Inhibiting DHT with Finasteride (Propecia)

by Kelly Makay.

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One of the few prescription medications that really works to replace hair lost from male pattern baldness is finasteride, more commonly known as Propecia. Here we describe why it works and for whom; we also get into some of the side effects and the pros and cons of taking the drug so that you can make an informed decision with your doctor.

The discovery of finasteride

There's a common misconception that finasteride was first conceived as a prostate medication and was coincidentally found to prevent hair loss. The reality is that in 1974, researchers described a group of male children from the Dominican Republic who were deficient in the enzyme 5-alpha reductase (5AR). These male children had very low levels of DHT, and throughout their lives, their prostates remained small and they didn't develop male pattern hair loss or acne.

The scientists' goal was to find a drug that could block the 5AR enzyme and mimic the abnormality found in these boys. The scientists then could use this drug to prevent both prostate enlargement and hair loss. A deliberate (business) decision was made to seek Food and Drug Administration (FDA) approval for its use in treating prostate enlargement (a medical condition) rather than hair loss (a cosmetic problem).

In 1992, 5 mg finasteride was released under the brand name Proscar for use in men over 50 with prostate enlargement. Some men taking Proscar noted hair growth in balding or bald areas of their scalps. Scientific studies were done to determine if this drug would reduce the balding process and possibly grow hair. Varying doses of finasteride were tested to determine the safest and most effective dose for the treatment of hair loss, and in 1997, the FDA approved finasteride 1 mg per day (Propecia) for the treatment of male pattern baldness.

How finasteride works

Male pattern baldness (androgenetic alopecia in medical lingo) is caused by the effects of the male hormone dihydrotestosterone (DHT) on genetically susceptible hair follicles predominantly in the front, top, and crown of the scalp (not the back and sides).

DHT causes hair loss by shortening the growth phase of the hair cycle, which leads to a decreased size (thickness) or miniaturization of the follicles. The affected hair grows more slowly or stops growing completely and progressively evolves into a shorter and finer hair until it eventually disappears.

Two of the male sex hormones are testosterone and dihydrotestosterone (DHT). Cells in the body metabolize testosterone and turn it into DHT. The traffic cop that supervises this process is an enzyme called 5-alpha reductase (5AR). The two types of 5AR are:

Type I is located mainly in sebaceous (sweat) glands, keratinocytes, and fibroblasts. Its exact role in hair growth has not been determined. This enzyme catalizes the conversion of testosterone into androstenedione (another hormone) which seems to be related to the production of sebum. The role of Type II 5AR in hair loss is not well defined.

Type II is found in the skin and the sheath of hair follicles on the scalp. This form of the enzyme seems to cause hair loss in those with the gene for hair loss, and can be blocked by the actions of drugs like finasteride.

The drug finasteride makes 5AR work less effectively, reducing the body's ability to produce DHT. When you take the drug orally, it reaches the bloodstream and the scalp hair follicles, where it decreases the amount of DHT made in the hair follicles. Finasteride at the 1 milligram per day dose has been clinically shown to decrease serum DHT levels by almost 70 percent.

Although many professionals falsely think that finasteride lowers a man's testosterone level, in fact, on average finasteride causes a rise in serum testosterone levels by 9 percent, although this is still within the normal range.

The efficacy of finasteride

Propecia is the brand name for finasteride at the 1 mg dose, and it's proven to be very effective in the treatment of common pattern hair loss. Studies have shown that after five years of treatment, almost half of men treated with Propecia demonstrated an increase in hair growth, and 90 percent of men maintained most of their hair in previous thinning areas over this time period.

Only 10 percent were rated as having lost hair when compared to their baseline hair measurements. In those not taking the drug, 75 percent were rated as having lost hair during the course of the study.

One mg finasteride can help you to preserve the hair you've got at any age, but it works best for hair regrowth in younger patients or those who have had recent hair loss in the past two to three years. Occasionally, people over age 50 see regrowth of some hair with finasteride, but this is the exception rather than the rule.

It's important to know that finasteride will only work as long as you're taking it. Within two to six months of discontinuing treatment with finasteride, the previous hair loss pattern will generally return to its state as if the medication had never been used.

Although many doctors will tell you that finasteride doesn't work for balding in the frontal area of the scalp, the FDA did approve it for this type of hair loss.

Many people who have had early thinning in the frontal scalp may regrow hair if they start finasteride early in the thinning process. DHT causes frontal hair loss, and finasteride blocks the DHT impact on the loss of hair, but if there's no hair in the fontal area at all, you shouldn't expect any to appear.

You must take finasteride for at least one full year before your doctor can accurately determine its effects. During the first six months, you may note some thinning of existing hair as the new growing hair replaces the sickly miniaturized hair, so it's important to be patient during this period.

Does finasteride work for women?

There's some controversy on whether finasteride is effective in women. One study evaluating the efficacy of finasteride in postmenopausal women was terminated after one year with no significant hair growth.

Another study evaluated the effectiveness of the combination of a higher dose of oral finasteride (2.5 mg) with an oral contraceptive. This study only included perimenopausal women with pattern hair loss. After one year, 62 percent of the women in this study demonstrated some decrease of hair loss.

It's not clear if the success was due to the dosage (2.5 mg instead of 1 mg used in the previous study); the combination of use with an oral contraceptive containing drospirenone, which also has an effect on hair loss; or the fact that this study looked at perimenopausal instead of postmenopausal females.

The study group was too small to determine safety from a statistical point of view. Finasteride has not been approved for women. In addition, women shouldn't handle crushed or broken Propecia tablets when they're pregnant or may potentially be pregnant because of the possibility of absorption through the skin and the subsequent potential risk to a male fetus in the first trimester of pregnancy. However, there appears to be no risk to the fetus if a man taking finasteride impregnates a woman.

As of this writing, finasteride isn't recommended for women to treat pattern hair loss. Further studies are needed to better understand which women may respond to treatment before its use can be advocated, and safety issues (including a possibility of increased risk of breast cancer) also need further investigation.

What are finasteride's side effects?

Side effects from Propecia at the standard 1 mg daily dose are rare, and fortunately if they do occur, they're not permanent.

In a study of men taking finasteride 1 mg, around 2 to 4 percent experienced some form of sexual dysfunction (decreased libido, erectile dysfunction, or decreased volume of ejaculate) compared to just over 2 percent of men treated with a placebo.

For those men who reported cases of sexual dysfunction soon after starting the medication, it appeared generally within months. A small number of men saw a change in their libido or sexual function months or years into taking the drug.

You'll be happy to know that the sexual side effects were reversed in all men who discontinued therapy (and in 58 percent of those who continued treatment, the sexual side effects returned to their normal premedication levels).

After the medication was stopped, all sexual side effects generally disappeared within a few weeks. If you experience negative sexual side effects, you should consult with your doctor about stopping the medication until the side effects go away and then restarting at a lower dose (either a quarter or half of a 1 mg pill a day).

If you have no side effects after several weeks on the lower dose, you can work back up to the 1 mg per day dose. Even staying on a lower dose will offer some benefit, but if side effects occur at the lower dose, it may be time to quit therapy with this medication.

Another rare side effect to be aware of is breast tenderness or breast enlargement (in males this is called gynecomastia). This occurred in 0.4 percent of men on finasteride 1 mg but was no greater than in the control group. In men who developed gynecomastia, the appearance of breast cancer was slightly higher than in the control group, although this connection may not be statistically significant.

Other side effects that were no more common than those experienced in patients taking a placebo included rash, itching, hives, swelling of the lips and face, and testicular pain. Some rare cases of mood changes have also been reported. There have been no interactions between finasteride 1 mg and any other drugs reported at the time of this writing.

Finasteride's effects on the prostate

Prostate specific antigen (PSA) levels are used to screen for prostate enlargement and prostate cancer. Finasteride causes a decrease in PSA blood levels by approximately 50 percent in healthy men; therefore, it's important that your doctor know if you're taking finasteride so that he or she may take this into account when interpreting your PSA results.

A study in 2003 on 5 mg finasteride reported that men treated with 5 mg finasteride for seven years had a 25 percent reduction in prostate cancer compared to men treated with placebo.

The authors concluded that 5 mg finasteride prevents or delays the appearance of prostate cancer and that this possible benefit and a reduced risk of urinary problems must be weighed against sexual side effects and the remote possible increased risk of more aggressive prostate cancer.

Men aged 50 or over should inform their regular physicians or urologists if they're taking Finasteride 1 mg to treat hair loss. It's also recommended that all men aged 50 or over have routine annual evaluations for prostate disease, regardless of whether or not they're on Finasteride 1 mg. (African Americans or patients with a family history of prostate disease should start annuals exams at age 40.) An evaluation may include a rectal examination, a baseline PSA, and other tests that the physician feels are appropriate.

Proper dosing of finasteride

If your doctor prescribes finasteride to treat your hair loss, it's best to take the recommended dose of 1 mg per day as long as you have no side effects. Lower doses have been shown to be effective, but less so. There's also little evidence that a higher dose helps, although some doctors may increase the dose under certain circumstances. Studies don't yet show statistically valid connections between a higher dose of finasteride for the treatment of hair loss in men.

The 5 mg dose of finasteride now available in generic form is cheaper than five doses of Finasteride 1 mg. (The brand name of the 5 mg dose is Proscar.) You can use a pill cutter to divide the 5 mg tablet into approximately four pieces. Taking one piece every day is equivalent to 1.25 mg per day, but be advised that there's no scientific data ensuring that this is as effective as finasteride 1 mg.

Also, remember that there's a potential risk to pregnant women from handling broken or crushed tablets as finasteride can be absorbed through the skin.

Finasteride 1 mg isn't affected by food, so you can take it any time during the day without regard to meals. Taking it in the morning may have an advantage, though, because testosterone levels are highest in the morning in most men.

Combining finasteride and minoxidil

Finasteride and minoxidil have an increased effect if taken together because they work differently. Finasteride permits hair growth by blocking the negative effects of DHT, whereas minoxidil stimulates the hair follicle directly. Of the two, finasteride is far more effective. There are no contradictions to taking the two together, and you may see better results by taking both regularly.

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