Tuesday, December 9, 2014

Turning to Prescription Medications for Hair Loss : Being realistic about what drugs can do , Keeping DHT in check with finasteride and dutasteride , Targeting hair follicles with minoxidil and Checking out some additional medications for women

Turning to Prescription Medications for Hair Loss
In This Chapter
  • Being realistic about what drugs can do
  • Keeping DHT in check with finasteride and dutasteride
  • Targeting hair follicles with minoxidil
  • Checking out some additional medications for women
Take a pill, grow your hair back. Sounds like a winning arrangement, doesn’t it? Unfortunately, although a few prescription
medications can help with specific types of hair loss, the magic hair pill has yet to be invented.
In this chapter, we look at prescription drugs that help with hair loss, drugs that may help some people some of the time (and that may include you), and drugs that are of no help whatsoever.
Managing Expectations
People generally expect miracles from prescription medications, and medications touted for hair loss are no exception. It’s important to recognize the capabilities and limitations of medical treatments for hair loss therapies before you start using one. What topical (the ones you pour on your head) and oral drugs can do is stop hair loss in some people and sometimes regrow hair in areas that aren’t yet totally bald. What they can’t do is regrow all the hair you’ve lost.
Hair that you lost many years ago isn’t likely to start growing. If you’re satisfied with the idea of stopping hair loss and perhaps experiencing some mild regrowth, then you may be very happy
with the results of taking some medications. But if you expect to regain the flowing locks you had in your teens, then you’re sure to be disappointed.
Be patient when starting pharmaceutical hair loss treatment. Results take many months, not days or weeks. You must commit to treatment for at least one year to know if you’re truly going to see any real benefit for pharmaceutical treatment. Remember, hair grows slowly, and it will take a considerable amount of time before you notice a difference.
Always use the medication as prescribed — whether that’s once daily, twice a day, or what ever regime your doctor prescribes for the best possible chance of results. If you stop using the medicine, you can expect to lose all the hair that you may have gained from this therapy as well as any hair you would have lost while you were on the therapy, but luckily not more. After about six months your hair will look as if you’d never used the medication, and you’ll resume losing hair at your natural rate.
The thought of taking a pill or using a solution on your scalp daily forever may seem discouraging. However, we encourage patients not to think of it that way. You can always decide at some point in the future that hair isn’t as important to you as it once was and stop using the medicine.
In addition, it’s possible that the future will bring better treatments for hair loss and perhaps a permanent cure. People use medication regularly for all kinds of conditions, such as high blood pressure or cholesterol, and it just becomes part of the daily routine. In time, the same is true with hair loss prescription medication.
Inhibiting DHT with Finasteride (Propecia)
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 deci- sion 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 treat- ment 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
As we explain in Chapter 4, 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 dihydrotestos- terone (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.
Testing 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 treat- ment 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 (see Chapter 18 for more on the FDA). 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 post- menopausal women was terminated after one year with no signifi- cant 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 demon- strated 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 peri- menopausal 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 under- stand 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 sev- eral 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 inter- actions between finasteride 1 mg and any other drugs reported at the time of this writing.
Checking 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 (brand name Rogaine; see the section, “Stimulating Hair Growth with Minoxodil,” later in this chapter) have an increased effect if taken together because they work differ- ently. 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.
Dutasteride — Another Inhibitor of DHT
In 2002, the FDA approved a drug called Avodart (dutasteride 0.5 mg) for the treatment of prostate enlargement in men, but the drug also works to inhibit DHT and therefore permit hair growth. This section helps you understand dutasteride and how it may be able to treat your hair loss.
Dutasteride isn’t approved specifically for the treatment of male pattern hair loss, and there are no long-term studies assessing its safety and efficacy in hair loss, although short-term study results have been promising.
How dutasteride works
Like finasteride, dutasteride inhibits the enzyme 5AR, which is responsible for the conversion of testosterone to DHT. However, unlike finasteride, which only inhibits one type of the enzyme, dutasteride inhibits both types, making the drug possibly more potent but also increasing the incidence of adverse reactions and side effects.
A dosage of dutasteride 0.5 mg per day decreases serum DHT 91 percent and scalp DHT 54 percent. In comparison, 5 mg finasteride decreases serum DHT 71 percent and scalp DHT 38 percent. Based on these numbers, you may expect dutasteride to be more effec- tive in the treatment of male pattern hair loss than finasteride.
However, because the type of 5AR that dutasteride blocks isn’t present in significant quantities in the hair follicle, the effects may not significant. Further studies are needed to answer this impor- tant question of which is more effective: dutasteride or finasteride.
Assessing the efficacy of dutasteride
Only a couple of studies have examined the effectiveness of dutas- teride for pattern hair loss.
In 2007, a study was published that compared the efficacy of dutas- teride to that of placebo in the treatment of androgenetic alopecia in 17 pairs of identical twin males over a one-year period. One twin from each pair received dutasteride 0.5 mg/day for 12 months while the other received placebo.
At the end of the study 15 of the 17 sets of twins correctly guessed which one was using dutasteride. The investigators concluded that dutasteride significantly improves hair growth and reduces hair loss progression in men with male pattern hair loss.
In 2006, a larger study was conducted with 416 men. The partici- pants received either dutasteride (in doses of 0.05, 0.1, 0.5 or 2.5 mg), finasteride 5 mg, or placebo daily for 24 weeks. The investiga- tors found that dutasteride increased area hair count versus placebo, with the level of success depending on the dosage.
In addition, dutasteride 2.5 mg was superior to finasteride 5 mg at 12 and 24 weeks. Scalp and serum dihydrotestosterone levels decreased, and testosterone levels increased, both with the level of success depending on the dosage. A major limitation of this study was that it was limited to only 24 weeks.
What are dutasteride’s side effects?
Dutasteride has a greater incidence of sexual side effects com- pared to finasteride (refer to the earlier section “What are finasteride’s side effects?”). Dutasteride was investigated in controlled multicenter studies involving men aged 50 and above with prostate enlargement. Drug-related side effects during the first six months included impotence (at 4.7 percent, the highest percentage of
occurrence), decreased libido, ejaculation disorders, and breast tenderness and breast enlargement (at 0.5 percent, the lowest percentage of occurrence).
The good news is that most drug-related sexual side effects decreased with time in this study. However, drug-related breast tenderness and breast enlargement remained constant over the treatment period.
In recent cases, dutasteride has caused significant drops in sperm count, which could result in problems with male fertility.
As with finasteride, dutasteride reduces the amount of PSA measured in the blood, which must be taken into account when PSA levels are used in the detection of prostate cancer. Women who are pregnant or may become pregnant shouldn’t handle dutasteride because of the possibility of absorbing it through the skin and sub- sequent potential risk to a male fetus.
Dutesteride hangs around in your bloodstream much longer that finasteride does; the half-life of dutasteride is five weeks compared to six to eight hours for finasteride, and blood tests can detect dutasteride in your system up to four to six months after you stop taking the drug. Therefore, you shouldn’t donate blood until at least six months after you final dose of dutasteride to prevent giving it to a pregnant woman through a blood transfusion.
At the time of this writing, dutasteride is being researched in an approved FDA format. This study is expected to address all the issues concerning safety and effectiveness of dutasteride as well as the side effects mentioned in this chapter. Stay tuned and talk to your doctor.
Stimulating Hair Growth with Minoxidil
The first FDA-approved medication for the treatment of hair loss was topical minoxidil, also known by the brand name Rogaine. Rogaine is a topical solution that’s applied directly to the scalp. Originally available only with a doctor’s prescription, it’s now avail- able over-the-counter as both Rogaine and generic minoxidil solu- tion, and it comes in concentrations of 5 percent for men and 2 percent for women. Recently, Rogaine developed a new minoxidil formulation in a 5 percent topical foam. This product is less greasy and easier to apply for some people.
How minoxidil works
Before minoxidil was available topically, it was an oral blood pressure medication. Doctors observed that many people taking oral minoxidil not only had a decrease in blood pressure but began growing body hair as well. It was reasoned that applying minoxidil directly to a bald scalp may cause hair to grow in this area without producing the side effects of the oral medication. Researchers developed a topical formulation, and studies showed modest hair growth on the scalp.
Just how minoxidil works in hair growth is unknown. The drug is a vasodilator (vasodilators cause the blood vessels to dilate, or expand) and may increase the flow of blood to the hair follicle, but how this relates to hair loss is unclear. In addition, minoxidil also increases the duration of the hair follicle growth cycle and improves the quality of the hair by increasing the diameter and length of fine, miniaturized hair.
How effective is minoxidil and on which areas of the scalp?
The original studies on minoxidil were performed on the crown of the head, so there’s a misconception that it only works in this area. Although minoxidil may work best in the crown area, it also works to a lesser degree in other areas as long as there’s some fine (miniaturized) hair (such as at the front of the scalp). However, it doesn’t work if the area is totally bald.
The greatest benefit from minoxidil is visible between six months to two years from the beginning of treatment. After this time, you see a gradual decrease in effectiveness, so you’ll continue to lose hair, but at a slower rate than if you weren’t on the drug.
The effectiveness of minoxidil to treat men with pattern hair loss has been investigated since the mid-1980s and is well established. Even though both 5 percent and 2 percent solutions have been shown to decrease hair loss and increase hair, the 5 percent solu- tion seems to work better.
If you stop using minoxidil, the effects wear off within three months, and the previous pattern of hair loss resumes. When you restart it, you generally don’t regain the hair that was lost, so it’s best not to stop and start the mediation but rather to use it regularly.
Does minoxidil work for women?
Yes, minoxidil works for women with pattern hair loss, but only the 2 percent concentration of minoxidil has been approved for their use. In 1994, a study was conducted in which 256 women with androgenic alopecia used 2 percent minoxidil twice daily for 32 weeks. At the end of the study, the investigators found that 60 per- cent of the patients in the 2 percent minoxidil group reported new hair growth compared with 40 percent of the patients in the placebo group.
The investigators concluded that minoxidil is an effective treatment for pattern hair loss in women but that it doesn’t work on all patients.
Although the 2 percent minoxidil solution is the only approved dose in women, there’s evidence that the 5 percent solution may be superior. In 2004, a study with 381 female patients with pattern hair loss was conducted comparing 5 percent minoxidil with 2 per- cent minoxidil. Both strengths were shown to help regrow hair, but the 5 percent topical minoxidil group demonstrated superiority over the 2 percent group.
What are minoxodil’s side effects?
By far the most common side effect of topical minoxidil is local irritation, although the foam formulation is much less irritating than the original version.
Another side effect sometimes seen in women is the development of facial hair. Although this may decrease when the medication is discontinued, at times the hair may need to be removed after treat- ment with either electrolysis or lasers. To reduce the chances of this problem (although you can’t eliminate it entirely), you should be careful when applying minoxidil and try to avoid the medication dripping down onto the temples and forehead, unless, of course, a hairy forehead is the look you’re going for! (Although the 2 percent solution is standard for women, there’s a significantly greater incidence of this side effect when the 5 percent solution is used.)
Female patients also seem to be more sensitive to the potential systemic side effects of minoxidil in decreasing blood pressure (a condition called hypotension). Rarely women may get lightheaded (a symptom of low blood pressure) from topically applying minoxidil. Women also have an increased risk of developing allergic skin reactions on the scalp.
It is important to know that minoxidil can cause birth defects. Women who are pregnant, planning to become pregnant, or nursing shouldn’t use this medication.
Comparing minoxidil to finasteride
Studies have demonstrated that minoxidil is an inferior treatment for male pattern hair loss compared to finasteride. In 2004, a study was conducted in which male androgenetic alopecia patients used either 1 mg oral finasteride or 5 percent topical minoxidil twice daily for one year. Eighty percent of the men using finasteride and 52 percent of those using minoxidil had an increase in hair density. The study demonstrated that while both medications are effective, finasteride is superior. Additional studies have shown that the combination of finasteride with minoxidil is superior to finasteride alone, which suggests a synergistic effect, meaning that two med- ications together work better than either medication used alone.
Applying minoxidil
Doctors recommend that you apply minoxidil directly to the scalp (not the hair) twice a day. In order to regain lost hair, you need to apply the solution to all thinning areas, including the frontal hair- line and temples.
Once a day topical use of minoxidil is probably almost as effective as twice a day use because it has a long half-life of almost 24 hours. Once a day dosing is a reasonable option if it’s not practical for you to apply it twice daily.
In fact, a study in 2007 showed that using a combination of 5 percent minoxidil and 0.01 percent tretinoin (a cream that makes the minoxidil penetrate the scalp better) once a day was equivalent conven- tional 5 percent minoxidil twice-daily therapy for the treatment of pattern hair loss in men.
One caveat is that topical tretinoin can sometimes be irritating to the scalp and may increase the amount of minoxidil entering the bloodstream, which could result in unwanted side effects (covered in the earlier section, “What are minoxidil’s side effects?”).
Medications for Women Only
Two prescription medications for women with pattern hair loss deserve special mention: spironolactone and cyproterone acetate. Both are anti-androgens, meaning they suppress the actions of testosterone, and have been studied in women to treat female pat- tern hair loss. These medications should be used by women only; for men, they cause decreased sex drive and other unacceptable side effects.
Spironolactone
Spironolactone (brand name Aldactone) is an oral diuretic (or water pill) that’s FDA-approved to treat congestive heart failure and high blood pressure. The drug also has been shown in a few small studies to help reduce unwanted hair in females and has been studied in women with pattern hair loss — but with mixed results. It may have some effect in reducing thinning in women with very limited pattern hair loss.
Spironolactone has been associated with an increased risk of bleeding from the gastrointestinal tract, although a definite link hasn’t been established. It isn’t used in men because it can cause testicular atrophy and breast enlargement as well as decreased sexual function.
Cyproterone acetate
Because it’s an anti-androgen (anti-androgens block the effects of male hormones in women), cyproterone acetate should be used only by women. A few studies have been published documenting mild effectiveness of cyproterone acetate in the treatment of both hirsutism (excessive hairiness) and female pattern hair loss. It’s available in combination with estrogen for use as an oral contraceptive in Europe, but it’s not FDA-approved and not available in the U.S.
The most serious potential side effect of cyproterone acetate is liver toxicity; the drug also has been linked to increased rate of blood clots.