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Metabolism of a new synthetic progestagen, Org 2969, in female volunteers. The distribution and excretion of radioactivity after an oral dose of the labelled drug

Abstract

The metabolism of a new synthetic progestagen, Org 2969 was studied in 4 healthy female volunteers. During the first part of the study (Phase I), the volunteers ingested 50 ..mu..g (about 0.1 mCi) of (16-/sup 3/H)Org 2969 together with 50 ..mu..g of ethinyloestradiol as a single dose. During the second part of the study (Phase II), a 10-day pre-treatment with the same dosage of non-radioactive compound preceded the administration of the radioactive steroid. A peak level of total radioactivity, representing 3.16-5.02% of the dose given/l of serum, was achieved within 2-3 h in Phase I. During Phase II, the corresponding figures were 4.54-5.13% after 1.5-3 h. The difference was mainly due to an increase of freely-extractable steroids during Phase II. The difference can at least partly be explained by assuming a change in the kinetics of the metabolism of Org 2969 by pre-treatment with Org 2969 and ethinyloestradiol. The mean recovery of radioactivity in urine and faeces was 83.0%/48.1%/34.9% (total/urine/faeces) of the total dose in Phase I and 76.1%/45.2%/30.9% during Phase II. The differences in the total excretion and in the radioactivity excreted in the faeces were significant.
Authors:
Viinikka, L; Ylikorkala, O; Vihko, R; [1]  Hasenack, H G; Nieuwenhuyse, H [2] 
  1. Oulu Univ. (Finland)
  2. Organon Scientific Development Group, Organon Int., Oss, The Netherlands
Publication Date:
Jan 01, 1980
Product Type:
Journal Article
Reference Number:
AIX-11-538034; EDB-80-098237
Resource Relation:
Journal Name: Acta Endocrinol.; (Denmark); Journal Volume: 93
Subject:
59 BASIC BIOLOGICAL SCIENCES; HYDROXYPREGNENONE; METABOLISM; DISTRIBUTION; ESTRADIOL; EXCRETION; LABELLED COMPOUNDS; ORAL ADMINISTRATION; TRITIUM COMPOUNDS; WOMEN; ANIMALS; CLEARANCE; ESTRANES; ESTROGENS; FEMALES; HORMONES; HYDROXY COMPOUNDS; KETONES; MAMMALS; MAN; ORGANIC COMPOUNDS; PREGNANES; PRIMATES; STEROID HORMONES; STEROIDS; VERTEBRATES; 550501* - Metabolism- Tracer Techniques
OSTI ID:
5212721
Country of Origin:
Denmark
Language:
English
Other Identifying Numbers:
Journal ID: CODEN: ACENA
Submitting Site:
INIS
Size:
Pages: 375-379
Announcement Date:
Jul 01, 1980

Citation Formats

Viinikka, L, Ylikorkala, O, Vihko, R, Hasenack, H G, and Nieuwenhuyse, H. Metabolism of a new synthetic progestagen, Org 2969, in female volunteers. The distribution and excretion of radioactivity after an oral dose of the labelled drug. Denmark: N. p., 1980. Web.
Viinikka, L, Ylikorkala, O, Vihko, R, Hasenack, H G, & Nieuwenhuyse, H. Metabolism of a new synthetic progestagen, Org 2969, in female volunteers. The distribution and excretion of radioactivity after an oral dose of the labelled drug. Denmark.
Viinikka, L, Ylikorkala, O, Vihko, R, Hasenack, H G, and Nieuwenhuyse, H. 1980. "Metabolism of a new synthetic progestagen, Org 2969, in female volunteers. The distribution and excretion of radioactivity after an oral dose of the labelled drug." Denmark.
@misc{etde_5212721,
title = {Metabolism of a new synthetic progestagen, Org 2969, in female volunteers. The distribution and excretion of radioactivity after an oral dose of the labelled drug}
author = {Viinikka, L, Ylikorkala, O, Vihko, R, Hasenack, H G, and Nieuwenhuyse, H}
abstractNote = {The metabolism of a new synthetic progestagen, Org 2969 was studied in 4 healthy female volunteers. During the first part of the study (Phase I), the volunteers ingested 50 ..mu..g (about 0.1 mCi) of (16-/sup 3/H)Org 2969 together with 50 ..mu..g of ethinyloestradiol as a single dose. During the second part of the study (Phase II), a 10-day pre-treatment with the same dosage of non-radioactive compound preceded the administration of the radioactive steroid. A peak level of total radioactivity, representing 3.16-5.02% of the dose given/l of serum, was achieved within 2-3 h in Phase I. During Phase II, the corresponding figures were 4.54-5.13% after 1.5-3 h. The difference was mainly due to an increase of freely-extractable steroids during Phase II. The difference can at least partly be explained by assuming a change in the kinetics of the metabolism of Org 2969 by pre-treatment with Org 2969 and ethinyloestradiol. The mean recovery of radioactivity in urine and faeces was 83.0%/48.1%/34.9% (total/urine/faeces) of the total dose in Phase I and 76.1%/45.2%/30.9% during Phase II. The differences in the total excretion and in the radioactivity excreted in the faeces were significant.}
journal = []
volume = {93}
journal type = {AC}
place = {Denmark}
year = {1980}
month = {Jan}
}