hyperlipidemia drugs Flashcards
Pro-atherogenic effects of Ox-LDL
Inhibits macrophage motility
• Induces T-cell activation and VSMC division /
differentiation
- Toxic to endothelial cells
- Enhances platelet aggregation
Old Classes of Lipid Lowering Drugs
● Statins - simvastatin
● Cholesterol lipase inhibitors - ezetimibe
● Nicotinic acid / niacin
● Fibrates – fenofibrate
● Resins - colestyramine
● Omega-3 fatty acids - omacor
● ? Plant sterols
which drug class doesnt have much of systemic effects and why?
Ezetimibe and its active glucuronide metabolite
bc they circulate enterohepatically
• Delivers agent back to the site of action
• Limits systemic exposure
Statins
Mechansim of action of statins
Adverse Drug Reactions of Statins
• Increased transaminase levels
• 0.1%-2.5% of treated patients develop increases of >
3 x upper-normal limit, especially at higher doses
• Rapidly reversible, no evidence of chronic liver disease
• Myopathy
- Diffuse muscle pain and CPK > 10 x upper-normal limit
- Primarily seen when higher doses of statins are used in combination with cyclosporine, gemfibrozil, and occasionally erythromycin and niacin
• Miscellaneous
• Gastrointestinal complaints, arthralgias, and headaches
Some secondary benefits of Statin treatment
Anti-inflammatory
●Plaque reduction
● Improved endothelial cell function
● Reduced thrombotic risk
decreases endothelin>> which causes vasoconstriction
Statin therapy is recommended as part of the management strategy for who?
for the primary prevention of CVD for adults who have a 20% or greater 10-year risk of developing CVD.
which statin is now withdrawn from the market?
Cerivastatin >> causes drug0drug interaction due to reports of fatal rhabdomyolysis.
Mechanism of action of fibric acids and side effects
mainly to reduce TAG!
SE:
GI upset (8%), cholelithiasis, myositis,
AbnormL LFTs
changing ur diet has a greater impact on which lipids in the body?
TAG is modified much more easily than cholestrol!
Fibric Acid Derivatives
Indications, Efficacy , Side Effects, Contraindications:
Nicotinic Acid
- Adverse effects,
- Contraindications
indication
how do we reduce side effects of niacin>> Flushing, itching, headache ?
reduced by immediate-release, Niaspan® or combination with low-dose aspirin
Ezetimibe: Mechanism of Action
what is the main class of lipid therapy?
statins
when would u wanna use combination therapy?
like statins and smth else?
for those who cant tolerate statins or have a specific need for, (ex: having high TAG levels)
which drug, when combined with statins, is thought to impair glucuronidation of statins ?
Gemfibrozil
which drug has a much better effect when combined with statins?
(combination statin therapy)
Ezetimibe
which drug class has flushing and itching as ADR?
Nictonic acid
what is the best drug to increase HDL?
those who have hypercholestermia and statin drugs don’t work well, what do we give them instead?
Evolocumab >> PSCK9 Inhibitor
reating adults with primary hypercholesterolaemia (heterozygous-familial and non-familial) or mixed dyslipidaemia
non-drug dietary approaches to lipid lowering
– Fish oils
– Fibre
– Vitamin C / E
– Alcohol increses (HDL)
– plant sterols (instead of butter)
some ppl will still have cholestrol levels of 7 or 8 mmol/L even w/ a good diet, why?
bc vast majority of cholestrol is under genetic control!
Learn how to undertake a CV Risk Assessment
Qrsik calculator
-ask age, ethnicity, postcode ( could asscess poverty)
describe the NICE guidance relating to lipid-lowering drug prescribing
function of omega-3 fatty acids
decrease TAG
which drug increases the most HDL?
nicotinic acid
(hawraa likes smoking lol)
which drug has a more effect in decreasing TAG?
fibrates
what and how much is gibven for piramry prevention of ppl with HIGH RSIK of CVD event >10%
low dose>> 20mg atrovastatin
