Pharmacokinetics of cocaine and metabolites in human oral fluid and correlation with plasma concentrations after controlled administration

Karl Scheidweiler, Erin Kolbrich-Spargo, Tamsin Kelly, Edward Cone, Allan Barnes, Marilyn Huestis

Research output: Contribution to journalArticle

49 Citations (Scopus)

Abstract

Oral fluid is an attractive alternative matrix for drug testing with a noninvasive and directly observed collection, but there are few controlled cocaine administration studies to guide interpretation. Materials and Methods: While residing on a closed research unit for up to 10 weeks under constant medical supervision, 19 participants were administered 75 mg/70 kg subcutaneous cocaine and 14 received 150 mg/70 kg. The disposition of cocaine, benzoylecgonine (BE), and ecgonine methyl ester (EME) into oral fluid was determined by gas chromatography-mass spectrometry for 0.08 to 48 hours after administration. Results: In oral fluid collected by citric acid candy-stimulated expectoration, cocaine first appeared in oral fluid 0.08 to 0.32 hours after dosing and was rapidly eliminated with half-lives of 1.1 to 3.8 hours. BE and EME were first detected 0.08 to 1.0 hours after dosing with longer half-lives of 3.4 to 13.8 (BE) and 2.4 to 15.5 hours (EME) (P < 0.05). Oral fluid and plasma concentrations were significantly correlated for cocaine, BE, and EME (P < 0.0001). There were no significant differences (P > 0.05) in first and last detection times with the 8-μg/L cutoff proposed by the Substance Abuse and Mental Health Services Administration or the 10-μg/L cutoff from the European initiative, Driving Under the Influence of Drugs, Alcohol and Medicines. Metabolite:cocaine ratios increased after cocaine administration, potentially helpful for interpreting time of last use. Comparison of oral fluid collection through citric acid candy-stimulated expectoration, citric acid-treated Salivette, and neutral cotton Salivette devices did not reveal significant differences between devices for areas under the curve for cocaine, BE, or EME (P > 0.05). Discussion and Conclusion: These results provide additional evidence for interpreting cocaine and metabolite concentrations in oral fluid and oral fluid's usefulness as an alternative matrix for drug testing
Original languageEnglish
Pages (from-to)628-637
Number of pages10
JournalTherapeutic Drug Monitoring
Volume32
Issue number5
DOIs
Publication statusPublished - 2010

Fingerprint

Cocaine
Pharmacokinetics
Citric Acid
Candy
Health Services Misuse
Health Services Administration
Pharmaceutical Preparations
Equipment and Supplies
Mental Health Services
Gas Chromatography-Mass Spectrometry
Area Under Curve
Substance-Related Disorders
Alcohols
ecgonine methyl ester
benzoylecgonine
Research

Cite this

Scheidweiler, Karl ; Kolbrich-Spargo, Erin ; Kelly, Tamsin ; Cone, Edward ; Barnes, Allan ; Huestis, Marilyn. / Pharmacokinetics of cocaine and metabolites in human oral fluid and correlation with plasma concentrations after controlled administration. In: Therapeutic Drug Monitoring. 2010 ; Vol. 32, No. 5. pp. 628-637.
@article{68f280d9635b4ff2b61595d822815d60,
title = "Pharmacokinetics of cocaine and metabolites in human oral fluid and correlation with plasma concentrations after controlled administration",
abstract = "Oral fluid is an attractive alternative matrix for drug testing with a noninvasive and directly observed collection, but there are few controlled cocaine administration studies to guide interpretation. Materials and Methods: While residing on a closed research unit for up to 10 weeks under constant medical supervision, 19 participants were administered 75 mg/70 kg subcutaneous cocaine and 14 received 150 mg/70 kg. The disposition of cocaine, benzoylecgonine (BE), and ecgonine methyl ester (EME) into oral fluid was determined by gas chromatography-mass spectrometry for 0.08 to 48 hours after administration. Results: In oral fluid collected by citric acid candy-stimulated expectoration, cocaine first appeared in oral fluid 0.08 to 0.32 hours after dosing and was rapidly eliminated with half-lives of 1.1 to 3.8 hours. BE and EME were first detected 0.08 to 1.0 hours after dosing with longer half-lives of 3.4 to 13.8 (BE) and 2.4 to 15.5 hours (EME) (P < 0.05). Oral fluid and plasma concentrations were significantly correlated for cocaine, BE, and EME (P < 0.0001). There were no significant differences (P > 0.05) in first and last detection times with the 8-μg/L cutoff proposed by the Substance Abuse and Mental Health Services Administration or the 10-μg/L cutoff from the European initiative, Driving Under the Influence of Drugs, Alcohol and Medicines. Metabolite:cocaine ratios increased after cocaine administration, potentially helpful for interpreting time of last use. Comparison of oral fluid collection through citric acid candy-stimulated expectoration, citric acid-treated Salivette, and neutral cotton Salivette devices did not reveal significant differences between devices for areas under the curve for cocaine, BE, or EME (P > 0.05). Discussion and Conclusion: These results provide additional evidence for interpreting cocaine and metabolite concentrations in oral fluid and oral fluid's usefulness as an alternative matrix for drug testing",
author = "Karl Scheidweiler and Erin Kolbrich-Spargo and Tamsin Kelly and Edward Cone and Allan Barnes and Marilyn Huestis",
year = "2010",
doi = "10.1097/FTD.0b013e3181f2b729",
language = "English",
volume = "32",
pages = "628--637",
journal = "Therapeutic Drug Monitoring",
issn = "0163-4356",
publisher = "Lippincott Williams and Wilkins",
number = "5",

}

Pharmacokinetics of cocaine and metabolites in human oral fluid and correlation with plasma concentrations after controlled administration. / Scheidweiler, Karl; Kolbrich-Spargo, Erin; Kelly, Tamsin; Cone, Edward; Barnes, Allan; Huestis, Marilyn.

In: Therapeutic Drug Monitoring, Vol. 32, No. 5, 2010, p. 628-637.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Pharmacokinetics of cocaine and metabolites in human oral fluid and correlation with plasma concentrations after controlled administration

AU - Scheidweiler, Karl

AU - Kolbrich-Spargo, Erin

AU - Kelly, Tamsin

AU - Cone, Edward

AU - Barnes, Allan

AU - Huestis, Marilyn

PY - 2010

Y1 - 2010

N2 - Oral fluid is an attractive alternative matrix for drug testing with a noninvasive and directly observed collection, but there are few controlled cocaine administration studies to guide interpretation. Materials and Methods: While residing on a closed research unit for up to 10 weeks under constant medical supervision, 19 participants were administered 75 mg/70 kg subcutaneous cocaine and 14 received 150 mg/70 kg. The disposition of cocaine, benzoylecgonine (BE), and ecgonine methyl ester (EME) into oral fluid was determined by gas chromatography-mass spectrometry for 0.08 to 48 hours after administration. Results: In oral fluid collected by citric acid candy-stimulated expectoration, cocaine first appeared in oral fluid 0.08 to 0.32 hours after dosing and was rapidly eliminated with half-lives of 1.1 to 3.8 hours. BE and EME were first detected 0.08 to 1.0 hours after dosing with longer half-lives of 3.4 to 13.8 (BE) and 2.4 to 15.5 hours (EME) (P < 0.05). Oral fluid and plasma concentrations were significantly correlated for cocaine, BE, and EME (P < 0.0001). There were no significant differences (P > 0.05) in first and last detection times with the 8-μg/L cutoff proposed by the Substance Abuse and Mental Health Services Administration or the 10-μg/L cutoff from the European initiative, Driving Under the Influence of Drugs, Alcohol and Medicines. Metabolite:cocaine ratios increased after cocaine administration, potentially helpful for interpreting time of last use. Comparison of oral fluid collection through citric acid candy-stimulated expectoration, citric acid-treated Salivette, and neutral cotton Salivette devices did not reveal significant differences between devices for areas under the curve for cocaine, BE, or EME (P > 0.05). Discussion and Conclusion: These results provide additional evidence for interpreting cocaine and metabolite concentrations in oral fluid and oral fluid's usefulness as an alternative matrix for drug testing

AB - Oral fluid is an attractive alternative matrix for drug testing with a noninvasive and directly observed collection, but there are few controlled cocaine administration studies to guide interpretation. Materials and Methods: While residing on a closed research unit for up to 10 weeks under constant medical supervision, 19 participants were administered 75 mg/70 kg subcutaneous cocaine and 14 received 150 mg/70 kg. The disposition of cocaine, benzoylecgonine (BE), and ecgonine methyl ester (EME) into oral fluid was determined by gas chromatography-mass spectrometry for 0.08 to 48 hours after administration. Results: In oral fluid collected by citric acid candy-stimulated expectoration, cocaine first appeared in oral fluid 0.08 to 0.32 hours after dosing and was rapidly eliminated with half-lives of 1.1 to 3.8 hours. BE and EME were first detected 0.08 to 1.0 hours after dosing with longer half-lives of 3.4 to 13.8 (BE) and 2.4 to 15.5 hours (EME) (P < 0.05). Oral fluid and plasma concentrations were significantly correlated for cocaine, BE, and EME (P < 0.0001). There were no significant differences (P > 0.05) in first and last detection times with the 8-μg/L cutoff proposed by the Substance Abuse and Mental Health Services Administration or the 10-μg/L cutoff from the European initiative, Driving Under the Influence of Drugs, Alcohol and Medicines. Metabolite:cocaine ratios increased after cocaine administration, potentially helpful for interpreting time of last use. Comparison of oral fluid collection through citric acid candy-stimulated expectoration, citric acid-treated Salivette, and neutral cotton Salivette devices did not reveal significant differences between devices for areas under the curve for cocaine, BE, or EME (P > 0.05). Discussion and Conclusion: These results provide additional evidence for interpreting cocaine and metabolite concentrations in oral fluid and oral fluid's usefulness as an alternative matrix for drug testing

U2 - 10.1097/FTD.0b013e3181f2b729

DO - 10.1097/FTD.0b013e3181f2b729

M3 - Article

VL - 32

SP - 628

EP - 637

JO - Therapeutic Drug Monitoring

JF - Therapeutic Drug Monitoring

SN - 0163-4356

IS - 5

ER -