大剂量的药代学和药效学活性准备海洛因,opioid-dependent患者静脉或吸入途径。

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车EJ,范Ree JM, van den W,边缘接触MJ, Huitema广告,hendrik VM, Beijnen JH

大剂量的药代学和药效学活性准备海洛因,opioid-dependent患者静脉或吸入途径。

基本Toxicol杂志》2006年1月,98 (1):86 - 96。doi: 10.1111 / j.1742-7843.2006.pto_233.x。

PubMed ID
16433897 (在PubMed
]
文摘

pharmacokinetic-pharmacodynamic研究opioid-dependent患者在荷兰,他们目前准备接受高剂量的医学医疗处方海洛因。除了静脉注射海洛因,海洛因吸入的是规定“追龙”的方法。在这种技术中,海洛因碱加热在铝箔上,和海洛因蒸气吸入到肺部。我们不太清楚这个特定的政府的药物动力beplayapp学概况和生物利用度的方法。因此,研究海洛因吸入的药代学和药效学和静脉注射使用。11个病人注射海洛因和9患者吸入海洛因进入学习。他们在稳态海洛因治疗至少12个月。由于安全原因,之间没有互换海洛因注射或者吸入。在双盲随机的一项研究中,67 - 100 - 150%的常规海洛因维持剂量是每个病人的管理。最大的单一海洛因剂量为450毫克。 Plasma concentrations of heroin and its metabolites 6-monoacetylmorphine, morphine and morphine-glucuronides were analysed using LC-MS-MS. Blood pressure, heart rate, skin temperature and reaction time were assessed. Furthermore, visual analogue scales regarding craving and appreciation of heroin effect were scored by the subjects. Both in inhaling and injecting patients, the areas under curve of heroin and all measured metabolites were linearly related to heroin dose. Mean C(max) of heroin and its metabolites were 2-6 times lower after inhalation, than after intravenous injection. Bioavailability (F) of heroin inhalation was estimated as 52% (95% CI 44-61%). Heroin was rapidly cleared from plasma. Cl/F was 930 l/hr (95% CI 799-1061 l/hr) after intravenous administration, and 1939 l/hr (95% CI 1661-2217 l/hr) after inhalation. Heroin Cl and Vd were correlated to body weight (R(2) 15-19%). Morphine-glucuronides levels were inversely related to creatinine clearance. After heroin administration, the reaction time was significantly prolonged with 28+/-5.3 msec. in injecting and 13+/-4.9 msec. in inhaling patients. Cardiovascular changes were only mild after heroin administration. Craving-scores declined immediately after heroin administration in both administration groups. Subjective heroin effect was rated more positively in heroin inhaling than in injecting patients, despite the lower C(max) levels following heroin inhalation. In both groups, in this blinded study heroin dose increments were more appreciated than dose reductions. Increments of 50% of the regular heroin dose did not cause any serious side effect.

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