Drugs used in hyperlipidemias Flashcards
1
Q
HMG-CoA reductase inhibitors
A
Known as Statins:
- Lovastatin (prodrug)
- Simvastatin (prodrug)
- Pravastatin
- Atorvastatin
- Fluvastatin
- Pitavastatin
- Rosuvastatin
2
Q
Statins; mechanism
A
- Site of action: liver
- Analogs of HMG
- Competitively inhibit mevalonate synthesis, a step in production of cholesterol
- Liver compensates by increasing LDL-receptors, which clear LDL from blood
- Can also increase HDL and decrease triglyceride levels
- Atorvastatin have the highest efficacy
3
Q
Statins; indication
A
- Reduce risk of coronary events and mortality in patients with ischemic heart disease
- Effective in lowering cholesterol levels in all type of hyperlipidemias (except homozygous familial hypercholesterolemia)
- May increase warfarin levels
- Contraindicated in pregnancy and nursing mothers
4
Q
Resins
A
- Cholestyramine
- Colestipol
- Colesevalam
5
Q
Resins; mechanism
A
- Bind to bile acids and similar steroids in intestine
- By reducing absorption of dietary cholesterol and reabsorption of bile acids, hepatic cholesterol are diverted to produce new bile acids –> lower amount of cholesterol
- Liver compensates by increasing LDL-receptors, which clear LDL from blood
6
Q
Resins; indication
A
- Drugs of choice in treating type IIA (familial hypercholesterolemia) and type IIB (familial combine hyperlipidemia) hyperlipidemias
- Can also relieve pruritus
- Also used to treat diarrhea
7
Q
Resins; indication
A
- Used in patients with hypercholesterolemia
- Drugs of choice in treating type IIA (familial hypercholesterolemia) and type IIB (familial combine hyperlipidemia) hyperlipidemias
- Can also relieve pruritus
- Also used to treat diarrhea
- Adverse effects; bloating, constipation, and an unpleasant gritty taste. Impaired absorption of vitamins and drugs
8
Q
Ezetimibe; mechanism
A
- Cholesterol absorption inhibitor
- Prodrug
- Prevent GI uptake of cholesterol and phytosterols
- Liver compensates by increasing LDL-receptors, which clear LDL from blood
- Also decrease triglycerides and elevate HDL levels
9
Q
Ezetimibe; indications
A
- Used to treat hypercholesterolemia and phytosterolemia
10
Q
Niacin; mechansim
A
- Directly reduces secretion of VLDL from liver
- Inhibits lipolysis in adipose tissue –> decrease circulating free fatty acids
- Inhibits hepatic synthesis of apolipoproteins or cholesterol
- Consequently, LDL formation is reduced
- Increased clearance of VLDL by lipoprotein lipase in the periphery has also been demonstrated
- As a result, both triglyceride and cholesterol are lowered
- Most effective agent to increase HDL levels
- Also decreases circulating fibrinogen and increases t-PA
11
Q
Niacin; indications
A
- Since it lower both triglycerides and cholesterol, and increase HDL, it has wide clinical utility
- Particularly useful in treatment in familial hyperlipidemias
- Adverse effects; intense cutaneous flush, pruritus, nausea, abdominal discomfort, hyperuricemia, glucose intolerance
12
Q
Fibric acid derivatives
A
- Gemfobrizil, Fenofibrate, Clofibrate
13
Q
Fibrates; mechanism
A
- They are ligands for the peroxisome proliferator-activated receptor-α (PPAR-α) protein
- PPAR-α is a receptor that regulates transcription of genes involved in lipid metabolism
- Results in increased activity of lipoprotein lipase and enhanced clearance of triglyceride-rich lipoproteins
- Reduce serum triglycerides, small reduction in LDL and small increase in HDL
14
Q
Fibrates; indications
A
- Used in treatment of hypertriglyceridemias
- Particularly useful in treating type III (familial dysbetalipoproteinemia)
- Adverse effects; nausea, skin rashes, cholelithiasis
15
Q
Treatment for type IIA (familial hypercholesterolemia)
A
- Block in LDL degradation
1. Cholestyramine and niacin
2. Statin
