SOFT - TIAFT 1998 Scientific Session 1 Wednesday October 7, 1998
Click Picture Amanda J. Jenkins, and Edward J. Cone

Addiction Research Center, IRP, NIDA, NIH, Baltimore, MD 21224, U.S.A.

Clinical data regarding the disposition of heroin and metabolites after oral heroin administration is limited to case reports of overdoses by "body packers". We conducted a controlled clinical study during which nine healthy male volunteers with a history of heroin use were administered 10 mg heroin hydrochloride in the form of a gelatin capsule. Blood and saliva specimens were collected prior to drug administration and periodically thereafter up to 24 hours. All urine specimens were collected. Specimens were analyzed by solid phase extraction followed by gas chromatography/mass spectrometry for heroin, 6-acetylmorphine and morphine. The assay had a limit of quantitation (LOQ) of 1 ng/ml for each analyte. The total morphine concentration also was measured in the urine specimens.

Heroin and 6-acetylmorphine were not detected in blood after ingestion. Morphine was first detected 7.5 to 30 minutes after drug administration with peak concentrations ranging from 2.2-15 ng/ml (mean=7.7 ng/ml, N=9), achieved 7.5 minutes to 4 hours later. Morphine concentrations declined thereafter, reaching the assay LOQ by 1-12 hours.

No analytes were detected in saliva after oral heroin administration.

Heroin and 6-acetylmorphine were not detected in urine. Morphine was detected in the first void after drug administration for each subject (Mean time of void= 2.35 h, N=9). Peak free morphine concentrations ranging from 172-491 ng/ml were achieved at an average of 4.2 hours after drug administration. Peak levels typically occurred in the 1st-3rd voids. Peak total morphine concentrations ranging from 4317-12580 ng/ml were achieved at an average of 4.6 hours after drug administration. The time to the first negative sample for free morphine averaged 33.2 hours (Range= 21.5-54.7 h) with total morphine being detectable in 6/9 subjects at the last collected void at 68-75 hours. The time to the first total morphine negative for the remaining 3 subjects ranged between 53.1-77.9 hours.

These data indicate that after low dose administration of heroin by the oral route, heroin and 6-acetylmorphine are not detected in blood, saliva or urine. However, measurable concentrations of free and total morphine are excreted in the urine for approximately 30 and 53 hours, respectively.

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