PharmaSourcesJune 04, 2021
Tag: Finasteride , antiandrogen , prostatic hypertrophy
Finasteride belongs to the group of drugs called benign prostatic hypertrophy agents. It is commonly used to manage enlarged prostate and reduce the need for surgery and prevent acute urinary retention. It may also be used for male pattern hair loss.
Finasteride is an antiandrogen— a 5α-reductase inhibitor.[9] It reduces the production of dihydrotestosterone, especially in the prostate gland and scalp.
CAS Number: 98319-26-7
Molecular Formula: C23H36N2O2
Weight: 372.5
Appearance: White or off-white crystalline solid
Melting point: 252-254 °C
Solubility: Slightly soluble
Finasteride is marketed under many brand names worldwide.
In China, it is commonly sold as Propecia and Proscar.
It is available in the mentioned forms:
Finasteride Tablets (1mg, 5mg)
Finasteride API Powder
Topical Finasteride
Both Dutasteride and Finasteride are 5α-reductase inhibitors. They work by combating the conversion of testosterone to dihydrotestosterone, which is responsible for the enlargement of the prostate and baldness.
There are three main types of 5α-reductase enzymes, with type 1 and 2 being specific for treating male pattern baldness. Type 1 enzyme is found in sweat glands, sebaceous glands, and the scalp. While type 2 is present in the prostate and hair follicles.
The main difference between Dutasteride and Finasteride is that the former is selective for type 2 5α-reductase enzyme, and the latter inhibits both type 1 and type 2.
Finasteride and Minoxidil are popular hair loss treatment options.
Minoxidil is a piperidino-pyrimidine derivative, which is a potent vasodilator. In contrast, Finasteride is a 5α-reductase enzyme inhibitor.
Minoxidil is mainly available as a topical medication to be applied on your scalp, promoting hair growth locally.
On the other hand, Finasteride is available as a tablet form with a systemic effect throughout the body.
Finasteride is an artificial 4-azasteroid compound. It is a competitive inhibitor of the 5α- reductase enzyme mainly present in the prostate cells, which converts the hormone testosterone to 5α-dihydrotestosterone (DHT).
DHT plays a vital role in the enlargement and development of the prostate gland. It is also a hormonal mediator for hyperplasia when it collects in the prostate gland. The active metabolite DHT has a higher affinity for androgen receptors in the prostate gland than testosterone. By binding with the androgen receptors, DHT modifies the genes responsible for cell enlargement.
As mentioned above, there are three main types of 5α-reductase enzymes. While Finasteride has a significantly higher affinity for the type 2 isoenzyme, long-term treatment is seen to affect type 1 receptors, which are present in the scalp, skin, and liver.
The mechanism of action of Finasteride is inhibition of type 2 5α-reductase, blocking the conversion of testosterone to DHT, lowering its level in the tissues and blood. As DHT is the principal androgen for prostatic enlargement, reducing its level also decreases prostatic volume.
It is seen that it can reduce the prostate size by 20% - 30% within six to 24 months.
Studies have shown that Finasteride lowers serum DHT levels to healthy levels present in a hairy scalp. By reducing DHT levels in the scalp, Finasteride slows hair loss and increases hair regrowth. However, its effect on the scalp promotes hair growth as long as the medicine is taken.
It is also seen that Finasteride reduces bleeding due to prostate problems by preventing vascular endothelial growth factor in the prostate gland, causing it to shrink.
Two main uses of Finasteride include:
Benign Prostate Enlargement
Male pattern hair loss
Proscar is mainly used to manage the symptoms of benign prostate hyperplasia. It can be used alone or in combination with other drugs for the same.
On the other hand, Propecia is usually recommended for male pattern hair loss
As with other medicines, Finasteride can also cause side effects in some individuals.
Common side effects include:
Trouble maintaining or getting an erection
Low sex drive
Breast tenderness
Increase in breast size
Skin rash
Other ejaculation disorders
Serious side effects include:
Depression
Nipple discharge
Pain or lump in the breasts
Swelling of tongue, face, lips, or throat
The use of Finasteride in elderly patients and those with kidney disorders do not require dose adjustment.
The market size of Finasteride in 2019 was about USD 110 Million worldwide. It is expected to grow 2.5% between 2020 and 2026.
The increasing prevalence of prostate hypertrophy and hair loss due to pollution and extreme weather conditions are likely to foster its growth.
In China, about 20 companies are selling Finasteride. Its sales increased by 2% from 2013 to 2017.
Experts believe that as the Chinese population ages, the number of patients with BPH will increase, and the Finasteride market will continue to grow.
The average cost of Finasteride in China is USD 1,641.
Many reputed manufacturers offer Finasteride in China. Some of them include:
Hunan Yuxin Pharmaceutical Co., Ltd.: It is a renowned pharmaceutical company that specializes in hormone and steroid intermediate pharma and API. They
provide high-quality raw materials and are among important players, especially in the international steroid market.
Lianyungang Hengfei Pharmaceutical Co., Ltd: It comes under the of world’s top 500 pharmaceutical companies. Their high-quality and market-
oriented approach has made them a preferred supplier globally.
You can also buy Finasteride in bulk from PharmaSources.com. It is a vertical e-commerce online destination with many quality global suppliers. PharmSources offers high-quality products to about 211 countries and regions. You can also compare products sold by various distributors and companies and thus make an informed decision.
The peak-plasma concentration is seen about 1-2 hours post-administration. This duration also depends on the dose. However, its bioavailability is not altered with food intake.
The ideal dose depends on various factors, including the condition for which the product is used. For prostate enlargement, the usual dose is 5 mg once a day. On the other hand, for male pattern baldness, the dose is 1 mg once a day.
However, the dose may differ for everyone, and it is not recommended to take the product without consulting your doctor.
https://pubchem.ncbi.nlm.nih.gov/compound/Finasteride
https://go.drugbank.com/drugs/DB01216
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6691938/
https://www.ncbi.nlm.nih.gov/books/NBK513329/
https://www.ncbi.nlm.nih.gov/books/NBK513329/
https://www.pharmacompass.com/price/finasteride
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