Abstract
Endogenous and exogenous chemicals alter the expression and activity of enzymes responsible for biotransformation of drugs. Expression of microsomal Cytochrome P (CYP) 450 is a major source of variation in pharmacokinetics of drugs. CYP450 is the superfamily of drug-metabolizing enzymes (DMEs) primarily involved in phase I reactions, which render drugs more polar and enhance their excretion. Various factors alter the expression and activity of CYP including genetic factors and hormones. Hormones (i.e., steroid, thyroid, glucocorticoids, reproductive, and growth hormones) have a probable effect on enzyme inhibition and/or activation. The most abundant polymorphic forms of CYPs are CYP3A4, CYP2C9, CYP2C8, CYP2E1, and CYP1A2. However, the most frequently regulated isoforms by hormones are CYP3A and CYP2E. During the course of metabolic diseases, CYP expression alters due to endocrine dysregulation in conditions such as pregnancy, diabetes mellitus, and malnutrition. This chapter overviews the effect of hormones on DMEs. However, data ascertaining the impact of hormones on DMEs in human are limited. Future controlled and well-designed studies are the need of time to clarify the association of CYP enzymes with hormones. This chapter summarizes the regulation of DMEs expressions by hormones that might further help in foreseeing and preventing the untoward effects of the drugs metabolized via corresponding DMEs.
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