Answer to Question #23606 in Organic Chemistry for BIRHANU SIMON

Question

Which one is more susceptible: slow or fast acetylator by Isoniazid drug side effect?

Answer 1

Enzymatic acylation of the antitubercular isoniazid (INH) by N-acetyl transferases reduces the therapeutic effectiveness of the drug. Because it represents a major metabolic pathway for INH in human beings, such acetylation has serious consequences for tuberculosis treatment regimens. Among patients in whom this process is efficient, the rapid acetylators, the resultant chronic underdosing of INH may give rise to the development of resistance, as well as inadequate therapy.
fast acetylators = drug resistance
slow acetylators = hepatotoxicity
Isoniazid causes hepatitis in fast acetylators (due to access drug metabolites), and peripheral neuropathy in slow acetylators (due to higher drug concentration).