Sustained-release (SR) bupropion (Zyban) is approved as a smoking cessation aid for adults. Since smoking often begins in adolescence, we determined the single-dose pharmacokinetics of bupropion SR in 75 adolescent subjects ranging from 13 to 18 years old. Subjects self-reported their smoking status. Urinary cotinine concentration was used to verify smoking status. Thirty-seven subjects (18 males, 19 females) were classified as cigarette smokers and 38 were nonsmokers (19 males, 19 females). Fasted subjects received one tablet (150 mg) of bupropion SR, and plasma samples were collected before (0) and 1/2, 1, 2, 3, 4, 6, 8, 24, 48, and 72 hours after dosing. Plasma samples were analyzed for bupropion and its three major metabolites (hydroxybupropion and the aminoalcohol isomers, erythrohydrobupropion plus threohydrobupropion, expressed as a composite) by solid-phase extraction, followed by LC/MS/MS. Factorial analysis of variance (ANOVA) was used to evaluate the effects of smoking and gender on pharmacokinetic parameters. Smokers and nonsmokers differed significantly (p < 0.05) in age and urinary cotinine (p < 0.01) concentration but did not differ significantly in mean weight, height, body surface area, or body mass index. The pharmacokinetic (PK) parameters for bupropion and hydroxybupropion did not differ between smokers and nonsmokers, but differences were found between male and female subjects. Mean values for area under the plasma concentration versus time curve (AUC0-->infinity), volume of distribution (Vd beta) normalized to body weight, maximum plasma concentration (Cmax), and elimination half-life (t1/2 beta) for bupropion were significantly (p < 0.05) greater in females than males, while clearance of bupropion normalized to body weight (CL/f) did not differ between males and females. Females also exhibited significantly (p < 0.05) larger values for hydroxybupropion mean AUC0-->infinity and Cmax than males. The mean ratio of hydroxybupropion to bupropion AUC for adolescents was approximately 4 to 5, which is lower than that previously reported for adults. In conclusion, smoking status does not affect the single-dose pharmacokinetics of bupropion SR in adolescents. However, females differ from males in several potentially important PK parameters for bupropion and its major metabolite, hydroxybupropion.
This study was designed to evaluate the antimotion sickness activity of ginger root (Zingiber officinale) and to characterize the effects of ginger on gastric function. Twenty-eight human volunteers participated in the project. Subjects made timed head movements in a rotating chair until they reached an endpoint of motion sickness short of vomiting (malaise III or M-III). Each subject was tested with either ginger or scopolamine and a placebo. A substance was judged to possess antimotion sickness activity if it allowed a greater number of head movements compared to placebo control. Gastric emptying of a liquid was measured by nuclear medicine techniques in normal and motion sick subjects. Gastric electrical activity was monitored by cutaneous (surface) electrodes positioned over the abdominal area. Powder ginger (whole root, 500 or 1,000 mg) or fresh ginger root (1,000 mg) provided no protection against motion sickness. In contrast, subjects performed an average of 147.5 more head movements (p < 0.01) after scopolamine (0.6 mg p.o.) than after placebo. The rate of gastric emptying was significantly (p < 0.05) slowed when tested immediately after M-III but was inhibited less when tested 15 min after M-III. Powdered ginger (500 mg) had no effect on gastric emptying in normal or motion-sick subjects. Gastric motility was also changed during motion sickness. The frequency of the electrogastrogram (EGG) was increased after M-III (tachygastria) and the normal increase in EGG amplitude after liquid ingestion was reduced in motion sick subjects. Although powdered ginger (500 mg) partially inhibited tachygastria in motion sickness, it did not enhance the EGG amplitude in motion sick subjects. We conclude that ginger does not possess antimotion sickness activity, nor does it significantly alter gastric function during motion sickness.
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