cvs - lipid lowering drugs Flashcards
name 3 HMG-CoA reductase inhibitors
- lovastatin
- fluvastatin
- simvastatin
moa of HMG-CoA reductase inhibitors
- inhibit HMG-CoA reductase, the rate-limiting step in cholesterol synthesis
- upregulate LDL receptors → removal of cholesterol from blood
clinical uses of HMG-CoA reductase inhibitors
- lower LDL-C levels in hyperlipidemia
- reduce risk of coronary events and mortality in pts w IHD
why are statins best taken in the evenings?
at night, no food intake (= no cholesterol) → HMG-CoA reductase work the most at night to form cholesterol → statins should be taken in evening to have max efficacy at night
adverse effects of HMG-CoA reductase inhibitors
- biomedical abnormalities in liver func
- myopathy
- rhabdomyolysis (muscle soreness, tea-coloured urine)
contraindications for HMG-CoA reductase inhibitors
- pregnancy
- nursing mothers
- children/teens
reason: affects neurodevt of foetus and child
name 2 PCSK9 inhibitors
- evolocumab
- alirocumab
moa of PCSK9 inhibitors
inhibition of PCSK9 reduces LDL receptor degradation → more LDL receptors can internalise circulating LDLs
clinical uses of PCSK9 inhibitors
lower LDL-C levels in familial hypercholesterolemia/ clinically significant atherosclerotic CVD
adverse effects of PCSK9 inhibitors
- hypersensitivity rxns
- injection site inflam (swelling, pain etc)
- increased incidence of nasopharyngitis and sinusitis
name 2 fibrinates
- gemfibrozil
- fenofibrate
moa of fibrinates
- ligand for PPAR-α → interaction w PPAR-α results in increased activity of lipoprotein lipase → decrease in plasma triacylglycerol lvls
- HDL lvls rise moderately
clinical uses of fibrinates
hypertriglyceridemias w VLDL elevation
adverse effects of fibrinates
- skin rash
- gallstones
- myositis
- nausea
name 1 omega-3 acid ethyl ester
omacor
moa of omega-3 acid ethyl ester
- reduces hepatic triglyceride prodn and increases triglyceride clearance of VLDL
- functional inhibition of diglycerides acyltransferase (responsible for triglyceride synthesis)
clinical uses of omega-3 acid ethyl ester
- hypertriglyceridemia (type IV) monotherapy
- familial combined hyperlipidemia (type IIb)
what condition is not indicated for omega-3 acid ethyl ester
hyperchylomicronemia (type I)
adverse effects of omega-3 acid ethyl ester
- GI symptoms (pain, constipation, diarrhoea)
- increased LDL-C in some pts
- reduces prodn of thromboxane A2 → increased bleeding time
contraindications for omega-3 acid ethyl ester
fish allergy
name a bile acid binding resin
cholestyramine
moa of bile acid binding resins
resin bind to bile acids in small intestine → lower [bile acid] → hepatocytes increase conversion of cholesterol to bile acids → cholesterol conc decreases
clinical uses of bile acid binding resins
- primary hypercholesterolemia (IIa)
- add Niacin to treat LDL elevations in pts w combined hyperlipidemia (IIb)
adverse effects of bile acid binding resins
- flatulence, constipation
- impaired absorption of vit A (night blindness), D (depression), E (peripheral neuropathy), K (easy bruising)
name an intestinal sterol absorption inhibitor
ezetimibe
moa of intestinal sterol absorption inhibitors
inhibit NPC1L1 to reduce cholesterol absorption at small intestine → reduced plasma cholesterol lvls
clinical use of intestinal sterol absorption inhibitors
- reduce LDL
- vytorin: ezetimibe + simvastatin
adverse effects of intestinal sterol absorption inhibitors
- diarrhoea, flatulence
- myopathy
- rhabdomyolysis (more common when combined w statins)
- low incidence of reversible hepatotoxicity
