Pharmacology and Pharmcotherapy of Lipid Drugs and Disorders 2 Flashcards
What is the most potent oral LDL- lowering agents
Statins
What are the significant health benefits of using statins
significant reduction in coronary heart disease death, nonfatal MI, revascularization procedures, strokes and total mortality
What is the MOA of HMG CoA reductase
Competitively inhibit HMG CoA reductase
T/F: Statins can lower triglycerides due to causing a reduction in hepatocellular cholesterol prompting more LDL receptors on liver and reducing the secretion of VLDL while increasing clearance
True
What are the two main enzymes of the liver that metabolize statins
3A4 and 2C9
What statin would be used if patients can’t handle side effects, why
Pravastatin, has no CYP metabolism
What are the low intensity statins
Pravastatin 10, 20 mg/ Lovastatin 20 mg
What are the moderate intensity statins
Atorvastatin 10 mg/ Rouvastatin 10 mg/ Simvastatin 20 mg, 40 mg/ Pravastatin 40 mg/ Lovastatin 40 mg/ Fluvastatin 40 mg BID
What are the high intensity statins
Atorvastin 40, 80 mg/ Rosuvastatin 20 mg
T/F: Low intensity statins are mostly used to treat hyperlipidemia
False: Low-intensity statins reserved for those who cannot tolerate higher intensity statins
Who would qualify for moderate-intensity doses when high intensity doses would predispose patients to side effects
Greater than 75 years, impaired renal or hepatic impairment, history
T/F: Efficacy is greater when taken in the morning
False: Increased efficacy when taken in the evening to coincide with nighttime upturn in endogenous cholesterol biosynthesis
What are the contraindications for statins
Pregnancy, Lactation, active liver disease
What medications can simvastatin interact with at a maximum dose of 10 mg, 20 mg
Verapamil and Dilitiazem/ Amiodarone, Amlodipine, Ranolazine
What is the most unique adverse effect to statins, what are the other adverse effects
Myalgia and Rhabdomyolysis, headache, fatigue, GI upset
T/F: It is advised to check LFT levels at baseline but not routinely monitored. IF LFTs are high the statin should be decreased or held until normalized
True
If a patient complains about severe muscle symptoms or fatigue possibly due to the statin what should be done
Discontinue Statin
If a patient complains about mild to moderate muscle symptoms or fatigue possibly due to the statin what should be done
Evaluate other risk, discontinue the statin
If the symptoms of mild to moderate muscle fatigue are resolved after a statin is discontinued what further options can be done
Re-initiate same or lower dose of same statin AND if the relationship is casual discontinue and start low dose of different statin till tolerated than gradually increase dose as tolerated
T/F: ASCVD risk reduction benefit outweighs risk of diabetes and cognitive impairment in most patients
True
When a statin is taken a lipid panel is done at baseline when would another one be done after initaition, when is the next after that
Within 4 to 12 weeks, every 3 to 12 months
How much should LDLs reduce due to statin intensity use
Greater than 50% (high intensity), 30% to 50% (moderate intensity)
If a patient is on a high intensity statin what would the LDL level need to be over time in order to consider adding on non-statin cholesterol-lowering medication
Greater than 70 mg/dl
What is the first drug that would be added to a statin in order to lower cholesterol, what is the MOA
Ezetimibe, selectively inhibits absorption of dietary and biliary cholesterol at brush border of intestine
What are the contraindications of ezetimibe
Acute liver disease, pregnancy, lactation
What are the advere effects of using ezetimibe, drug interactions
Diarrhea and Abdominal pain/ Fibrates and Cholestyramine
What do LDL- receptors on the hepatocyte do when LDL binds
Bind to free LDL circulating where they are brought into the cell metabolized to release the LDL-receptor then placed back on the surface
T/F: PCSK9 proteins lead to lower chosterol
T/F: PCSK9 proteins lead to more circulating LDL since it doesn’t allow the LDL to be brought into the hepatocyte by the LDL-Receptors to be metabolized
What type of medication is PCSK9 inhibitors, what is the MOA
Monoclonal antibody, indirectly decreases LDL levels by binding PCSK9 leading to more LDL receptors on hepatocytes
What is a large adverse effect of PCSK9 inhibitors
Decrease in neurocognitive ability
Why are PCSK9 not indicated to be used before ezetimibe
The cost does not outweigh the benefit
What are the bile acid sequestrants
Cholestyramine, Colestipol, Colesevelam
Though patients could add bile acid sequestrants they are not preferred over adding ezetimibe and PCSK9 inhibitors
True
When would fibrates be first line medicationsm what are the fibrates
If the patient has triglycerides over 500 mg/dl/ gemfibrozil, fenofibrate, fenofibric acid
T/F: Niacin can decrease TG and increase HDL but has not proven to reach clinical endpoints and therefore there is no scenario in which a patient would need to use Niacin
True