Androgen Deficiency Syndromes

Table 6. Clinical pharmacology of some testosterone formulations Formulation† T gels and solution‡ Regimen Two formulations containing 1% testosterone gel, one formulation containing 2% testosterone gel, and one containing 2% axillary testosterone solution are available in the US. The dose and regimen vary with the formulation.‡ Buccal, bioadhesive, T tablets 30 mg controlled release, bioadhesive tablets used twice daily. T pellets 3–6, 75–200 mg pellets implanted SC (dose and regimen vary with formulation). 17a methyl T This 17a alkylated compound should not be used because of potential for liver toxicity. Pharmacokinetic Profile When applied in appropriate dose, these formulations can restore T levels into the physiological male range. DHT and E2 Advantages DHT levels are generally higher, and DHT to testosterone ratio is increased aſter transdermal gel applications. E2 levels and E2 to testosterone ratios remain within the physiological male range. Corrects symptoms of androgen deficiency; ease of application; good skin tolerability. Disadvantages Potential for transfer to female partner and child by direct skin-to- skin contact; moderately elevated DHT levels are of undetermined significance. The clinical experience with the 2% gel and the testosterone solution is limited. Absorbed from the buccal mucosa. Normal- izes serum T and DHT levels in hypogonadal men. Serum T peaks at 1 month and then sustained in normal range for 4–6 months. Orally active. T:DHT and T:E2 ratios do not change. Corrects symptoms of androgen deficiency in healthy, hypogonadal men. Corrects symptoms of androgen deficiency. Gum-related adverse events in 16% of treated men. Requires surgical incision for insertions; pellets may extrude spontaneously. Clinical responses are variable; potential for liver toxicity. Should not be used for treatment of androgen deficiency. T, Testosterone; DHT, dihydrotestosterone; E2, estradiol. † Brand names: enanthate (Delatestryl® 1%, Testim® (Axiron® ), subcutaneous pellets (Testopel® 1%, Fortesta™ ‡ 2%), tablets (Striant® ). ), transdermal systems (Testoderm® ), 17a methyl testosterone (capsules) (Testred® , Androderm® ), gel (AndroGel® ), solution 1% testosterone gels are typically applied at a dose of 5 to 10 g gel containing 50 to 100 mg of testosterone daily. Two formulations - one available in sachets or a metered-dose pump (4-8 compressions) and applied daily to shoulders/upper arms/abdomen, and another available in tubes (1-2) and applied daily to shoulders/upper arms, have been approved in the US. A 2% testosterone gel formulation is available in a metered-dose pump (4-7 compressions) and is applied daily to thighs. Clinical experience is limited at this time with this recently approved formulation. One formulation containing a 2% testosterone solution is applied to the axilla at a daily dose of 30-120 mg using an applicator. Deodorant or antiperspirant use is acceptable before testosterone application. Clinical experience is limited at this time with this recently approved formulation. 5 (continued)

• Cover
• Key Points
• Assessment and Diagnosis
• Selecting a Treatment Regimen
• Monitoring