Lipid lowering medications Flashcards
What are the 2 classes of lipid lowering drugs that reduce absorption of fats?
Bile acid binding resins and ezetimide (reduce intestinal sterol reabsorption)
What are the 2 classes of lipid lowering drugs that increase peripheral clearance of cholesterol?
- ** Statins (HMG-CoA reductase inhibitors)
- Fibrates
What is the class of lipid lowering drugs that reduce LDL receptor degradation?
PCSK9 inhibitors
Which class of lipid lowering drugs reduces triglyceride synthesis?
Omega-3-acid ethyl esters
Name at least 2 statins
Atorvastatin
Pravastatin
Simvastatin
Lovastatin
What is the MOA of statins?
Inhibits HMG-CoA reductase, an enzyme which is involved in the rate limiting step in cholesterol synthesis.
Upregulates LDL receptors to internalize more LDL
What is the unique property of statins?
Advised to be taken in the evening
- Peak endogenous cholesterol synthesis is in the night
- Synchronisation of statin peak concentration with the peak synthesis
What are the adverse effects of statins?
- Liver abnormalities
- Myopathy & rhabdomyolysis
- Urine turns tea colour
Which groups of patients are contraindicated to take statins?
- Pregnant
- Nursing mothers
- Children
- Teenagers
Affects neurodevelopment of fetus and child
What is the class of drug recommended if patients are intolerant to statins?
PCKS9 inhibitors
Name 2 PCKS9 inhibitors
Evolocumab
Alirocumab
What is the MOA of PCKS9 inhibitors?
Inhibits PCKS9 which is an enzyme that catalyses the degradation of LDL receptors.
Reduce LDL receptor degradation, more LDL receptors that can bind to and internalise circulating LDLs
What is the ROA of PCKS9 inhibitors?
Injection! because they are monoclonal antibodies
What are the adverse effects of PCKS9 inhibitors?
- Serum sickness - contraindicated in patients with previous hypersensitivity reactions
- Injection site inflammatory reaction
- Nasopharyngitis and sinusitis
Name 2 fibrates
Gemfibrozil, fenofibrate
What is the MOA of fibrates?
Increase peripheral clearance by increasing activity of lipoprotein lipase (break down triglycerides)
More used in treatment of hypertriglyceridemias
What is a unique adverse effect of fibrates?
Gall stones
What is the drug name of omega 3 acid ethyl ester?
Omacor
What is the MOA of omega 3 acid ethyl esters?
Reduce triglyceride production and increase free fatty acid breakdown via beta oxidation.
What are the contraindications and adverse effects of omega 3 acid ethyl ester?
Contraindicated in patients who are allergic to fish.
- GIT symptoms
- Reduced production of thromboxane A2 (coagulant) -> increased bleeding time
Name a resin
Cholestyramine
What is the MOA of resins?
Bile acids bind to bile salts leading to a decrease in bile acid concentration.
This causes hepatocytes to increase conversion of cholesterol to bile acids
Intracellular cholesterol concentration decreases.
What is the unique adverse effect of bile acid binding resins?
Impaired absorption of vitamin A, D, E, K
What is the MOA of ezetimibe?
Reduces cholesterol absorption at the small intestine
