Showing posts with label Blood Lipid-Lowering Agent (Fibric Acid Derivative). Show all posts
Showing posts with label Blood Lipid-Lowering Agent (Fibric Acid Derivative). Show all posts

Probucol (Lorelco)

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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.

 

Clofibrate (Atromid-S) mnemonic

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Name: Clofibrate (Atromid-S) mnemonic

Class: Blood Lipid-Lowering Agent (Fibric Acid Derivative)

Mechanism: ­ catabolism of VLDL, in part 2° to ­ activity of lipoprotein lipase in adipose tissue. Moderate ¯ in TG & VLDL. Zero-mild ¯ in cholesterol. Zero-mild ­ in HDL. Mild ­ or ¯ in LDL.

Absorption:

Dist.:

Metabolism.: Glucuronide conjugation.

Excretion, t½: Renal excretion.

Toxicity/S.E.s: Generally well tolerated. Gallstones, nausea, diarrhea, abdominal discomfort. Displaces weakly acidic drugs (T3, T4, warfarin, phenytoin) from plasma proteins. Binds cholestyramine.

Utility: Treat severe hyperlipidemia IV refractory to gemfibrozil or niacin.

Special Features: Does not appear to decrease frequency of CHD-related incidents.

 

Gemfibrozil (Lopid) mnemonic

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Name: Gemfibrozil (Lopid) mnemonic

Class: Blood Lipid-Lowering Agent (Fibric Acid Derivative)

Mechanism: ­ catabolism of VLDL, in part 2° to ­ activity of lipoprotein lipase in adipose tissue. Moderate ¯ in TG & VLDL. Mild ¯ in LDL and cholesterol. Moderate ­ in HDL.

Absorption:

Dist.:

Metabolism.: Glucuronide conjugation.

Excretion, t½: Renal excretion.

Toxicity/S.E.s: Generally well tolerated. GI distress, rash, musculoskeletal pain, blurred vision, anemia, leukopenia, gallstones. Adjust dose in pts. w/renal insufficiency.

Utility: DOC for hyperlipidemia III. Better tolerated than niacin for type IV, although less effective. Decreases frequency of CHD-related incidents.

Special Features: