Description of the time course of the prolactin suppressant effect of the dopamine agonist CQP201-403 by an integrated pharmacokinetic-pharmacodynamic model
Détails
ID Serval
serval:BIB_AC017405F649
Type
Article: article d'un périodique ou d'un magazine.
Collection
Publications
Institution
Titre
Description of the time course of the prolactin suppressant effect of the dopamine agonist CQP201-403 by an integrated pharmacokinetic-pharmacodynamic model
Périodique
British Journal of Clinical Pharmacology
ISSN
0306-5251 (Print)
Statut éditorial
Publié
Date de publication
07/1986
Volume
22
Numéro
1
Pages
1-13
Notes
Clinical Trial
Comparative Study
Journal Article
Randomized Controlled Trial --- Old month value: Jul
Comparative Study
Journal Article
Randomized Controlled Trial --- Old month value: Jul
Résumé
Six male volunteers (mean age 24 years) received a single oral dose of 0.025 mg CQP201-403 and placebo in a randomised double-blind crossover design. Fifteen plasma samples were collected over 48 h and were assayed by radioimmunoassay for drug substance and prolactin (PRL). Three of the samples were drawn during sleep on the first study day. The pharmacological effect (E%) of CQP201-403 was expressed as reduction in plasma PRL levels. The pharmacokinetic (PK)-pharmacodynamic (PD) model consisted of two kinetic compartments and an effect compartment linked to the central compartment. A sigmoid Emax model (Hill equation) described the relationship between the drug concentration in the effect compartment and E%. Curve-fitting of PK and PD data provided individual parameter estimates which served to generate computer-simulated PK and PD profiles after single and multiple doses in order to: investigate the in vivo concentration-effect relationship; evaluate the consequence of dosage reduction on the steady-state PD profile; and study the robustness of the response to changes in drug potency and bioavailability.
Mots-clé
Adult
Dose-Response Relationship, Drug
Double-Blind Method
Ergolines/blood/*pharmacology
Humans
Kinetics
Male
*Models, Biological
Prolactin/*blood
Radioimmunoassay
Random Allocation
Software
Time Factors
Pubmed
Web of science
Création de la notice
15/02/2008 17:57
Dernière modification de la notice
20/08/2019 16:16