Lipid lowering Flashcards
Classes of drug
Niacin, fibrates, Bile-acid binding resins, HMG-CoA reductase inhibitor, inhibitors of intestinal sterol absorption
MoA of Niacin
Increase HDL levels
Inhibit lipolysis in adipose tissue to decrease TAG in VLDL, cholesterol in VLDL
Decrease fibrinogen, increase t-PA to reverse thrombosis a/w chol & atherosclerosis
SE of niacin
Intense cutaneous flush, pruritus, hyperuricaemia & gout
Fibrates
Gemfibrozil, fenofibrate, clofibrate
MoA of fibrates
Ligand for PPAR-a –> increase LPL activity and decrease plasma TAG
Decrease VLDL secretion by liver
SE of fibrates
Nausea, rash, gallstones, myositis
Bile-acid binding resins
Cholestyramine, colestipol
MoA of bile-acid binding resin
Bind to bile acids & salts –> increase excretion of bile acids in faeces causes increase hepatic conversion of cholesterol to bile salts –> decrease intracellular cholesterol
Increase hepatic uptake of LDL
SE of bile-acid binding resin
Constipation, nausea, flatus, decrease absorption of fat-soluble vitamins (ADEK)
HMG-CoA reductase inhibitors
“statins” — Lovastatin, simvastatin
MoA of statins
Inhibit HMG-CoA reductase which is the rate-limiting step in cholesterol synthesis
also increase LDL receptors to increase internalization of circulating LDL
SE of statin
Myopathy, rhabdomyolysis, abnormal liver function
Contraindications of statin
Pregnancy, nursing mothers, children & teens (developing CNS)
Use of statins
Give @ night as cholesterol synthesis is highest in fasting state
Inhibitors of intestinal sterol absorption
Ezetimibe
