Exam 2: Hyperlipidemia Drugs Flashcards
What is the cause of Familial hypercholesterolemia?
LDL receptor deficiency
What are the 3 statin drugs?
Lovastatin, Simvastatin, and Atorvastatin
What is the MOA of statins?
Active forms are structural analogs of HMG-CoA reductase intermediate in mevalonate synthesis . Reduces plasma LDL by inhibiting the reductase to increased high affinity LDL receptor
What is the DOC to lower LDL?
Statins
What are the indications of statins?
To lower LDL, lower plasma TGs, and raise HDL
What are the other beneficial effects of statins that do not involve hyperlipidemia?
- Decreased CRP in patients with CHD
- enhance endothelial production of NO
- Increase plaque stability
- decrease lipoprotein oxidation
- decrease platelet aggregation
Which statin is high intensity dosage used in high risk ASCVD patients?
Atorvastatin
Which two statins needs to be hydrolyzed to their active form and when should they be taken because of this?
Lovastatin and simvastatin
Take in the evenings
How are statins metabolized?
P450s
What are the adverse effects of statins?
Increased level of serum aminotransferases
- May produce liver damage in alcoholics and patients with pre-existing liver problems
- Myopathy and muscle pain
- Increased serum CK
What are the contraindications of statins?
- pregnancy
- Active liver disease
- P450 inhibitors or activators
What kind of drug is Cholestyramine?
Bile acid binding resin
What is the MOA of Cholestyramine?
Binding of bile acids prevent their intestinal reabsorption
What are the indications of Bile acid bindings resins?
- elevated LDL
- No effect in homozygous familial hypercholesterolemia because their is no functional LDL receptor
- Not effective in hypertriglyceridemia (may increase VLDL)
What are the adverse effects of bile acid binding resins?
- Constipation and bloating (most common)
- Gallstones if obese
- hypoprothrombinemia
- may impair absorption of certain drugs
What drugs can bile acid resins inhibit absorption of?
Aspirin, Thyroxine, Tetracycline, Digitalis, statins, and thiazides
All Terrible Toddlers Demonstrate Scary Tantrums
What is the MOA of Niacin?
Lowers plasma VLDL and LDL by inhibiting VLDL secretion
-also inhibits hepatic cholesterologenesis
What are the indications of Niacin?
- Increase clearance in the LPL pathway (decrease VLDL further)
- increase levels of HDL
- Most effective in hypercholesterolemia
What kind of patients often receive Niacin?
Patients who cant exercise
What are the adverse effects of Niacin?
- generally mild
- Cutaneous vasodilation, warm sensation, dry skin
- Nausea, abd pain
- increased ALT/AST, impairs glucose tolerate
- Rarely hepatotoxicity
What kind of drug is Gemfibrozil?
FIbric acid derivative
What is the MOA of Gemfibrozil?
PPAR-alpha ligand, upregulates LPL and other genes involves in fatty acid oxidation
What are the indications of Gemfibrozil?
- Increases lipoprotein lipase activity
- Decreases TGs
- Decreases cholesterol
What are the adverse effects of Gemfibrozil?
- Increase incidence of Cholelithiasis and gallstones
- May increase LDL
What is the MOA of Ezetimibe?
Selectively blocks intestinal absorption of cholesterol and relegated phytosterols
What are the indications of Ezetimibe?
- Moderate decrease in LDL ( no decrease in CV mortality)
- Needs to be combined with statin
What kind of drugs Alirocumab and Evolocumab?
PCSK9 inhibitors
What is the MOA of PCSK9 inhibitors?
Antibodies that inhibit PCSK9 from binding to LDLR.
What are the indications of PCSK9 inhibitors?
-Increases LDLRs
Gemfibrozil is most effective in what disease?
Hypertriglyceridemia
