Go to:
Logótipo
Comuta visibilidade da coluna esquerda
Você está em: Start > Publications > View > Chronopharmacology of nebicapone, a new catechol-O-methyltransferase inhibitor
Publication

Publications

Chronopharmacology of nebicapone, a new catechol-O-methyltransferase inhibitor

Title
Chronopharmacology of nebicapone, a new catechol-O-methyltransferase inhibitor
Type
Article in International Scientific Journal
Year
2010
Authors
Almeida, L
(Author)
Other
The person does not belong to the institution. The person does not belong to the institution. The person does not belong to the institution. Without AUTHENTICUS Without ORCID
Loureiro, AI
(Author)
Other
The person does not belong to the institution. The person does not belong to the institution. The person does not belong to the institution. Without AUTHENTICUS Without ORCID
Vaz Da Silva, M
(Author)
FMUP
View Personal Page You do not have permissions to view the institutional email. Search for Participant Publications View Authenticus page Without ORCID
Torrao, L
(Author)
Other
The person does not belong to the institution. The person does not belong to the institution. The person does not belong to the institution. Without AUTHENTICUS Without ORCID
Maia, J
(Author)
Other
The person does not belong to the institution. The person does not belong to the institution. The person does not belong to the institution. Without AUTHENTICUS Without ORCID
Fernandes Lopes, C
(Author)
Other
The person does not belong to the institution. The person does not belong to the institution. The person does not belong to the institution. Without AUTHENTICUS Without ORCID
Falcao, A
(Author)
Other
The person does not belong to the institution. The person does not belong to the institution. The person does not belong to the institution. View Authenticus page Without ORCID
Igreja, B
(Author)
Other
The person does not belong to the institution. The person does not belong to the institution. The person does not belong to the institution. Without AUTHENTICUS Without ORCID
Wright, L
(Author)
Other
The person does not belong to the institution. The person does not belong to the institution. The person does not belong to the institution. Without AUTHENTICUS Without ORCID
soares-da-silva, p
(Author)
FMUP
View Personal Page You do not have permissions to view the institutional email. Search for Participant Publications View Authenticus page View ORCID page
Journal
Vol. 26
Pages: 1097-1108
ISSN: 0300-7995
Publisher: Taylor & Francis
Other information
Authenticus ID: P-003-6XP
Abstract (EN): Objective: To investigate the chronopharmacology of nebicapone, a new catechol-O-methyltransferase (COMT) inhibitor currently being developed for use as an adjunct to levodopa/carbidopa or levodopa/benserazide in the treatment of Parkinson's disease. Methods: This was a double-blind, randomised, placebo-controlled, parallel-group study. Eighteen Caucasian subjects were randomly assigned to treatment with either nebicapone 100 mg (n = 6), nebicapone 200 mg (n = 6) or placebo (n = 6) at 4-h intervals for 7 days. First dose occurred at 8: 00 AM on day 1 and last dose at 8: 00 AM on day 8. Blood samples for the determination of plasma drug concentrations of nebicapone and its glucuronidated and methylated metabolites and for the assay of erythrocyte soluble COMT (S-COMT) activity were taken at frequent times following the first and last doses, and before the 8: 00 AM and 8: 00 PM doses on days 2-7. Results: Three men and three women in each group participated in the study. Mean +/- SD (range) age of study participants was 23.7 +/- 3.1 (21-28) years in the nebicapone 100 mg group, 22.2 +/- 0.4 (22-23) years in the nebicapone 200 mg group and 24.3 +/- 5.4 (18-32) in the placebo group. A circadian variation in the pre-dose nebicapone and nebicapone-glucuronide plasma concentrations was apparent. Both nebicapone and nebicapone-glucuronide levels were lower before the 8 PM dose in comparison to the 8 AM dose, suggesting that the absorption of nebicapone may follow a circadian variation. S-COMT activity showed no circadian variation in the placebo group. Therefore, the S-COMT activity variation found in nebicapone-treated subjects is considered to be due to changes in plasma concentrations of nebicapone, which is consistent with the fact that the pre-dose S-COMT activity was lower at the time at which nebicapone levels were maximal. Four subjects in the nebicapone 100 mg and placebo groups and six subjects in the nebicapone 200 mg group reported at least one adverse event (AE). All AEs were of mild or moderate intensity. Both nebicapone treatment regimens were subjectively well-tolerated, but a clinically relevant elevation in aspartate transaminase was observed in one subject of each nebicapone group. Conclusion: Nebicapone showed chronopharmacology in young Caucasian healthy subjects. The clinical impact of the circadian variation in the nebicapone metabolism and activity in Parkinson's disease patients deserves evaluation as it may have implications for drug prescription by modulating the distribution of the total daily dose along the 24-h scale.
Language: English
Type (Professor's evaluation): Scientific
No. of pages: 12
Documents
We could not find any documents associated to the publication.
Related Publications

Of the same journal

Validation of the HPV Impact Profile in Portuguese women with human papilloma virus (2019)
Article in International Scientific Journal
Santos, BD; moreira, cs; Vilhena, E; Carvalho, E; Pereira, MG
Reliability and validity of the Bowel Function Index for evaluating opioid-induced constipation: translation, cultural adaptation and validation of the Portuguese version (BFI-P) (2017)
Article in International Scientific Journal
Duenas, M; Mendonca, L; Sampaio, R; Gouvinhas, C; Oliveira, D; Castro-Lopes J.M.; Azevedo L
Cost-effectiveness and budget impact of long-acting risperidone in Portugal: a modeling exercise (2008)
Article in International Scientific Journal
B. M. S. Heeg; J. Antunes; M. L. Figueira; J. M. Jara; João Marques Teixeira; A. P. Palha; Adriano Vaz Serra; E. Buskens; S. Caleo; C. Gouveia-Pinto; B. A. van Hout
Recommend this page Top
Copyright 1996-2025 © Faculdade de Direito da Universidade do Porto  I Terms and Conditions  I Acessibility  I Index A-Z
Page created on: 2025-07-16 at 07:38:39 | Privacy Policy | Personal Data Protection Policy | Whistleblowing