buy Finasteride, sold under the brand names Proscar and Propecia among others, is a medication used to treat pattern hair loss and benign prostatic hyperplasia (BPH) in men.[6] It can also be used to treat excessive hair growth in women. It is usually taken orally but there are topical formulations for patients with hair loss, designed to minimize systemic exposure by acting specifically on hair follicles.
Finasteride is a 5α-reductase inhibitor and therefore an antiandrogen. It works by decreasing the production of dihydrotestosterone (DHT) by about 70%.
In addition to DHT, finasteride also inhibits the production of several anticonvulsant neurosteroids including allopregnanolone, androstanediol, and THDOC.
Adverse effects from finasteride are rare; however, some men experience sexual dysfunction, depression, and breast enlargement. In some men, sexual dysfunction may persist after stopping the medication. It may also hide the early symptoms of certain forms of prostate cancer.
Finasteride was patented in 1984 and approved for medical use in 1992. It is available as a generic medication. In 2021, it was the 88th most commonly prescribed medication in the United States, with more than 8 million prescriptions.
Indications and Usage Finasteride is a basic drug to treat benign prostatic hyperplasia and prostatitis, a synthetic 4-nitrogen steroid hormone compound and a sex hormone drug.
It is used for benign prostatic hyperplasia, men’s prostatic fat and other diseases. Finasteride is the only oral drug approved by the US Food and Drug Administration (FDA) to treat male pattern baldness.
Mechanisms of Action Finasteride can selectively inhibit 5α-reductase, changing the conversion process of testosterone into 5α dihydrotestosterone (DHT), decreasing androgen levels in prostate cells, and prostate-specific antigens in serum, decreasing prostate swelling, and increasing urine flow rate, thereby alleviating the symptoms of prostatic hyperplasia. It acts by selectively blocking androgen stimulation of the prostate, but affects sexual function very rarely. Meanwhile, due to blocking of testosterone conversion and reduced synthesis of dihydrotestosterone, it can reduce dihydrotestosterone levels in the serum and scalp hair follicles, recovering the function of previously inhibited hair follicles, promoting hair growth and preventing loss.
clinical trials Three controlled clinical trials were performed in men (18 to 41 years), with mild-to-moderate degrees of androgenetic alopecia. In these studies, 1879 men ingested either a 1- mg finasteride tablet or placebo tablet once daily for 12 months; after 12 months, finasteride-treated patients were switched to placebo and placebo-treated patients were switched to finasteride and they were followed for an additional 12 months. Clinical improvement was seen as early as 3 months in finasteride-treated patients and hair regrowth continued throughout the trial. Finasteride also had a stabilizing effect on hair loss, which was maintained through the second year of treatment. Hair counts in placebo-treated patients decreased during the study. Finasteride was generally well tolerated in these studies. Some men, however, experienced decreased libido, difficulty in achieving an erection, and decreased semen volume (<2% of patients in each case). These side effects resolved in 58% of the men who continued treatment and completely abated upon discontinuation of the drug.
Description Finasteride, a novel 4-azasteroid, is a breakthrough in the treatment and control of benign prostatic hyperplasia. Mechanistically, it inhibits the prostatic-specific enzyme 5-alpha reductase, thereby decreasing the conversion of testosterone to dihydrotestosterone. It is reportedly effective in reducing urinary symptoms and prostatic volume and increasing maximal urinary flow rate. Finasteride is also being investigated as a treatment for prostatic cancer.
Chemical Properties White or off-white crystalline powder. Soluble in chloroform, dimethyl sulfoxide, ethanol, methanol, or n-propanol. Insoluble in propylene glycol or polyethylene glycol 400. Very slightly soluble in 0.1mol/L hydrochloric acid, 0.1mol/L sodium hydroxide solution, or water.topical finasteride
Indications Finasteride (Proscar) is a 5-reductase inhibitor that blocks the conversion of testosterone to DHT in target tissues. Since DHT is the major intracellular androgen in the prostate, finasteride is effective in suppressing DHT stimulation of prostatic growth and secretory function without markedly affecting libido. It is approved for the treatment of benign prostatic hyperplasia. Although there is usually some regression in the size of the prostate gland following administration of It, clinical response may take 6 to 12 months. If the obstructive symptoms are severe, there is often not enough time to allow this compound to work.The principal adverse effects of finasteride are impotence, decreased libido, and decreased volume of ejaculate. The compound is generally well tolerated in men.
Application Finasteride is a specific inhibitor of steroid type II 5α-reductase, an intracellular enzyme that converts testosterone to DHT. By inhibiting type II 5α-reductase, this conversion is blocked, resulting in significant decreases in serum and tissue DHT concentrations. Merck & Co. developed finasteride as an oral treatment for androgenetic alopecia after men taking finasteride (5 mg/ day) for prostate enlargement noticed regrowth of their hair. Finasteride is indicated for use in men only. Women of childbearing age cannot take finasteride because it may cause hypospadia (a developmental abnormality of the penis) in the male offspring if taken during pregnancy.
Clinical Use The selective inhibition of the type 2 5α-reductase isozyme produces a rapid reduction in plasma DHT concentration, reaching 65% suppression within 24 hours of administering a 1-mg oral tablet (106). At steady state, finasteride suppresses DHT levels by approximately 70% in plasma and by as much as 85 to 90% in the prostate. The remaining DHT in the prostate likely is the result of type 1 5α-reductase. The mean circulating levels of testosterone and estradiol remained within their physiological concentration range. Long-term therapy with It can reduce clinical significant end points of BPH, such as acute urinary retention or surgery. Finasteride is most effective in men with large prostates. Finasteride has no affinity for the AR and no androgenic, antiandrogenic, estrogenic, antiestrogenic, or progestational effects.
Veterinary Drugs and Treatments Finasteride may be useful in treating the benign prostatic hypertrophy in canine patients. Because of the drug’s relative expense and the long duration of therapy required to see a response, its usefulness may be limited in veterinary medicine.
It may also be useful in the adjunctive treatment of adrenal disease in ferrets.finasteride wholesale
Metabolism Finasteride is metabolised primarily via the cytochrome P450 3A4 enzyme subfamily. Following an oral dose of 14C-finasteride in man, two metabolites of the drug were identified that possess only a small fraction of the 5α-reductase inhibitory activity of finasteride. 39% of the dose was excreted in the urine in the form of metabolites (virtually no unchanged drug was excreted in the urine) and 57% of total dose was excreted in the faeces.
Melting point 253 °C
alpha 405 -59° (c = 1 in methanol)
Boiling point 576.6±50.0 °C(Predicted)
density 1.065±0.06 g/cm3(Predicted)
storage temp. room temp
solubility DMSO: 32 mg/mL, soluble
form solid
pka 14.17±0.70(Predicted)
color white to beige
Water Solubility insoluble
Merck 14,4082
BCS Class 1
InChIKey DBEPLOCGEIEOCV-WSBQPABSSA-N
LogP 3.030
CAS DataBase Reference 98319-26-7(CAS DataBase Reference)
EPA Substance Registry System 1H-Indeno[5,4-f]quinoline-7-carboxamide, N-(1,1-dimethylethyl)-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-4a,6a-dimethyl-2-oxo-, (4aR,4bS,6aS,7S,9aS,9bS,11aR)- (98319-26-7)
More Introduction:https://en.wikipedia.org/wiki/Finasteride
