Drugs to Treat Hyperlipidemia Flashcards
1
Q
statins
A
- competitively block HMG-CoA Reductase, the rate-limiting enzyme in cholesterol synth pathway
- also stabilize plaques, reduce inflammation, reverse endothelial dysfunction, decrease thrombogenicity
- risk of bilateral muscle pain, diabetes, hepatitis, cognitive effects
- metabolized via CYP450 pathway
2
Q
ezetimibe
A
- cholesterol absorption inhibitor that impairs dietary and biliary cholesterol absorption at the brush border of the intestine
- inhibit the Niemann-Pick C1 like 1 (NPC1L1) protein
- risk of hepatitis, rhabdomyolysis
3
Q
- Alirocumab (Praluent®)
- Evolocumab (Repatha®)
A
- PCSK9-inhibitors
- antibodies against PCSK9 interfere with its binding of the LDL-R, this leads to higher LDL-R and less LDL-C levels
4
Q
- colesevalam
- colestipol
- cholestyramine
A
Bile Acid Sequestrants
- used to reduce LDL by binding bile acids and preventing their reabsorption
- contraindicated in pts with dysbetalipoproteinemia
- risk of GI effects, vitamin ADEK deficiency, PKU
5
Q
Fibrates
A
- Fibrates activate PPARɑ to increase the expression of genes that encode enzymes that increase the metabolism of triglycerides and enhances the production of HDL
- risk of hepatitis, GI effects, gallstones, myopathy, presence in breast milk
- many drug interxns: bile acid sequestrants, colchicine…
- GEMFIBROZIL is CYP2C8 inhibitor
6
Q
Niacin
vitamin B3
A
- lowers VLDL and LDL, antioxidant
- risk of flushing, blood glucose elevation, uric acid elevation, hepatitis, and muscle toxicity, prolonged PT