Name: Probucol (Lorelco)
Class: Blood Lipid-Lowering Agent (Fibric Acid Derivative)
Mechanism: Stim. LDL clearance by non-receptor pathways. May reduce risk of atherogenesis w/o altering serum cholesterol levels. May block oxidation of LDL. Moderate ¯ in cholesterol, LDL, & HDL. No effect on TG or VLDL.
Absorption:
Dist.: Stored in fat.
Metabolism.:
Excretion, t½:
Toxicity/S.E.s: Generally very well tolerated (2-6% incidence). Flatulence, n/v/d, abd. pain, headache, rash. C/i in monkeys (cardiac arrhythmias). Stored in fat. \ E advised to wait 6 mo. after last dose before becoming pregnant.
Utility: Treat hyperlipidemia IIA/IIB, but prob. not drug o’ first choice. May be useful for homozygous familial hypercholesterolemia (IIA). May cause regression of xanthomas.
Special Features: ¯ in LDL takes 1-3 mo., but some pts. don’t respond. Does not further reduce LDL when used w/lovastatin.