Anti-Lipid Drugs Flashcards
(29 cards)
Anti-lipid Drugs:
HMG CoA reductase inhibitors; decrease cholesterol synthesis and increase LDL receptors; risk of VTE, hepatotoxicity and myopathy
Statins (Class 1)
Statin drugs with the highest potency (best reductions at low doses)
Atorvastatin (Lipitor)
Rosuvastatin (Crestor)
Why must some statin drugs be taken at night?
Liver cholesterol synthesis peaks between midnight and 2am (depending on sleep cycles), and some statins have short half-lives
Which anti-lipid drugs have the highest risk of birth defects (Category X)
Statins
Risks of statin drugs
VTE
Hepatotoxicity
Myopathy (Rhabdomyolysis)
Why might inhibitors of liver cytochromes make statin side effects worse?
Since statins are degraded by the liver, inhibiting statin metabolism will increase adverse effects
Statin drugs primarily decrease LDL and TG; no effects on HDL (True or False)
True
Example of Bile Acid Binding Agents (BABA)
Colestipol
Anti-lipid Drugs:
Increase elimination of bile acids by binding to them, drawing more cholesterol out of liver; increase LDL receptors; mainly GI side effects
Bile Acid Binding Agents (BABA) (Class II)
Why are pregnant women given BABAs instead of statins
BABAs stay in the GI tract, so don’t enter the blood stream of the mother or fetus
Risks for BABAs
GI symptoms (flatulence, constipation, diarrhea) Reduce absorption of other drugs
When should you take other drugs around a BABA?
Either 1 hour before or 3 hours after
What is Niacin also known as?
Vitamin B3
Anti-lipid Drugs:
Inhibits the synthesis of TGs in the liver; can cause flushing and insulin resistance; possibilities of birth defects (Category C)
Niacin (Class 3)
Which anti-lipid drug can cause insulin resistance, and thus should be used cautiously in diabetics
Niacin
Anti-lipid Drugs:
Inc. LDL receptor; activate LPL; increase FFA metabolism; have “-fib” root in name; can cause myopathy when used with high-dose statins; increase bleeding risk (warfarin effects); variable effects on LDL, TG and HDL
Fibric Acid Derivatives (Class 4)
Why might fibric acid derivatives being used with statin drugs cause myopathies?
FADs inhibit statin absorption into liver, so stays in serum
How do fibric acid derivatives affect serum warfarin levels?
Compete with warfarin binding site on albumin, displacing warfarin and increasing the amount in the blood
Anti-lipid Drugs:
Blocks absorption of cholesterol from intestines via NPC1; stimulates LDL receptor due to dec. cholesterol; can be combined with statins (block synthesis)
Ezetimibe (Class 5)
Why might coupling statins with Ezetimibe (absorption inhibitor) be beneficial?
Block both synthesis and absorption of cholesterol, addressing the two main sources of cholesterol
Anti-lipid Drugs:
promote uptake of cholesterol into the liver via PCSK9 inhibition; monoclonal antibody; can’t take orally
Alirocumab (Class 6)
How does Alirocumab help clear serum cholesterol?
It’s an antibody against a chemical that promotes the degradation of LDL receptor (it inhibits and inhibitor, in a sense)
Which anti-lipid drug can not be taken orally, due to potential degradation in the GI tract?
Alirocumab (monoclonal antibody)
Most widely prescribed anti-lipid drug
Statins
