Hyperlipidemia Drugs Flashcards
1
Q
Hypertriglyceridemia
A
- increased CHD (coronary heart disease) risk associated with TG > 150 mg/dl
- elevated triglycerides can lead to pancreatitis (>500 mg/dl)
2
Q
Hypercholesterolemia and Atherosclerosis Risk Indicators
A
- LDL-C
- Apo B100
- Non HDL-C
3
Q
Total Cholesterol Levels
A
-Desirable (240 mg/dl)
4
Q
HDL-C Levels
A
-Low (60 mg/dl)
5
Q
LDL-C
A
-Optimal for very high risk (190)
6
Q
Triglycerides
A
-Normal (500 … can lead to pancreatitis)
7
Q
Recommendations for Statin Therapy
A
- individuals with clinical ASCVD (arteriosclerotic cardiovascular disease)
- individuals with primary elevations of LDL-C (>190 mg/dl)
- individuals 40 to 75 years of age with diabetes with LDL-C 70-189 mg/dl
- individuals without clinical ASCVD or diabetes who are 40 to 75 years of age with LDL-C 70-189 mg/dl and an estimated 10 year ASCVD risk of 7.5% or higher
8
Q
Familial Hypercholesterolemia
A
- LDL receptors genetically defective in liver
- increased LDL levels in blood
- treated with bile acid binding resin and an inhibitor of HMG-CoA reductase
9
Q
Rationale for the use of bile acid binding resin and HMG-CoA inhibitor for FH heterozygotes
A
- reduces production of cholesterol
- increased cholesterol uptake from LDL binding to liver
- increased cholesterol secretion into intestines via bile acids
10
Q
Statins: Mechanism of Action
A
- competitive inhibitors of HMG-CoA reductase
- inhibit cholesterolgenesis
- increase expression of LDL receptor
- increase removal of LDL (VLDL, IDL) from blood
- decrease hepatic VLDL production
- TG levels >250 mg/dl reduced by statins
- HDL-C levels: some studies show slight increase
- LDL-C Levels: lower by 20%-55% (dose dependent)
11
Q
Statins: Pharmacokinetics
A
- Lovastatin and Simvastatin are inactive lactone prodrugs, hydrolyzed to active form in liver
- absorption varies from 40% to 75% except for fluvastatin (almost complete)
- absorption is enhanced by food
- high first pass extraction by liver
- most absorbed dose excreted in bile as metabolites
- 5% to 30% excreted in urine (statin-dependent)
- half-lives: 1-3 hrs except for atorvastatin (14 hrs) and rosuvastatin (19 hrs)
- hepatic cholesterol biosynthesis maximal midnight - 2 am, take in evening (except ones with long half-lives)
12
Q
Statins: Therapeutic Use
A
- alone or in combination with resins, niacin, or ezetimibe
- contraindicated in pregnancy, lactating, or likely to become pregnant
- some approved for children with FH hypercholesterolemia
13
Q
Lovastatin
A
-HMG-CoA Reductase Inhibitor (statin)
14
Q
Atorvastatin
A
- HMG-CoA Reductase Inhibitor (statin)
- longer half-life (14 hours), so doesn’t have to be dosed in the evenings
- most efficacious agent for severe hypercholesterolemia (along with rosuvastatin)
- more TG lowering activity compared to other statins
15
Q
Fluvastatin
A
-HMG-CoA Reductase Inhibitor (statin)