Single and Multiple Dose PK-PD Characterization for Carisoprodol. Part I: Pharmacokinetics, Metabolites, and 2C19 Phenotype Influence. Double-Blind, Placebo-Controlled Clinical Trial in Healthy Volunteers.

2C19 carisoprodol central muscle relaxants clinical trial drug abuse liability meprobamate pharmacokinetics phenotype

Journal

Journal of clinical medicine
ISSN: 2077-0383
Titre abrégé: J Clin Med
Pays: Switzerland
ID NLM: 101606588

Informations de publication

Date de publication:
06 Feb 2022
Historique:
received: 30 12 2021
revised: 01 02 2022
accepted: 03 02 2022
entrez: 15 2 2022
pubmed: 16 2 2022
medline: 16 2 2022
Statut: epublish

Résumé

Carisoprodol was authorised in 1959 without a full pharmacokinetic-pharmacodynamic (PK-PD) characterisation. We designed a crossover, double-blind, placebo-controlled, randomized clinical trial to characterize the PKs of carisoprodol and its main active metabolite, meprobamate, after single (350 mg), multiple (350 mg/8 h, 14 days), and double (700 mg) doses of carisoprodol. Thirteen healthy volunteers were enrolled. After a single (350 mg) dose, the main carisoprodol parameters were (mean ± SD) Cmax: 2580 ± 1214 ng/mL, AUC

Identifiants

pubmed: 35160309
pii: jcm11030858
doi: 10.3390/jcm11030858
pmc: PMC8836664
pii:
doi:

Types de publication

Journal Article

Langues

eng

Subventions

Organisme : Belmac Laboratories
ID : N.A.

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Auteurs

Aitana Calvo (A)

Clinical Pharmacology Department, Hospital Clínico San Carlos, IdISSC, 28040 Madrid, Spain.

Saioa Alonso (S)

Clinical Pharmacology Department, Hospital Clínico San Carlos, IdISSC, 28040 Madrid, Spain.

Esther Prieto (E)

Clinical Pharmacology Department, Hospital Clínico San Carlos, IdISSC, 28040 Madrid, Spain.

Ana Ascaso-Del-Rio (A)

Clinical Pharmacology Department, Hospital Clínico San Carlos, IdISSC, 28040 Madrid, Spain.

Jordi Ortuño (J)

Anapharm Bioanalytics, 08038 Barcelona, Spain.

Nieves Fernandez (N)

Belmac Laboratories, 28700 Madrid, Spain.

Antonio Portolés (A)

Pharmacology & Toxicology Department, Facultad de Medicina, Universidad Complutense de Madrid, 28040 Madrid, Spain.

Classifications MeSH