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Estradiol Valerate (Injection)

HRTprescriptionim · inferred

Injectable estradiol ester for IM administration. Duration of elevated estradiol ~7-8 days per injection. Used in menopause HRT and gender-affirming feminizing therapy. Typical dosing: 10-40 mg IM every 1-2 weeks.

Projected serum levels — 10 mg, weekly

Estradiol Valerate (Injection) (precursor)
Estradiol Valerate (Injection) modeled serum levels, 10 mg weekly over 35 days Population-based pharmacokinetic estimate. Steady state reached after approximately 14 days. 0 0.25 0.50 0.75 1 Day 0 Day 9 Day 18 Day 26 Day 35 Time on a regular schedule ≈ steady state · day 14
Estradiol Valerate (Injection) modeled serum levels with a loading dose of 14.1 mg, then 10 mg weekly The first dose is larger so levels approach steady state faster. 0 0.25 0.50 0.75 1 Day 0 Day 9 Day 18 Day 26 Day 35 Time on a regular schedule

Maintenance schedule: 10 mg weekly (im).

Loading schedule: 14.1 mg on day 1, then 10 mg weekly — reaching therapeutic levels sooner.

Modeled steady state after ~14 days: peak ≈ 0.10 mg, trough ≈ 0.030 mg body load. Population-based estimate over 35 days for a 10 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.

Key facts

Category
HRT
Route modeled
IM
Model confidence
inferred
Half-life
4 days
Common dose
10 mg
Suggested maximum
40 mg/day
Reference dose range
1–40 mg (single dose)
Suggested cadence
weekly
Validated against
5 mg im — Cmax 0.001 mg/L at 48 h

Documented interactions

  • danger
    Carbamazepine (Tegretol) + Estradiol Valerate (Injection) CYP induction

    Carbamazepine (Tegretol) inducer of CYP3A4 predicted to change Estradiol Valerate (Injection) AUC by ~0.49x

  • danger
    Efavirenz (Sustiva) + Estradiol Valerate (Injection) CYP induction

    Efavirenz (Sustiva) inducer of CYP3A4 predicted to change Estradiol Valerate (Injection) AUC by ~0.35x

  • danger
    Levothyroxine (Synthroid) + Estradiol Valerate (Injection) Protein binding

    Estradiol Valerate (Injection) may displace Levothyroxine (Synthroid) from plasma protein binding sites, transiently raising free drug concentration. This drug has a narrow therapeutic index; free…

  • danger
    Rifampin + Estradiol Valerate (Injection) CYP induction

    Rifampin inducer of CYP3A4 predicted to change Estradiol Valerate (Injection) AUC by ~0.35x

  • danger
    Tacrolimus (Prograf) + Estradiol Valerate (Injection) Protein binding

    Estradiol Valerate (Injection) may displace Tacrolimus (Prograf) from plasma protein binding sites, transiently raising free drug concentration. This drug has a narrow therapeutic index; free…

  • danger
    Warfarin (Coumadin) + Estradiol Valerate (Injection) Protein binding

    Estradiol Valerate (Injection) may displace Warfarin (Coumadin) from plasma protein binding sites, transiently raising free drug concentration. This drug has a narrow therapeutic index; free…

Serum checks 231 modeled interaction pairings for estradiol valerate (injection) across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.

Research behind this entry

  1. A Comparison of the Pharmacokinetic Properties of Three Estradiol Esters Oriowo MA et al. · Journal of Steroid Biochemistry, 1980 DOI

    Compared benzoate, valerate, and cypionate esters showing valerate maintains elevated estradiol for 7-8 days with peak at day 2 after IM injection.

  2. Pharmacokinetics and Biotransformation of Estradiol Valerate in Ovariectomized Women Dusterberg B, Nishino Y · Hormone Research, 1982 DOI

    Characterized IV and IM estradiol valerate metabolism showing rapid ester hydrolysis to estradiol followed by conversion to estrone and conjugates.

  3. Injectable Estradiol Valerate for Gender-Affirming Hormone Therapy Tangpricha V, den Heijer M · Endocrine Reviews, 2017 DOI

    Endocrine Society review of injectable estradiol pharmacology in transgender women, including dosing, monitoring, and target estradiol levels.

3 published studies referenced in the app, each with a plain-language summary.