Finasteride CAS 98319-26-7 Enlargement of prostate Prostatic hyperplasia

Finasteride is a 4-azosteric compound that acts as a specific inhibitor of the intracellular enzyme type II 5A-reductase during the metabolism of testosterone to the stronger dihydrotestosterone. Benign prostatic hyperplasia or prostatic hypertrophy depends on the conversion of testosterone to dihydrotestosterone in the prostate. This drug is very effective in reducing dihydrotestosterone in the blood and prostate. Finasteride has no affinity for androgen receptors. Finasteride, a 5α reductase inhibitor, reduces the size of the prostate gland by inhibiting the conversion of testosterone to dihydrotestosterone (DHT), improving symptoms, increasing urine flow rate, and preventing the progression of benign prostatic hyperplasia (BPH) through its hormonal mechanism.

Basic information

Chinese name

Finasteride

English name

Finasteride

nickname

Finasteride, finasteride

CAS login number

98319-26-7

The commodity name of its preparation

paulic

packing

Plastic packaging

directory

1 Functional effect

2 Usage and Dosage

3 Applicable Groups

4 Precautions

5 Pharmacological Effects

6 Toxicity Study

7 Influence

8 Pharmacokinetics

9 Side effects

10 Applications

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Finasteride is a 4-azosteric compound that acts as a specific inhibitor of the intracellular enzyme type II 5A-reductase during the metabolism of testosterone to the stronger dihydrotestosterone. Benign prostatic hyperplasia or prostatic hypertrophy depends on the conversion of testosterone to dihydrotestosterone in the prostate. This drug is very effective in reducing dihydrotestosterone in the blood and prostate. Finasteride has no affinity for androgen receptors.

In a long-term efficacy and safety study (PLESS), 3016 patients with moderate to severe symptoms of BPH taking the drug for 4 years were evaluated for BPH related urinary management (surgical intervention), such as transurethral resection of the prostate and other prostatectomies, or acute urinary retention requiring catheter insertion. In this double-blind, randomized, placebo-controlled multicenter study, treatment with this drug resulted in a 51% reduction in the overall risk of urinary disposal, significant and sustained reduction in prostate volume, and sustained increase in maximum urinary flow velocity and symptom improvement.

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Paolecide orally, 5mg/ time, once/day. 5 mg/ day, morning and evening, before and after meals can be taken, long-term use is recommended.

Patients with renal insufficiency: Dose adjustment is not required for patients with various degrees of renal insufficiency (creatinine clearance as low as 9 mL/ min).

Older adults: Pharmacokinetic studies in patients over 70 years of age showed reduced clearance of finasteride, but no dose adjustment was required.

When finasteride is used for alopecia treatment, oral administration is 1mg/ time, once/day, 4 months for a course of treatment.

This paragraph is applicable to people.

· BPH patients with enlarged prostate and lower urinary tract symptoms

· Patients with larger prostate volume (≥40ml) and/or higher serum PSA level (PSA≥1.4ng/ml) fared better

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Note: Women, children and allergic patients should not use this product. Patients with significant residual urine and/or severe decreased urinary flow should be closely monitored for urinary obstruction.

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Pharmacological action: Finasteride is a compound of 4-azosteroid hormone. It is a specific type II 5α-reductase inhibitor, which inhibits the conversion of peripheral testosterone to dihydrotestosterone and reduces the level of dihydrotestosterone in blood, prostate, skin and other tissues. The growth and development of prostate and benign hyperplasia depend on dihydrotestosterone. Finasteride can inhibit prostatic hyperplasia and improve the related clinical symptoms of benign prostatic hyperplasia by reducing the level of dihydrotestosterone in the blood and prostate tissue.

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Folding genotoxicity

Genotoxicity: In vitro bacterial and mammalian cell mutation tests and in vitro alkaline elution tests showed no mutagenicity. In vitro studies on chromosome aberration of CHO cells showed that the chromosomal aberration rate of CHO cells increased slightly at the concentration of 450~550μmol of finasteride, which was 4000~5000 times of the peak plasma concentration of 5mg of this product. In vivo chromosomal aberration test, mice were given 250mg/kg/ day of finastandroide (228 times of the recommended daily dose of 5mg for human clinical use in terms of AUC, and the dose was calculated in the same way for all toxicological studies below), and the chromosomal aberration did not increase.

Folding reproductive toxicity

Reproductive toxicity: finasteride 80mg/kg/ day (as calculated above, equivalent to 543 times the daily human dose), continuous administration for 12 weeks had no effect on the fertility of sexually mature male rabbits and male rats. When the rats were given 80mg/kg/ day of finasteride for more than 24 weeks, the weight of seminal vesicles and prostates were also significantly reduced, and the spermatosupposal formation failed during mating, which resulted in decreased fertility of rats. But it has no effect on testicles and mating behavior of rats and rabbits. These toxic effects recovered within 6 weeks after discontinuation.