Lipid lowering drugs Flashcards
List the 4 main classes of lipid lowering drugs
- statins
- cholesterol lipase inhibitors
- nicotinic acid/ niacin
- fibrates
give 2 examples of statins
atorvastatin, simvastatin, pravastatin
How do statins work?
Inhibit HMG co- a reductase, which decreases lipid synthesis in the liver, so increases LDL receptors and decreases production of LDLs
Who should receive a statin?
Anyone with a >10% risk of developing CVD in the next 10 yrs and those with familial hypercholesterolaemia
State 3 common side effects of statins
- Muscle and joint aches and pains–> creatine kinase may be raised, often seen with higher doses
- GI upset
- headaches
What effect can statins have on the liver which warrants LFT monitoring as they start treatment?
In rare cases it can increase transaminase levels, no chronic liver disease persists and is rapidly reversible on stopping treatment
What secondary benefits can statin have?
anti- inflammatory, plaque reduction, improved endothelial function, reduced thrombus risk
Name 2 fibric acid derivatives?
bezafibrate, fenofibrate
How do fibric acid derivates work to reduce cholesterol?
They are peroxisome proliferation activated receptor agonists, so increase lipoprotein lipase and so reduce TAG production. Also some knock on LDL decrease.
When are fibric acid derivates used?
adjuncts to statins/ diet therapy and in familial hypertriglyceridaemia
Name 3 ADRs of fibric acid derivates
- GI upset
- Gall stone risk
- muscle inflammation
When are fibric acid derivates contraindicated?
- hepatic and renal dysfunction
- pre- existing gall bladder disease
Name one nicotinic acid drug used to lower cholesterol?
Niacin
When is niacin indicated and contraindicated?
Indication: alongside statins
Contraindication: Liver disease of unexplained LFT elevation, also peptic ulcer disease
Name 3 ADRs seen with nicotinic acids?
- Flushings, itchings, headahces
- hepatotoxicity
- GI Upset
- Peptic ulcers
- reduced insulin sensitivity
How do nicotinic acids work?
Inhibit lipoprotein synthesis, so reduced VLDL and LDL, also good at increasing HDL
Name one cholesterol lipase inhibitor
Ezetimibe
How does ezetimibe work?
inhibits cholesterol lipase so inhibits cholesterol absorbtion on brush boarder of intestine, so less LDL delivery to liver and upregulation of LDL receptors. It never enters the systemic circulation.
When is ezetimibe used?
as adjunct to statins or when theyre poorly tolerated
What ADRs may arise from cholesterol lipase inhibitors?
Headache, abdo pain, diarrhoea
Why are resins not often used now to lower cholesterol?
theyre poorly tolerated
What new therapies could be used in the future to lower cholesterol?
PCSK9 inhibitors (evolocumab)- monoclonal antibodies to a protein which destroys the LDL receptors. Very effective but far too expensive for widespread use.
What dietary factors can reduce cholesterol?
fish oils, fibre, vitamin C and E, alcohol and plant sterols
How is CVD risk calculated?
Using Qrisk2 calculator.
Takes into account age, sex, postcode, race, BMI, smoking, Fhx, AF, CKD, BP, Cholesterol and HDL levels
What % reduction in non HDL cholesterol is aimed for?
40%
What dose of atrovastatin is generally used?
20mg for primary prevention with elevated CVD risk.
80mg for primary prevention if already have CVD- if can tolerate this high a dose.
