Meta Information
ID:17-alpha-estradiol
Name:
Schema Version:AIM-2.0
Interactions
Target id:
/class/cyp3a4-strong-inhibitors
Target name:
Strong CYP3A4 Inhibitors
Severity:
major
Interaction type:
adverse
Nature:
absolute
Temporal spacing:
null
Description:
Strong CYP3A4 inhibitors (e.g., ketoconazole, ritonavir) significantly block the primary metabolic pathway for steroid hormones, which can lead to dangerously high and unpredictable levels of this experimental compound.
Actionable advice:
Avoid using strong CYP3A4 inhibitor medications while taking 17-alpha-estradiol.
Target id:
/class/broad-spectrum-inducers
Target name:
Broad-Spectrum Metabolic Enzyme Inducers
Severity:
major
Interaction type:
diminishing
Nature:
absolute
Temporal spacing:
null
Description:
These substances (e.g., rifampin, carbamazepine, phenytoin) dramatically speed up the metabolism of 17-alpha-estradiol in the liver, which would likely render it ineffective.
Actionable advice:
Avoid using strong enzyme inducers, as they will significantly lower the effectiveness of 17-alpha-estradiol.
Target id:
/intervention/saint-johns-wort
Target name:
Saint John's Wort
Severity:
major
Interaction type:
diminishing
Nature:
absolute
Temporal spacing:
null
Description:
St. John's Wort is a potent inducer of the CYP3A4 enzyme, which will significantly accelerate the breakdown of 17-alpha-estradiol and severely reduce its potential efficacy.
Actionable advice:
Do not take St. John's Wort while using 17-alpha-estradiol.
Target id:
/dietary/grapefruit-pomelo
Target name:
Grapefruit or Grapefruit Juice
Severity:
major
Interaction type:
adverse
Nature:
temporal
Temporal spacing:
Hours before target:
72
Hours after target:
4
Description:
Grapefruit contains compounds that irreversibly inhibit the CYP3A4 enzyme in the gut, which can dangerously increase the absorption and systemic levels of 17-alpha-estradiol.
Actionable advice:
Completely avoid grapefruit and its juice for at least 3 days before and during the entire period of use.
Target id:
/condition/history-of-hormone-sensitive-cancer
Target name:
History of Hormone-Sensitive Cancer
Severity:
major
Interaction type:
adverse
Nature:
absolute
Temporal spacing:
null
Description:
Despite low affinity for classical estrogen receptors, any potential for off-target hormonal activity makes its use in individuals with a history of cancers (e.g., breast, uterine, prostate) an unacceptable risk.
Actionable advice:
Absolutely contraindicated in individuals with a personal history of hormone-sensitive cancers.
Target id:
/condition/history-of-vte
Target name:
History of Venous Thromboembolism (VTE)
Severity:
major
Interaction type:
adverse
Nature:
absolute
Temporal spacing:
null
Description:
Conventional estrogens increase the risk of blood clots. While the risk with 17-alpha-estradiol is unknown, it is a prudent and absolute contraindication for individuals with a history of DVT or pulmonary embolism.
Actionable advice:
Absolutely contraindicated in individuals with a personal history of blood clots.
Target id:
/condition/hepatic-impairment
Target name:
Hepatic Impairment
Severity:
major
Interaction type:
adverse
Nature:
absolute
Temporal spacing:
null
Description:
17-alpha-estradiol is expected to be extensively metabolized by the liver. Impaired liver function could lead to accumulation and unpredictable toxicity.
Actionable advice:
Avoid use in individuals with moderate to severe liver disease.
Target id:
/condition/pregnancy
Target name:
Pregnancy
Severity:
major
Interaction type:
adverse
Nature:
absolute
Temporal spacing:
null
Description:
The effects of 17-alpha-estradiol on fetal development are unknown. All experimental hormonal compounds are strictly contraindicated during pregnancy.
Actionable advice:
Absolutely contraindicated during pregnancy.
Target id:
/condition/lactation
Target name:
Breastfeeding (Lactation)
Severity:
major
Interaction type:
adverse
Nature:
absolute
Temporal spacing:
null
Description:
It is not known if 17-alpha-estradiol is excreted in breast milk or what its effects on a nursing infant would be. Use is contraindicated.
Actionable advice:
Absolutely contraindicated while breastfeeding.
Target id:
/class/estrogens
Target name:
Estrogens and Progestins (Hormonal Therapy & Contraceptives)
Severity:
major
Interaction type:
adverse
Nature:
absolute
Temporal spacing:
null
Description:
Combining 17-alpha-estradiol with other estrogenic compounds leads to an unknown and potentially harmful additive hormonal effect, even if their primary mechanisms differ.
Actionable advice:
Avoid using any other form of estrogen or hormone replacement therapy concurrently.
Target id:
/class/selective-estrogen-receptor-modulators
Target name:
Selective Estrogen Receptor Modulators (SERMs)
Severity:
major
Interaction type:
adverse
Nature:
absolute
Temporal spacing:
null
Description:
The interaction between 17-alpha-estradiol and SERMs (e.g., tamoxifen, raloxifene) is unknown and could lead to unpredictable and potentially adverse outcomes on estrogen-sensitive tissues.
Actionable advice:
Do not use SERMs concurrently with 17-alpha-estradiol.
Target id:
/class/cyp3a4-moderate-inhibitors
Target name:
Moderate CYP3A4 Inhibitors
Severity:
moderate
Interaction type:
adverse
Nature:
absolute
Temporal spacing:
null
Description:
Moderate CYP3A4 inhibitors can increase levels of 17-alpha-estradiol by slowing its breakdown in the liver, raising the risk of unknown side effects from this experimental compound.
Actionable advice:
Use with extreme caution and under medical supervision; consider avoiding if possible.
Target id:
/dietary/meal
Target name:
Any Meal
Severity:
moderate
Interaction type:
requirement
Nature:
temporal
Temporal spacing:
Hours before target:
0
Hours after target:
0
Description:
As a lipophilic steroid hormone, taking 17-alpha-estradiol with food, particularly containing some fat, may enhance and standardize its absorption, leading to more consistent blood levels.
Actionable advice:
Take with a meal to ensure consistent absorption and minimize variability.
Target id:
/biomarker/estradiol
Target name:
Estradiol Blood Test
Severity:
moderate
Interaction type:
assay_interference
Nature:
absolute
Temporal spacing:
null
Description:
17-alpha-estradiol is a stereoisomer of 17-beta-estradiol and may cross-react with standard immunoassays, leading to falsely and dramatically elevated estradiol readings.
Actionable advice:
If measuring estradiol, use a highly specific LC-MS/MS method and inform the lab of your use of this compound.
Target id:
/intervention/quercetin
Target name:
Quercetin
Severity:
minor
Interaction type:
adverse
Nature:
temporal
Temporal spacing:
Hours before target:
4
Hours after target:
4
Description:
Quercetin is a mild inhibitor of CYP3A4 and other metabolic enzymes, which could theoretically increase levels of 17-alpha-estradiol if taken at the same time.
Actionable advice:
Separate doses of quercetin and 17-alpha-estradiol by at least 4 hours.
Target id:
/intervention/curcumin-and-piperine
Target name:
Curcumin and Piperine
Severity:
minor
Interaction type:
adverse
Nature:
temporal
Temporal spacing:
Hours before target:
4
Hours after target:
4
Description:
Piperine, often combined with curcumin for absorption, is a known inhibitor of CYP3A4, which could slow the metabolism of 17-alpha-estradiol and increase its concentration.
Actionable advice:
Separate doses of curcumin/piperine and 17-alpha-estradiol by at least 4 hours.