Table 1:
Pharmacokinetics, Efficacy, and Potential Risks of Short-acting and Long-Acing Testosterone Therapy
| Testosterone Therapy | Pharmacokinetics | Efficacy | Potential Risks |
|---|---|---|---|
| Short-acting Testosterone Therapy | |||
| Intranasal Gel 24–26 | • Reaches maximum concentrations in around 40 minutes • Serum half-life: 10–100 minutes |
• 90-day open trial reported 69 (90%) of 73 men had an average testosterone concentration within the specified normal range (300–1,050 ng/dL) after using 2 actuations (11 mg) three times daily | • Not recommended for patients with a history of nasal disorders • Nasopharyngitis • Rhinorrhea • Epistaxis • Headache • Sinusitis • Upper Respiratory Tract Infections • Bronchitis |
| Transdermal Testosterone Gels 27–31 | • Variable pharmacokinetic profiles and solubilities • Varied absorption profiles may make dose adjustments necessary |
• 74–87% of men achieve testosterone levels in the normal range | • Application site reactions (erythema) • Transference risk • Irritation to the axillae • Headache • Increased hematocrit • Nasopharyngitis • Diarrhea • Vomiting • Increase in hematocrit by 3 % |
| Transdermal Testosterone Patches 32–33 | • Dependent on dosing, location, and scheduling of administration • Topical patches: levels achieved directly relate to the amount of surface area exposed to drug. |
• Achieve testosterone levels within normal physiologic ranges (2 patches every 24–48 hours) in 77–100% of individuals with >85% achieving values >300 ng/dL. | • Application site reactions (reported in up to 60% of patients) • Pruritus • Application site vesicles • Back pain • Increase in hematocrit by 1.4% |
| Oral Testosterone Pills 34–35 | • Oral mucosa absorption avoids liver deactivation | • Serum testosterone levels rise rapidly after absorption • Peak levels reached by the second 12-hour daily dose. • Restores circulating testosterone level to physiological range |
• Gum/mouth irritation • gum tenderness • gum pain • gum edema • elevated hematocrit |
| Long-acting Testosterone Therapy | |||
| Testosterone Cypionate (TC) & Testosterone Enanthate (TE) 42,53–54 | • IM T achieves higher peak T, faster time-to-peak levels, and a shorter half-life (i.e., 173 hours) | • IM TE achieved trough levels of 239 ng/dL | • Injection site wounds • Hematomas • Return of symptoms of testosterone deficiency (subtherapeutic testosterone and hypertension) • TE – increased BP and discomfort |
| Testosterone Undecanoate 55–56 | • Peak concentrations achieved at a mean 7 days after injection (range 4–42 days). | • 94 % of men in study maintained normal testosterone levels after administration at weeks 0,4, and every 10 weeks after | • Injection site pain • Acne • Fatigue • Coughing secondary to pulmonary microemboli • Patients should be monitored 30 minutes after administration |
| Testosterone Pellets 57–61 | • Dissolves slow in SQ spaces | • Mean peak testosterone levels is dose-dependent • Therapeutic levels in 100% of men at 4 weeks and maintained levels >300 ng/dL at 4 months. |
• polycythemia • ecchymosis • tenderness • pain • swelling • risk of under-dosing due to dose-dependency by BMI • pellet extrusion • fibrosis around implantation sites |
Data Source: AUA Guidelines Appendix B (Therapeutic Agents for Treatment of Testosterone Deficiency)7 and sources cited within the short-acting and long-acting sections