistically significant effect is recorded after 3 (decrease in prostate volume) and 7 (weakening of symptoms associated with gland hyperplasia) months after the start of the course.
In the human body, several types of 5-α-reductase are detected - I and II. They are distributed unevenly in tissues: the type II isoenzyme is found in the testes and their epididymis, in the prostate, scrotum, glans penis, seminal vesicles, liver and chest; The type I isoenzyme is found mainly in the skin of the back, chest and head, in the sebaceous glands, adrenal glands, kidneys and liver. Finasteride inhibits primarily the type II isoenzyme, which is responsible for most of the DHT in the blood. A single dose of the active substance rapidly and significantly changes the plasma concentration of DHT. A single dose of the drug equal to 5 mg reduces the plasma DHT content by 75%, which reaches its minimum by 24 hours, and then returns to the initial level within 7 days.
Proteride retains its effectiveness with repeated use. In the prostate itself, finasteride lowers DHT by ≤ 15% and causes a corresponding increase in testosterone levels. When compared with surgical or chemical castration, drug therapy provides a more significant reduction in the content of DHT in the prostate.
After several months of treatment with Proterid, the level of PSA (prostate-specific antigen), which is a sensitive and specific androgen-dependent marker of prostate carcinoma, in the overwhelming majority of cases quickly decreased, and subsequently remained stable at new levels. When using an antiandrogenic agent at a dose of 5 mg for 1 year, the average PSA content decreased by 50%.
Finasteride has no affinity for androgen receptors and does not show any other hormonal action. After the discovery of 5-α-reductase and the description of type II 5-α-reductase deficiency syndrome (male hermaphroditism), the role of androgens in the onset of BPH was once again revised. Being a strong androgen, DHT affects the development of the prostate; in adults, against the background of normal / high testosterone concentration, with a lack of 5-α-reductase, the atrophy of the gland is observed.
By activating androgen receptors, DHT, after attaching to them, forms dimers, which interact with DNA directly or indirectly affect cell proliferation as a result of changes in the expression of genes responsible for apoptosis and cell proliferation. These processes of regulation of the cell cycle in the intact prostate are in equilibrium. Although the molecular factors behind prostatic hyperplasia are unknown, DHT plays an important role in this. Specific inhibitors of type II 5-α-reductase can reduce prostate DHT levels and assist in the regression of hyperplastic prostate.
In preclinical studies, significant lethality was recorded in mice and rats of both sexes when feeding finasteride to the former at a single dose of 1500 mg / m2 (500 mg / kg), and to the latter at a dose of 2360 mg / m2 (400 mg / kg) to females and 5900 mg / m² (1000 mg / kg) for males. When using the drug in pregnant rats in small doses, malformations of the genitals were observed in male offspring.
Pharmacokinetics
The active substance is rapidly absorbed from the gastrointestinal tract (GIT). After 2 hours after administration, the maximum concentration (C max) in plasma is observed - 37 ng / ml. With repeated use of Proteride or after it in the time to reach C max and in the half-life (T 1/2), no significant difference was found. During 7 days of administration, no cumulation was observed, the saturation stage was noted after 4 days. Food intake did not affect absorption and plasma content of finasteride, bioavailability was 80%.
The active substance binds to plasma proteins by 90%, a decrease in renal function does not affect this indicator.
Proterid penetrates well into body tissues and biological fluids, including cerebrospinal fluid and semen. The volume of distribution (V d) when infused at a dose of 5 mg for 1 hour is 76 ± 14 L. The substance is extensively metabolized in the liver through oxidation. Of the 5 metabolites, 2 are active and exhibit an inhibitory effect of 20% of that of the basic substance.
The biological effect of a single dose of the drug is observed on average for 4 days. At the T 1/2 no effect dose administered, it may be -. 4,7-7,1 h Plasma clearance equal to 164 ± 55 ml / min. Approximately 39% (32–46%) is excreted in the urine in the form of metabolites, about 57% (51–64%) in the feces. In unchanged form, 0.04 ± 0.02% of the dose is excreted by the kidneys, 0.01% by the intestines. In semen, the concentration of finasteride can range from less than 1 ng / ml (undetectable) to 21 ng / ml.
With prolonged use of Proterid, for 3-7 months at a daily dose of 5 mg, the serum concentration of 5α-DHT in the blood decreases by 70%.
Indications for use
Proterid is recommended for use in BPH therapy for the following purposes:
- reduction in the size of the prostate gland;
- increasing the maximum rate of urine outflow;
- weakening of the severity of symptoms caused by hyperplasia;
- reducing the threat of acute urinary retention and the associated likelihood of surgery.
Contraindications
Absolute:
- childhood;
- prostate cancer;
- obstruction of the urinary tract;
- hypersensitivity to the constituents of Proterid tablets.
In the presence of liver failure, the antiandrogenic agent should be used with caution.
Proterid, instructions for use: method and dosage
Sterid tablets are intended for oral administration.
The therapy is carried out exclusively in men. Typically, the daily dose is 5 mg (1 tablet).
The duration of the course is at least 6 months.
Side effects
Against the background of drug treatment, such undesirable reactions as decreased libido, impotence, and a decrease in ejaculate volume can most often be observed. There may be disorders in the form of gynecomastia, breast tenderness. Sometimes hypersensitivity reactions are recorded (skin rash, swelling of the lips), an increase in the level of follicle-stimulating and luteinizing hormones in the blood (by approximately 10%, but not exceeding the normal range).
Finasteride therapy is usually well tolerated, these side effects are not very common, in most cases they are temporary and are mild.
Overdose
With the daily intake of Proteride at a dose of 80 mg for 3 months or a single use at a dose of 400 mg, no side effects were observed.
In case of suspicion of an overdose, specific therapy is not necessary.
special instructions
Before starting the course of therapy, it is required to exclude diseases that simulate BPH, which may include infectious prostatitis, bladder hypotension and impaired innervation, urethral stricture, and prostate cancer.
Improvement of the condition does not occur immediately, as a result, in the presence of large residual volumes of urine or severe forms of difficulty in urinating, the patient should be monitored to avoid obstructive uropathy.
Proterid leads to a decrease in PSA by 48% 12 months after administration, even against the background of prostate carcinoma, which makes it difficult to recognize this malignant neoplasm. Before the start of the course of therapy and then periodically during its implementation, it is recommended to conduct a rectal digital examination of the organ, to exclude the possible presence of cancer.
Finasteride in small doses, if ingested in any way into the body of a pregnant woman, can provoke anomalies in the development of the external genitals in a male fetus. The amount of the drug absorbed by contact with a broken tablet or with the sperm of a man receiving finasteride is unknown. As a result, to prevent damage to the male fetus, pregnant women or women with suspected pregnancy should not touch the damaged tablets of the drug and contact the ejaculate of men who are being treated with this agent. Since it has not been established how long finasteride can be excreted with sperm, after completion of therapy with Proterid, men should continue to observe precautions for 2 months.
Before starting treatment and then every 6 months during its implementation, it is recommended to conduct laboratory analyzes of urine sediment, the functional state of the liver and kidneys.
Influence on the ability to drive vehicles and complex mechanisms
Proterid does not affect the ability to drive a car and control other complex mechanisms.
Application during pregnancy and lactation
The drug is not intended for use in women.
Pediatric use
Proterid is not used in pediatric practice.
With impaired renal function
In groups of patients with a clearance of ≥ 90, 30-50 and <30 ml / min after a single dose of 10 mg Proteride, in such basic pharmacokinetic parameters as C max, T 1/2 and the area under the concentration-time curve (AUC), no difference was found.
Since the excretion of the drug occurs mainly through the intestines, dose reduction is not required in the presence of renal failure.
For violations of liver function
Patients with hepatic impairment should be treated with Proterid with caution.
Use in the elderly
In the age groups 46–60 years old and patients over 70 years old, the kinetics of finasteride was nonlinear. In patients of the older group, a moderate, but clinically insignificant increase in the plasma level of the drug was recorded. Elderly patients, despite the delayed elimination of finasteride from the body (approximately 8 hours), dose adjustment is not required.
Drug interactions
No clinically significant interaction of finasteride with other drugs has been identified.
Analogs
The analogues of Proteride are Zerlon, Alfinal, Penester, Proscar, Urofin, Finast, Finpros, Finasterid-Teva, Finasterid-OBL, etc.
Terms and conditions of storage
Store out of the reach of children, protected from light, at a temperature of 15-30 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Proterida
According to the few reviews about Proteride, left on specialized forums, it is highly effective in the treatment of BPH, provides a shrinkage of the prostate and helps to alleviate the symptoms of dysuria. By reducing the risk of developing acute urinary retention, the drug reduces the likelihood of surgical treatment of the disease.
The disadvantages of Proterid include the occurrence of side effects, such as decreased libido and worsening erection.
The price of Sterid in pharmacies
The price of Sterid, 5 mg film-coated tablets, can be 500–650 rubles. per package containing 28 pcs.
Proterid: prices in online pharmacies
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Drug name Price Pharmacy |
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Proterid 5 mg film-coated tablets 28 pcs. RUB 671 Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
