Proscar
Proscar: 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: Proscar
ATX code: G04CB01
Active ingredient: Finasteride (Finasteride)
Producer: Merck Sharp & Dohme (Netherlands)
Description and photo update: 2019-13-08
Prices in pharmacies: from 434 rubles.
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Proscar is an antiandrogenic drug.
Release form and composition
Proscar is produced in the form of film-coated tablets: apple-shaped, blue, engraved “PROSCAR” on one side, “MSD 72” on the other (14 pcs. In blisters, 1 or 2 blisters in a cardboard box).
The composition of 1 tablet includes:
- Active ingredient: finasteride - 5 mg;
- Additional components: lactose monohydrate, corn pregelatinized starch, sodium salt of carboxymethyl ether starch, yellow iron oxide, sodium docusate, microcrystalline cellulose, magnesium stearate;
- Film shell: methylhydroxypropyl cellulose, talc, indigo carmine aluminum varnish, hydroxypropyl cellulose, titanium dioxide.
Pharmacological properties
Pharmacodynamics
Finasteride, which is a synthetic 4-azasteroid compound, is a specific inhibitor of type II 5-alpha reductase, an intracellular enzyme that converts testosterone to the more active androgen dihydrotestosterone (DHT). The degree of enlargement of the prostate gland in benign hyperplasia depends on the conversion of testosterone to DHT in the prostate gland.
The drug Proscar effectively reduces the concentration of DHT in the blood and in the prostate gland. With suppression of DHT formation, there is also a decrease in the size of the prostate gland, a decrease in the severity of symptoms associated with prostatic hyperplasia, and an increase in the maximum velocity of urine flow.
Finasteride has no affinity for the androgen receptor, does not significantly affect the lipid profile (total cholesterol, triglycerides, low and high density lipoproteins) and does not alter bone mineral density. Compared with placebo, finasteride does not affect the blood levels of estradiol, cortisol, thyroid-stimulating hormone, thyroxine and prolactin.
A single intake of 5 mg of finasteride causes a rapid decrease in the concentration of dihydrotestosterone in the blood serum with a maximum effect after 8 hours. Fluctuations in plasma concentration of finasteride occur within 24 hours, which does not directly affect the concentration of DHT.
In patients with DHT who took 5 mg of finasteride per day for 4 years, the concentration of DHT in the blood decreased by 70%, which was associated with a decrease in prostate volume by about 20%. Along with this, the content of prostate-specific antigen (PSA) decreased by approximately 50% in comparison with its initial concentration, which indicates a decrease in the growth rate of prostate epithelial cells. A decrease in DHT concentration and a decreased severity of prostatic hyperplasia, accompanied by a decrease in PSA concentration, persisted over the course of four years of studies. At the same time, the concentration of testosterone in the blood increased by 10–20%, but remained within the limits of physiological values.
In the case of using Proscar for 7-10 days in patients after prostatectomy, there was an 80% decrease in the concentration of DHT in the tissues of the prostate gland and a 10-fold increase in the content of testosterone in the tissues of the prostate in comparison with the content before the start of treatment.
It was recorded that with prolonged (over 4 years) use of the drug in patients with DHT and moderately or significantly severe symptoms of the disease, the risk of urological complications (surgical interventions: transurethral resection of the prostate or prostatectomy; acute urinary retention requiring catheterization) decreased by 51%. In these patients (the PLESS study), there was a pronounced and persistent decrease in prostate volume, a persistent increase in urine flow rate and improvement in symptoms.
In patients who took Proscar for 3 months, upon discontinuation of treatment after reducing the volume of the prostate gland by 20% after 3 months, restoration of the previous size of the prostate gland was observed.
Pharmacokinetics
When taken orally, the time to reach the maximum concentration of finasteride in the blood plasma is about 2 hours. Absorption of finasteride from the gastrointestinal tract occurs within 6-8 hours.
When taken orally, the bioavailability of finasteride does not depend on the meal regimen and is about 80% of the intravenous reference dose.
About 93% of finasteride binds to plasma proteins. Plasma clearance is about 165 ml / min, volume of distribution is 76 liters.
During long-term therapy, a slow accumulation of small amounts of finasteride was recorded. With a daily intake of 5 mg of the substance, the minimum equilibrium concentration in the blood plasma is 8-10 ng / ml, remaining stable over time.
In patients who received finasteride for 7–10 days, the active substance was found in the cerebrospinal fluid. In the case of taking 5 mg of Proscar per day, finasteride is also found in semen. The concentration of the active substance in the semen is 50-100 times lower than its dose, which did not affect the circulating DHT content.
The half-life of finasteride is on average about 6 hours.
After a single dose of finasteride labeled with 14 C, 57% of the dose is displayed through the gut, 39% is excreted as metabolites kidneys (unmodified finasteride hardly excreted by the kidneys). In the course of research, 2 finasteride metabolites have been identified with a slight inhibitory effect relative to 5-alpha reductase.
In elderly patients, the rate of elimination of finasteride slightly decreases, and the half-life increases: in patients aged 18-60 years, this figure is 6 hours, in patients over 70 years old - 8 hours. These changes are not clinically significant, therefore, when treating elderly men, a decrease in the dose of the drug is not required.
In chronic renal failure (creatinine clearance from 9 to 55 ml / min) with a single dose of the drug, the distribution of 14 C- labeled finasteride did not differ from that of healthy volunteers. In case of impaired renal function, there were also no abnormalities in binding to blood plasma proteins.
In renal failure, part of the metabolites of finasteride, which are normally excreted by the kidneys, are excreted through the intestine. As a result, the amount of metabolites in the feces increases, while in the urine it decreases. No dose adjustment of Proscar is required in dialysis patients.
Indications for use
Proscar is prescribed for the treatment of benign prostatic hyperplasia (BPH) to prevent the development of urological complications (reduce the risk of acute urinary retention), reduce the need for surgery, improve urine flow, reduce the size of an enlarged prostate and the severity of symptoms associated with the disease.
The drug is indicated for patients with an enlarged prostate gland.
Contraindications
Contraindication to the use of Proscar is the presence of hypersensitivity to its components.
Caution is required in the appointment of the drug with a large volume of residual urine and / or significantly reduced urine flow (requires careful monitoring for obstructive uropathy).
Proscar is not prescribed for women and children.
Due to the likelihood of the penetration of finasteride into the body, women of childbearing age and pregnant women should avoid contact with lost integrity or crushed tablets (there is a risk of exposure to the male fetus with the development of pathology of intrauterine formation of the external genital organs).
Instructions for the use of Proscar: method and dosage
Proscar is taken orally, regardless of food intake, as monotherapy or concurrently with doxazosin.
The daily dose is 1 tablet (5 mg) in 1 dose.
With renal failure of varying severity (creatinine clearance from 9 ml / min), as well as elderly patients, the dose should not be individually selected.
Side effects
In the first year of treatment, patients taking Proscar compared with placebo patients were more likely to experience such disorders as impotence, decreased libido and ejaculation disorders. As a rule, with further administration of the drug (for 2-4 years), the incidence of the above adverse reactions in patients taking Proscar did not differ from that in patients who took placebo.
Possible side effects:
- Endocrine system: soreness and enlargement of the mammary glands;
- Reproductive system: decrease in ejaculate volume, decreased libido, impotence, soreness of the testicles, ejaculation disorders;
- Allergic reactions: rash, urticaria, pruritus, angioedema of the face and lips.
The duration of therapy does not affect the frequency of development and the severity of violations, and the number of cases of sexual dysfunctions associated with taking Proscar decreases with prolonged use.
The tolerance and safety profile of Proscar when used concomitantly with 4 or 8 mg of doxazosin per day is comparable to the safety profiles of these drugs alone.
As a result of a seven-year placebo-controlled study, prostate cancer was detected by biopsy results in 18.4% of Proscar-treated patients and 24.4% of placebo-treated patients, with a Gleason score of 7-10 in 6.4% and 5.1% of men, respectively.
Therapy can affect laboratory values by lowering prostate-specific antigen levels.
Overdose
There is evidence that with a single dose of 400 mg of Proscar or taking a daily dose of up to 80 mg for 3 months, patients did not have any symptoms of overdose.
There are no specific recommendations for the treatment of Proscar overdose.
special instructions
To date, no positive clinical effect from the use of Proscar in patients with prostate cancer has been observed.
Before prescribing a treatment course and during therapy, it is necessary to conduct rectal examinations, as well as studies by other methods for the presence of prostate cancer. As a rule, with a baseline level of prostate-specific antigen (PSA) above 10 ng / ml, a broader examination is indicated, including, if necessary, a biopsy. If the PSA level is in the range of 4-10 ng / ml, further examination of the patient is recommended. In patients with prostate cancer and patients who do not have this disease, there is a significant overlap in PSA levels. In this regard, in BPH, regardless of treatment with Proscar, normal values of prostate-specific antigen do not allow to exclude prostate cancer. It also cannot be ruled out if the baseline PSA level is below 4 ng / ml.
In controlled clinical trials in patients with BPH and an elevated level of prostate-specific antigen (with multiple PSA determinations and prostate biopsy), the drug had no effect on the incidence of prostate cancer.
Even in the presence of prostate cancer during therapy, a significant decrease in serum prostate-specific antigen (about 50%) is observed.
For any prolonged increase in PSA levels in patients receiving treatment with finasteride, it is necessary to conduct a thorough examination to determine the cause (possibly, it consists in non-compliance with the regimen of Proscar).
Proscar does not significantly reduce the percentage of free PSA (the ratio of free PSA to total). This figure remains unchanged even under the influence of finasteride. In cases where the percentage of free PSA is used to diagnose prostate cancer, it is not necessary to adjust the values of this indicator.
The concentration of prostate-specific antigen in the blood serum depends on the patient's age and the volume of the prostate gland, and the volume of the prostate, in turn, depends on the patient's age. When determining the PSA level, it should be borne in mind that this indicator decreases in patients taking Proscar. In most cases, a rapid decrease in PSA level is observed in the first months of treatment, after which this indicator stabilizes at a new level, which, as a rule, is half of the value measured before starting therapy. Therefore, patients undergoing a long course of therapy with Proscar (from 6 months) need to double the value of the PSA level in order to compare it with normal values in men who do not take the drug.
Application during pregnancy and lactation
It is contraindicated to use Proscar for the treatment of women of childbearing age and pregnant women. There are no data on the excretion of finasteride in breast milk.
Type II 5-alpha reductase inhibitors inhibit the conversion of testosterone to dihydrotestosterone, so taking finasteride by pregnant women can lead to abnormal development of the external genital organs of the male fetus.
Pediatric use
According to the instructions, Proscar is contraindicated for the treatment of patients under the age of 18.
With impaired renal function
No dose adjustment is required in renal failure.
For violations of liver function
In hepatic impairment, the drug should be used with caution.
Use in the elderly
When treating elderly patients, the drug should be used with caution.
Drug interactions
No clinically significant interaction of Proscar with other drugs / substances was found.
Analogs
Proscar's analogues are: Zerlon, Alfinal, Penester, Finasteride-OBL, Proterid, Finast, Urofin, Finasterid Teva, Finpros.
Terms and conditions of storage
Store in a dark place, out of reach of children, at temperatures up to 30 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Proscar
Reviews of Proscar indicate that this drug is effective in cases where it is necessary to stop the symptoms characteristic of BPH and reduce the size of the prostate gland. Reported side effects are rare.
Price for Proscar in pharmacies
The approximate price for Proscar is: 14 tablets of 5 mg - 380 rubles, 28 tablets of 5 mg - 660 rubles.
Proscar: prices in online pharmacies
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Drug name Price Pharmacy |
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Proscar 5 mg film-coated tablets 28 pcs. 434 r 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!
