Cholesterol Drugs Flashcards
Statins that are prodrugs
Lovastatin, Simvastatin (they’re metabolized SL-owly)
Statins metabolized by CYP3A4
Lovastatin, Simvastatin, Atorvastatin (also oxidized)
Statins metabolized by CYP2C9
Fluvastatin, Rosuvastatin
Statin metabolized solely by Sulfonation
Pravastatin
Statin mechanism of action?
Inhibit HMG-CoA Reductase, the rate limiting step in cholesterol biosynthesis. Also cause indirect up-regulation of hepatic LDL receptors
Statins with highest potency/efficacy?
Atorvastatin, Rosuvastatin (longest half lives)
Statins with moderate potency/efficacy?
Lovastatin, Simvastatin
Statin with lowest potency/efficacy?
Pravastatin
Niacin mechanism of action?
Inhibits VLDL secretion, thereby decreasing LDL
Niacin’s most useful clinical aspects?
Best way to increase HDL, only agent that lowers Lp(a)
Adverse effects seen with Statin therapy?
Sleep disturbance/memory loss (most common) Elevations in serum aminotransferases, myositis. Severe CK activity increase can cause rhabdomyolysis
Niacin adverse effects?
The 3 H’s
- Harmless cutaneous vasodilation (flushing, sense of warmth)
- Hepatotoxicity (rare)
- Hyperuricemia that can exacerbate gout
When should statins be administered?
At night, most cholesterol biosynthesis occurs at night. Should be given with food to increase absorption
Mechanism of action of Fibrates?
Ligands for PPAR-a. Transcriptionally up-regulate LPL, apo A-1, apo A-II, and down-regulate apo C-III. Also increase fatty acid oxidation in liver/striated muscle
What statin should be given to someone with Renal dysfunction?
Atorvastatin
Names of the Fibrates?
Gemfibrozil, Fenofibrate
Mechanism of action of Bile acid sequestrants?
Positively charged drugs that inhibit the enterohepatic recycling of bile acids–> cause the liver to use cholesterol to make more bile
Most common adverse effects seen with Bile acid sequestrants
GI side effects (bloating and constipation)
Drug-drug intercations seen with Bile acid sequestrants?
Inhibit the absorption of drugs like warfarin, digoxin, beta-blockers, and thyroxine
Bile acid sequestrants
Colestipol, Cholestyramine, Colesevelam
Unique form of bile acid sequestrant administration?
They come in powder form
Mechanism of action of Ezetimibe?
Inhibits the cholesterol uptake transporters NPC1L1
How does Niacin cause hyperuricemia?
It competes with uric acid for excretion in the Renal tubules
Dietary substance that has significant hypotriglyceridemic effect?
Omega-3 fatty acids, found in cold water fish. Also has anti-platelet, anti-arrhythmic, and blood pressure lowering effects
