Pharmacology: Mechanism of Action: Metoprolol is readily and completely absorbed from the gastrointestinal tract but is subject to considerable first-pass metabolism, with a bioavailability of about 50%. Peak plasma concentrations vary widely and occur about 1.5 to 2 hours after a single oral dose. It is moderately lipid-soluble. Metoprolol is widely distributed; it crosses the blood brain barrier and the placenta, and is distributed into breast milk. It is about 12% bound to plasma protein. It is extensively metabolized in the liver, mainly by the cytochrome P450 isoenzyme CYP2D6. The metabolites are excreted in the urine with only small amounts of unchanged metoprolol. The half-life of metoprolol in fast hydroxylators is stated to be 3 to 4 hours, whereas in poor hydroxylators it is about 7 hours.