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cure of hair loss with medications PDF Print E-mail

Medications

Medications serve an important role in both the prevention and treatment of hair loss particularly in the early stages of the balding process. The FDA approved medication Propecia finasteride), which inhibits DHT, is particularly helpful in reversing genetic baldness in its early stages. Rogaine (minoxidil) can sometimes be useful for early hair loss by stimulating hair growth, but it is more effective when used in conjunction with Propecia. Because medical therapy works to thicken hair in areas that are thinning (miniaturized), rather than to grow hair once it is lost, medical treatment is best started as soon as possible.                

This section focuses on the FDA approved hair loss treatments, how they work, how they should be used, and their potential problems.Avodart (dutasteride) is approved for prostate enlargement, but is not yet indicated for hair loss. The diuretic Aldactone (spironolactone), a treatment for hair loss occasionally used in women, will be discussed briefly.

Rogaine (Minoxidil)

Rogaine, the brand name for minoxidil, was the first FDA approved medication for the treatment of hair loss. Rogaine is a topical solution that is applied directly to the scalp. It can now be purchased without a prescription and in generic formulations in concentrations of 5% (for men) and 2% (for women).

Rogaine was developed from the oral blood pressure medication minoxidil (Loniten). Minoxidil taken orally has potential serious side effects on the heart and circulatory system and is used only when other blood pressure medications have been unsuccessful. It was observed that patients who were taking minoxidil began growing body hair and it was reasoned that applying minoxidil directly to a bald scalp might cause hair to grow in this area as well.

The original studies on Rogaine were performed on the crown, so there is a misconception that it only works in this area. Although minoxidil usually works best in the crown, it also works to a lesser degree in other areas, such as the front of the scalp, as long as there is some fine (miniaturized) hair in the area. It does not work when the area is totally bald. The greatest benefit from the medication is seen from 5 months to 2 years, with a gradual decrease in effectiveness after that. Those using minoxidil long-term will continue to lose hair, but at a somewhat slower rate.

The exact mechanism by which minoxidil works is not known, but the drug is felt to increase the duration of the hair follicle growth cycle (called anagen). This improves the quality of the hair by increasing the diameter and length of fine (miniaturized) hair. The simultaneous use of minoxidil and Propecia, which directly inhibits the formation of DHT, may have some synergistic benefit in the treatment of hair loss, although the latter medication is significantly more effective.

Using Minoxidil

Minoxidil should be applied to the scalp twice a day. The medication only works if it is in direct contact with the scalp (not the hair) and only works in areas where it is applied. Therefore, it is important to use the medication in the front part of the scalp if this is an area of thinning.

The 5% formulation is twice as effective as the 2% solution, but contains propylene glycol, a compound that can irritate the scalp and can make the hair feel sticky and difficult to manage. If this is a problem, one should consider using the 5% solution at bedtime and the 2% solution (which is alcohol based and less sticky) in the morning. When using minoxidil, it may take 6-12 months before any results are seen.

The majority of patients who see an effect from minoxidil experience a delay, or decrease, in the rate of hair loss. The drug also serves to thicken already existing hair, but most patients who do have results, grow only short, thin fuzz. It will not grow any new hair on a bald scalp.

Use in Women

Only the 2% concentration of minoxidil is approved for use in women. Women are generally more sensitive to the side effects of minoxidil in decreasing blood pressure (hypotension) and may get light-headed from the medication. Women also have an increased risk of developing allergic skin reactions (contact dermatitis).

 An annoying local reaction that women sometimes get from topical minoxidil is the development of facial hair. Although the facial hair slowly resolves when the medication is discontinued, at times the hair may need to be removed. Carefully trying to avoid the medication dripping down onto the temples and forehead seems to reduce, but not totally prevent, this problem. There is a significantly greater incidence of these side effects if the 5% solution is used.

Propecia

Male pattern baldness or androgenetic alopecia is caused by the effects of the male hormone dihydrotestosterone (DHT) on genetically susceptible hair follicles that are present mainly in the front, top, and crown of the scalp (rather than the back and sides). DHT causes hair loss by shortening the growth, or anagen, phase of the hair cycle, causing miniaturization (decreased size) of the follicles. The effected hair becomes progressively shorter and finer until it eventually disappears

DHT is formed by the action of the enzyme 5-alpha reductase on testosterone. Finasteride is a drug that works by blocking the enzyme 5-alpha reductase Type II that converts testosterone to dihydrotestosterone (DHT) in the hair follicle. Propecia, the brand name for finasteride, is the only FDA approved oral medication for hair loss.

Finasteride causes a significant drop in both scalp and blood levels of DHT and its effect is felt to be related to both of these factors. Finasteride 1-mg/day decreases serum DHT levels by almost 70%. Serum testosterone levels actually increased by 9%, but this is within the range of normal.

It is commonly thought that finasteride was first conceived as a prostate medication and that, only by chance, was found to prevent hair loss. The fact is that in 1974 the researcher Imperato-McGinley described a group of genetically male children from the village of Salinas in the Dominican Republic who were deficient in the enzyme 5-alpha reductase. These male children had very low levels of DHT and throughout their life, their prostates remained small and they did not develop male pattern hair loss or acne.

The objective of the researchers was to find a drug that could block the 5-alpha reductase enzyme and mimic the abnormality found in these men. They could then use this drug to prevent both prostate enlargement (BPH) and hair loss. The decision was made, however, to obtain FDA approval for the medical indication first, rather than the cosmetic one. As a result, in 1992, Finasteride 5-mg was released under the brand name Proscar, for use in men over 50 with prostate enlargement (the prostate also has the type II enzyme). Five years later, i n 1997, the FDA approved finasteride 1-mg/day (Propecia) for the treatment of male pattern baldness.

Studies have shown that after five years of treatment, 90% of men taking finasteride maintained their hair or increased hair growth. At five years, 48% of men treated with Propecia demonstrated an increase in hair growth, 42% were rated as having no change (no further visible progression of hair loss from baseline) and 10% were rated as having lost hair when compared to baseline.

In comparison, 6% of men treated with placebo demonstrated an increase in hair growth, 19% were rated as having no change and 75% were rated as having lost hair when compared to baseline.

Using Propecia

Propecia should be taken once daily with or without meals. Patients must take Finasteride for one year or longer before its effects in preventing hair loss and re-growing hair can be accurately assessed. Finasteride takes up to a year or more to exert its full effects in both preventing hair loss and in re-growing hair. During the first six months you may note some thinning of your existing hair. This may be due to either progression of your hair loss before finasteride has had a chance to work or some shedding of miniaturized hair that makes way for the new healthy anagen hair to grow. It is important to be patient during this period. You should continue the medication for at least one year before you and your doctor can assess its benefits.

 Side Effects

Side effects from finasteride at the 1-mg dose are uncommon, but reversible. The one- year drug related side effects were 1.5% greater than in the control group. The data showed that 3.8% of men taking finasteride 1mg experienced some form of sexual dysfunction verses 2.1% in men treated with a placebo. The five-year side effects profile included: decreased libido (0.3%), erectile dysfunction (0.3%), and decreased volume of ejaculate (0.0%).

Most reported cases of sexual dysfunction occurred soon after starting the medication, but there have been reports of sexual dysfunction that have occurred at later points in time. The sexual side effects were reversed in all men who discontinued therapy, and in 58% of those who continued treatment. After the medication was stopped, side effects generally disappeared within a few weeks. When finasteride is discontinued, only the hair that had been gained or preserved by the medication is lost. In effect, the patient returns to the level of balding where he would have been had he never used the drug in the first place.

Adverse Reactions

Adverse reactions related to the breast, including breast tenderness or breast enlargement (gynecomastia), occurred in 0.4% of men taking finasteride 1-mg (Propecia), but this was no greater than in the control group. Other side effects that were not statistically significant included hypersensitivity reactions including rash, pruritus, urticaria, swelling of the lips and face, and testicular pain

Caution during Pregnancy

Finasteride use is contraindicated in women when they are, or may be, pregnant. Women should not handle crushed or broken Propecia tablets when they are pregnant, or may potentially be pregnant, because of the possibilities of absorption of finasteride and the subsequent potential risk to a male fetus. Propecia tablets are coated and will prevent contact with the active ingredient during normal handling, provided that the tablets have not been broken or crushed Exposure of pregnant women to semen from men treated with Propecia poses no risk to the fetus.

Use in Post-Menopausal Women

Merck recently carried out a study to evaluate the efficacy of finasteride in post-menopausal women. After one year there was no significant hair growth and, as a result, the study was terminated. An explanation is that hair loss in women is related more to the action of the enzyme aromatase (which is unaffected by finasteride) rather than DHT. It is also possible that the low DHT levels observed in postmenopausal women are responsible for the lack of significant response to finasteride. (See causes of hair loss in women)

Long-Term Benefits and Risks

The effects of finasteride are confined to areas of the scalp that are thinning, but where there is still some hair present. It does not grow hair in areas that are completely bald. Although it can regrow hair in thin areas, the major benefit of finasteride seems to be in its ability to slow down or halt hair loss. Results generally peak around one year and then are stable in the second year or decrease very slightly. Although the long-term ability of finasteride to maintain one's hair is unknown, the majority of men find that after 5 years the medication is still working.

The benefits of finasteride will stop if the medication is discontinued. Over the 2-6 months following discontinuation, the hair loss pattern will generally return to the state that it would have been if the medication had never been used.

Propecia and Hair Transplantation

Propecia (finasteride) has shown to be useful in complementing a hair transplant for several reasons

  • Propecia works best in the younger patient who may not yet be a candidate for hair transplantation
  • Propecia is less effective in the front part of the scalp, the area where surgical hair restoration can offer the greatest cosmetic improvement
  • Propecia can regrow, or stabilize hair loss, in the back part of the scalp where hair transplantation may not always be indicated

For those who choose not to take Propecia, or who cannot take it due to its side effects, the surgical hair restoration is just as effective. The only difference is that medications can prevent further hair loss whereas surgery cannot. Medicationsare not needed for a hair transplant to be successful or the transplanted hair to grow and be permanent.

Generic Finasteride

 Finasteride 5mg (Proscar) is available in a generic formulation. (Propecia) will not be available generically until the year 2012. For those wanting to take generic finasteride, we recommend buying a pill cutter at the pharmacy and taking ¼ of a 5mg tablet every day. Please be advised that there is no scientific data insuring that this will be as effective as Propecia 1mg a day. Also, remember that there is a potential risk to pregnant women from handling broken or crushed tablets (see Caution during Pregnancy)

Increasing the Dose

We are often asked if one should increase the dose of Propecia. Although we do increase the dose under certain circumstances, there is no scientific evidence that increasing the dose will have any additional effects. There are published data demonstrating that 5 mg is no better than 1 mg from controlled clinical trials. In practice, I often increase the dose when someone has been on the same dose of medication for about three years and then stops responding.

Patient Monitoring

It is recommended that men aged 50, or over, should inform their regular physicians or urologists that they are taking Propecia (finasteride 1mg). It is also recommended that all men aged 50 or over have a routine annual evaluation for prostate disease, regardless of whether or not Propecia is used.

The above are general guidelines recommended for all men of appropriate age, regardless of whether they use Finasteride or not. Specific recommendations for each Patient should be based upon the judgment of his own physician.

Common Misconceptions about Finasteride

Myth: Women can't touch the medication.
Fact: Pregnant women should not handle crushed or broken tablets.

Myth: It only works in the crown.
Fact: It potentially works any where on the scalp where there is some hair, even in the front of the scalp.

Myth: Once you start it you must take it for ever.
Fact: You can stop the medication any time you want - you just lose its benefits when one stops.

Myth: Finasteride lowers testosterone
Fact: The medication, on average, causes a rise in serum testosterone levels by 9%.

Myth: The sexual side effects are frequent and irreversible.
Fact: The sexual side effects occur in 2% and are completely reversible when the medication is stopped.

Myth: Finasteride causes birth defects if a man takes it when his wife is pregnant.
Fact: Exposure of pregnant women to semen from men treated with Propecia poses no risk to the fetus.

Myth: Propecia was originally a prostate medication that was found to prevent hair loss.
Fact: Propecia is not a prostate medication that was by chance noted to have a side effect of hair growth, it is a medication that was known since its discovery that it could grow hair.

Avodart

In 2002, the FDA approved Avodart (dutasteride 0.5mg) for the treatment of prostate enlargement in men (the medical term is symptomatic benign prostatic hyperplasia or BPH). Dutasteride is not approved for the treatment of male pattern hair lost.

Like finasteride (the active ingredient in Propecia), dutasteride is an inhibitor of the enzyme 5 alpha-reductase responsible for the conversion of testosterone to DHT (dihydrotestosterone). However, unlike finasteride, which only inhibits the Type I form of the enzyme, dutasteride inhibits both the Type I and Type II forms of the 5 alpha-reductase enzyme. This dual effect makes the drug more potent but also increases the incidence of adverse reactions.

 The Type II form of the enzyme is found predominantly in the hair follicle. The Type I form of the enzyme has been found in the scalp and sebaceous glands, but its exact role in hair growth has not been determined.

Effects on Hair Growth

 Dutasteride 0.5mg/day decreases serum DHT 91% and scalp DHT 54%. Finasteride 5mg/day decreases serum DHT 71% and scalp DHT 38%. Based on these results, dutasteride should be significantly more effective in the treatment of androgenetic alopecia than finasteride. However, since the Type I form of the 5 alpha-reductase that dutasteride blocks is not present in significant quantities in the hair follicle, these effects may not be as significant as one might expect. The increased efficacy of Dutasteride is felt to be due, in part, to its effects on lowering serum DHT.

A study by Olsen et al. published in the Journal of the American Academy of Dermatology in 2006 has showed the benefits of dutasteride over finasteride in a scientifically rigorous, placebo-controlled study

Side Effects

 Dutasteride was investigated in controlled multi-center studies involving 4,325 men aged 50 and above with prostate enlargement. Drug-related side effects during the first six months were as follows: impotence (4.7 percent vs. 1.7 percent for placebo), decreased libido (3 percent vs. 1.4 percent), breast tenderness and breast enlargement (gynecomastia; 0.5 percent vs. 0.2 percent) and ejaculation disorders (1.4 percent vs. 0.5 percent).

 The incidence of most drug-related sexual adverse events decreased with duration of treatment. The incidence of drug-related breast tenderness and breast enlargement remained constant over the treatment period. Ejaculate volume may be decreased in some patients with continued treatment. This decrease did not appear to interfere with normal sexual function.

Precautions

The precautions when using dutasteride for prostate enlargement are more significant than for finasteride and include:

  • Women who are pregnant or may become pregnant should not handle dutasteride because of possibility of absorption of dutasteride and subsequent potential risk to a male fetus.
  • Men treated with dutasteride should not donate blood until at least six months after their final dose to prevent giving dutasteride to a pregnant woman through a blood transfusion.
  • Men with an allergic reaction to dutasteride or its ingredients should not take it.
  • Men with liver disease should talk to their doctor before taking dutasteride.
  • Because of the potential for drug-drug interactions, care should be taken when administering dutasteride to patients taking potent, chronic CYP3A4 enzyme inhibitors
Some Additional Points to Consider Regarding Dutasteride
  • Unlike finasteride, were families that had a deficiency of the Type II 5-alpha reductase enzyme were followed for years without any adverse effects, there is no natural biologic model for dutasteride
  • The half life of dutasteride is 5 weeks compared to 6-8 hours for finasteride and serum concentrations of dutasteride are detectable up to 4-6 months after discontinuation of treatment.

Aldactone (Spironolactone)

 Aldactone (spironolactone 25mg, 50mg, 100mg) is a medication that is primarily used to treat high blood pressure (hypertension). Therapy is usually started at a dose of 25mg twice a day. It works as a diuretic causing increased amounts of sodium and water to be excreted from the body, while potassium is retained.

Because of its ability to retain potassium, the medication can elevate the blood levels of potassium to dangerous levels (hyperkalemia). It should, therefore, only be used under a doctor's supervision.

Spironolactone has anti-androgenic affects and has been used in the treatment of hair loss in women. It is a weak competitive inhibitor of the binding of androgens to their cellular receptors and decreases the synthesis of testosterone.

 Studies suggest that spironolactone requires at least 200mg/day for stopping loss and that it has little effect on regrowth of hair. Unfortunately, this dose is high enough to elevate potassium levels and place the patient at risk of hyperkalemia and other side effects, including cramps and diarrhea.

Since spironolactone is an anti-androgen (inhibits testosterone), it causes sexual dysfunction and breast enlargement in men. Because of these side effects, it is not used as a treatment for male pattern alopecia

 

 
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