Dyslipidemia Flashcards
What is the MOA for statins?
They inhibit HMG-CoA reductase, a vital step in cholesterol synthesis. The liver then increases cholesterol uptake by increasing the number of LDL receptors
Statin: indications?
First-line therapy for primary and secondary prevention of ASCVD
Familial hypercholesterolemia
Statin: contraindications?
Active liver disease, pregnancy (cat. X), breast feeding
Statin: side effects?
Myopathy, increase in liver enzymes, nausea, ha
Statin: onset?
Varies, peak effect in a few weeks
Statin: interactions?
Red yeast rice (redundant), Niacin, alcohol, grapefruit, st. john’s wort, sweet orange
Ezetimibe: MOA?
Prevents absorption of dietary and biliary cholesterol
Ezetimibe: indications?
Adjunctive therapy in homozygous familial hypercholesterolemia and primary hyperlipidemia
Typically used when statin intolerant
Ezetimibe: contraindications?
Pregnancy (cat. C) or breast feeding
Ezetimibe: side effects?
Increase in liver enzymes
Ezetimibe: metabolism?
~30% undergoes glucuronide conjugation in the SI and liver
Ezetimibe: interactions
It would lower effectiveness of green tea, O3FA, sitostanol and beta-sitosterol
Fibrates: MOA?
Lower production and increased clearance of VLDL
Increased HDL production
Lowers TG
Fibrates: indications?
Hypercholesterolemia or mixed dyslipidemia as adjunct therapy or monotherapy in pts who can’t tolerate statins
Hypertriglyceridemia first-line pharmacotherapy
Fibrates: contraindications?
Active liver disease, severe renal impairment or ESRD and pre-existing GB disease, and breast feeding
Fibrates: side effects?
Dyspepsia, gallstones, myopathy (increased risk with statins)
Fibrates: interactions?
Red yeast rice, niacin, alcohol
Gemfibrozil increases risk for what side effect when used with statin therapy? and how can we assess severity of this effect?
Myopathy
CK
Niacin: MOA?
Unclear, but..it increases lipoprotein lipase activity, enhancing removal of triglycerides from plasma.
Reduces TG synthesis
Increases HDL-C levels
Niacin: indications?
Hypercholesterolemia or mixed dyslipidemia as adjunct therapy for pts who do not tolerate fibrates or O3FA, or as monotherapy for pts who do not tolerate statins, BAS, or fibrates
Hypertriglyceridemia second-line pharmacotherapy
Niacin: contraindications?
Active liver disease, gout, peptic ulcer disease
Niacin: side effects?
Hepatotoxicity, hyperglycemia, hyperuricemia, upper GI distress, flushing itching
Niacin: interactions?
Red yeast rice, alcohol
Niacin causes flushing, the extended release form has less flushing as a side effect. However, it is not used very often because of an increased risk for what major side effect?
Hepatotoxicity > Acute necrosis
Omega-3 fatty acids: MOA?
Inhibits the release of FA from adipose tissue. Inhibits beta oxidation of hepatic FA. Inhibits FA synthesis Increases VLDL clearance Lowers TG and increases HDL
Omega-3 fatty acids: indications?
Hypertriglyceridemia second-line pharmacotherapy
Omega-3 fatty acids: contraindications?
Hypersensitivity to fish oil
Omega-3 fatty acids: side effects?
Eructation, nausea, dyspepsia, taste changes, and may increase bleeding time.
Bile Acid Sequestrants (BAS): MOA?
Resins bind bile acid in the intestine. This reduces enterohepatic recycling.
Increases hepatic conversion of cholesterol to bile acid. Up regulates LDL receptors on the liver
Bile Acid Sequestrants (BAS): indications?
Hypercholesterolemia for high risk patient who are statin-intolerant or are on maximal tolerated doses of statins
Bile Acid Sequestrants (BAS): contraindications?
TG > 300 mg/dL
complete biliary obstruction
Bile Acid Sequestrants (BAS): side effects?
Constipation, abdominal discomfort, intestinal gas, dyspepsia, heartburn, diarrhea
BAS and ezetimibe both work in the intestine to lower absorption of cholesterol. What change occurs in the liver to lower LDL?
Increase in LDL receptors
Bile Acid Sequestrants (BAS): interactions?
Niacin absorption may be hindered
