Effects of
The next most common group of medications known to be substrates of CYP2D6 include two cardiovascular drug classes
Cytochrome P450 (CYP450) are a group of enzymes encoded by the P450 genes and responsible for the metabolism of most drugs seen in clinical practice
Propranolol, used to treat high blood pressure and irregular heart rate, is mainly metabolized by cytochrome P450 2D6 (CYP2D6) to 4-hydroxypropranolol (4
Poor metabolizers of the CYP2D6 C/T188
Keep in mind that many drugs are metabolized by more than one CYP450 enzyme, and CYP2D6 may represent only one pathway
The clinical importance of this “dual metabolism Abstract Cytochrome P450 2D6 is a major drug-metabolising enzyme with a wide substrate range
Of the total 57 isozymes discovered to date, 6 of these are responsible for 90%
Drugs may be metabolized by only one CYP450 enzyme (e
Human cytochrome P450 enzyme 1A2 (CYP1A2) is one of the most important cytochrome P450 (CYP) enzymes in the liver, accounting for 13% to 15% of hepatic CYP enzymes
Co-administration of SSRIs with medications that are substrates of CYP2D6 will increase the serum concentrations of those medications, including beta-blockers such as labetalol, metoprolol, propranolol, and timolol
Avoids CYP drug interactions
The substrate employed was propranolol because it is well metabolized by CYP2D6
8, respectively
Zanger UM, Raimundo S, Eichelbaum M (2004) Cytochrome P450 2D6: overview and update on pharmacology, genetics, biochemistry
Cytochrome P450 2D6 (CYP2D6) The CYP 2D6 represents a small percentage of all hepatic cytochrome P 450s (Ingelman-Sundberg, 2005)
Classification
, CYP1A, CYP2D) and are then differentiated by a number for the isoform or individual enzyme (e