Lipid Lowering Drugs Flashcards
Name the 6 drug classes to treat dyslipidemias
- Omega-3-acid ethyl esters
- PCSK9 inhibitors
- Fibrates
- Resins
- HMG-CoA reductase inhibitors (Statins)
- Ezetimibe
Name 3 examples of statins
Atorvastatin, pravastatin, simvastatin
MOA of statins
- Competitive inhibitor of HMG-CoA reductase (rate limiting enzyme for endogenous cholesterol synthesis), reduce conversion of HMG-CoA to mevalonic acid, thus overall decreasing cholesterol synthesis
- Upregulates LDL receptor on cell surface: Decreased intracellular cholesterol causes the cell to increase specific cell-surface LDL receptors that can bind and internalise circulating LDLs
2 clinical uses of statins
- Lower LDL levels in all types of dyslipidemias
- Reduce the risk of coronary events or mortality in patients with IHD
Which time of the day are statins commonly given?
Evening (because dietary cholesterol is low, so body needs to produce more endogenously, thus statins most effective)
Give 2 ADRs of statin use
- Biomedical abnormalities in liver function
- Muscles: myopathy and rhabdomyolysis (causes tea coloured urine)
Statins are contraindicated in (4 types of patients)… because…
- Pregnancy
- Nursing mothers
- Children
- Teenagers
Known to affect neurodevelopment in foetus and child
State 2 examples of PCSK9 inhibitors
- Evolocumab
- Alirocumab
MOA of PCSK9 inhibitor
Inhibits PCSK9 which targets LDL receptors for degradation by lysosomes.
Thus reduces degradation of LDL receptors, so increases the number of cell-surface LDL receptors that can bind and internalise circulatory LDL
State 2 clinical uses of PCSK9 inhibitors
- Lower LDL levels in the blood in familial hypercholesterolemia patients especially if they’re intolerant to statins
- Clinically significant atherosclerotic CVD patients requiring additional LDL lowering therapy after being on diet control and maximally tolerated statin therapy
Administration of PCSK9 inhibitors
IV (monoclonal antibody)
Advantage of taking PCSK9 in combination with statins
Can lower LDL levels by about 50-60% more than if statins are used alone
Give 2 ADRs of PCSK9 inhibitor use
- Inflammatory reactions at the site of injection
- Increased incidence of nasopharyngitis and sinusitis
PCSK9 inhibitors are contraindicated in patients that develop…
Hypersensitivity reactions
Name 2 examples of fibrates / fibric acid derivatives
- Gemfibrozil
- Fenofibrate