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首页> 外文期刊>The Journal of Clinical Pharmacology: Official Journal of the American College of Clinical Pharmacology >Absolute bioavailability and electroencephalographic effects of conventional and extended-release formulations of venlafaxine in healthy subjects.
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Absolute bioavailability and electroencephalographic effects of conventional and extended-release formulations of venlafaxine in healthy subjects.

机译：文拉法辛的常规和延长释放制剂在健康受试者中的绝对生物利用度和脑电图作用。

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摘要

Venlafaxine is currently marketed for treatment of depressive disorders as a conventional tablet formulation with a twice or three times daily dosage regimen. The absolute bioavailability of the conventional (CF) and extended-release (XR) formulations and their effects on electroencephalograms (EEG) and on a visual analog scale (VAS) for nausea were assessed in a randomized, double-blind, four-way crossover, placebo-controlled study of 16 healthy young men who were given either a single oral dose of 50 mg of CF venlafaxine, 75 mg of XR venlafaxine, or an intravenous dose of 10 mg of venlafaxine, or a placebo at 1-week intervals. The absolute bioavailability of venlafaxine was between 40% and 45% and was similar for both the CF and XR formulations. Venlafaxine produced central effects of a desipramine-like antidepressant. Regardless of formulation tested, the main EEG changes were an increase in fast beta (20-30 Hz) energy, which was more pronounced over the frontotemporal regions and extended within the full beta range (16-40 Hz). Maximum effect was reached at 6 hours for the CF and reached a plateau from 10 to 24 hours for the XR formulation. A dose-proportional increase in central activity, expressed as area under the effect curve (AUE) of the beta band, was observed between the CF (50 mg) and XR (75 mg) formulations. Compared with the CF tablet, the XR formulation also produced a much less intense maximum effect and a decrease of 63% in the AUE of nausea normalized by dose. The XR formulation has the same absolute bioavailability and the same central activity as assessed by EEG, but produced less intensive nausea than CF venlafaxine. The present findings suggest that a once-daily dosage regimen should be sufficient. This was confirmed by several clinical trials in depressive patients.
机译：目前，文拉法辛作为一种常规的片剂制剂，以每日两次或三倍的剂量给药，用于治疗抑郁症。在随机，双盲，四向交叉试验中评估了常规（CF）和缓释（XR）制剂的绝对生物利用度及其对脑电图（EEG）和视觉模拟量表（VAS）的恶心作用。 ，安慰剂对照研究，对16位健康的年轻人进行了研究，他们每隔1周接受一次口服50毫克CF文拉法辛，75毫克XR文拉法辛或静脉注射10毫克文拉法辛或安慰剂。文拉法辛的绝对生物利用度在40％至45％之间，对于CF和XR制剂均相似。文拉法辛产生了像地昔帕明一样的抗抑郁药的中心作用。不管测试的制剂如何，主要的EEG变化都是快速β（20-30 Hz）能量的增加，在额颞叶区域更明显，并在整个β范围（16-40 Hz）内扩展。 CF在6小时时达到最大效果，而XR制剂在10到24小时达到平稳。在CF（50 mg）和XR（75 mg）制剂之间观察到中心活性呈剂量比例增加，表示为β带效应曲线下面积（AUE）。与CF片剂相比，XR制剂产生的强效作用要小得多，按剂量归一化后的恶心AUE降低了63％。 XR制剂具有与EEG相同的绝对生物利用度和相同的中枢活性，但比CF文拉法辛产生的恶心更小。目前的发现表明，每天一次的剂量方案应足够。抑郁症患者的多项临床试验证实了这一点。

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