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