Lipid Deck 2 Flashcards
Fibrates MOA
Inhibition of cholesterol synthesis
Decreased triglyceride synthesis
Inhibition of lipolysis in adipose tissue
Decreased production of VLDL/increased clearance
Increased plasma and hepatic lipoprotein lipase (LPL) activity
Fibrates effect on lipids
Decreases: total cholesterol (TC), LDL, TGs
Increases: HDL
Fibric acid derivatives are effective TG-lowering drugs that may modestly lower LDL and raise HDL for some patients. Because these drugs usually do not produce
substantial reductions in LDL cholesterol, they are not appropriate for first-line lowering of LDL levels unless the patient is statin-intolerant. They also have a role in familial hypercholesterolemia.
Fibrate Effective
TG-lowering drugs that modestly lower LDL and raise HDL for only some patients
Fibrates work for patients with
very high TG levels, such as patients with type 2 diabetes and patients with familial dysbetalipoproteinemia.
Fibrates do not produce substantial reduction in
LDL, so are not appropriate as initial or monotherapy.
Fibreates ADR
nausea, diarrhea, cholelithiasis, phototoxicity
Fibric acid derivatives do have a significant
gastrointestinal (GI) side effect profile
Fibrate dug interactions
Increased risk of hepatotoxicity and/or myalgias with concurrent statins and/or niacin
Protein-binding displacement (e.g., warfarin)
Fibrates Monitoring
Lipid levels in 4 to 6 weeks, then every 3 to 4 months until control established
LDL levels will drop when triglycerides drop
LFTs before starting and as needed
Fibrate ADR incldues
constipation and flatulence
Bile Acid Sequestrants (BAS)
By promoting an increase in bile acid excretion, they enhance conversion of cholesterol to bile acids by the liver and increase uptake of LDL
BAS bind with cholesterol in the intestine and are NOT
metabolized by the liver
BAS are excreted in
bound form in the feces
BAS may use with patients with
active liver disease
BAS lower and increase
Lower TC, LDL, and TG, and increase HDL, in theory
BAS have a strong record for
efficacy and safety
BAS are most useful for patients with
moderately elevated LDL levels and low coronary heart disease (CHD) risk profile
BAS patients who are not able to re
to reduce their LDLs with lifestyle modifications
BAS can be used together with
fibrates
BAS ADR
GI – constipation, bloating, abdominal pain, unpleasant taste and texture; HA
BAS reduced ___ with long trerm use
folate levels
BAS initial dose
one packet mixed with juice; never swallowed in dry form
BAS interactionos
Interfere with absorption of other medications
BAS Monitoring
lipid levels
bowel issues
BAS patient education
Taken with meals mixed with 4 to 6 ounces of fluid
Other Drug absorption impaired if taken at same time
BAS ADRs
constipation, may need stool softeners
BAS never
swallow in dry form
Niacin no longer
approved by the U.S. Food and Drug Administration (FDA) for use in lipid management
Niacin previous touted effects
on lipids
Lower TC, LDL, and TG, and elevate HDL
Niacin increased risk of
CV events if taken at doses to change lipids. Adverse events stronger than any benefit!
Ezetimibe (Zetia) MOA
Selectively inhibits intestinal absorption of cholesterol and related phytosterols
Ezetimibe has been shown to reduce
reduce total cholesterol, LDL, and TG while increasing HDL-C
Ezetimibe no good
outcome data yet, but most effective in combination with statin
Ezetimibe dosing
10 mg/day
Ezetimibe pregnancy category
category C; not for children younger than 10 years of age
