Introduction: This focused set of antihyperlipidemic drugs MCQs With Answer is designed for B. Pharm students to reinforce core concepts in pharmacology and therapeutics. Covering mechanisms of action, clinical uses, adverse effects, monitoring, drug interactions and newer agents such as PCSK9 inhibitors, the questions emphasize key keywords: antihyperlipidemic drugs, statins, fibrates, bile acid sequestrants, ezetimibe, LDL-C, triglycerides, lipid profile and drug safety. Each MCQ tests practical understanding required for dispensing, counseling and clinical decision-making. Clear options and answers promote active recall and exam readiness while deepening knowledge of pharmacokinetics and molecular targets. Now let’s test your knowledge with 30 MCQs on this topic.
Q1. Which of the following is the primary mechanism of action of statins?
- Activation of PPAR-alpha
- Inhibition of HMG-CoA reductase
- Binding bile acids in the intestine
- Blocking NPC1L1 cholesterol transporter
Correct Answer: Inhibition of HMG-CoA reductase
Q2. The most clinically significant adverse effect associated with statin therapy is:
- Renal failure
- Myopathy and rhabdomyolysis
- Severe hypoglycemia
- Excessive weight gain
Correct Answer: Myopathy and rhabdomyolysis
Q3. Fibrates lower triglyceride levels mainly by which mechanism?
- Inhibition of HMG-CoA reductase
- Activation of PPAR-alpha increasing lipoprotein lipase activity
- Blocking intestinal cholesterol absorption
- Monoclonal antibody against PCSK9
Correct Answer: Activation of PPAR-alpha increasing lipoprotein lipase activity
Q4. Which lipid parameter is most reduced by fibrate therapy?
- LDL-C
- HDL-C
- Triglycerides
- Total cholesterol
Correct Answer: Triglycerides
Q5. Bile acid sequestrants lower LDL cholesterol primarily by:
- Directly inhibiting HMG-CoA reductase
- Increasing hepatic conversion of cholesterol into bile acids and upregulating LDL receptors
- Activating PPAR-gamma
- Blocking intestinal triglyceride absorption
Correct Answer: Increasing hepatic conversion of cholesterol into bile acids and upregulating LDL receptors
Q6. Ezetimibe lowers LDL cholesterol by inhibiting which intestinal transporter?
- NPC1L1
- ABCG5/ABCG8
- SR-BI
- Microsomal triglyceride transfer protein (MTP)
Correct Answer: NPC1L1
Q7. PCSK9 inhibitors reduce LDL-C primarily by:
- Inhibiting intestinal cholesterol absorption
- Increasing LDL receptor recycling on hepatocytes
- Stimulating HDL synthesis
- Blocking VLDL secretion from the liver
Correct Answer: Increasing LDL receptor recycling on hepatocytes
Q8. The characteristic flushing seen with high-dose niacin is mediated by:
- Histamine release from mast cells
- Prostaglandin-mediated vasodilation
- Direct cholinergic stimulation
- Complement activation
Correct Answer: Prostaglandin-mediated vasodilation
Q9. Gemfibrozil increases the risk of statin-induced myopathy primarily because it:
- Enhances renal excretion of statins
- Induces CYP3A4 metabolism of statins
- Inhibits statin glucuronidation leading to higher statin levels
- Competes with statins at the LDL receptor
Correct Answer: Inhibits statin glucuronidation leading to higher statin levels
Q10. Which class of antihyperlipidemic drugs is most effective at markedly lowering triglyceride levels in severe hypertriglyceridemia?
- HMG-CoA reductase inhibitors (statins)
- Bile acid sequestrants
- Fibrates
- PCSK9 inhibitors
Correct Answer: Fibrates
Q11. Which statement about statin use in pregnancy is correct?
- Statins are safe and recommended in pregnancy
- Use only lipophilic statins in pregnancy
- Statins are contraindicated in pregnancy due to teratogenic risk
- Statins should be doubled during pregnancy for efficacy
Correct Answer: Statins are contraindicated in pregnancy due to teratogenic risk
Q12. Baseline and periodic monitoring for a patient starting statin therapy should routinely include:
- Serum creatinine only
- Lipid profile and liver enzymes (ALT/AST)
- HbA1c only
- Serum amylase and lipase
Correct Answer: Lipid profile and liver enzymes (ALT/AST)
Q13. Bile acid sequestrants can interfere with the absorption of which of the following?
- Water-soluble vitamins (B and C)
- Fat-soluble vitamins (A, D, E, K)
- Minerals like sodium and chloride
- Peptide antibiotics only
Correct Answer: Fat-soluble vitamins (A, D, E, K)
Q14. Which antihyperlipidemic agent class typically produces the greatest percentage reduction in LDL-C when added to maximum tolerated statin therapy?
- Fibrates
- Bile acid sequestrants
- PCSK9 inhibitors
- Niacin
Correct Answer: PCSK9 inhibitors
Q15. Which of the following statins is relatively hydrophilic and less likely to penetrate extrahepatic tissues?
- Simvastatin
- Atorvastatin
- Rosuvastatin
- Lovastatin
Correct Answer: Rosuvastatin
Q16. Ezetimibe exerts its effect primarily at which anatomical site?
- Duodenal brush border of enterocytes
- Hepatocyte endoplasmic reticulum
- Pancreatic acinar cells
- Adipocyte plasma membrane
Correct Answer: Duodenal brush border of enterocytes
Q17. The most common gastrointestinal adverse effect of bile acid sequestrants is:
- Diarrhea
- Constipation
- Pancreatitis
- Malabsorption of carbohydrates
Correct Answer: Constipation
Q18. Mipomersen lowers LDL-C by which novel mechanism?
- PCSK9 inhibition
- MTP inhibition
- Antisense oligonucleotide against apoB-100 mRNA
- Activation of LXR nuclear receptor
Correct Answer: Antisense oligonucleotide against apoB-100 mRNA
Q19. Lomitapide reduces circulating LDL and VLDL by inhibiting:
- HMG-CoA reductase
- Microsomal triglyceride transfer protein (MTP)
- Niemann-Pick C1-like protein
- CETP activity
Correct Answer: Microsomal triglyceride transfer protein (MTP)
Q20. Which agent is most effective at raising HDL cholesterol levels?
- Bile acid sequestrants
- Niacin (nicotinic acid)
- PCSK9 inhibitors
- Ezetimibe
Correct Answer: Niacin (nicotinic acid)
Q21. Fibrate-induced increase in HDL is mediated primarily through which action?
- Inhibition of CETP
- Activation of PPAR-alpha leading to increased ApoA-I and ApoA-II expression
- Blocking intestinal cholesterol absorption
- Direct stimulation of hepatic HDL receptors
Correct Answer: Activation of PPAR-alpha leading to increased ApoA-I and ApoA-II expression
Q22. “Pleiotropic effects” of statins refer to:
- Only their LDL-lowering properties
- Additional benefits such as improved endothelial function and anti-inflammatory effects
- Their capacity to chelate metals
- Direct increase of triglyceride synthesis
Correct Answer: Additional benefits such as improved endothelial function and anti-inflammatory effects
Q23. Bile acid sequestrants are relatively contraindicated in patients with:
- Severe hypertriglyceridemia (>400 mg/dL)
- Familial combined hyperlipidemia with low triglycerides
- Isolated low HDL without elevated LDL
- Mild gastroesophageal reflux disease
Correct Answer: Severe hypertriglyceridemia (>400 mg/dL)
Q24. First-line pharmacotherapy to reduce the risk of pancreatitis in patients with very high triglycerides is typically:
- Bile acid sequestrants
- Fibrates (e.g., fenofibrate)
- Ezetimibe
- PCSK9 inhibitors
Correct Answer: Fibrates (e.g., fenofibrate)
Q25. In a patient on a statin who develops muscle pain, which laboratory test is most appropriate to order first?
- Serum amylase
- Serum creatine kinase (CK)
- Thyroid-stimulating hormone only
- Fasting glucose
Correct Answer: Serum creatine kinase (CK)
Q26. Which statin has the highest risk of clinically significant interactions with strong CYP3A4 inhibitors?
- Pravastatin
- Rosuvastatin
- Simvastatin
- Fluvastatin
Correct Answer: Simvastatin
Q27. The LDL-lowering effect of bile acid sequestrants is partly due to which hepatic response?
- Decreased LDL receptor expression
- Increased synthesis of VLDL
- Upregulation of LDL receptors to import more cholesterol into hepatocytes
- Direct inhibition of ApoB synthesis
Correct Answer: Upregulation of LDL receptors to import more cholesterol into hepatocytes
Q28. Which antihyperlipidemic drug is specifically associated with hepatic steatosis and requires careful liver monitoring?
- Ezetimibe
- Lomitapide
- Bile acid sequestrants
- Niacin at low dose
Correct Answer: Lomitapide
Q29. Which of the following is a monoclonal antibody approved as a PCSK9 inhibitor?
- Aspirin
- Alirocumab
- Fenofibrate
- Lomitapide
Correct Answer: Alirocumab
Q30. For statins with short half-lives (e.g., simvastatin), the optimal time to administer the dose is:
- In the morning with breakfast
- At bedtime or in the evening
- A single weekly dose is sufficient
- Only when triglycerides are high
Correct Answer: At bedtime or in the evening

I am a Registered Pharmacist under the Pharmacy Act, 1948, and the founder of PharmacyFreak.com. I hold a Bachelor of Pharmacy degree from Rungta College of Pharmaceutical Science and Research. With a strong academic foundation and practical knowledge, I am committed to providing accurate, easy-to-understand content to support pharmacy students and professionals. My aim is to make complex pharmaceutical concepts accessible and useful for real-world application.
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