Cocaine and Metabolite Excretion in Saliva under Stimulated and Nonstimulated Conditions

Abstract

The accessibility of saliva for rapid, noninvasive sampling makes it an attractive biological fluid for detecting drug use. However, little is known about salivary excretion patterns of the major cocaine metabolites, benzoylecgonine (BE) and ecgonine methyl ester (EME). Additionally, there is a general lack of information on the effects of salivary collection conditions on cocaine excretion in saliva. This study documents the profile of cocaine and metabolites in human saliva under stimulated and nonstimulated saliva flow conditions. Saliva samples were obtained periodically from six healthy volunteers who were administered three, equally spaced, single intravenous doses of 25 mg of cocaine during a 6-h test session. On different days, whole saliva was obtained either under nonstimulated or stimulated (sour candy) conditions. The samples were analyzed for cocaine and metabolites by GC/MS. Cocaine, BE, and EME were detected and quantitated in the saliva of all subjects. Cocaine was the predominant analyte identified in all samples. Nonstimulated saliva contained substantially more drug than stimulated samples. The ratio of the area under the curve (AUC) of cocaine in nonstimulated saliva to that of stimulated saliva was variable and ranged from 3.0 to 9.5. The AUC ratios of BE and EME were similar to those observed for cocaine. The lowering of cocaine concentration in saliva in the stimulated flow condition was likely due to an increase in saliva pH associated with increased saliva flow rate; it is known that an increase in saliva pH retards cocaine partitioning into this biological fluid.(ABSTRACT TRUNCATED AT 250 WORDS)

Oral fluid as an alternative matrix to monitor opiate and cocaine use in substance-abuse treatment patients

“…The oral fluid collection device can seriously impact analytical findings in oral fluid drug testing (Kato et al, 1993;O'Neal et al, 2000). Crouch recently suggested in a review of collection methods that drug and volume recovery be determined, since these variables greatly impact the validity of oral fluid test results (Crouch, 2005).…”

“…Cocaine, with or without metabolites, was identified in oral fluid after intravenous (Cone et al, 1988;Cone et al, 1997;Jenkins et al, 1995;Kato et al, 1993;Thompson et al, 1987), smoked Cone et al, 1997;Jenkins et al, 1995), intranasal (Cone, 1993;Cone et al, 1997) and oral (Jufer et al, 2000) administration, as well as, during withdrawal (Cone and Weddington, 1989;Moolchan et al, 2000). The primary analyte was cocaine followed by BE and EME, the major metabolites of cocaine; AEME was identified in oral fluid after smoked cocaine exposure (Cone et al, 1997;Jenkins et al, 1995;Moolchan et al, 2000).…”

“…Disadvantages include variability of salivary flow and pH, and a shorter detection window than urine for active drugs. In addition, specimen collection can have a serious impact on analytical findings and smaller volumes of oral fluid are generally collected (Kato et al, 1993;O'Neal et al, 1999). Furthermore, there are few reports of drug concentration data to guide interpretation of oral fluid test results (Cooper et al, 2005).…”

“…Controlled drug administration studies have investigated the presence and pharmacokinetic characteristics of a number of these drugs in oral fluid (Cone, 1993;Cone et al, 1997;Jenkins et al, 1995;Jufer et al, 2000;Kacinko et al, 2004;Kato et al, 1993;Kim et al, 2002;Kintz et al, 1998;Kopecky et al, 1997;Moolchan et al, 2000;Navarro et al, 2001;O'Neal et al, 1999;Schepers et al, 2003;Skopp et al, 2001;Wang et al, 1994) Furthermore, oral fluid has been successfully applied in criminal justice programs (Yacoubian et al, 2001), workplace (Cone, 2001) and roadside drug testing (DUI) (Peel et al, 1984;Samyn and van Haeren, 2000), but little is known of the usefulness of oral fluid drug monitoring in a population of substance-abuse treatment patients. Schramm et al assessed oral fluid as an alternative matrix for drug testing to serum and urine in volunteers attending a substance abuse treatment program, with self-reported cocaine-use within the previous 24h (Schramm et al, 1993).…”

Can the prevalence of high blood drug concentrations in a population be estimated by analysing oral fluid? A study of tetrahydrocannabinol and amphetamine

“…Physical or chemical stimulation of the production of oral fluid is often used in order to increase the sample volume; however, the concentration of drugs might in these cases be different from concentrations in non-stimulated oral fluid [8,[13][14][15]. The sampling device itself may also affect the analytical results because the recoveries of some drugs might vary from one device to another [7][8].…”