RESUMO
INTRODUCTION: The effects of escitalopram (10 mg/d) coadministration on plasma concentrations of aripiprazole and its active metabolite, dehydroaripiprazole, were studied in 13 Japanese psychiatric patients and compared with those of paroxetine (10 mg/d) coadministration. METHODS: The patients had received 6-24 mg/d of aripiprazole for at least 2 weeks. Patients were randomly allocated to one of 2 treatment sequences: paroxetine-escitalopram (n=6) or escitalopram-paroxetine (n=7). Each sequence consisted of two 2-week phases. Plasma concentrations of aripiprazole and dehydroaripiprazole were measured using liquid chromatography with mass spectrometric detection. RESULTS: Plasma concentrations of aripiprazole and the sum of aripiprazole and dehydroaripiprazole during paroxetine coadministration were 1.7-fold (95% confidence intervals [CI], 1.3-2.1, p<0.001) and 1.5-fold (95% CI 1.2-1.9, p<0.01) higher than those values before the coadministration. These values were not influenced by escitalopram coadministration (1.3-fold, 95% CI 1.1-1.5 and 1.3-fold, 95% CI 1.0-1.5). Plasma dehydroaripiprazole concentrations remained constant during the study. CONCLUSION: The present study suggests that low doses of escitalopram can be safely coadministered with aripiprazole, at least from a pharmacokinetic point of view.
Assuntos
Citalopram/sangue , Transtornos Mentais/sangue , Piperazinas/sangue , Quinolonas/sangue , Adulto , Aripiprazol , Povo Asiático , Citalopram/uso terapêutico , Citocromo P-450 CYP2C19/genética , Citocromo P-450 CYP2D6/genética , Quimioterapia Combinada , Eletrocardiografia , Eletroencefalografia , Feminino , Genótipo , Humanos , Masculino , Transtornos Mentais/tratamento farmacológico , Transtornos Mentais/genética , Pessoa de Meia-Idade , Paroxetina/sangue , Paroxetina/uso terapêutico , Piperazinas/uso terapêutico , Quinolonas/uso terapêuticoRESUMO
The influence of cooling on the intracellular concentration of Ca2+ ([Ca2+]i) was tested in cell lines expressing chemical receptors. First, when ATP was externally added to rat basophilic leukemia (RBL-2H3) cells, cooling from 37 degrees C to 27 degrees C induced a transient rapid increase in [Ca2+]i. In the absence of extracellular Ca2+, the [Ca2+]i response was induced whereas an inhibitor of microsomal Ca2+ ATPase, thapsigargin, largely abolished the [Ca2+]i response, suggesting that the internal Ca2+ store liberate the Ca2+. A purinergic receptor antagonist, suramin, completely inhibited the [Ca2+]i response to the cooling. Secondly, when serotonin (5-HT) was added to rat glioma C6BU-1 cells, the cooling induced a transient increase in [Ca2+]. This [Ca2+]i response was induced in the absence of external Ca2+, suggesting that the internal Ca2+ stores liberate the Ca2+. These results raise the possibility that some G protein-coupled receptors are sensitive to cooling in the presence of agonist for the receptor.
Assuntos
Cálcio/metabolismo , Proteínas de Ligação ao GTP/metabolismo , Receptores de Superfície Celular/fisiologia , Serotonina/farmacologia , Suramina/farmacologia , Trifosfato de Adenosina/farmacologia , Compostos de Anilina , Animais , ATPases Transportadoras de Cálcio/antagonistas & inibidores , Temperatura Baixa , Corantes Fluorescentes , Glioma , Cinética , Leucemia Basofílica Aguda , Microssomos/enzimologia , Ratos , Receptores de Superfície Celular/efeitos dos fármacos , Transdução de Sinais/fisiologia , Tapsigargina/farmacologia , Fatores de Tempo , Células Tumorais Cultivadas , XantenosRESUMO
Three patients who had hot nodules on I-123 scan were found to have thyroid cancers in the nodule. Two of the cancers were follicular, one was a follicular variant of papillary cancer.