The AmpliChip CYP450 test (Roche Molecular Systems, Pleasanton CA) is a drug metabolizing enzyme (DME) genotyping system that detects genetic variations (polymorphisms) in two CYP450 genes, CYP2D6 and CYP2C19, using deoxyribonucleic acid (DNA) extracted from patients’ blood. It is used with the GeneChip System 3000Dx microarray platform developed by Affymetrix (Santa Clara CA). The test is cond...

Countries in Africa have a high burden of communicable disease, and are experiencing an increase in non-communicable diseases due to the effects of globalization, industrialization and urbanization. The costs incurred through adverse drug reactions and non-responsiveness to therapy further aggravate the situation, and the application of pharmacogenetic principles is likely to provide some relie...

Cocktail method was used to evaluate the influence of ketamine on the activities of CYP450 isoforms CYP1A2, CYP2D6, CYP3A4, CYP2C19, CYP2C9 and CYP2B6, which were reflected by the changes of pharmacokinetic parameters of six specific probe drugs phenacetin, metroprolol, midazolam, omeprazole, tolbutamide and bupropion, respectively. The experimental rats were randomly divided into two group, co...

The incidence of polypharmacy-which can result in drug-drug interactions-has increased in recent years. Drug-metabolizing enzymes and drug transporters are important polypharmacy modulators. In this study, the effects of bosentan and rifampin on the expression and activities of organic anion-transporting peptide (OATP) and cytochrome P450 (CYP450) 2C9 and CYP3A4 were investigated in vitro. HEK2...

Understanding the mechanisms of drug metabolism and interactions can help to prevent side-effects. Not only drug interactions, environmental factors, disease processes and ageing are factors in the inter-individual metabolic capacity variance but also genetic factors probably play an important role, as is illustrated in the case presented. Besides therapeutic drug monitoring, genotyping some im...

Recent sequencing of amphioxus and sea urchin genomes has provided important data for understanding the origins of enzymes that synthesize adrenal and sex steroids and the receptors that mediate physiological response to these vertebrate steroids. Phylogenetic analyses reveal that CYP11A and CYP19, which are involved in the synthesis of adrenal and sex steroids, first appear in the common ances...

Androgens are transformed into aromatic estrogens by CYP450 aromatase in a three-step reaction consuming three equivalents of oxygen and three equivalents of NADPH. Estrogens are substrates for nuclear estrogen receptors (ERs) and play a key role in estrogen-dependent tumour cell formation and proliferation. Natural phytoestrogens are proved to be competitive inhibitors of aromatase enzyme at I...

Antiretrovirals are prone to drug-drug and drug-food interactions that can result in subtherapeutic or supratherapeutic concentrations. Interactions between antiretrovirals and medications for other diseases are common due to shared metabolism through cytochrome P450 (CYP450) and uridine diphosphate glucuronosyltransferase (UGT) enzymes and transport by membrane proteins (e.g., p-glycoprotein, ...

In this study, Channa punctatus was treated with sub-lethal concentration of cypermethrin (6.6 μg/L) for 5, 10 and 15 days and its effect on total CYP 450 and the activity of hepatic CYP450 isoforms measured. Total CYP450 content and CYP1A mediated EROD activity was significantly induced (p<0.05) in all three treated groups compared to control whereas only 15 days treated group showed significa...

Epilepsy is a common neurological disorder worldwide and anti-epileptic drugs (AEDs) are always the first choice for treatment. However, more than 50% of patients with epilepsy who take AEDs have reported bone abnormalities. Cytochrome P450 (CYP450) isoenzymes are induced by AEDs, especially the classical AEDs, such as benzodiazepines (BZDs), carbamazepine (CBZ), phenytoin (PT), phenobarbital (...