Serum concentrations of estriol vary widely after application of vaginal oestriol cream.
Br J Clin Pharmacol
; 87(5): 2354-2360, 2021 05.
Article
en En
| MEDLINE
| ID: mdl-33129232
ABSTRACT
AIMS:
The aim of this study was to establish the pharmacokinetic profile of serum oestriol (E3 ) concentrations over 24 h following application of vaginal E3 in chronic users (>12 weeks of E3 use). The interindividual and intraindividual differences before and after E3 were examined.METHODS:
Ten women participated. Vaginal cream was omitted for ≥36 h prior to the study days. Blood sampling was performed for E3 , oestradiol and oestrone concentrations prior to cream application and at 1, 2, 3, 5, 8, 10, 12 and 24 h afterwards. In five women, all samples were repeated on a separate day.RESULTS:
E3 was absorbed rapidly in most women. Peak serum E3 concentration occurred around 2 h (range 1-5 h). The decline in E3 concentrations was also rapid falling <100 pmol L-1 in six out of ten women within 8 h and returning to ≤ 10 pmol L-1 at 24 h in nine out of the ten patients. Interindividual variability for peak concentrations was considerable (mean 546 pmol L-1 ; 95% CI 349-743). Area under the concentration-time curve (AUC) values over a dosage interval also varied widely mean 2145 pmol.h L-1 ; 95% CI 1422-3233. However, repeated measurements in the same woman were highly (peaks ρ = 0.94) or moderately (AUC P = 0.74) correlated.CONCLUSIONS:
Postmenopausal E3 concentrations are negligible. Serum E3 concentrations of chronic users of E3 cream varied greatly; however, concentrations declined rapidly within 8 h, generally reaching 'postmenopausal' levels by 24 h. The basis for the variation between subjects needs further elucidation. Additional research is required to establish the safety of topical E3 .Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Cremas, Espumas y Geles Vaginales
/
Estriol
Límite:
Female
/
Humans
Idioma:
En
Revista:
Br J Clin Pharmacol
Año:
2021
Tipo del documento:
Article
País de afiliación:
Australia