Low Testosterone
Low Testosterone
TRT alternatives in low T hypogonadal men include oral, transdermal, intramuscular, buccal, and subcutaneous implants. TRT options are summarized in Table 4. The TRT goal is for serum testosterone levels to reach the eugonadal range. The Endocrine Society considers 280 to 300 ng/dL to be the normal lower limit range, whereas the AACE considers 280–800 ng/dL to be the normal range. It is recommended that testosterone levels reach mid-normal levels to avoid supraphysiological peaks.
Though easy to use, oral therapy is not natural, physiologic, or healthy. Oral testosterone dramatically increases testosterone levels initially, but the level tends to drop a few hours later. Oral testosterone may have limited bioavailability as a result of the enzymatic activity in the gastrointestinal system and liver that decreases effectiveness. The major concern with oral testosterone 17 alpha-alkylated derivatives such as methyltestosterone (MeT) is hepatotoxicity, and it is considered obsolete in the United States. Oral MeT raises LDL cholesterol and lowers HDL cholesterol.
Patches are the therapy of choice for older men because of convenience and reversible action. An evening application provides a good approximation of normal circadian plasma testosterone levels. Corticosteroid cream should be applied for skin irritation.
These gels are colorless hydroalcoholic gels of 1%, 1.62%, and 2% testosterone applied daily to the upper arms and shoulders or abdomen to achieve physiologic testosterone levels. Advantages are easy use, lower incidence of skin irritation, invisible application, and flexible dosing. The disadvantage is that it can be transferred from the patient to others via contact, which can be minimized by handwashing after applying the gel, covering the application area after the gel has dried, and washing the application site when skin-to-skin contact is expected.
Testosterone ester injections (testosterone enanthate and testosterone cypionate) may be administered at home. After testosterone ester injections, serum testosterone rises to supraphysiological levels within 72 hours, then gradually declines to the hypogonadal range over 1 to 2 weeks. It is not uncommon for patients to experience variations in breast tenderness, sexual activity, anger or depression, and general well-being as the testosterone levels change over time. Injections occur once every 2 weeks and may be increased to once weekly to decrease the frequency of oscillations in serum testosterone.
These tablets are applied to the gum just above the incisor teeth, bypassing the first pass effect. Testosterone is released slowly via this delivery system. These tablets are administered once every 12 hours and may cause gum and buccal irritation.
Subcutaneous pellets are used cautiously since their duration of action may last up to 6 months. Pellet administration is accomplished via a trochar and cannula as 6–10 pellets are implanted at 1 time into the gluteus muscle. Subcutaneous pellets are the only long-acting testosterone therapy approved in the United States and should be administered only to men in whom TRT tolerance has been established.
Testosterone Therapy
TRT alternatives in low T hypogonadal men include oral, transdermal, intramuscular, buccal, and subcutaneous implants. TRT options are summarized in Table 4. The TRT goal is for serum testosterone levels to reach the eugonadal range. The Endocrine Society considers 280 to 300 ng/dL to be the normal lower limit range, whereas the AACE considers 280–800 ng/dL to be the normal range. It is recommended that testosterone levels reach mid-normal levels to avoid supraphysiological peaks.
Oral Formulations
Though easy to use, oral therapy is not natural, physiologic, or healthy. Oral testosterone dramatically increases testosterone levels initially, but the level tends to drop a few hours later. Oral testosterone may have limited bioavailability as a result of the enzymatic activity in the gastrointestinal system and liver that decreases effectiveness. The major concern with oral testosterone 17 alpha-alkylated derivatives such as methyltestosterone (MeT) is hepatotoxicity, and it is considered obsolete in the United States. Oral MeT raises LDL cholesterol and lowers HDL cholesterol.
Transdermal Patches
Patches are the therapy of choice for older men because of convenience and reversible action. An evening application provides a good approximation of normal circadian plasma testosterone levels. Corticosteroid cream should be applied for skin irritation.
Transdermal Gels
These gels are colorless hydroalcoholic gels of 1%, 1.62%, and 2% testosterone applied daily to the upper arms and shoulders or abdomen to achieve physiologic testosterone levels. Advantages are easy use, lower incidence of skin irritation, invisible application, and flexible dosing. The disadvantage is that it can be transferred from the patient to others via contact, which can be minimized by handwashing after applying the gel, covering the application area after the gel has dried, and washing the application site when skin-to-skin contact is expected.
Intramuscular Injections
Testosterone ester injections (testosterone enanthate and testosterone cypionate) may be administered at home. After testosterone ester injections, serum testosterone rises to supraphysiological levels within 72 hours, then gradually declines to the hypogonadal range over 1 to 2 weeks. It is not uncommon for patients to experience variations in breast tenderness, sexual activity, anger or depression, and general well-being as the testosterone levels change over time. Injections occur once every 2 weeks and may be increased to once weekly to decrease the frequency of oscillations in serum testosterone.
Buccal Tablets
These tablets are applied to the gum just above the incisor teeth, bypassing the first pass effect. Testosterone is released slowly via this delivery system. These tablets are administered once every 12 hours and may cause gum and buccal irritation.
Subcutaneous Pellets
Subcutaneous pellets are used cautiously since their duration of action may last up to 6 months. Pellet administration is accomplished via a trochar and cannula as 6–10 pellets are implanted at 1 time into the gluteus muscle. Subcutaneous pellets are the only long-acting testosterone therapy approved in the United States and should be administered only to men in whom TRT tolerance has been established.
