Bond C M
Department of General Practice and Primary Care, University of Aberdeen, Foresterhill Health Centre.
Curr Med Res Opin. 1998;14(4):203-12. doi: 10.1185/03007999809113360.
The dizziness inherent in vertiginous disorders is often accompanied by nausea and/or vomiting. While prochlorperazine is effective in relieving nausea and vomiting, its low bioavailability following first pass metabolism in the liver and metabolism in the intestinal wall, compounded by the likelihood of regurgitation in the nauseous patient, may limit the therapeutic value of the oral preparation. A buccal preparation achieves higher plasma concentrations by direct absorption into the systemic circulation. In this randomised, double-blind, double-dummy trial in patients with vestibular disorders, in keeping with previous pharmacokinetic studies, buccal prochlorperazine achieved a significantly faster onset of effect compared with oral prochlorperazine (p = 0.04), and was significantly better in reducing the frequency of nausea (p = 0.02) and severity of vomiting (p = 0.05) at 24-36 hours. The frequency of vomiting was also reduced by buccal prochlorperazine compared with oral prochlorperazine, but this difference was only of borderline significance (p = 0.07). Buccal prochlorperazine was well tolerated and well rated by both patients and investigators, having no more adverse effects on the buccal mucosa than placebo and causing less drowsiness and sedation compared with the oral preparation. No advantages were reported for the oral preparation over buccal prochlorperazine. Buccal prochlorperazine is therefore safe and effective, and suitable for the treatment of dizziness associated with nausea and/or vomiting in patients suffering from vertiginous disorders.
眩晕症所固有的头晕常常伴有恶心和/或呕吐。虽然氯丙嗪在缓解恶心和呕吐方面有效，但其在肝脏首过代谢及肠壁代谢后生物利用度较低，再加上恶心患者可能出现反流，这可能会限制口服制剂的治疗价值。颊部制剂通过直接吸收进入体循环可达到更高的血浆浓度。在这项针对前庭疾病患者的随机、双盲、双模拟试验中，与之前的药代动力学研究一致，颊部氯丙嗪与口服氯丙嗪相比起效明显更快（p = 0.04），并且在24 - 36小时时，在减少恶心频率（p = 0.02）和呕吐严重程度（p = 0.05）方面明显更优。与口服氯丙嗪相比，颊部氯丙嗪也降低了呕吐频率，但这种差异仅具有临界显著性（p = 0.07）。颊部氯丙嗪耐受性良好，患者和研究者评价都很高，对颊部黏膜的不良反应不超过安慰剂，且与口服制剂相比引起的嗜睡和镇静作用更小。未报告口服制剂相对于颊部氯丙嗪有任何优势。因此，颊部氯丙嗪安全有效，适用于治疗眩晕症患者伴有恶心和/或呕吐的头晕。
