Hormone Therapy: Gender Transitioning
Dosage Recommendations for Hormone Therapy when Used at High Doses for Gender Transitioning
| HIV Drugs | Starting Dose | Average Dose | Maximum Dose | ||
|---|---|---|---|---|---|
| Estrogens | Estradiol oral | No predicted effect a | 2 mg/day | 4 mg/day | 8 mg/day |
| Inhibits metabolism b,f | 1 mg/day | 2 mg/day | 4 mg/day | ||
| Induces metabolism c | Increase estradiol dosage as needed based on clinical effects and monitored hormone levels. | ||||
| Estradiol gel (preferred for >40 y and/or smokers) |
No predicted effect a | 0.75 mg bid | 0.75 mg tid | 1.5 mg tid | |
| Inhibits metabolism b,f | 0.5 mg bid | 0.5 mg tid | 1 mg tid | ||
| Induces metabolism c | Increase estradiol dosage as needed based on clinical effects and monitored hormone levels. | ||||
| Estradiol patch (preferred for >40 y and/or smokers) |
No predicted effect a | 25 μg/day | 50-100 μg/day | 150 μg/day | |
| Inhibits metabolism b,f | 25 μg/day* | 27.5-75 μg/day | 100 μg/day | ||
| Induces metabolism c | Increase estradiol dosage as needed based on clinical effects and monitored hormone levels. | ||||
| Conjugated estrogen † | No predicted effect a | 1.25-2.5 mg/day | 5 mg/day | 10 mg/day | |
| Inhibits metabolism b,f | 0.625-1.25 mg/day | 2.5 mg/day | 5 mg/day | ||
| Induces metabolism c | Increase estradiol dosage as needed based on clinical effects and monitored hormone levels. | ||||
| Ethinylestradiol | No predicted effect a | No interaction expected, but not recommended due to thrombotic risks | |||
| Inhibits metabolism b,f | Not recommended | ||||
| Induces metabolism c | Not recommended | ||||
| Androgen Blockers ‡ | Spironolactone | No predicted effect a | 50 mg/day | 150 mg/day | 400 mg/day |
| Inhibits metabolism d | No interaction expected. No dose adjustment required. | ||||
| Induces metabolism e | No interaction expected. No dose adjustment required. | ||||
| Finasteride | No predicted effect a | 2.5 mg/day | 2.5 mg/day | 5 mg/day | |
| Inhibits metabolism d | Finasteride has a large safety margin. No dose adjustment required. | ||||
| Induces metabolism e | Increase finasteride dosage as needed based on clinical effects and monitored hormone levels. | ||||
| Cyproterone acetate | No predicted effect a | 50 mg/day | 150 mg/day | 150 mg/day | |
| No predicted effect a | 25 mg/day | 75 mg/day | 75 mg/day | ||
| Induces metabolism c | Increase cyproterone dosage as needed based on clinical effects and monitored hormone levels. | ||||
| Goserelin | No predicted effect a | 3.6 mg/month | 3.6 mg/month | 3.6 mg/month | |
| Inhibits metabolism d | No interaction expected. No dose adjustment required. | ||||
| Induces metabolism e | No interaction expected. No dose adjustment required. | ||||
| Leuprorelin acetate | No predicted effect a | 3.75 mg/month | 3.75 mg/month | 3.75 mg/month | |
| Inhibits metabolism d | No interaction expected. No dose adjustment required. | ||||
| Induces metabolism e | No interaction expected. No dose adjustment required. | ||||
| Triptorelin | No predicted effect a | 3.75 mg/month | 3.75 mg/month | 3.75 mg/month | |
| Inhibits metabolism d | No interaction expected. No dose adjustment required. | ||||
| Induces metabolism e | No interaction expected. No dose adjustment required. | ||||
| Androgens | Testosterone topical gel 1% | No predicted effect a | 12.5-25 mg in the morning | 50 mg in the morning | 100 mg in the morning |
| Inhibits metabolism d | 12.5-25 mg in the morning | 25-50 mg in the morning | 50-100 mg in the morning | ||
| Induces metabolism e | Increase testosterone dosage as needed based on clinical effects and monitored hormone levels. | ||||
| Testosterone enanthate or cypionate | No predicted effect a | Not applicable | 50-100 mg in the morning | Not applicable | |
| Inhibits metabolism d | Not applicable | 25-50 mg in the morning | Not applicable | ||
| Induces metabolism e | Increase testosterone dosage as needed based on clinical effects and monitored hormone levels. | ||||
| Testosterone undecanoate | No predicted effect a | Not applicable | 750 mg IM, repeat after 4 weeks and then every 10 weeks | Not applicable | |
| No predicted effect a | Not applicable | 375-500 mg IM, repeat after 4 weeks and then every 10 weeks | Not applicable | ||
| Induces metabolism c | Increase testosterone dosage as needed based on clinical effects and monitored hormone levels. | ||||
| Testosterone mixed esters | No predicted effect a | Not applicable | 250 mg/2-3 weeks | Not applicable | |
| Inhibits metabolism d | Not applicable | 125 mg/2-3 weeks | Not applicable | ||
| Induces metabolism e | Increase testosterone dosage as needed based on clinical effects and monitored hormone levels. | ||||
Comments
- ARVs with no predicted effect: CAB, DOR, RPV, MVC, BIC, DTG, RAL, ABC, FTC, 3TC, TAF, TDF, ZDV
- ARVs predicted to inhibit estrogen metabolism: ATV alone, ATV/c, DRV/c, EVG/c
- ARVs predicted to induce estrogen metabolism: ATV/r, DRV/r, LPV/r, EFV, ETV, NVP
- ARVs predicted to inhibit androgen blocker and androgen metabolism: ATV alone, ATV/c, DRV/c, EVG/c, ATV/r, DRV/r, LPV/r
- ARVs predicted to induce androgen blocker and androgen metabolism: EFV, ETV, NVP
- FTR inhibits only estrogens
* Matrix type transdermal patch can be cut in order to reduce the amount of hormone delivered/day
† Conjugated estrogen is associated with high thromboembolic risk and therefore should be avoided
‡ Androgen deprivation treatment may prolong the QT interval.
Caution should be taken when using with ARVs that can potentially prolong the QT interval (i.e., ATV alone, ATV/r, ATV/c, FTR, LPV/r, RPV)
Recommendations for dose changes
- Dose changes in presence of inhibitors of estrogen metabolism are based on the assumption that the magnitude of the DDI is expected to be less pronounced for transdermal or topical applications than for oral drug administration as the first-pass metabolism is avoided
- Dose changes in presence of inhibitors of testosterone metabolism are based on the assumption that the magnitude of the DDI is expected to be less pronounced for topical and intramuscular applications than for oral drug administration as the first-pass metabolism is avoided
- Note: hormone therapy doses in the table are indicative, dose titration upwards may occur in practice based on single individual goals, clinical response and hormone levels.