The acetylation polymorphism is one of the most common inherited variations in the biotransformation of drugs and chemicals. Its association with drug toxicity and increased risk of developing certain diseases and certain types of chemically induced cancers has made it one of the oldest and best studied examples of pharmacogenetic conditions. N-Acetylation of sulfamethazine was studied in 74 unrelated healthy Iranian volunteers. The frequency of slow acetylators, determined by using free and total plasma sulfamethazine concentrations, was 78.4%. The mean acetylation ratio was 19.48% for slow acetylators, and the frequency of the recessive allele controlling slow acetylation was found to be 0.88. This percentage is similar to that observed in various Arab countries and higher than that observed in Europeans.