PubMed · 13102643
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K B HANSEN. 1953-08-20. [Codeine administration to infants].. https://pubmed.ncbi.nlm.nih.gov/13102643/
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Identification of 6-acetylmorphine, a specific metabolite of heroin, is considered to be definitive evidence of heroin use. Although 6-acetylmorphine has been identified in oral fluid following controlled heroin administration, no prevalence data is available for oral fluid specimens collected in the workplace. We evaluated the prevalence of positive test results for 6-acetylmorphine in 77,218 oral fluid specimens collected over a 10-month period (January-October 2001) from private workplace testing programs. Specimens were analyzed by Intercept immunoassay (cutoff concentration=30 ng/ml) and confirmed by GC-MS-MS (cutoff concentrations=30 ng/ml for morphine and codeine, and 3 ng/ml for 6-acetylmorphine). Only morphine-positive oral fluid specimens were tested by GC-MS-MS for 6-acetylmorphine. A total of 48 confirmed positive morphine results were identified. An additional 107 specimens were confirmed for codeine only. Of the 48 morphine-positive specimens, 32 (66.7%) specimens were positive for 6-acetylmorphine. Mean concentrations (+/-S.E.M.) of morphine, 6-acetylmorphine and codeine in the 32 specimens were 755+/-201, 416+/-168 and 196+/-36 ng/ml, respectively. Concentrations of 6-acetylmorphine in oral fluid ranged from 3 to 4095 ng/ml. The mean ratio (+/-S.E.M.) of 6-acetylmorphine/morphine was 0.33+/-0.06. It is suggested that, based on controlled dose studies of heroin administration, ratios >1 of 6-acetylmorphine/morphine in oral fluid are consistent with heroin use within the last hour before specimen collection. The confirmation of 6-acetylmorphine in 66.7% of morphine-positive oral fluid specimens indicates that oral fluid testing for opioids may offer advantages over urine in workplace drug testing programs and in testing drugged drivers for recent heroin use.
UDP-glucuronosyltransferase 2B7 (UGT2B7) is involved in the glucuronidation of a wide array of clinically important drugs and endogenous compounds in humans. The aim of this study was to identify an isoform-selective probe substrate that could be used to investigate genetic and environmental influences on glucuronidation mediated by UGT2B7. Three potential probe substrates [3'-azido-3'-deoxythymidine (AZT), morphine, and codeine], were evaluated using recombinant UGTs and human liver microsomes (HLMs; n = 54). Of 11 different UGTs screened, UGT2B7 was the principal isoform mediating AZT glucuronidation, morphine-3-glucuronidation, and morphine-6-glucuronidation. Codeine was glucuronidated equally well by UGT2B4 and UGT2B7. Enzyme kinetic analysis of these activities typically showed higher apparent Km values for HLMs (pooled and individual) compared with UGT2B7. This difference was least (less than 2-fold higher Km) for AZT glucuronidation and greatest (3- to 6-fold higher Km) for codeine glucuronidation. Microsomal UGT2B7 protein content correlated well with AZT glucuronidation (rs = 0.77), to a lesser extent with morphine-3-glucuronidation (rs = 0.50) and morphine-6-glucuronidation (rs = 0.51), but very weakly with codeine glucuronidation (rs = 0.33). Livers were also genotyped for the UGT2B7*2 (H268Y) polymorphism. No effect of genotype on microsomal glucuronidation or UGT2B7 protein content was observed. In conclusion, although both AZT and morphine can serve as in vitro probe substrates for UGT2B7, AZT appears to be more selective than morphine. Codeine is not a useful UGT2B7 probe substrate because of significant glucuronidation by UGT2B4. The UGT2B7*2 polymorphism is not a determinant of glucuronidation of AZT, morphine, or codeine in HLMs.