Pharmacology · MU Sofia

47. Antidyslipidemic drugs.

Introduces lipid-lowering drugs and their five classes: statins, fibrates, bile acid sequestrants, cholesterol absorption inhibitors and PCSK9 inhibitors, with the example agents for each. Covers how each class acts, a comparative table of routes, metabolism, excretion and half-life, and the common and rare side effects. Also lists key drug interactions, therapeutic uses, pregnancy and lactation cautions, and closes with recap questions.

Inside: 9 sections · 5 labelled pictures · 1 table · 10 flashcards · 3 min

Topic 46 of 93 in the MU Sofia syllabus for Pharmacology (Medicine, Year 3). The free AceMed note covers it in 9 sections, about 307 words (3 min of reading), with 10 flashcards.

In this note

  1. Antidyslipidemic Drugs
  2. Classification
  3. Pharmacodynamics (Mechanism of Action)
  4. Pharmacokinetics
  5. Side Effects
  6. Drug Interactions
  7. Therapeutic Uses
  8. Pregnancy & Lactation Considerations
  9. Key Recap Questions

Antidyslipidemic Drugs

Antidyslipidemic drugs, also known as lipid-lowering agents, are medications used to manage dyslipidemia, which refers to abnormal levels of lipids (fats) in the blood.

Classification

  1. 1. Statins: Atorvastatin, Simvastatin, Rosuvastatin
  2. 2. Fibrates: Gemfibrozil, Fenofibrate
  3. 3. Bile Acid Sequestrants: Cholestyramine, Colesevelam
  4. 4. Cholesterol Absorption Inhibitors: Ezetimibe
  5. 5. PCSK9 Inhibitors: Alirocumab, Evolocumab

Pharmacodynamics (Mechanism of Action)

  1. 1. Statins
  • Inhibit HMG-CoA reductase, reducing cholesterol synthesis in the liver.
  • Increase LDL receptor expression, leading to enhanced LDL clearance.
  1. 2. Fibrates
  • Activate peroxisome proliferator-activated receptor-alpha (PPAR-α).
  • Increase lipolysis of triglycerides and reduce VLDL production.
  1. 3. Bile Acid Sequestrants
  • Bind bile acids in the intestine, preventing their reabsorption.
  • Promote cholesterol excretion in feces.
  1. 4. Cholesterol Absorption Inhibitors
  • Inhibit Niemann-Pick C1-like 1 (NPC1L1) protein, reducing cholesterol absorption in the intestine.
  1. 5. PCSK9 Inhibitors
  • Block proprotein convertase subtilisin/kexin type 9 (PCSK9).
  • Increase LDL receptor expression, enhancing LDL clearance.

Side Effects

  • Common Side Effects
  • Gastrointestinal symptoms (nausea, diarrhea).
  • Muscle pain or weakness (especially with statins).
  • Elevated liver enzymes (hepatic toxicity risk).
  • Rare but Serious Side Effects
  • Rhabdomyolysis (muscle breakdown, statins & fibrates).
  • Liver damage (statins & fibrates).
  • Pancreatitis (fibrates).
  • Allergic reactions.

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