The aim of the present study was to identify human cytochrome P450 enzymes (P450s) involved in mono-2-, di-2-, and 5-sulfoxidation, and N-demethylation of the piperidine-type phenothiazine neuroleptic thioridazine in the human liver. The experiments were performed in vitro using cDNA-expressed human P450s (Supersomes 1A2, 2A6, 2B6, 2C9, 2C19, 2D6, 2E1, and 3A4), liver microsomes from different ...

Thioridazine and metabolites were measured in brain, liver, and kidney specimens, obtained postmortem from two subjects whose deaths were related to acute intoxication with thioridazine, by gas-liquid chromatography. Although the absolute concentration measured for thioridazine and metabolites differed in the two cases, the metabolic pattern for each tissue, expressed in terms of the percentage...

BACKGROUND Some non-antibiotic drugs, such as the phenothiazine antipsychotic agents, may have antimicrobial activity. MATERIALS AND METHODS We sought to determine the in vivo antimicrobial effects of the phenothiazine thioridazine in two mouse models of Staphylococcus aureus skin infection. RESULTS Thioridazine significantly suppressed dissemination from skin to spleen and kidney after ino...

Chlorpromazine and thioridazine are phenothiazines employed in the treatment of psychosis. These agents inhibited the respiration of clinical isolates of Mycobacterium tuberculosis resistant to streptomycin, rifampin, isoniazid, ethambutol and/or pyrazinamid, all first line drugs. Since any adverse reaction to thioridazine is generally less severe than to chlorpromazine, the possibility is attr...

Despite the fact that thioridazine is used clinically as a neuroleptic drug, little is known about the molecular mechanisms underlying its biological effects, in particular about its interactions with membranes. In the present work we investigate the influence of thioridazine on model and cell membranes, using calorimetry, DPH fluorescence polarization measurements, studies of haemolysis and sc...

Treatment with thioridazine resulted in hyperpyrexia and ventricular tachycardia in a young woman who was later shown to have thyrotoxicosis. The reasons why hyperthyroidism may enhance thioridazine toxicity are reviewed.

Mycobacterium avium-intracellulare complex (MAC) causes an intractable intracellular infection that presents as chronic pulmonary disease. Currently, therapy consists of ethambutol and macrolides and takes several years to complete. The neuroleptic phenothiazine thioridazine kills mycobacteria by inhibiting the electron transport chain. In several experiments with bacterial populations of up to...

• Do not use with thioridazine due to QTc interval prolongation or HIGHLIGHTS OF PRESCRIBING INFORMATION potential for elevated thioridazine plasma levels. Do not use These highlights do not include all the information needed to use thioridazine within 5 weeks of discontinuing SYMBYAX (4, 7.7) SYMBYAX safely and effectively. See full prescribing information for SYMBYAX. -----------------------W...

When oxygen is slowly depleted from growing cultures of Mycobacterium tuberculosis, they enter a state of nonreplicating persistence that resembles the dormant state seen with latent tuberculosis. In this hypoxic state, nitrate reductase activity is strongly induced. Nitrate in the medium had no effect on long-term persistence during gradual oxygen depletion (Wayne model) for up to 46 days, but...

Historically, multiplicity of actions in synthetic compounds is a rule rather than exception. The science of non-antibiotics evolved in this background. From the antimalarial and antitrypanosomial dye methylene blue, chemically similar compounds, the phenothiazines, were developed. The phenothiazines were first recognised for their antipsychotic properties, but soon after their antimicrobial fu...