Moy Kathleen V, Ma Joseph D, Morello Candis M, Atayee Rabia S, Best Brookie M
Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego (UC San Diego), La Jolla, California.
Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego (UC San Diego), La Jolla, California; Doris A. Howell Palliative Care Service, San Diego, California.
J Opioid Manag. 2014 Jan-Feb;10(1):47-56. doi: 10.5055/jom.2014.0191.
Saliva is purported to have a close correspondence to plasma concentrations due to a passive diffusion process from plasma to saliva. However, limited data are available characterizing oxycodone and its metabolites in saliva. The purpose of this analysis was to evaluate the use of saliva monitoring in patients prescribed oxycodone and to compare the disposition of oxycodone in saliva and urine.
This retrospective analysis examined deidentified urine and saliva specimens collected from patients with chronic pain. These specimens were received at Millennium Laboratories between March and June 2012 and analyzed using LCMS/MS to quantitate oxycodone, noroxycodone, and oxymorphone concentrations.
The geometric mean metabolic ratio (MR) of noroxycodone to oxycodone in saliva was 0.11, whereas the geometric mean MR in urine was 1.7. The geometric mean oxycodone concentration in saliva was 860 ng/mL (range, 1.5-8,600,000 ng/mL; 95% CI, 770-950 ng/mL), whereas the geometric mean noroxycodone concentration was 98 ng/mL (range, 2.3-8,800 ng/mL; 95% CI, 90-107 ng/mL). Fifty-four of the saliva specimens (6 percent) had oxycodone concentrations between 10,000 and 9,000,000 ng/mL.
Oxycodone is predominant over noroxycodone in saliva (similar to plasma), while the reverse relationship exists in urine. Much greater oxycodone concentrations were found in saliva than are expected in plasma (up to a 1,000-fold difference). Saliva concentrations are lower than urine concentrations but still may not reflect plasma disposition. Possible explanations include medication residue in the mouth (recent medication use or misuse) or active secretion into saliva. Saliva analysis may be used for qualitative drug monitoring of oxycodone, with detection rates similar to urine; however, further characterization is needed for appropriate interpretation.
由于从血浆到唾液的被动扩散过程，唾液被认为与血浆浓度密切相关。然而，关于羟考酮及其代谢物在唾液中的特征数据有限。本分析的目的是评估唾液监测在服用羟考酮患者中的应用，并比较羟考酮在唾液和尿液中的代谢情况。
这项回顾性分析检查了从慢性疼痛患者收集的匿名尿液和唾液标本。这些标本于2012年3月至6月间在千禧实验室接收，并使用液相色谱-串联质谱法（LCMS/MS）分析以定量羟考酮、去甲羟考酮和羟吗啡酮的浓度。
唾液中去甲羟考酮与羟考酮的几何平均代谢率（MR）为0.11，而尿液中的几何平均MR为1.7。唾液中羟考酮的几何平均浓度为860 ng/mL（范围为1.5 - 8,600,000 ng/mL；95%置信区间为770 - 950 ng/mL），而去甲羟考酮的几何平均浓度为98 ng/mL（范围为2.3 - 8,800 ng/mL；95%置信区间为90 - 107 ng/mL）。54份唾液标本（6%）的羟考酮浓度在10,000至9,000,000 ng/mL之间。
在唾液中羟考酮比去甲羟考酮占主导（类似于血浆），而在尿液中则相反。唾液中发现的羟考酮浓度比血浆中预期的要高得多（相差高达1000倍）。唾液浓度低于尿液浓度，但仍可能无法反映血浆代谢情况。可能的解释包括口腔中的药物残留（近期用药或滥用）或向唾液中的主动分泌。唾液分析可用于羟考酮的定性药物监测，检测率与尿液相似；然而，为了进行适当的解读还需要进一步的特征描述。
