Effect of cytochrome P450 3A4 inhibitor ketoconazole on risperidone pharmacokinetics in healthy volunteers.

What Is Known And Objective: Risperidone is an atypical antipsychotic agent used for the treatment of schizophrenia. It is mainly metabolized by human cytochrome P450 CYP2D6 and partly by CYP3A4 to 9-hydroxyrisperidone. Ketoconazole is used as a CYP3A4 inhibitor probe for studying drug-drug interactions.

Pharmacokinetic interactions between ciprofloxacin and itraconazole in healthy male volunteers.

Objective: To investigate the pharmacokinetic interaction between ciprofloxacin and itraconazole in healthy male volunteers.

Methods: Ten healthy male volunteers were assigned into a 2-sequence, 3-period pharmacokinetic interaction study. In phase 1, all subjects were randomly assigned to receive 500 mg of ciprofloxacin alone and 200 mg of itraconazole alone twice daily for 7 days with a 14 day wash-out period in a crossover design.

Relative bioavailability and pharmacokinetic comparison of two 2-mg risperidone tablet formulations: A single dose, randomized-sequence, double-blind, 2-way crossover study in healthy male volunteers in Thailand.

Background: Data regarding the pharmacokinetic properties of risperidone in the Thai population are limited. A new generic tablet formulation was recently developed, but bioequivalence research is necessary to obtain marketing authorization for it in Thailand.

Objective: The aim of this study was to evaluate and compare the pharmacokinetic properties of risperidone and its active metabolite, 9-hydroxyrisperidone (which reportedly contributes to the drug's pharmacodynamic effects), in a newly developed generic tablet formulation (test) and a branded formulation (reference) in healthy, fasting, male Thai volunteers.

Development of an analytical method for cefpirome in plasma by simplified HPLC technique and its applications.

The objective of this study was to develop a rapid and simplified, reliable high-performance liquid chromatography (HPLC) method for quantification of cefpirome (CAS 98753-19-6) in plasma. After precipitation of the plasma containing the internal standard, hydrochlorothiazide, with 5% trichloroacetic acid (TCA), the analysis of the cefpirome level in the plasma samples was carried out using a reverse-phase C18 column with the ultraviolet detector set at a wavelength of 258 nm. The chromatographic separation was accomplished with an isocratic mobile phase consisting of acetonitrile-acetate buffer pH 5.

Bioequivalence study of a generic quetiapine in healthy male volunteers.

Aim: To study the bioequivalence of a generic quetiapine (Quantia 200, manufactured by the Unison Laboratories Co., Ltd., Bangkok, Thailand) and the innovator product (Seroquel, AstraZeneca, Macclesfield, UK).

Pharmacokinetic interaction between ketoconazole and praziquantel in healthy volunteers.

Background: Praziquantel, a broad-spectrum anthelminthic, has been reported to undergo extensive first-pass metabolism by cytochrome P450 (CYP) enzymes in vivo. Ketoconazole, a potent CYP3A4 inhibitor, is known to markedly increase plasma concentrations of many co-administered drugs. However, no data are available on the potential pharmacokinetic drug interaction between ketoconazole and praziquantel in humans.

Rifampin, a cytochrome P450 3A inducer, decreases plasma concentrations of antipsychotic risperidone in healthy volunteers.

Background: Although cytochrome P450 (CYP) 2D6 is often thought to be the only CYP responsible for the metabolism of risperidone, many reports suggest that CYP3A may be involved too. Rifampin, a potent CYP3A inducer, has been known to markedly decrease plasma concentrations of various drugs, which are concomitantly administered during treatment.

Objective: To examine the effect of rifampin on plasma concentrations of a single oral dose of risperidone in healthy Thai male volunteers.

Effect of efavirenz on the pharmacokinetics of ketoconazole in HIV-infected patients.

Objective: To investigate the effect of efavirenz on the ketoconazole pharmacokinetics in HIV-infected patients.

Methods: Twelve HIV-infected patients were assigned into a one-sequence, two-period pharmacokinetic interaction study. In phase one, the patients received 400 mg of ketoconazole as a single oral dose on day 1; in phase two, they received 600 mg of efavirenz once daily in combination with 150 mg of lamivudine and 30 or 40 mg of stavudine twice daily on days 2 to 16.

CYP2C19 genetic polymorphism in Thai, Burmese and Karen populations.

The genetic polymorphism of CYP2C19 was examined in three Southeast Asian populations. This study was conducted in 774 Thais, 127 Burmeses and 131 Karens. Genomic DNA was extracted from leucocytes and analyzed by the PCR-RFLP technique.

Clinical drug interactions in outpatients of a university hospital in Thailand.

Background: A clinical event is likely to occur in patients receiving a pair of drugs, that have the potential to cause an interaction. The occurrence of a clinical drug-drug interaction in outpatients of university hospitals in Thailand is unknown.

Purpose: To investigate the occurrence of a clinical event associated with drug-drug interactions in outpatients at a Thai university hospital.

LC determination of praziquantel in human plasma.

A simple high-performance liquid chromatographic (HPLC) method for the determination of praziquantel in human plasma was developed and validated. The present method was described by adding drop-wise 0.2 M Zinc sulfate and acetonitrile to plasma sample for deproteinization.

Effect of rifampin on plasma concentrations of mefloquine in healthy volunteers.

Mefloquine is a 4-quinolinemethanol compound structurally related to quinine. Quinine is mainly metabolized by the cytochrome P450 3A4 isozyme (CYP3A4), whereas rifampin, a potent inducer of CYP3A4, is known to markedly decrease plasma quinine concentration. Our aim was to study the effect of rifampin on the pharmacokinetics of mefloquine, and explore a possible role of CYP3A4 on mefloquine metabolism.