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Agents Used in Dyslipidemia (AGENTS UNDER DEVELOPMENT (CETP INHIBITION:…
Agents Used in Dyslipidemia
INHIBITORS OF INTESTINAL STEROL ABSORPTION
Ezetimibe inhibits intestinal absorption
TREATMENT WITH DRUG COMBINATIONS
AGENTS UNDER DEVELOPMENT
CETP INHIBITION: Cholesteryl ester transfer protein (CETP) transfers cholesteryl esters from HDL to TG rich lipoprs; accumulation of large HDL particles does not have anticipated cardioprotective effect. Thus far no drug (eg, torcetrapib anacetrapib) in this class has been approved
AMP KINASE ACTIVATION
CYCLODEXTRINS
COMPETITIVE INHIBITORS OF HMG-COA REDUCTASE (REDUCTASE INHIBITORS: “STATINS”)
examples: lovastatin, atorvastatin, simvastatin
Mechanism of Action: HMG-CoA reductase mediates 1st step in sterol biosynthesis (of mevalonate); reductase inhibitors clearly induce an :arrow_up: in high-affinity LDL Rs--> :arrow_down: LDL; Modest :arrow _down: in plasma TGs + small :arrow_up: in HDL also occur.
Toxicity: Minor :arrow_up: in CK activity in plasma observed in some patients; Rarely, patients may have marked elevations in CK activity, often accompanied by generalized discomfort or weakness in skeletal muscles; Myopathy
FIBRIC ACID DERIVATIVES (FIBRATES)
Examples: Gemfibrozil and fenofibrate
Mechanism of Action: :arrow_up: lipolysis of lipoprotein TG via LPL; reductions of LDL; HDL cholesterol :arrow_up: moderately
Toxicity: skin, GI
NIACIN (NICOTINIC ACID)
Mechanism of Action: Niacin inhibits VLDL secretion--> :arrow_down: production of LDL; also :arrow_up: clearance of VLDL via the LPL pathway contributes to :arrow_down: TGs; :arrow_up: HDL levels
Toxicity: skin
ANTISENSE INHIBITION OF APO B-100 SYNTHESIS
PCSK9 INHIBITION
INHIBITION OF MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN
Microsomal TG transfer pr (MTP) plays an essential role in addition of TGs to nascent VLDL in liver, and to CMs in intestine. Its inhibition :arrow_down: + VLDL secretion and consequently accumulation of LDL in plasma
lomitapide: causes accumulation of TGs in liver in some individuals. Elevations in transaminases can occur. given orally
BILE ACID–BINDING RESINS
bind bile acids in intestinal lumen + prevent their reabsorption. The resin itself is not absorbed.
constipation and bloating; Heartburn and diarrhea; Malabsorption of vit K; Malabsorption of folic acid; Increased formation of gallstones
Colestipol, cholestyramine, and
colesevelam
are useful only for isolated increases in LDL