Drugs to Treat Hyperlipidemia Flashcards
What is the MOA of statins?
Competitively block HMG-CoA reductase
What is the most severe form of muscle damage that statins can cause which may lead to severe kidney damage?
Rhabdomyolysis
What non lipid lowering MOA do statins have?
1) Plaque stabilization
2) Reduced Inflammation
What contraindications do statins have?
1) Active hepatic disease
2) Unexplained persistent elevations in aminotransferase levels
3) Pregnancy and while breastfeeding
A potential causal relationship between statin therapy and the risk of developing what condition has been noted?
Diabetes
What accounts for the low bioavailability of statins?
They undergo hepatic first pass metabolism
Which transaminase is higher in statin related liver dysfunction?
ALT greater than AST
Because of statins act on this particular organ, what may it cause?
Severe liver injury
Simvastatin and lovastatin the only two of the class administered as?
Prodrugs
The effect of statins in the body is almost universally affected by the concurrent metabolism of other pharmacologic agents which induce or inhibit?
CYP450
What needs to be done with warfarin prescription when given alongside statins?
Dose reduction
What is the MOA of ezetimibe?
Impairs dietary and biliary cholesterol absorption at the brush border of the intestine
What protein does ezetimibe inhibit?
Niemann-Pick C1 like 1 (NPC1L1)
Ezetimibe is also used in combination with?
Statins and fenofibrate
What are the contraindications and adverse effects of ezetimibe?
Pretty much same as statins
Ezetimibe is primarily metabolized in the liver and the small intestine via?
Glucuronide conjugation
What is the MOA of proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors?
Cleaves LDL receptors at serine residues
PCSK9-Inhibitors are indicated for patients with?
Heterozygous Familial Hypercholesterolemia
What is the MOA of bile acid sequestrants (BAS)?
Reduce low-density lipoprotein-cholesterol (LDL-C)
What happens to BAS after oral administration?
They are not absorbed, but bind to bile acids in the intestine and prevent their reabsorption into the body
Alirocumab and Evolocumab make up what class of drug?
PCSK9-Inhibitors
Colesevelam, colestipol, and cholestyramine make up what class of drug?
Bile Acid Sequestrants
What contraindications do BAS have?
Patients with dysbetalipoproteinemia
BAS may decrease the absorption of?
Fat soluble vitamins (A,D,E,K) and folic acid
What is the MOA of fibrates?
Activate Peroxisome Proliferator Antigen Receptor-alpha- (PPARɑ)
What general side effects are noted with fibrates?
GI issues
What should be done when prescribing fibrates?
1) Monitor liver enzymes
2) Monitor serum creatinine
At what GFR should fenofibrates not be used?
GFR < 30 ml/min
Why should gemfibrozil (fibrate) not be taken with statin?
Increased muscle toxicity risk
What may occur because fibrates may increase the concentration of cholesterol in the gallbladder?
Gallstones
Why does gemfibrozil have a lot of drug interactions?
It is a CYP2C8 strong inhibitor
Can fibrates be taken by nursing mothers?
No it appears in breast milk
What vitamin can be prescribed to reduce the levels of cholesterol and triglycerides (fatty substances) in your blood, and decrease your risk of a heart attack?
Niacin (vit B3)
What may nancin inhibit release of from adipose tissue?
Free fatty acids
What effect does niacin have with blood sugar and diabetes?
Raises blood sugar
Why does niacin affect patients with gout?
May raise uric acid levels
Why should niacin be used with caution in patients with active bleeding or bleeding disorders?
Prolongs prothrombin time
