OTHER LIPID MODIFYING DRUGS Flashcards
Ezetimibe - MOA
inhibits the intestinal absorption of cholesterol
Is Ezetimibe effective on its own?
- If used alone it has a modest effect on lowering LDL
concentration - It has little effect on other lipoproteins (e.g. Triglycerides)
What is the dose of Ezetimibe?
10mg OD
What are the indications for Ezetimibe?
- Adjunct to dietary measurements and statins in primary hypercholesterolaemia
- Primary hypercholesterolaemia (if statins are not tolerated/ contraindicated)
- Heterozygous familial hypercholesterolaemia
What are the common side-effects of Ezetimibe?
- Gl disorders
- Diarrhoea
What are Alirocumab and Evolocumab used for?
- Licensed for treatment of primary hypercholesterolaemia (heterozygous familial and non-familial) or mixed
dyslipidaemia as an adjunct to dietary measures
Can Alirocumab or
Evolocumab be used in combination with other lipid-modifying drugs?
- Yes, it statins are not tolerated
How do Bile acid sequestrants work?
- Binds to and sequesters bile acids.
- Liver then produces more bile acids to replace those lost.
- Body uses cholesterol to make bile acids = reduced LDL cholesterol circulating in the blood.
Bile Acid Sequestrants - examples
Colesevelam
Colestipol
Colestyramine
Bile Acid Sequestrants - administration counselling points
Take other drugs 1 hour before (4 hours for colesevelam) or 4 hours after bile sequestrant.
Bile Acid Sequestrants - interactions
- Impairs absorption of fat-soluble vitamins (ADEK and folic acid) and other drugs
Impairs absorption of fat-soluble vitamins (ADEK) and other drugs
Impairs absorption of fat-soluble vitamins (ADEK) and other drugs
Fibrates - examples
- Bezafibrate
- Ciprofibrate
- Fenofibrate
- Gemfibrozil
Fibrates - MOA
- They act by decreasing serum triglycerides
- They have a variable effect on LDL-cholesterol
When are fibrates mainly used?
- In those with a serum-triglyceride concentration of greater than 10mmol/L
- Or in those who cannot tolerate statin (specialist use)
What is a common side-effect of Fibrates?
- Gl disorders
- Myotoxicity in renal impairment
Can fibrates be used in renal impairment?
Dose adjustment required
Statin + Fibrates =
increased risk of muscle related side-effects
rhabdomyolysis
* Statin + gemfibrozil (do not use together)
Nictoinic acid - examples
Acipimox
Nicotinic acid
Omega-3 fatty acid
Nicotinic acid - indication
Adjunct to statin OR alone if statin not tolerated
Nicotinic acid - MOA
Lowers cholesterol and triglyceride concentrations by inhibiting synthesis.
Increases HDL cholesterol
Nicotinic acid - CI
Active peptic ulcer disease
Arterial bleeding
What is a common side-effect of nicotinic acid which limits its use?
- Vasodilation (e.g. flushing)
Omega-3 Fatty Acids - Indication
- Used in adjunct to statin/diet.
- Not be used alone
- No evidence for use
Omega-3 Fatty Acids - cautions
Anticoagulant treatment
Haemorrhagic disorders
- Has natural anticoagulant properties so can thin the blood
Omega-3 Fatty Acids - side effects
AF
Burping
Constipation
GI distubrances
N + V
