Medical Solutions for the 21st Century . . .
Meeting Tomorrow's Challenges Today

[Back to Newsletter Page]
[Go to Main Page]


Androgen Therapy in Women

E-Newsletter No. 53

Considerations related to androgen therapy in women include preparations, risks, and monitoring. In terms of preparations, testosterone replacement therapy is available in oral, buccal, transdermal, and injectable forms. Methyltestosterone, the most commonly used oral preparation, is usually given combined with esterified estrogen. The product is FDA approved only for use in vasomotor symptoms associated with menopause, but it has been used offlabel to treat decreased libido in postmenopausal women.

Although the liver metabolizes a large amount of methyltestosterone, a much lower amount reaches the bloodstream. Testosterone undeconate, by contrast, is absorbed via the intestinal lymphatic system, bypassing the initial liver metabolism. This preparation is not available in the United States but has been tested elsewhere. Preliminary data on its use in women showed increased sexual desire and sexual activity. Another means of androgen treatment is through the use of oral dehydroepiandrosterone (DHEA) made by compounding pharmacies. Its use must be closely monitored as there is a variable increase in testosterone levels after ingestion of DHEA .

Buccal preparations of testosterone have been tested experimentally, but none are available from a pharmaceutical company. They are, however, prepared by compounding pharmacies. A key factor with this delivery system is that dosages and absorption vary.

Several transdermal preparations are undergoing trials. Compounding pharmacies also provide creams and gels, but as with the buccal preparations the levels of testosterone in the circulation may be very high or very low.

Injectable preparations include testosterone enanthate, testosterone cypionate, mixed testosterone esters, and nandrolone decanoate. Given intramuscularly, testosterone enanthate and cypionate last from one to three weeks. Considerable fluctuation in testosterone concentration is possible, causing some patients to experience emotional lability. Mixed testosterone esters act similarly. There are no data on use of nandrolone decanoate to treat interest/ sexual desire disorder.

Adverse Effects
Adverse effects in women occur mainly among those abusing androgens for bodybuilding or weightlifting purposes. Acne and hirsutism are the primary androgenic side effects. Acne is seen more often with high-dose methyltestosterone than other preparations. Virilization is rarely seen with physiologic doses.

Other possible side effects:
  • Fluid retention – can be caused by large doses;
  • Polycythemia – seen in men given pharmacologic doses but not in women given physiologic or slightly superphysiologic doses; hemoglobin and hematocrit may increase slightly;
  • Hepatic injury – described for the oral androgen preparations; unlikely with the replacement dosages used in women;
  • Sleep apnea – possible with overweight individuals;
  • Lipid abnormalities – more commonly seen with oral preparations; rarely seen with intramuscular or subcutaneous preparations; not seen with transdermal delivery systems;
  • Breast hyperplasia/neoplasia – testosterone may be aromatized to estrogen in various tissues, but no evidence shows that androgens increase the risk of breast cancer -some studies suggest decreased risk;
  • Endometrial hyperplasia/neoplasia – potential of aromatization of testosterone to estradiol in the uterus, no data demonstrating this occurrence; and
  • Emotional lability – possible, especially with injectable preparations.

Monitoring Therapy
Management of female patients receiving androgen therapy should include clinical monitoring, biochemical evaluation, radiographic determinations, and possibly testosterone measurements. As part of clinical monitoring, skin and hair should be checked for acne and hirsutism. Virilization, though rare, should be watched for. A breast examination before a woman starts therapy and twice a year thereafter is recommended. Hematocrit or hemoglobin determinations are reasonable, especially in patients receiving oral preparations. Lipids are important to examine, especially with oral preparations, because of possibly decreased high-density lipoprotein. Yearly mammography and, for women with an intact uterus, endometrial ultrasound are recommended. Serum free testosterone correlates best with androgen efficacy and safety profiles. Some experts suggest serum free testosterone should be measured before starting treatment. An accurate measurement of free testosterone, however, cannot be obtained without an accurate assay for total testosterone. Although the ideal method of measuring free testosterone is controversial, equilibrium dialysis is generally preferred.1 Among women with sexual interest/desire disorder, androgen therapy has been suggested for those whose free testosterone level falls within the lower quartile of the reference range.2

1. Miller et al. J Clin Endocrinol Metab. 2004;89;525-33.
2. Bachmann et al. Fertil Steril. 2002;77:660-5..

Click here to go to the Sexual Enhancement web page

Also see:
FDA Acts on Fraudulent Claims of Bioidentical Hormone Benefits

Go to Top

[Back to Newsletter Page]    
[Go to Main Page]