Estriol

Estriol

Basics

Estriol or estriol is a female sex hormone of the estrogen group. It is a metabolic product of the estrogen estradiol and therefore exhibits a weaker estrogen effect. A large amount of estriol is produced by the placenta during pregnancy.

It is used to relieve vaginal discomfort and in hormone replacement therapy during menopause. Estriol is mostly applied vaginally as a cream or administered in tablet form.

Effect

Pharmacodynamics

Estriol binds to the estrogen receptor in the nucleus, thereby stimulating cells to produce proteins. Increased sex hormone-binding globulin and thyroid hormone-binding globulin are synthesized and follicle-stimulating hormone is suppressed. The proteins formed mediate the effect of estriol on the target cell. It also positively affects the microflora of the vagina and alleviates the discomfort of vaginal mucosal involution.


Pharmakokinetik

Estriol is rapidly and completely absorbed, with only 1-2% of the ingested dose entering the systemic circulation. Metabolism occurs in the liver and intestine. In plasma, it circulates at 91% protein-bound, with maximum plasma concentration reached after 5 hours. In relation to other estrogens, the effect lasts shorter and is weaker. Estriol is almost entirely excreted renally.

Contraindications

Estriol should not be used in case of:

  • Hypersensitivity
  • Breast cancer
  • estrogen-dependent tumors
  • Endometriosis
  • Thromboembolic diseases
  • severe renal failure
  • Liver disease
  • Pregnancy and lactation

Drug interactions

Estriol may interact with drugs that affect the CYP450 enzyme, resulting in either increased or decreased plasma estriol levels. Systemic interactions are unlikely when used topically.

Toxicity

Side effects

The following side effects are common during estriol therapy:

  • Itching
  • Discharge
  • breast pain or tenderness
  • Edema
  • Nausea

Toxicological data

LD50 (rat, oral): >2000 mg/kg

Chemical & physical properties

ATC Code G03CA04, G03CC06, G03CD01
Formula C18H24O3
Molar Mass (g·mol−1) 288,3814
Physical State solid
Density (g·cm−3) 1,27
Melting Point (°C) 82-86
PKS Value 10,54
CAS Number 50-27-1
PUB Number 5756
Drugbank ID DB04573

Editorial principles

All information used for the content comes from verified sources (recognised institutions, experts, studies by renowned universities). We attach great importance to the qualification of the authors and the scientific background of the information. Thus, we ensure that our research is based on scientific findings.
Markus Falkenstätter, BSc

Markus Falkenstätter, BSc
Author

Markus Falkenstätter is a writer on pharmaceutical topics in Medikamio's medical editorial team. He is in the last semester of his pharmacy studies at the University of Vienna and loves scientific work in the field of natural sciences.

Mag. pharm. Stefanie Lehenauer

Mag. pharm. Stefanie Lehenauer
Lector

Stefanie Lehenauer has been a freelance writer for Medikamio since 2020 and studied pharmacy at the University of Vienna. She works as a pharmacist in Vienna and her passion is herbal medicines and their effects.

The content of this page is an automated and high-quality translation from DeepL. You can find the original content in German here.

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