Cholesterol meds Flashcards
Which enzyme makes more cholesterol?
HMG-CoA reductase
Which lipoproteins contribute to atherosclerosis?
LDL; deliver cholesterol to non hepatic tissue
Which lipoprotein protects against atherosclerosis?
HDL
What does very low density lipoprotein do (VLDL) do?
delivers triglycerides to non hepatic tissue
What non therapeutic interventions should pts try first before meds?
diet modification, exercise, quit smoking, manage DM and HTN, med compliant
MOA of statins?
- Inhibit HMG-CoA reductase
- increase # of LDL receptors on hepatic cells
Statin uses?
- lower LDL and total cholesterol
- can raise HDL and lower TG in some patients
T/F. Statins have a heavy 1st pass effect?
True
Which enzyme metabolizes statins?
CYP3A4 (the 3A4 is isoenzyme of cytochrome P450)
Adverse effects of statins?
- myopathy/rhabdo
- hepatotoxicity
- new onset diabetes, memory loss, and cataracts
How do CYP3A4 inhibitors and grapefruit juice interact with statins?
Will suppress the enzyme that metabolizes the med → increasing levels in the bloodstream
What are some CYP3A4 inhibitors?
- Macrolide abx: erythromycin
- Azole antifungal drugs
- HIV protease inhibitors
- Amiodarone
- Cyclosporine (immunosuppressant)
Statins are contraindicated in?
pregnancy and liver failure
Which labs should be monitored before administering statins?
lipid panel, baseline LFTs and CK level
What is a CK level?
creatinine kinase: biomarker for msl injury
Be cautious when taking statins with what other lipid lowering agents d/t risk of liver damage?
ezetimibe or fibrates
When giving statins we should monitor for development of which complications?
gallstones, myopathy, and liver disease
What are bile acid sequestrants?
reduce LDL levels typically used as adjuncts to statins
What is the prototype for bile acid acid sequestrants?
Colesevelam (Welchol)
MOA of Colesevelam?
- Increase LDL receptors on hepatocytes
- actively binding to bile acids to prevent its reabsorption in the intestines.
- Need cholesterol to make bile
- Low levels of bile acids will results in increase cholesterol in the liver to be and increase receptor site → less LDL in the blood stream
Adverse effects of Colesevelam?
Slight constipation
Which older agents affect vitamin absorption and worsening constipation?
Cholestyramine and colestipol
Bile acid sequestrants should not be taken at the same time as what other drugs?
thiazide diuretics, digoxin, warfarin, and some abx
If taking bile acid sequestrants with meds that have a drug interaction when should it be taken?
other meds 1 hour before or 4 hours after
Bile acid sequestrants are contraindicated in?
liver failure, severe renal dysfunction, and gallbladder disease
Which labs should be checked before administering bile acid sequestrants?
lipid panel
How to limit esophageal irritation and impaction when taking bile acid sequestrants?
If powder or granules, mix with water, soup, fruit juice, or applesauce
MOA of Ezetimibe?
- acts on small intestines to inhibit dietary cholesterol absorption.
- prevents reabsorption of cholesterol secreted in the bile.
- can produce a small increase in HDL
Can Ezetimibe be taken with a statin?
Yes or alone
Ezetimibe adverse effects?
- gall stones if combined with fibrates
- can increase the risk of liver damage if combined with statins
Fibrate uses?
reduce VLDLs and may have slight increase in HDLs
Prototype for fibrates?
Gemifibrozil
Adverse effects of Gemifibrozil?
Rash, GI disturbances, gallstones, hepatotoxicity, myopathy
Possible side effect of Gemifibrozil if taken with warfarin?
Increase bleeding
Possible side effect of Gemifibrozil if taken with statins?
rhabdomyolysis
What labs should be checked prior to administration of Gemifibrozil?
lipid panel and LFTs
Gemifibrozil is contraindicated in?
liver failure, severe renal dysfunction, and gallbladder disease
When should Gemifibrozil be taken?
30 minutes before morning and evening meals
Which bile acid sequestrant does not affect vitamin absorption?
Colesevelam (Welchol)
Which bile acid sequestrants cause fat-soluble vitamin deficiency?
Cholestyramine and colestipol
