Lipid lowering drugs Flashcards
What is the first step in cholesterol synthesis
Hydroxymethylglutaryl is reduced into mevalonate by
HMG-CoA reductase (important)
What is the enzyme involved in first step in cholesterol synthesis
HMG-CoA reductase
What is the role of statins
HMG-CoA reductase inhibitors
What else does using statins do apart from reduce plasma cholesterol
The reduction in hepatic cholesterol synthesis leads to an up regulation of hepatic LDL receptors, promoting LDL uptake
(Increased uptake of cholesterol from plasma by liver)
What genetic condition affects LDL uptake
Homozygous familial hypercholesterolaemia (cannot make LDL receptor)
Are statins effective in familial hypercholesterolaemia
Atorvostatin may be effective in the homozygous version
Statins are effective in the heterozygous version
What sort of selectivity do statins have
Are hepatoselective
What metabolism do statins undergo
First pass metabolism in liver
When does the NICE guidance suggest you use statins
Patients with CVD
Patients with >10% risk of CVD
When should statins be taken
At night (that’s when cholesterol synthesis occurs)
Except atorvastatin
Adverse events of statins
Muscle pain (patients must report) -->Very rarely can lead to rhabdomyolysis
Increased diabetes but it is outweighed by CV benefits
Nocebo effects- patients imagine that they have side effects
What to monitor when using statins and why
Liver disease
Monitor LFT before and during
What drugs are simvastatin contraindicated with
Macrolides
Amlodipine, verapamil, diltiazem
(lower max dose of simvastatin when using amlodipine)
What foods shouldnt be used with simvastatin
Grapefruit juice
How to counsel patients for statin use
Look for signs of hepatotoxicity- jaundice, itching, dark urine
Muscle pain
Action of cholesterol absorption inhibitors such as ezetimibe
When to use
Inhibit uptake of cholesterol In GI.
Use in conjunction with statins if they are not controlling cholesterol
Action of alirocumab
PCSK9 inhibitor
PCKSK9 usually binds to LDL receptors and leads to its degradation. Using Alirocumab increases the number of hepatic LDL receptors and lowers LDL
When is alirocumab used
In addition to max dose statins (has a SC administration every 2 weeks)
What are fibres
Activates PPAR-a
Alters lipoprotein metabolism. Reduces triglycerides. reduce IDH but not mortality
Adverse effects of fibres
Rhabdomyolysis
Do antioxidants have a benefit in reducing IHD
No
Do functional foods such as benecol have an effect on cholesterol
YEs they lower it
-Helpful additions to statin therapy
Treatment of hypertriglyceridaemia
Lifestyle changes
+fibrate as a next life option
