Pharmacology (Cholesterol, TG) Flashcards
Class and MOA of:
Atorvastatin (Lipitor)
Rosuvastatin (Crestor)
Simvastatin
Fluvastatin
Lovastatin
Pravastatin
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
Indication for “statins”
Atorvastatin (Lipitor)
Rosuvastatin (Crestor)
Simvastatin
Fluvastatin
Lovastatin
Pravastatin
First line: Hyperlipidemia, dyslipidemia, hypertriglyceridemia
High intensity statin
- LDL >190
Moderate intensity statin
- diabetes
- prevention of CVD
- reduce risk of ASCVD
Statin Contraindications
Atorvastatin (Lipitor)
Rosuvastatin (Crestor)
Simvastatin
Fluvastatin
Lovastatin
Pravastatin
Liver disease
Pregnancy
Statin Side Effects
Atorvastatin (Lipitor)
Rosuvastatin (Crestor)
Simvastatin
Fluvastatin
Lovastatin
Pravastatin
Myalgias (muscle aches) (1/20)
Myopathy (muscle weakness) (1/2000)
Abnormal LFTs
Diarrhea
Atorvastatin route/dose
Oral
High Intensity (40-80 mg)
Moderate Intensity (10-20 mg)
Rosuvastatin route/dose
Oral
High Intensity (20-40 mg)
Moderate Intensity (5-10 mg)
Tell patients: Do not take statin medication with ____.
grapefruit juice
Class and MOA of Fenofibrate (Tricor)
Fibrates
Lower TG and Increase HDL-C
- Blocks VLDL production
- Activates LPL (Increasing lipolysis)
- Reduces apoCIII (LPL inhibitor)
Class and MOA of Gemfibrozil
Fibrates
Lower TG and Increase HDL-C
- Blocks VLDL production
- Activates LPL (Increasing lipolysis)
- Reduces apoCIII (LPL inhibitor)
Indication for Fibrates
Hypertriglyceridemia
- TG >400-500 mg/dL
- low HDL-C + high TG
Contraindications for Fibrates
Liver disease
severe kidney disease
gall stones
pregnancy
Caution with statins and in elderly
Fibrates Side Effects
Abdominal pain
Gall stones
Increased Creatinine (secretion, not GFR reduction)
Myalgia/Myopathy (especially with statins)
Bile acid resins/ Sequestrants Class and MOA
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
Ezetimibe (Zetia) Class and MOA
Azetidinone (cholesterol absorption inhibitor)
Lower LDL Cholesterol
- Blocks absorption of cholesterol in the jejunum by inhibiting NPC1L1 protein- goes out in stool
Indication for Cholesterol Absorption Inhibitors
Hyperlipidemia
Use in combo w/ statin due to compensatory increase in HMG-CoA which limits effectiveness as monotherapy
Contraindications for Cholesterol Absorption Inhibitors
Elevated TG (>200 mg/dL)
multiple complex medication regimens
Bowel or Biliary Obstruction
Pregnancy
Liver disease
Cholesterol Absorption Inhibitor Side Effects
Abdominal discomfort
Constipation
Decre absorption of other drugs
Reduced absorption of fat soluble vitamins (A,D,E,K)
Proprotein Convertase Subtilsin/Kexin Type 9
(PSCK9 Inhibitor) MOA
Lowers LDL-C
- Blocks PSCK9
- Prevents from tagging –> LDL doesn’t get tagged for breakdown and allows body to recycle LDL receptors
PSCK9 inhibitor Route
SubQ
Niacin (Niaspan) Class and MOA
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)
Niacin Indication
Hypertriglyceridemia
Hypercholesterolemia/mixed hyperlipidemia
Niacin Contraindications
Liver disease
Gout
Uncontrolled DM2
Niacin Side Effects
Flushing and Itching- reduced with aspirin taken 30 min prior
Abdominal pain/ulcers
Insulin resistance/Hyperglycemia
Hepatotoxicity
Gout
Myalgia/Myopathy (especially with statins)
Fish Oils (Omega-3 Fatty Acids) MOA
Lower TG and Increase HDL-C
- Decr VLDL production
- Decr lipolysis in adipocytes
- Decr TG synthesis
