 Lofexidine is extensively metabolized by the liver, and primarily cleared by the kidney.It is 80-90% plasma protein bound.Lofexidine exists as a solid at room temperature, with a melting point of 127 degrees C. The pair of ortho chlorine (Cl−) atoms on the phenyl ring are necessary for lofexidine's agonism at the α2a adrenergic receptor subtype; removal of either chlorine atom results in antagonism at the receptor.