| Formulation |
Regimen |
Pharmacokinetic profile |
DHT and E2 |
Advantages |
Disadvantages |
|
| T enanthate or cypionate |
100 mg/wk im or 200 mg every 2 wk im |
After a single im injection, serum T levels rise into the supraphysiological range, then decline gradually into the hypogonadal range by the end of the dosing interval. |
DHT and E2 levels rise in proportion to the increase in T levels. T:DHT and T:E2 ratios do not change. |
Corrects symptoms of androgen deficiency. Relatively inexpensive, if self-administered. Flexibility of dosing. |
Requires im injection. Peaks and valleys in serum T levels |
| Scrotal T patch1 |
One scrotal patch designed to nominally deliver 6 mg over 24 h applied daily |
Normalizes serum T levels in many but not all androgen-deficient men |
Serum E2 levels are in the physiological male range, but DHT levels rise into the supraphysiological range. T:DHT ratio is significantly lower than in healthy men. |
Corrects symptoms of androgen-deficiency |
To promote optimum adherence of the patch, scrotal skin needs to be shaved. High DHT levels |
| Nongenital transdermal system |
1 or 2 patches, designed to nominally deliver 5–10 mg T over 24 h applied daily on nonpressure areas |
Restores serum T, DHT, and E2 levels into the physiological male range |
T:DHT and T:E2 levels are in the physiological male range |
Ease of application, corrects symptoms of androgen deficiency and mimics the normal diurnal rhythm of T secretion. Lesser increase in hemoglobin than injectable esters |
Serum T levels in some androgen-deficient men may be in the low-normal range; these men may need application of 2 patches daily. Skin irritation at the application site may be a problem for some patients. |
| T gel |
5–10 g T gel containing 50–100 mg T should be applied daily. |
Restores serum T and E2 levels into the physiological male range |
Serum DHT levels are higher and T:DHT ratios are lower in hypogonadal men treated with the T gel than in healthy eugonadal men. |
Corrects symptoms of androgen deficiency, provides flexibility of dosing, ease of application, good skin tolerability |
Potential of transfer to a female partner or child by direct skin-to-skin contact; moderately high DHT levels |
17- -methyl T |
This 17--alkylated compound should not be used because of potential for liver toxicity |
Orally active |
|
|
Clinical responses are variable; potential for liver toxicity. Should not be used for treatment of androgen deficiency |
| Buccal, bioadhesive, T tablets |
30 mg controlled release, bioadhesive tablets used twice daily |
Absorbed from the buccal mucosa |
Normalizes serum T and DHT levels in hypogonadal men |
Corrects symptoms of androgen deficiency in healthy, hypogonadal men |
Gum-related adverse events in 16% of treated men |
| Oral T undecanoate2 |
40 to 80 mg orally 2 or 3 times daily with meals |
When administered in oleic acid, T undecanoate is absorbed through the lymphatics, bypassing the portal system. Considerable variability in the same individual on different days and among individuals |
High DHT to T ratio |
Convenience of oral administration |
Not approved in the United States. Variable clinical responses, variable serum T levels, high DHT:T ratio |
| Injectable long-acting T undecanoate in oil2 |
1000 mg injected im, followed by 1000 mg at 6 wk, and 1000 mg every 12 wk |
When administered at a dose of 1000 mg im, serum T levels are maintained in the normal range in a majority of treated men. |
DHT and E2 levels rise in proportion to the increase in T levels; T:DHT and T:E2 ratios do not change. |
Corrects symptoms of androgen deficiency. Requires infrequent administration |
Requires im injection of a large volume (4 ml) |
| T pellets |
Four to six 200-mg pellets implanted sc |
Serum T peaks at 1 month and then sustained in normal range for 4–6 months |
T:DHT and T:E2 ratios do not change |
Corrects symptoms of androgen deficiency |
Requires surgical incision for insertions; pellets may extrude spontaneously |
