Abstract
Objective:
We studied the dose-proportion and time-course relationships for the incorporation of codeine into human hair after the administration of three different doses.
Subjects:
Male volunteers, with dark hair, were given oral codeine either as a single dose of 60 mg (n = 7) or 120 mg (n = 12), or as multiple doses of 30 mg 3 times daily for 5 days (n = 7) (450 mg total dose).
Methods:
Blood and urine were collected for various times for up to 72 h after dosing. Scalp hair was collected initially by plucking (up to 4 weeks) and later by cutting for up to 10 weeks. Plasma, urine, proximal 1 cm of hair and distal hair were each analyzed for codeine and its metabolites by positive-ion chemical ionization ion trap gas chromatography/mass spectrometry.
Results:
Codeine was detected in the proximal 1 cm of hair within 30 min of an oral 120-mg dose. Codeine was not detected in the distal hair segment until 3 weeks after receiving a dose of codeine. Codeine was detected in distal hair segments for at least 10 weeks at 30 pg mg−1 hair following a single 120 mg codeine dose and at 90 pg mg−1 hair following 30 mg codeine 3 times a day for 5 days. Morphine or the glucuronides of codeine or morphine were not detected in the hair specimens of these subjects.
Conclusion:
Codeine is rapidly distributed into the germanitive elements of hair in a dose-proportional manner. A portion of the codeine remains bound as the hair grows and can be detected in distal hair for up to 10 weeks after a single dose.
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Received: 26 July 1995/Accepted in revised form: 20 October 1995
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Rollins, D., Wilkins, D. & Krueger, G. Codeine disposition in human hair after single and multiple doses. E J Clin Pharmacol 50, 391–397 (1996). https://doi.org/10.1007/s002280050129
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DOI: https://doi.org/10.1007/s002280050129