34 Questions
What is a contraindication for bile acid binding resins?
Hypersensitivity
What is the effect of bile acid binding resins on LDL receptors?
Increased
What is a side effect of bile acid binding resins?
GI discomfort
What is the mechanism of action of Cholestyramine?
Binding to bile acid
When should bile acid binding resins be administered in relation to other drugs?
4 hours after other drugs
What is the effect of bile acid binding resins on absorption of vitamins and drugs?
Decreased
What type of patients may be prescribed Cholesterol absorption inhibitors as monotherapy?
Statin-intolerant patients
What is the effect of combining bile acid binding resins with statins?
Synergistic
What is the primary mechanism of action of Ezetimibe?
Inhibiting reabsorption of cholesterol excreted in bile
What is a potential side effect of Ezetimibe?
Abdominal pain
How do Bile acid binding resins affect Ezetimibe?
Inhibit the absorption of Ezetimibe
What is the mechanism of action of PCSK9 inhibitors?
Inhibiting the action of PCSK9
What population should avoid PCSK9 inhibitors?
Both pregnant women and breastfeeding mothers
What effect do PCSK9 inhibitors have on LDL-c levels?
Decrease LDL-c levels in patients with very high LDL-c
What is the mechanism of action of HMG CoA reductase inhibitors?
Inhibit HMG-CoA reductase, a rate-limiting enzyme
What is the effect of HMG CoA reductase inhibitors on LDL receptors?
Increase LDL receptors
Which of the following is a side effect of HMG CoA reductase inhibitors?
Myopathy, especially rhabdomyolysis
Which of the following HMG CoA reductase inhibitors is metabolized by CYP3A4?
ALS
What is the clinical usage of HMG CoA reductase inhibitors?
Hypercholesterolemia
What is the effect of HMG CoA reductase inhibitors on atherosclerosis?
Decrease plaque rupture
Which of the following medications may interact with HMG CoA reductase inhibitors?
Itraconazole, Ketoconazole
What is the alternative medication that may be considered in case of myopathy or rhabdomyolysis?
Rosuvastatin or Pravastatin
What is the purpose of using siRNA, including Inclisiran, in addition to statins?
To reduce PCSK9 levels and increase LDL receptor recycling
What is the main side effect of Gemfibrozil?
Myopathy, which needs to be monitored by CK levels
What percentage of fenofibrate is excreted in the urine?
60-90%
What is the main mechanism of action of fibric acid derivatives like fenofibrate?
Stimulating PPARα and increasing FA oxidation
What is the indication for using fibric acid derivatives like Gemfibrozil?
Hypertriglyceridemia and chylomicronemia syndrome
What is a potential complication of using fibric acid derivatives like fenofibrate?
Increased risk of gallstone formation
What is the effect of ω3-fatty acids on Liver TG?
↓
What is a potential side effect of Eicosapentaenoic acid (EPA)?
Prolonged bleeding time
What is the relationship between ω3-fatty acids and PPARα activity?
May modulate
What is the effect of Decosahexaenoic acid (DHA) on triglycerides?
45%↓
What is a potential interaction of ω3-fatty acids with other medications?
Antithrombotic drugs
What is a potential benefit of ω3-fatty acids in liver disease?
Reduced liver hyperlipidemia
Study Notes
HMG CoA Reductase Inhibitors
- Also known as statins
- Inhibit HMG-CoA reductase, a rate-limiting enzyme
- Result: inhibition of de novo synthesis of cholesterol
- Clinical usage: hypercholesterolemia, CVD prevention, and restoration of vessel function
- Increase LDL receptors and HDL
- Examples: Atorvastatin, Lovastatin, Simvastatin
- Side effects: transaminase enzyme increase, myopathy, and rhabdomyolysis
- Contraindications: liver disease, pregnancy, breastfeeding, and hypersensitivity
Bile Acid Binding Resins
- Examples: Cholestyramine, Colestipol, Colesvelam
- Mechanism of action: inhibit enterohepatic circulation by binding to bile acid
- Clinical usage: hypercholesterolemia, especially when statins are contraindicated
- Generally safe, but may cause GI discomfort and decrease absorption of vitamins and drugs
Cholesterol Absorption Inhibitors
- Example: Ezetimibe
- Mechanism of action: inhibit intestinal absorption of cholesterol by blocking NPC1L1
- Clinical usage: hypercholesterolemia, especially in statin-intolerant patients
- Side effects: abdominal pain, diarrhea, and steatorrhea
- Bile acid binding resins inhibit absorption of ezetimibe
PCSK9 Inhibitors
- Examples: Alirocumab, Evolocumab, Inclisiran
- Mechanism of action: monoclonal antibody that binds to PCSK9, increasing LDL receptor recycling
- Clinical usage: severe hypercholesterolemia, especially in addition to statins
- Avoided in pregnancy and breastfeeding mothers
Fibric Acid Derivatives
- Examples: Gemfibrozil, Fenofibrate, Bezafibrate
- Mechanism of action: stimulate PPARα, increasing FA oxidation and decreasing VLDL and LDL
- Clinical usage: hypertriglyceridemia, chylomicronemia syndrome, and dysbetalipoproteinemia
- Side effects: myopathy, increased risk of gallstone formation, and liver hyperlipidemia
- Contraindications: liver disease, pregnancy, and gout
ω3-Fatty Acids
- Examples: Eicosapentaenoic acid (EPA), Decosahexaenoic acid (DHA)
- Mechanism of action: uncertain, may modulate PPARα activity
- Clinical usage: triglyceride reduction
- Side effects: prolonged bleeding time, interaction with antithrombotic drugs
Learn about statins, a type of medication that inhibits HMG-CoA reductase, a rate-limiting enzyme, and its effects on cholesterol synthesis, clinical usage, and side effects.
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