The Avacor Hair Regrowth Blog
3Aug/111

Minoxidil Mini-Series: Part 5 – Benefits, Limitations, and Side Effects

This post will conclude the Avacor® Hair Regrowth Blog's five part “mini-series” on minoxidil, the first FDA-approved treatment for hair loss. Earlier episodes of the mini-series covered the early history of minoxidil, clinical trials showing its efficacy in treating androgenetic alopecia, and its approval by the FDA as a hair regrowth treatment. In this final segment we will highlight the benefits, limitations, and side effects associated with minoxidil.

Benefits of Minoxidil Treatment

Minoxidil products, such as Avacor Physicians Formulation® and Rogaine®, have helped thousands of men and women stop their hair loss and begin regrowing hair.

Several clinical trials have proven that minoxidil is able to prevent hair loss and regrow hair, with investigators observing hair growth in anywhere from 30-60% of patients (for details see our previous post on clinical trials). These studies also suggest that even if patients do not achieve noticeable hair regrowth with minoxidil treatment, they can at least stop losing hair and maintain their baseline hair count.

Minoxidil is the only hair regrowth medication that has been approved by the FDA for both men and women, unlike finasteride (Propecia®) which is only approved for use by men.

One of the other benefits of minoxidil is that it has not been associated with the sexual side effects experienced by some patients taking finasteride (Propecia®), such as decreased arousal and erectile dysfunction.1 For a description of the side effects that have been associated with minoxidil, keep reading for the section below on “Reported Side Effects of Minoxidil.”

Minoxidil’s Limitations

There is no magic cure for hair loss, so it is important to begin any hair regrowth regimen with accurate information and reasonable expectations. Minoxidil will not work for everyone; its effectiveness is limited to certain types of hair loss and the degree of hair regrowth experienced by each person will differ. In addition, minoxidil requires a consistent, diligent program of use to achieve maximum results.

Only Works for Certain Types of Hair Loss

The only types of hair loss for which minoxidil has been approved by the FDA are male and female androgenetic alopecia. Some studies have reported positive results for a small number of patients with alopecia areata, but the benefits have not been consistent enough to recommend widespread use of minoxidil for this condition.

Men: Minoxidil 5% topical solution, (such as Avacor Physicians Formulation® for Men) is only recommended for men with male pattern hair loss, and is not intended for treating frontal baldness or a receding hairline. Despite a conference presentation by the lead investigator of several early minoxidil trials suggesting that it is also effective in the frontal hairline area,2 the supporting data do not appear to have been published in any peer-reviewed journals or evaluated by the FDA. Patients using minoxidil should not expect to regrow hair in any areas other than the top of the scalp.

Women: Minoxidil 2% topical solution, (such as Avacor Physicians Formulation® for Women) is only recommended for women with female pattern hair loss (general thinning of hair on the top of the scalp). Minoxidil products are not indicated for hair loss that is sudden, patchy, or associated with stress or childbirth.

Minoxidil may not work for patients whose hair loss is too advanced. A general visual guide that shows the degrees of thinning hair for which minoxidil is most effective can be found on Avacor's product packaging.

Needs to be Used Consistently

In order to achieve the best possible results with minoxidil, it is essential to apply the topical solution regularly and consistently. The best way to do this is to commit to making it part of your daily routine, even if it's not your favorite part of the day. An analogy for this would be brushing your teeth: while no one particularly enjoys the act of brushing their teeth (at least that we are aware of), most people find the benefits are worth the little bit of time each day.

Like all good things, regrowing hair takes time. You may need to use minoxidil for at least 4 months before you see results, although you may begin to notice the effects as early as 2 months.

Continued use is necessary to prevent hair loss from progressing. One of the longest studies of minoxidil for male pattern hair loss (5 years) found that patients who continued to apply minoxidil twice per day were able to maintain nonvellus hair regrowth well beyond their baseline hair counts.3 Patients who stop using minoxidil will likely not maintain hair that has regrown during the course of treatment and will begin losing hair again.

Reported Side Effects of Minoxidil

More than 20 years after minoxidil was first approved for treating hair loss, the list of commonly reported side effects remains fairly limited. However, there are some rare side effects that should be watched for and taken very seriously.

Some of the most common side effects are:
• Localized scalp reactions or skin irritation (i.e., dryness, itching, redness and mild burning)
• GI discomforts (e.g., mild heartburn, nausea, constipation and diarrhea)
• Hair growth in other body areas (i.e., face, arms, back)

If you experience any of the following rare side effects, you should discontinue use immediately and consult your physician:
• Dizziness, light headedness, faintness, headaches
• Sudden unexplained weight gain, water retention
• Rapid heart beat or chest tightness/discomfort
• Swelling of the mouth, face, lips, or tongue

In addition to these side effects, some people have experienced changes in hair color and/or texture.

If you have heart disease you should talk to your doctor before using minoxidil. Minoxidil may be harmful if used when pregnant or breast-feeding, should not be used by children under the age of 18, and should be kept out of reach of children at all times.

Conclusion

Thanks again for checking out the “Minoxidil Mini-Series” here on the Avacor Hair Regrowth Blog. We hope the information we have collected here has given you a better understanding of the history, benefits, and limitations of minoxidil and that it will help you choose the best course of action for regrowing your hair.

If you have any questions or would like to see more information on a particular topic, please leave a comment below. We'd love to hear from you!

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1. Irwig MS, Kolukula S. Persistent sexual side effects of finasteride for male pattern hair loss. J Sex Med. 2011 Jun;8(6):1747-53. Link to Pubmed

2. Olsen EA, Whiting DA, Miller JJ. Increased Frontal Scalp Coverage and Frontal Hair Regrowth with 5% and 2% Minoxidil Solution. Presented at the American Academy of Dermatology 61st Annual Meeting, March 2003.

3. Olsen EA, Weiner MS, Amara IA, DeLong ER. Five-year follow-up of men with androgenetic alopecia treated with topical minoxidil. J Am Acad Dermatol. 1990 Apr;22(4):643-6. Link to Pubmed

23Jun/111

The Science Behind “Anti-Androgens”

Dihydrotestosterone (DHT), a hormone produced naturally in the body, has been linked to both prostate cancer growth and androgenetic alopecia (AGA; male pattern hair loss).

Those of you who visit hair loss forums or websites promoting hair restoration treatments have most likely seen some of the following terms:
• “Anti-androgens”
• “DHT blockers”
• “DHT inhibitors”
• “Androgen blockers”
• “AR blockers”

These terms are frequently used interchangeably and/or incorrectly. In this Avacor® Hair Regrowth Blog post we will explain the difference, at the molecular and biochemical level, between an androgen receptor antagonist and an inhibitor of DHT synthesis.

DHT, 5-Alpha Reductase and the Androgen Receptor

The androgen receptor (AR) is a protein found in many tissues in both men and women, including the prostate (men), bone marrow, muscle, brain, and hair follicles. When DHT binds to AR it “activates” the receptor, leading to changes in gene expression and cellular behavior. In the scalp, these changes can include miniaturization (shrinking) of hair follicles and eventually male pattern hair loss.1

Testosterone is converted to DHT in the body by enzymes called steroid 5-alpha reductases (5-ARs). Humans possess two types of 5-alpha reductase enzymes: Type 1 (expressed in the skin/scalp and liver) and Type 2 (skin/scalp, prostate, and liver).2, 3

There are two main classes of molecules that prevent the action of DHT in the body:

5-alpha reductase inhibitors reduce the amount of DHT produced in the body

Avacor Blog - Mechanism of Action of 5-Alpha Reductase Inhibitors (5-ARIs)FDA-approved 5-ARIs:
Finasteride (Propecia®, Proscar®)
Dutasteride (Avodart®)

Natural/botanical sources reported to inhibit 5-alpha reductases:
Saw Palmetto (Serenoa Repens)4
African Pygeum (Pygeum Africanum)5
Stinging Nettle Root (Urtica Dioica)5

Finasteride (Propecia®) inhibits only Type 2 5-alpha reductase. Dutasteride (Avodart®) inhibits both Types 1 and 2.

AR antagonists bind to AR and prevent its ability to respond to DHT

Avacor Blog - Mechanism of Action of Androgen Receptor (AR) AntagonistsAndrogen receptor “antagonists”:
Flutamide (Eulexin®)
Bicalutamide (Casodex®)
Cyproterone acetate (Androcur®)
MDV3100 (in Phase III trials)
Spironolactone* (Aldactone®)

*Note – Although some websites6, 7 mention Spironolactone in conjunction with the word “natural,” it is in fact a synthetic drug. The NIH's MedlinePlus website8 states: “Important Warning: Spironolactone has caused tumors in laboratory animals. Talk to your doctor about the risks and benefits of using this medication for your condition.”

If you have questions about the science surrounding AR antagonists, 5-alpha reductase inhibitors, or any of the substances mentioned in this post, please leave a comment here on the Avacor Hair Regrowth Blog so everyone can benefit from the discussion!

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1. Zouboulis CC, Degitz K. Androgen action on human skin -- from basic research to clinical significance. Exp Dermatol. 2004;13 Suppl 4:5-10. Link to Pubmed

2. Thigpen AE, Silver RI, Guileyardo JM, Casey ML, McConnell JD, Russell DW. Tissue distribution and ontogeny of steroid 5 alpha-reductase isozyme expression. J Clin Invest. 1993 Aug;92(2):903-10. Link to Pubmed

3. Asada Y, Sonoda T, Ojiro M, Kurata S, Sato T, Ezaki T, Takayasu S. 5 alpha-reductase type 2 is constitutively expressed in the dermal papilla and connective tissue sheath of the hair follicle in vivo but not during culture in vitro. J Clin Endocrinol Metab. 2001 Jun;86(6):2875-80. Link to Pubmed

4. Bayne CW, Donnelly F, Ross M, Habib FK. Serenoa repens (Permixon): a 5alpha-reductase types I and II inhibitor-new evidence in a coculture model of BPH. Prostate. 1999 Sep 1;40(4):232-41. Link to Pubmed

5. Hartman RW, Mark M, Soldati F. Inhibition of 5a-reductase and aromatase by PHL-00801 (Prostatonin), a combination of PY 102 (Pygeum africanum) and UR 102 (Urtica dioica) extracts. Phytomedicine. 1996 3:121–128.

6. “Revivogen & Topical Spironolactone: Natural Alternative to Propecia?” HairLossTalk.com. (Accessed June 22, 2011)
http://www.hairlosstalk.com/hair-loss-treatments/revivogen/revivogen-spironolactone.php

7. “natural dht inhibitors?” HairLossHelp.com Forums. (Accessed June 22, 2011)
http://www.hairlosshelp.com/FORUMS/messageview.cfm?catid=10&threadid=34449

8. “Spironolactone.” MedlinePlus, U.S. National Library of Medicine, National Institutes of Health. (Accessed June 22, 2011)
http://www.nlm.nih.gov/medlineplus/druginfo/meds/a682627.html

20Jun/111

FDA: “Label Change – Increased Risk of Prostate Cancer” for the hair loss drug Propecia®

On June 9, 2011, the FDA issued a Drug Safety Communication1 about a class of drugs called 5-alpha reductase inhibitors, which includes the hair loss drug Propecia® (finasteride).

FDA Drug Safety Communication: 5-alpha reductase inhibitors (5-ARIs) may increase the risk of a more serious form of prostate cancer

[6-9-2011] The U.S. Food and Drug Administration (FDA) is informing healthcare professionals that the Warnings and Precautions section of the labels for the 5-alpha reductase inhibitor (5-ARI) class of drugs has been revised to include new safety information about the increased risk of being diagnosed with a more serious form of prostate cancer (high-grade prostate cancer). This risk appears to be low, but healthcare professionals should be aware of this safety information, and weigh the known benefits against the potential risks when deciding to start or continue treatment with 5-ARIs in men.

Two large clinical trials, known as PCPT and REDUCE, were conducted to assess the use of 5-ARIs for preventing prostate cancer. The PCPT trial raised concern at the FDA because patients being treated with finasteride had a slightly higher risk of developing high-grade prostate cancer than patients receiving placebo (1.8% versus 1.1%, respectively). It should be noted that although the title of the FDA's Safety Alert2 reads "Increased Risk of Prostate Cancer," the data on increased risk appear to relate only to the incidence of high-grade prostate cancer (Gleason Score 8-10).

While the “risk appears to be low,” the labels for drugs including Propecia®, Proscar® (finasteride) and Avodart® (dutasteride) are all being modified to warn patients of this potential risk. Propecia® is also associated with sexual side effects3 in some men, including less desire for sex and difficulty in achieving an erection.

The FDA has provided a page of Questions and Answers on the change in label information for 5-ARIs. Below are a few Q/A’s pertaining to the use of Propecia® for male pattern hair loss.

Q6. Does FDA believe the benefits of 5-alpha reductase inhibitors (5-ARIs) still outweigh their risks for the approved indications?

A. Yes. FDA believes that 5-ARIs remain safe and effective for their approved indications. Proscar and Avodart have been effective in controlling symptoms of benign prostatic hyperplasia (BPH), as well as in reducing the risks of acute urinary retention and the need for surgical intervention related to BPH. Healthcare professionals and patients are still encouraged to discuss the risks and benefits of 5-ARIs when deciding the best treatment for their disease.

FDA will continue its risk/benefit assessment of using 5-ARIs for the treatment for male pattern hair loss and will update the public when additional information is available.

Q9. Are there other medications to treat benign prostatic hyperplasia (BPH) or male pattern baldness?

A. Yes. Another class of medications called alpha-blockers is approved to treat the symptoms of BPH. Medications in the alpha-blocker class include tamsulosin (Flomax), doxazosin (Cardura), terazosin (Hytrin), alfuzosin (Uroxatral), and silodosin (Rapaflo). However, 5-ARIs are the only medications that have been shown to reduce the risk of urinary retention or surgery related to an enlarged prostate.

Minoxidil is a topical product that is available over the counter in various formulations to treat male pattern hair loss.

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1. FDA Drug Safety Communication: 5-alpha reductase inhibitors (5-ARIs) may increase the risk of a more serious form of prostate cancer. June 9, 2011.
http://www.fda.gov/Drugs/DrugSafety/ucm258314.htm

2. 5-alpha reductase inhibitors (5-ARIs): Label Change - Increased Risk of Prostate Cancer. June 9, 2011.
http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm258529.htm

3. PROPECIA® labeling information, FDA website.
http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/020788s018lbl.pdf

17Jun/112

Carpe Diem: Delaying Treatment Affects Results?

A recent case report1 on androgenetic alopecia from the UK highlights the importance of not delaying treatment for hair loss.

The authors report a case of identical twins who sought medical treatment for progressive male-pattern hair loss when they were 26 years old. One of them chose to pursue a minoxidil-containing treatment regimen immediately (topical minoxidil and antiandrogens plus oral finasteride), while the other delayed treatment for one year. A photograph taken just twelve months later (Figure 1 in the article) shows an obvious difference in hair coverage. At this point the second twin chose to begin therapy.

After three years of continuous therapy, the patient who started treatment earlier achieved significantly better results than his brother who delayed treatment - 14.2% higher total hair density and over 25% higher “useful hair density” (as measured by unit area trichogram).

The authors conclude “the amount of hair that can be regrown might be affected by delaying treatment.

While this is only a case report and not a larger study, if the experience of these twins is an indicator of a general trend, anyone experiencing male-pattern hair loss should consider beginning treatment as soon as possible.

Avacor Physicians Formulation®, approved by the FDA to regrow hair, is used topically on the scalp to retard further hair loss and to start re-growing hair. Containing the proven hair growth medication minoxidil, the Avacor Physicians Formulation® results in new hair growth in as little as 2 months, although most will experience growth after several months.

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1. Rushton DH, Gilkes JJ. Delaying treatment in male-pattern hair loss affects the therapeutic response. Clin Exp Dermatol. 2011 Mar;36(2):204-5. Link to Pubmed