lipid lowering drugs

Question 1

what do lipid lowering drugs do

Answer 1

reduce change of atherosclerosis

Question 2

atherosclerosis

Answer 2

reduction in blood flow due to plaque buildup in arteries
- body produce too much fat
- damage endothelial cells, platelets activate and aggravate (could lead to complete occlusion)

Question 3

primary forms of lipid in blood

Answer 3

triglycerides and cholesterol
- water insoluble fats must be packaged for transport in blood

Question 4

what are transport mechanisms for fats

Answer 4

lipoproteins (fats and proteins)

Question 5

lipoprotein examples

Answer 5

chylomicrons - GI tract
VLDL (very low density) - produced by liver, transport TGs

LDL: less desired, bad cholesterol

HDH: highly desired
- recycling of cholesterol

Question 6

CAD (coronary artery disease)

Answer 6

caused by atherosclerosis
- unstable/stable angina
- MI

non modifiable risk factors
- age
- family history

modifiable risk factors
- smoking
- obesity
- hypertension
- DM
- LDL/HDL ratio

Question 7

4 groups of lipid lowering drugs

Answer 7

HMG-CoA reductase inhibitors (HMGs or statins)

inhibitors of cholesterol absorption, niacin, fibric acid derivatives

Question 8

HMG-CoA

Answer 8

3-hydroxy-3-methylglutaryl coenzyme A
- one of the metabolites in the cholesterol synthesis pathway

Question 9

HMG-CoA reductase

Answer 9

enzyme for liver cholesterol production (LDL)

Question 10

HMG-CoA reductase inhibitors

Answer 10

reduce plasma LDL levels
statins
- atorvastatin
- rosuvastatin
- lovastatin
- simvastatin

Question 11

HMG-CoA reductase inhibitors mechanism of action

Answer 11

• inhibit HMG-CoA reductase which produces cholesterol
• lower rate of cholesterol production
• causes increased liver LDL receptors so the cells take in more LDL and lower levels are in plasma

Question 12

added benefits of statins

Answer 12

• decrease VLDL
• raises HDL (improves LDL/HDL ratio)

Question 13

HMG-CoA reductase inhibitors indications

Answer 13

• firstline drug therapy for hypercholesterolemia
• treatment of types IIa and IIb hyperlipidemias (high LDL)

Question 14

HMG-CoA reductase inhibitors adverse effects

Answer 14

• mild, transient GI disturbances, headache
• muscle pain (myalgia), muscle breakdown (rhabdomyolysis)
• liver injury (elevations in liver enzymes - take care with liver dysfunction patients)
• not used in pregnancy

Question 15

considerations with statins

Answer 15

• rosuvastatin more effective in asians (low dose)
• grapefruit and grapefruit juice: CYP 3A4 inhibition

Question 16

interactions with statins

Answer 16

grapefruit and grapefruit juice

drug inhibitors of CYP3A4: warfarin, erythromycin, ritonavir