Composition, form of production and packaging
The tablets covered with a film cover of light blue color, round, biconcave.
finasteride 5 mg
Excipients: lactose monohydrate, pregelatinized starch, sodium carboxymethyl starch (type A), sodium docusate, microcrystalline cellulose, povidone, magnesium stearate.
Composition of the film shell: giprolose (hydroxypropyl cellulose), hypromellose, titanium dioxide (E171), talc, indigo carmine dye (E132).
10 pieces. - blisters (3) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
Finasteride is a synthetic 4-azasteroid compound, a competitive specific inhibitor of steroid 5-alpha-reductase, an intracellular enzyme that converts testosterone to a more active androgen-5-dihydrotestosterone (DHT), which stimulates the growth of prostatic tissue and the development of benign hyperplasia.
Under the influence of the drug, the concentration of dihydrotestosterone in both the blood plasma and in the gland tissue decreases, the size of the enlarged gland decreases and the symptoms associated with the prostatic adenoma decrease. Finasteride does not bind to androgen receptors, does not affect the level of plasma lipids and the level of cortisol, estradiol, prolactin, TSH, thyroxine.
With constant admission, a statistically significant effect is recorded after 3 months (decrease in the volume of the gland), 4 months (increase in the maximum urinary flow rate) and 7 months (decrease in the general symptoms and symptoms of obstruction of the urinary tract).
After taking the drug inside finasteride quickly absorbed from the gastrointestinal tract, the suction is completed 6-8 hours after oral administration. Bioavailability is about 80% and does not depend on food intake. The time to reach C max in plasma is 2 hours, the C max value is 8-10 ng / ml.
Well absorbed and penetrates into tissues and biofluids, is found in the ejaculate (at a concentration of 5 Ојg). The connection with plasma proteins is more than 90%. It penetrates through the BBB, after 7-10 days of treatment it is detected in cerebrospinal fluid in small amounts . System clearance - 165 ml / min, V d - 76 liters.Slightly cumulates with prolonged admission.
Metabolism and excretion
Metabolized by the liver and released as metabolites by the kidneys (approximately 39%) and through the intestine (57%). T 1/2 in men 18-60 years is 6 hours, over 70 years - 8 hours.
Pharmacokinetics in special clinical cases
In chronic renal failure part of the metabolites (which is normally excreted in the urine) is excreted with feces.
Benign hyperplasia prostate gland with the purpose:
- reducing the size of the prostate gland;
- improve the maximum urinary flow rate and reduce symptoms associated with hyperplasia;
- reduce the risk of acute urinary retention requiring catheterization or surgery, including transurethral resection of the prostate and prostatectomy.
Tablets are taken orally, regardless of food intake, without chewing.
Assign 5 mg 1 time / day, both in monotherapy, and in combination with the blocker? -adrenoceptors doxazosin.
The duration of therapy before evaluating its effectiveness should be at least 6 months. Approximately in 50% of patients, the disappearance of clinical symptoms occurred during treatment for 12 months.
Do not need to adjust the dose of the drug in elderly patients , incl. and with renal failure (with a decrease in CK up to 9 ml / min), because. pharmacokinetic studies have not revealed any changes in the distribution of finasteride in these categories of patients.
On the part of the reproductive system: decreased potency and / or libido, impaired ejaculation, decreased ejaculate volume (the frequency of these side effects does not exceed 3-4% and decreases during treatment).
On the part of the endocrine system: rarely (up to 1-2%) - the increase and soreness of the mammary glands, increasing concentrations of LH and FSH in the blood, a decrease in the concentration of PSA.
Allergic reactions: rash, itching, hives, swelling of the lips and face.
- malignant tumor of the prostate;
- Obstruction of the urinary tract;
- the drug is not intended for use in women;
- hypersensitivity to finasteride and / or to other components of the drug.
With caution should apply the drug in violation of liver function, obstructive uropathy.
PREGNANCY AND LACTATION
Women of childbearing age and pregnant women should avoid contact with the crushed or lost integrity tablets of the Zergon product because of the possibility of penetration of finasteride into the body of a pregnant woman, since finasteride has teratogenic properties (the ability to suppress the conversion of testosterone to dihydrotestosterone can cause impaired development of the reproductive organs in the male fetus) , penetrates into the seminal fluid.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution should be used in cases of liver failure.
APPLICATION FOR CHILDREN
Contraindication: children's age.
APPLICATION IN ELDERLY PATIENTS
Do not need to adjust the dose of the drug in elderly patients , incl. and with renal failure (with a decrease in CK up to 9 ml / min), because. pharmacokinetic studies did not reveal any changes in the distribution of finasteride in these categories of patients
In patients with a large volume of residual urine and / or a sharply reduced urine flow, it is necessary to carefully monitor the possible development of obstructive uropathy.
Before the start of therapy, it is necessary to exclude diseases that simulate benign prostatic hyperplasia - prostate cancer, urethral stricture, bladder hypotension, violations of its innervation and infectious prostatitis.
Against the backdrop of the use of Zergon, PSA declines by 6 and 12 months are 41% and 48%, respectively . To exclude the development of prostate cancer during therapy with finasteride, it is necessary to conduct a patient examination.
Impact on the ability to drive vehicles and manage mechanisms
The use of the drug does not affect the patient's ability to perform work requiring increased attention and speed of psychomotor reactions.
No cases of drug overdose have been reported.
There was no clinically significant interaction of Zergon with other drugs.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored in a dry place inaccessible to children at a temperature of no higher than 30 В° C. Shelf life - 3 years.