Finasteride (Propecia and Proscar): Finasteride is a prescription anti-androgen medication developed by Merck Pharmaceuticals and first prescribed for men with enlarged prostrate glands, sold under the brand name Proscar, and used at the 5 milligram per day level. It inhibits the enzyme 5-alpha-reductase that converts testosterone into DHT.
Finasteride as Propecia can stop further hair loss, and may be combined with other medications such as minoxidil to promote hair growth. Propecia is a one-milligram tablet form of finasteride. It is an oral treatment - taken once daily - for hair loss in men. In a two-year clinical studies in men between the ages of 18-41 with mild to moderate hair loss at the top of their heads, Propecia was shown to maintain or increase the amount of hair in 83% of men vs. 28% taking the placebo. A panel of dermatologists evaluating patient photographs found 37 percent of the patients treated with Propecia increased their hair growth, while 7 percent of those taking a placebo showed improvement. 53 percent of the men with frontal hair loss said Propecia treatments improved the appearance of their hair. This is interesting because minoxidil works best at the top of the scalp but more poorly in the frontal area.
Propecia works within about 3 months. Hair grows very slowly, about half an inch a month. Most men begin to see the first benefit of Propecia, slowing of hair loss, as easily as 3 months, and after 6 months begin to experience regrowth.
The side effect among the 1,879 men participating in Propecia clinical trials was decreased libido in 1.8 percent and erectile dysfunction in 1.3 percent. Some young men tell us that they view this decrease in libido drive as calming influence on their mental state.
Propecia is for use by men only and it may cause a birth defect known as hypospadias in a male fetus if used by pregnant women. Merck also studied Propecia in 136 postmenopausal women suffering hair loss. Despite a year of therapy, the women who took Propecia had no more hair than women who got a placebo pill.
Male pattern hair loss is characterized by progressive miniaturization of hair follicles. Finasteride inhibits a key factor responsible for this miniaturization. This leads to a reversal of the process of scalp hair loss in many men. A recent a double-blind clinical study of men using Propecia for one year, presented by Dr. David Whiting and based on microscopic analysis of 4 millimeter punch biopsies from the scalp in 26 patients (14 on finasteride, 12 on placebo pill), found that the drug increase the number of follicles growing terminal hairs by 29% and reduced the follicles growing vellus hair by 6.9% when compared to the placebo group. In normal non-balding men, the ratio of terminal hairs to vellus hairs male head is 6-8 terminal hairs to 1 vellus hair, but in balding men, the ratio ranges between 0.1 to 3.9 terminal hairs to 1 vellus hair. Balding persons on Propecia changed from a starting ratio of 1 terminal hair to 1.7 vellus hairs to final ratio of 1 terminal hair to 1.1 vellus hairs. This data demonstrates that Propecia helped to partially reverse the hair follicle miniaturization process.
A similar study by Dr. Whiting 127 postmenopausal females on Propecia failed to demonstrate a hair stimulating effect of propecia.
Experts estimate that cosmetically significant regrowth will probably be observed in about a quarter of the Propecia users. The reason for the relatively moderate effectiveness of Propecia in reversing baldness is that it counteracts only one (albeit important) factor involved in hair loss, a hormone dihydrotestosterone (DHT) and, of the two types of 5-alpha reductase (both type 1 and type 2) that produce DHT, it only blocks type 2 DHT. Propecia comes in a 1 mg pill form, available by prescription only, and costs about $40-50 per month.
Recent research indicates that the DHT that harms hair follicles comes from the the skin's sebocytes and sweat glands (sebaceous glands). (Chen et al 1996) 5 alpha-Reductase, the enzyme system that converts testosterone into DHT occurs in two enzyme forms. The type 1 represents the 'cutaneous type'; it is located primarily in the skin's sebocytes but also in epidermal and follicular keratinocytes, dermal papilla cells and sweat glands as well as in fibroblasts. The type 2 is located mainly in the seminal vesicles, prostate and in the inner root sheath of the hair follicle.
Propecia(c) (Finasteride), which has a higher affinity for the type 2 form, is best suited for for controlling prostate enlargement. It also must be administered by pills that spread the drug throughout the body.
Copper ion in the skin is more effective in inhibiting the type 1 form which is primarily producing the DHT that damages follicles and can be administered locally to the skin. Sugimoto et al (Sugimito 1995) found that copper ion is a potent inhibitor of 5-alpha reductase, inhibiting both types of 5-alpha reductase (both type 1 and type 2) that produce DHT and is the only metal to do so. Copper ion inhibits (50% reduction in activity) type 1 alpha reductase at 1.9 micromolar (0.12 micrograms copper ion per milliliter) and type 2 alpha reductase at 19.2 microM (1.2 micrograms copper ion per milliliter). No other metal has these effects.
The application of copper-peptides may provide sufficient copper ion into the hair follicle area to block DHT production in the scalp. Metabolically active copper ion (that is, copper ion free to block 5-alpha reductase) in the human body exists at about 1 microgram per milliliter in the blood and less in the skin. While the uptake of ionic copper from copper-peptides applied to the scalp is very low, human experiments by Prof. John Sorenson (University of Arkansas) have found that they can raise copper ion levels in the skin to the effective level of 1 microgram per milliliter.
The red saw palmetto berries of a small palm native to the south east US, or serenoa repens, possess activities that inhibit -alpha reductase and the binding of DHT to androgen receptors. In Europe the extract is called Permixon, and is extensively to treat benign prostatic hypertrophy. Numerous European studies have demonstrated its efficacy in reducing prostate hyperplasia in a manner similar to finasteride. It is both a 5-alpha reductase inhibitor and blocks 50% of the uptake of DHT at its target tissue receptor sites. Saw palmetto is very safe, being used by native Americans was long used by local Native Americans as a food and as a herbal treatment for enuresis, nocturia, atrophy of the testes, impotence, inflammation of the prostate and low libido in men. Many herbalists consider saw palmetto a mild aphrodisiac for men. Women used the berries to treat infertility, painful periods and problems with lactation.
Saw palmetto berries contain an oil with several fatty acids, including capric, caprylic, caproic, lauric, oleic and palmitic and acid, and their ethyl esters plus high amounts of phytosterols (beta-sitosterol, cycloartenol, stigmasterol, lupeol, lupenone and 24-methyl-cycloartenol), as well as other oils, resins, and tannins.
Saw palmetto is a "multi-site" inhibitor of the formation and actions of DHT. It inhibits 50% of the binding of DHT to receptor sites in the prostate, blocks the uptake of DHT into the nucleus of prostate cells, and inhibits the action of testosterone 5-alpha-reductase, which converts testosterone to DHT.
Because of its use is not patentable, it has not been developed by pharmaceutical companies and there are no published studies evaluating its effects on balding. Dr. James Duke in his book The Green Pharmacy lists Serenoa repens as his first choice for hair loss treatment He writes that the biochemistry certainly supports the use of serenoa repens. The herb blocks the formation of DHT much like Propecia. Serenoa repens has also been shown to reduce inflammation, a common factor seen in tissues involved in androgenic alopecia.
Saw palmetto effective in prostate hyperplasia.