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Published:
Journal of Analytical Toxicology,
ISSN 0146-4760,
Volume 30, Number 8, October 2006,
pp.501-510
Major and Minor Metabolites of Cocaine in Human Plasma
following Controlled Subcutaneous Cocaine Administration
Erin A. Kolbrich[1], Allan J. Barnes[1], David A. Gorelick[2], Susan
J. Boyd[3], Edward J. Cone[4], and Marilyn A. Huestis[1],
[1]Chemistry and Drug Metabolism, IRP, NIDA, NIH, 5500 Nathan Shock Drive, Baltimore,
Maryland 21224;
[2]Office of the Scientific Director, IRP, NIDA, NIH, 5500 Nathan Shock Drive,
Baltimore, Maryland 21224;
[3]University of Maryland School of Medicine, Baltimore, Maryland 21201; and
[4]Johns Hopkins School of Medicine, Baltimore, Maryland 21205
Cocaine is rapidly metabolized to major metabolites, benzoylecgonine
(BE) and ecgonine methyl ester (EME), and minor metabolites, norcocaine, p-hydroxycocaine,
m-hydroxycocaine, p-hydroxybenzoylecgonine (pOHBE), and m-hydroxybenzoylecgonine.
This IRB-approved study examined cocaine and metabolite plasma concentrations
in 18 healthy humans who provided written informed consent to receive low (75
mg/70 kg) and high (150 mg/70 kg) subcutaneous cocaine hydrochloride doses.
Plasma specimens, collected prior to and up to 48 h after dosing, were analyzed
by gas chromatography–mass spectrometry (2.5 ng/mL limits of quantification).
Cocaine was detected within 5 min, with mean ± SE peak concentrations
of 300.4 ± 24.6 ng/mL (low) and 639.1 ± 56.8 ng/mL (high) 30–40
min after dosing. BE and EME generally were first detected in plasma 5–15
min post-dose; 2–4 h after dosing, BE and EME reached mean maximum concentrations
of 321.3 ± 18.4 (low) and 614.7 ± 46.0 ng/mL (high) and 47.4 ±
3.0 (low) and 124.4 ± 18.2 ng/mL (high), respectively. Times of last
detection were BE > EME > cocaine. Minor metabolites were detected much
less frequently for up to 32 h, with peak concentrations ≤ 18 ng/mL for
all analytes except pOHBE (up to 57.7 ng/mL). These data improve our knowledge
of the pharmacokinetics of cocaine and its major and minor metabolites in plasma
following controlled subcutaneous cocaine administration.
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