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Hyperlipidaemia Treatment (Statins (Drugs: Atorvastatin, Fluvastatin,…
Hyperlipidaemia Treatment
Statins
Drugs:
Atorvastatin, Fluvastatin, Pravastatin, Rosuvastatin, Simvastatin
Mechanism of action:
Inhibits HMG-CoA reductase, an enzyme in cholesterol synthesis
This leads to decreased hepatic cholesterol synthesis & an increase in LDL receptors
Resulting in an increase in LDL clearance
Clinical effect:
LDL levels reduced by 30-50%
Minor reduction in TG
Minor increase in HDL
Many other systemic benefits
Adverse effects:
Common - Myalgia, GI disturbances
Rare - Rhabdomyolysis
Clinical use:
Hypercholesterolaemia
Mixed hyperlipidaemia
High risk of coronary heart disease
Bile Acid-Binding Resins
Drugs:
Cholestyramine, Colestipol
Mechanism of action:
Binds to bile acids in the intestine preventing their reabsorption and causing them to be excreted in faeces
Decreased absorption of exogenous cholesterol, increased metabolism of endogenous cholesterol for bile acid synthesis
Increased demand for cholesterol --> Increased LDL receptors --> Increased LDL clearance
Clinical effect:
LDL levels reduced by 15-25%
Adverse effects:
GI disturbances
May increase plasma TGs
Decreased absorption of fat-soluble vitamins (A, D, E, K)
May decrease absorption of some oral drugs
Clinical use:
Hypercholesterolaemia
Mixed hyperlipidaemia (use with caution)
Ezetimibe
Mechanism of action:
Inhibits exogenous cholesterol absorption by blocking the transport protein (NPC1L1) in the brush border of enterocytes
Increased demand for cholesterol --> Increased LDL receptors --> Increased LDL clearance
Clinical effects:
Reduces LDL levels by 18%
Adverse effects:
Generally well tolerated
Headache, abdominal pain, diarrhoea
Clinical use:
Hypercholesterolaemia
Fibrates
Drugs:
Fenofibrate, Gemfibrozil
Mechanism of action:
PPAR-alpha nuclear receptor agonists which increases transcription of lipoprotein lipase
This increases TG uptake from VLDL & chylomicrons
Leading to increased removal of TGs from plasma
Clinical effect:
Reduces TG levels by 40-80%
Moderately decreases LDL levels
Moderately increases HDL levels
Adverse effects:
GI disturbances
(Rare) rhabdomyolysis
Clinical use:
Hypertriglycerideaemia
Mixed hyperlipidaemia
Hypercholesterolaemia (2nd line)
Nicotinic Acid
Mechanism of action:
Inhibits hepatic VLDL secretion thus reducing LDL, TG and increasing HDL
Exact mechanism of unknown
Clinical effects:
Reduces LDL levels by 15-30%
Reduces TG levels by 25-40%
Increases HDL by 20-35%
Adverse effects:
Generally not well tolerated
Vasodilation (flushing, hypotension, headache), nausea, vomiting, diarrhoea
(Rare) Liver failure
Clinical use:
Hypercholesterolaemia
Hypertriglyceridaemia
Mixed hyperlipidaemia