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Effects of type 1 and type 2 diabetes on the pharmacokinetics of tramadol enantiomers in patients with neuropathic pain phenotyped as cytochrome P450 2D6 extensive metabolizers.
de Moraes, Natália Valadares; Lauretti, Gabriela Rocha; Lanchote, Vera Lucia.
Afiliação
  • de Moraes NV; Departamento de Análises Clínicas, Toxicológicas e Bromatológicas, Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Ribeirão Preto, São Paulo, Brazil.
J Pharm Pharmacol ; 66(9): 1222-30, 2014 Sep.
Article em En | MEDLINE | ID: mdl-24717054
OBJECTIVES: The aim of this study was to evaluate the influence of poorly controlled type 1 (T1DM) and type 2 diabetes mellitus (T2DM) on the pharmacokinetics and metabolism of tramadol enantiomers in patients with neuropathic pain. METHODS: Nondiabetic patients (control group, n = 12), patients with T1DM (n = 9) or T2DM (n = 9), all with neuropathic pain and phenotyped as cytochrome P450 2D6 extensive metabolizers, received a single oral dose of 100 mg racemic tramadol. Serial blood samples were collected over a 24-h period. KEY FINDINGS: Patients with T1DM showed reduced Cmax of both tramadol enantiomers. The plasma concentrations of the active (+)-M1 were significantly reduced in T1DM (area under the curve plasma concentration versus time (AUC∞ ): 313.1 ng·h/ml) when compared with nondiabetic patients (AUC∞ : 1246.6 ng·h/ml). The fraction unbound of (+)-M1 was increased in patients with T1DM. Patients with T1DM and T2DM showed reduced AUC and increased fraction unbound of (-)-M1. CONCLUSIONS: The reduced total plasma concentrations of the active (+)-M1 in patients with T1DM may not be of clinical relevance because they are counterbalanced by the increased fraction unbound.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Tramadol / Citocromo P-450 CYP2D6 / Diabetes Mellitus Tipo 1 / Diabetes Mellitus Tipo 2 / Neuropatias Diabéticas / Analgésicos Opioides / Neuralgia Tipo de estudo: Prognostic_studies Limite: Adult / Female / Humans / Male / Middle aged Idioma: En Revista: J Pharm Pharmacol Ano de publicação: 2014 Tipo de documento: Article País de afiliação: Brasil País de publicação: Reino Unido

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Tramadol / Citocromo P-450 CYP2D6 / Diabetes Mellitus Tipo 1 / Diabetes Mellitus Tipo 2 / Neuropatias Diabéticas / Analgésicos Opioides / Neuralgia Tipo de estudo: Prognostic_studies Limite: Adult / Female / Humans / Male / Middle aged Idioma: En Revista: J Pharm Pharmacol Ano de publicação: 2014 Tipo de documento: Article País de afiliação: Brasil País de publicação: Reino Unido