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 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 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 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 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 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

  1. ARVs with no predicted effect: DOR, RPV, MVC, BIC, DTG, RAL, ABC, FTC, 3TC, TAF, TDF, ZDV
  2. ARVs predicted to inhibit estrogen metabolism: ATV alone, ATV/c, DRV/c, EVG/c
  3. ARVs predicted to induce estrogen metabolism: ATV/r, DRV/r, LPV/r, EFV, ETV, NVP
  4. ARVs predicted to inhibit androgen blocker and androgen metabolism: ATV alone, ATV/c, DRV/c, EVG/c, ATV/r, DRV/r, LPV/r
  5. ARVs predicted to induce androgen blocker and androgen metabolism: EFV, ETV, NVP 

* 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, 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 [13] [14] [15] [16]