皮肤的药物代谢动力学情况芬太尼交付有或没有控制热量。

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Ashburn马,奥格登噢,张J,爱G, Basta SV

皮肤的药物代谢动力学情况芬太尼交付有或没有控制热量。

J痛苦。2003年8月,4 (6):291 - 7。

PubMed ID
14622685 (在PubMed
]
文摘

初步报告显示,本地热皮肤的应用芬太尼贴片显著增加系统交付芬太尼。本研究的目的是进一步评估当地的药代动力学影响热管理芬太尼通过皮肤药芬太尼贴片交付系统的志愿者。此外,这项研究的目的是记录的影响在稳态热皮肤芬太尼交付。三期,这是一个开放的交叉研究的药物动力学和安全评估25 microg / h皮肤芬太尼管理与当地,没有热量。A和B在练习过程中,受试者接受经皮的芬太尼30段。在会话期间,热量申请1小时在有关期间24小时时间点。在会话期间B,热量第一4小时,然后再申请1个小时在有关期间24小时时间点。会话A和B的顺序是随机的,分离和至少2周会议。五的10个主题回到参与会话期间C .会话C,受试者接受经皮的芬太尼25 microg / h 18个小时。热管理应用在第一个4小时又15分钟的时间在12 - 16小时的时间点。 Arterial blood samples for determination of serum fentanyl concentration were collected. Maximum concentration (C(max)), time to maximum concentration (t(max)), and area under the curve (AUC) were determined for each treatment period. Sedation, vital signs, oxygen saturation, and adverse events were recorded. During a period of 36 hours, there were no significant differences in C(max), AUC, or T(max) between transdermal fentanyl delivery with no heat and heat. However, significant differences were seen during the first 4 hours, with C(max) and AUC values almost 3 times higher for the heated administrations than for the administrations without heat. With heat, the mean C(max) was 0.63 ng/mL compared with a C(max) of 0.24 ng/mL without heat (P =.007). With early heat, the mean AUC was 1.22 ng/mL. h compared with 0.42 ng/mL. h without heat (P =.003). There was no statistically significant difference between the median times to achieve peak values (T(max)) during the first 4 hours. The addition of heat at 24 hours resulted in rapid increases in serum fentanyl concentrations for both groups and higher serum fentanyl concentrations for the administration that did not receive heat previously. Applying heat for 15 minutes at the 12-hour and 16-hour time points produced a rapid but short duration increase in serum fentanyl concentrations. The results suggest controlled heat might be used to significantly shorten the time needed to reach clinically important fentanyl concentrations. Controlled heat might be useful to produce rapid increases in serum concentrations for the rapid treatment of breakthrough pain.

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