The relationship between the acetylator and the sparteine hydroxylation polymorphisms.

Abstract

SUMMARY 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. ResultsThe acetylator phenotyping information is shown in

Genetic Polymorphism of NAT2 Metabolizing Enzymes on Phenytoin Pharmacokinetics in Indian Epileptic Patients Developing Toxicity

“…N ‐acetylation polymorphism causes interindividual variations in the biotransformation of various drugs, procarcinogens, and other xenobiotics with a primary aromatic or hydrazine structure [5]. The drugs sulfadimidine, hydralazine, dapsone, procainamide, sulfapyridine, nitrazepam, and caffeine are metabolized by NAT enzyme [6]. Hereditary differences in N ‐acetylation activity among individuals and in populations of diverse racio‐geographic origin, have led to the phenotype classification of humans as rapid and slow acetylators [7].…”

Rol de la farmacogenómica en el régimen de tratamiento de tuberculosis

“…Es una enzima detoxificante expresada principalmente en el hígado. Acetiliza varias drogas actualmente en el mercado, incluyendo, INH, sulfadmidina, hidralazina, dapsona, procaina amida, sulfapiridina y nitrazepam (23) . El gen NAT2, el cual contiene un solo exon de 870 pares de bases, codifica 290 aminoácidos, y se conocen 16 polimorfismos de nucleótido único (SNP) y una deleción de un par de bases, los cuales han sido asociados con una alteración en la actividad metabólica (24)(25)(26) .…”

NAT2 gene polymorphism

“…It is implicated in the modification of risk factors in the development of malignancies involving the urinary bladder, colorectal region, breast, prostate, lungs and the head and neck region. It is also shown to be involved in the development of Alzheimer's disease, schizophrenia, diabetes, cataract and parkinsonism 1 2 3 .…”

“…A Japanese study also reported good concordance between NAT2 genotype and metabolism of INH in patients with tuberculosis 11 . However, in patients with AIDS there was discordance between acetylator genotype and phenotype of NAT 2 as measured by caffeine as a probe drug 12 .…”