Pharmacology Of Dyslipidaemias Flashcards
HDL transport
Return of cholesterol from peripheral tissues to liver
LDL transport
Return of cholesterol from liver to non-hepatic tissue
VLDL transport
Return of cholesterol from liver to non-hepatic tissue
Exogenous pathway
Transport tissue/liver
Endogenous pathway
Transport of TGL to tissues. Mainly VLDL form.
Hyperlipidaemia
Elevation in serum lipids
Increased CHD risk
Type IIb
Familial combined/mixed hypercholesteraemia
Type IV
Familial hypertroglyceridemia
Statins
Simvastatin Atorvastatin Fluvastatin Lovastatin Pravastatin Rosuvastatin
Inhibitors of cholesterol absorption
Cholestyramine
Ezetimibe
Nicotinic acid
Niacin
Acipimox
Fibrates
Benzofibrate
Fenofibrate
Gemfibrozil
Statin inhibitors 5 steps
Acetyl CoA HMG CoA Mevalonate IPP Squalene Cholesterol
Absolute contraindication of statins
Renal insufficiency
Statins
Adverse effects
Myalgia
Rhabdomyolysis
Statins
- Main biochemical effect
- Secondary biochemical effect
- Reduced plasma LDL
2. Reduced TAG and increased HDL
Simvastatin
Familial hypercholesteraemia
Absorption not influenced by food
Extensive liver metabolism
Atorvastatin
Similar to simvastatin but longer acting
Mane/nocte
Fluvastatin
More likely to cause hepatic reactions
Lovastatin
Similar to simvastatin
Pravastatin
No interactions with CYP450 enzyme inhibitors
Rosuvastatin
Only drug used in children < 8 yo
Fibrates
- Mechanism of action
- Clinical use and indications
- Regulates gene expression
Stimulates lipoprotein lipase - Mixed dyslipidaemia
Bezafibrate
Caution in renal or hepatic failure or primary biliary cirrhosis
Fenofibrate
May cause haemolysis in G6PD deficiency
Gemfibrozil
May cause transient leukopenia
Cholestyramine
Drug interactions
Fat soluble vitamins Warfarin Digoxin Thiazide Tetracyclines Barbiturates
Ezetimibe
Mechanism
Lowers plasma cholesterol
Niacin
Can reduce LDL 10% - 20%
Can increase HDL 30%
Niacin
Adverse effects
Cutaneous flushing
Pruritis
Impairment of glucose tolerance
Acipimox
Not diabetogenic
Target values
LDL < 3
TAG < 1.7
HDL > 1.2