Pharmacology (Cholesterol, TG)

Question 1

Class and MOA of:

Atorvastatin (Lipitor)

Rosuvastatin (Crestor)

Simvastatin

Fluvastatin

Lovastatin

Pravastatin

Answer 1

HMG-CoA reductase inhibitor (“statins”)

Lowers LDL Cholesterol

• blocks VLDL production w/ inhibition of HMG-CoA reductase
• reduce intrahepatic cholesterol pool
• upregulation of hepatic LDL receptors and removal of LDL from bloodstream

Question 2

Indication for “statins”

Atorvastatin (Lipitor)

Rosuvastatin (Crestor)

Simvastatin

Fluvastatin

Lovastatin

Pravastatin

Answer 2

First line: Hyperlipidemia, dyslipidemia, hypertriglyceridemia

High intensity statin

• LDL >190

Moderate intensity statin

• diabetes
• prevention of CVD
• reduce risk of ASCVD

Question 3

Statin Contraindications

Atorvastatin (Lipitor)

Rosuvastatin (Crestor)

Simvastatin

Fluvastatin

Lovastatin

Pravastatin

Answer 3

Liver disease

Pregnancy

Question 4

Statin Side Effects

Atorvastatin (Lipitor)

Rosuvastatin (Crestor)

Simvastatin

Fluvastatin

Lovastatin

Pravastatin

Answer 4

Myalgias (muscle aches) (1/20)

Myopathy (muscle weakness) (1/2000)

Abnormal LFTs

Diarrhea

Question 5

Atorvastatin route/dose

Answer 5

Oral

High Intensity (40-80 mg)

Moderate Intensity (10-20 mg)

Question 6

Rosuvastatin route/dose

Answer 6

Oral

High Intensity (20-40 mg)

Moderate Intensity (5-10 mg)

Question 7

Tell patients: Do not take statin medication with ____.

Answer 7

grapefruit juice

Question 8

Class and MOA of Fenofibrate (Tricor)

Answer 8

Fibrates

Lower TG and Increase HDL-C

• Blocks VLDL production
• Activates LPL (Increasing lipolysis)
• Reduces apoCIII (LPL inhibitor)

Question 9

Class and MOA of Gemfibrozil

Answer 9

Fibrates

Lower TG and Increase HDL-C

• Blocks VLDL production
• Activates LPL (Increasing lipolysis)
• Reduces apoCIII (LPL inhibitor)

Question 10

Indication for Fibrates

Answer 10

Hypertriglyceridemia

• TG >400-500 mg/dL
• low HDL-C + high TG

Question 11

Contraindications for Fibrates

Answer 11

Liver disease

severe kidney disease

gall stones

pregnancy

Caution with statins and in elderly

Question 12

Fibrates Side Effects

Answer 12

Abdominal pain

Gall stones

Increased Creatinine (secretion, not GFR reduction)

Myalgia/Myopathy (especially with statins)

Question 13

Bile acid resins/ Sequestrants Class and MOA

Answer 13

Cholesterol absorption inhibitors

Lower LDL Cholesterol

• Blocks reabsorption of bile salts in terminal ileum
• Reduces intrahepatic cholesterol pool
• Upregulation of hepatic LDL receptors
• Removes LDL from the bloodstream

Question 14

Ezetimibe (Zetia) Class and MOA

Answer 14

Azetidinone (cholesterol absorption inhibitor)

Lower LDL Cholesterol

• Blocks absorption of cholesterol in the jejunum by inhibiting NPC1L1 protein- goes out in stool

Question 15

Indication for Cholesterol Absorption Inhibitors

Answer 15

Hyperlipidemia

Use in combo w/ statin due to compensatory increase in HMG-CoA which limits effectiveness as monotherapy

Question 16

Contraindications for Cholesterol Absorption Inhibitors

Answer 16

Elevated TG (>200 mg/dL)

multiple complex medication regimens

Bowel or Biliary Obstruction

Pregnancy

Liver disease

Question 17

Cholesterol Absorption Inhibitor Side Effects

Answer 17

Abdominal discomfort

Constipation

Decre absorption of other drugs

Reduced absorption of fat soluble vitamins (A,D,E,K)

Question 18

Proprotein Convertase Subtilsin/Kexin Type 9

(PSCK9 Inhibitor) MOA

Answer 18

Lowers LDL-C

• Blocks PSCK9
• Prevents from tagging –> LDL doesn’t get tagged for breakdown and allows body to recycle LDL receptors

Question 19

PSCK9 inhibitor Route

Answer 19

SubQ

Question 20

Niacin (Niaspan) Class and MOA

Answer 20

Nicotinic Acid, Vitamin B3

Lower TG and Increase HDL-C

• decrease lipolysis from adiposites
• decrease VLDL synthesis
• decrease Apo A-1 catabolism
• increase cholesterol removal from HDL (decreasing breakdown of HDL)

Question 21

Niacin Indication

Answer 21

Hypertriglyceridemia

Hypercholesterolemia/mixed hyperlipidemia

Question 22

Niacin Contraindications

Answer 22

Liver disease

Gout

Uncontrolled DM2

Question 23

Niacin Side Effects

Answer 23

Flushing and Itching- reduced with aspirin taken 30 min prior

Abdominal pain/ulcers

Insulin resistance/Hyperglycemia

Hepatotoxicity

Gout

Myalgia/Myopathy (especially with statins)

Question 24

Fish Oils (Omega-3 Fatty Acids) MOA

Answer 24

Lower TG and Increase HDL-C

• Decr VLDL production
• Decr lipolysis in adipocytes
• Decr TG synthesis