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Sulfamethazine (syn, sulfadimidine) is inactivated by conversion to its N-acetyl derivative. Individuals are phenotyped as either "rapid" or "slow" acetylators. We have tested the validity of this theory in a Nigerian population. The frequency distribution histograms of the percentage acetylsulfamethazine in urine and serum were found to be bimodal, indicating the existence of a genetic polymorphism as observed by earlier workers. A plot of the percentage of the drug acetylated in serum against that in urine of the same individual results in a satisfactory separation of the rapid and slow acetylator phenotypes. An incidence of the slow acetylator phenotype of 41% was observed in the Nigerian population tested. How this observation fits into the hypothesis that the slow frequency of the allele increases from the Arctic Circle toward the Equator is discussed.

Thirty-eight healthy white British Caucasian subjects were hydroxylator phenotyped with sparteine and acetylator phenotyped with sulphadimidine. The results showed that there was no significant difference in the mean sparteine metabolic ratio between eight rapid acetylator extensive hydroxylators and 27 slow acetylator extensive hydroxylators.

There is an association between exposure to aromatic amines and the development of bladder cancer. Aromatic amines such as are known to occur in tobacco smoke are polymorphically acetylated. One hundred bladder cancer patients have been acetylator phenotyped. Only three of them were non-smokers at the time of diagnosis. This new series, together with four previous series (each with its own control), have been statistically analysed together. The results show a significant association between the slow acetylator phenotype and bladder cancer. The slow acetylator phenotype is associated about 39% more with bladder cancer than is the rapid acetylator phenotype. This association can be interpreted in one of two ways: (1) rapid acetylators may be protected against developing bladder cancer because they are better able to render amines non-carcinogenic by acetylation, or (2) slow acetylators have greater survival with bladder cancer than rapid acetylators. Further evidence will be required to differentiate between these alternatives.