Antilipidemic Agents

Question 1

HMG-CoA Reductase Inhibitors

Answer 1

MOA
* competitively inhibit HMG-CoA reductase activity to block synthesis of
cholesterol in the liver
* Force upregulation of LDL receptors
* LDL endocytosis increased

Question 2

HMG-CoA Reductase Inhibitors Adverse Effects, Interactions, facts

Answer 2

Adverse Effects
* Myalgias (CK = creatine kinase)
* Rhabdomyolysis (breakdown of muscle; can lead to renal failure)
* Contraindications:
* Pregnancy (X), lactation
* Active liver disease
* Drug interactions
* atorvastatin, simvastatin, lovastatin metabolized by CYP 3A4
* Take in the evening
* Monitor LFTs at baseline, in 12 weeks (then as clinically indicated)
* Recheck Fasting Lipid Panel in 12 weeks to eval % reduction

Question 3

pitavastatin (Livalo)

Question 4

rosuvastatin

Answer 4

Crestor

Question 5

simvastatin

Answer 5

Zocor

Question 6

atorvastatin

Answer 6

Lipitor

Question 7

pravastatin

Answer 7

Pravachol

Question 8

Niacin MOA

Answer 8

Decreases synthesis of VLDL and subsequently LDL by the liver
* Reduces LDL 15-25%
* Reduces triglycerides by 50%
* Increases HDL by 25-35%
* Take with meal/snack
* AE:
* Flushing (Pretreat with 325 mg ASA 30 min prior to dose)

Question 9

Bile Acid Sequestrants

Answer 9

• MOA: bind bile acids in the gut, interrupting reabsorption (thus, more
  cholesterol is used to make more bile acids)
• Ex:
• cholestyramine (Questran) (powder)
• colestipol (Colestid) (tablet, granules)
• colesevelam (WelChol) (tablet, powder)

Question 10

Bile Acid Sequestrants Adverse Effects

Answer 10

Adverse Effects: GI
* Constipation
* Abd pain/cramping/N/V/flatulence/belching
* Malabsorption of fat soluble vitamins
* Take before meals
* Powders mixed with 4-6 oz of juice, water or other noncarbonated beverage
* separate other drugs 1 hr before or 4 hrs after
* off label use: chronic diarrhea (irritable bowel syndrome)

Question 11

Fibric Acid Derivatives

Answer 11

• MOA
• Works to decrease triglycerides by increasing lipolysis and elimination of triglyceride-rich particles from
  plasma by activating lipoprotein lipase
• Ex: fenofibric acid (Trilipix)
• gemfibrozil (Lopid) – Do NOT combine with statins
• fenofibrate (Tricor)
• Reduces triglycerides by 50%
• Reduces LDL by 15-20%
• Increase HDL by 15-25%
• Adverse Effects
• Myalgias
• LFT abnormalities

Question 12

Cholesterol Absorption Inhibitor

Answer 12

Ezetimibe (Zetia)
* Add-on therapy
* MOA
* Inhibits cholesterol absorption at small intestine
* Decreases hepatic cholesterol stores
* Increases blood cholesterol clearance
* Contraindications
* ACTIVE liver disease
* AE (minimal)
* GI
* myalgias

Question 13

Omega 3 Fatty Acids Indications

Answer 13

Indicated for severe hypertriglyceridemia

Question 14

Lovaza

Answer 14

Omega 3 fatty acide
decreases tryglycerides by 45%

Question 15

icosapent ethyl (Vascepa)

Answer 15

no increase in HDL

Question 16

PCSK-9 Inhibitors

Answer 16

Proprotein convertase subtilisan/kexin- type 9 = enzyme produced by liver

Question 17

PCSK-9 Inhibitors

Answer 17

Proprotein convertase subtilisan/kexin- type 9 = enzyme produced by liver

Question 18

PCSK-9 benefits

Answer 18

 Lower LDL-C level (60-70%)
 Lower triglyceride level (12-31%)
 Increased HDL level (5-9%)
 SIGNIFICANT lowering of CV event-risk (up to 50%)
 Low risk of adverse events
$$$$$
SC injection every 2-4 weeks