What is the Optimal Form of Testosterone for Replacement Therapy?

Testosterone USP is natural testosterone that has a monograph in the United States Pharmacopoeia (USP). Upon a prescription order, compounding pharmacists can use pure Testosterone USP to compound numerous dosage forms. The information that follows should be considered as doctor or health care practitioner, patient, and pharmacist work together to meet each patient’s specific needs. Compounded preparations can have many advantages. For example, there is no need to shave the area to apply transdermal testosterone preparations. The medication can be administered as a single dose (rather than multiple patches), and there is no skin irritation from patch adhesive. The cream or gel can be applied two or three times daily to simulate the normal circadian rhythm.

A healthy adult male secretes 8-15mg/day of testosterone. This “physiologic dose” should be considered when prescribing replacement therapy. Excessive doses leading to high serum levels of testosterone can result in a greater conversion to estradiol (and side-effects resulting from abnormally high estradiol levels), because the body cannot effectively store excess testosterone. This may be a reason to administer testosterone on a daily basis, rather than using long-lasting injections.

Transdermal drug administration allows application of a specific dose of a hormone to be applied to the skin and then be absorbed into the systemic circulation. Transdermal medications have the advantage of high bioavailability, absence of hepatic first pass metabolism, increased therapeutic efficacy, and steadiness of plasma concentrations of the drug. Testosterone is well-absorbed from transdermal creams/gels. Dosage forms also include sublingual drops or troches.
Natural testosterone must not be confused with synthetic derivatives or “anabolic steroids,” which when used by athletes and body builders have caused disastrous effects, such as heart problems and cancer. Use of synthetic androgens, like stanozolol or methyltestosterone, causes profound decreases in HDL-C and significant increases in LDL-C, and has been associated with serious heart disease. However, natural testosterone lowers total cholesterol and LDL cholesterol levels while having little to no impact on serum HDL cholesterol levels.

Screening for potential risks of androgen therapy should be performed prior to the initiation of treatment. Contraindications to testosterone replacement therapy include an elevated level of Prostate-Specific Antigen (PSA), or history or presence of prostate or breast cancer. There is a risk of worsening symptoms of benign prostatic hypertrophy (enlarged prostate), sleep apnea, congestive heart failure, gynecomastia (breast enlargement), infertility and skin diseases.