Antihyperlilpidemic (Dyslipidemia) Drugs
Terms
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- complexes of cholesterol, TGs, and protein used to transport cholesterol from the liver to peripheral cells and back.
- lipoproteins
- transports fatty acids and cholesterol derived from the diet or synthesized in the intestine from the gut to the liver
- chylomicrons
-
- formed mainly in the liver
- transports endogenous TGs and cholesterol
- contains 15-20% of the total blood cholesterol and most of the TGs measured in the fasting pt - VLDLs
- the cholesterol in VLDL is about ___ of total TG conc
- 1/5
-
- formed by VLDL catabolism
- transports (60-70%) of cholesterol to the cells
- greatest contribution to the development of artherosclerosis
- main target of cholesterol lowering drugs - LDLs
-
- formed in the liver and intestine
- transports cholesterol from peripheral cells to the liver - HDLs
- a ___ hr fast is req'd to measure cholesterol
- 12
- TG level must be < ___ to measure cholesterol
- 400 mg/dL
- total cholesterol - (HDL + VLDL) = ___
- LDL
- what is not directly measured with a cholesterol measurement
- VLDL (TG/5) and LDL (cholesterol - HDL and VLDL)
- Type I hyperlipoproteinemia
- elevated chylomicrons
- Type IIa hyperlipoproteinemia
- elevated LDL
- Type IIb hyperlipoproteinemia
- elevated LDL and VLDL
- Type III hyperlipoproteinemia
- elevated IDL
- Type IV hyperlipoproteinemia
- elevated VLDL
- Type V hyperlipoproteinemia
- elevated VLDL and chylomicrons
- MC lipid abnormality
- polygenic hypercholesterolemia
- according to ATP III classification, what are goals for LDL, HDL, TG, and total cholesterol levels?
-
LDL < 100 mg/dL
HDL 40-60 mg/dL
TG < 150 mg/dL
Total cholesterol <200 - three categories of risk that modify LDL goals
-
(1) CHD and Diabetes < 100 mg/dL
(2) 2+ risk factors < 130 mg/dL
(3) <2 risk factors < 160 mg/dL - major risk factors
-
- cigarettes
- HTN (>140/90 mmHg)
- low HDLs (<40 mg/dL)
- FamHx of premature CHD
- men >45 y/o women >55 y/o - HMG CoA Reductase Inhibitors
- "-statins"
- contraindications for statins
-
absolute: liver dz
relative: drugs that inhibit P450 3A4 (macrolides, CCBs, and azole antifungals) - BCF statin
- Simvastatin
- most efficacious statins (2)
- atorvastatin and rosuvastatin
- statins that can be dosed anytime
- atorvastatin and rosuvastatin
- statins that can be used w/ renal insufficiency
- atorvastatin and fluvastatin
- statins that are not affected by C P450 drug interactions
- pravastatin and fluvastatin
- statin not highly protein bound
- pravastatin
- statin assoc w/ rhabdomyolysis or myopathy when combined w/ fibric acid
- lovastatin
- what must be monitored when administering statins?
-
CPK (myopathy and rhabdomyolysis)
LFTs (obtain baseline and repeat q 6 mos) - how long in between dosing changes w/ statins?
- 6 wks
- which antihyperlipid drug class if liver dysfunction is present?
- bile acid sequestrants (BAS)
- what are SEs of BAS agents?
-
- GI distress/constipation
- decreased absorption of other drugs - MOA of BAS agents
- more cholesterol gets converted into bile acids
- how long between BAS agents and fat-soluble vits, folic and ascorbic acid?
- 6 hrs
-
colestipol (colestid) BCF
cholestyramine (questran)
colesevelam (welchol) - bile acid sequestrants
- which antihyperlipid class is last line due to GI side effects?
- BAS
- which BAS agent reqs the smallest dose (best for pt compliance)?
- colesevelam
- which antihyperlipid class is DoC for pregnancy?
- BAS
- demonstrated therapeutic benefits of BAS incl:
-
- reduce major coronary events
- reduce CHD mortality
- only approved agent in pregnancy - MOA of nicotinic acid (niacin)
- reduces VLDLs resulting in reduced LDLs
- what is best antihyperlipid agent for increasing HDLs?
- nicotinic acid (niacin)
- what are SEs of Niacin?
-
- flushing and itching
- hyperglycemia
- hyperuricemia
- upper GI stress
- hepatotoxicity - how can flushing and itching assoc w/ niacin be minimized?
-
- ASA 30 min prior
- take w/ meals
- titrate up slowly
- use controlled release products - CIs for Niacin use:
-
- liver dz
- PUD
- hypersensitivity
- caution w/ statins (myopathy and rhabdomyolysis) - MOA of Fibric acids
- stimulates lipoprotein lipase which removes chyolmicrons and VLDLs from plasma
- what is best agents for decreasing TGs?
- fibric acids
- what happens to VLDLs when they are catabolized by lipases?
- broken down into IDLs and LDLs
- SEs of fibric acids:
-
- GI distress
- gallstones (Lithiasis)
- myopathy and muscle inflammation - CIs of Fibric Acids
-
- severe renal dz
- severe liver dz
- caution w/ statins (myopathy and rhabdomyolysis) - therapeutic benefits of fibric acids
-
- reduce progression of coronary lesions
- reduce major coronary events - Ezetimibe (Zetia)
- Selective Cholesterol Absorption Inhibitor
- lower doses of statins may be possible during combined therapy with:
- Ezetimibe (Zetia)
- antihyperlipidemic approved for children 10-18 y/o
- Ezetimibe (Zetia)
- tx for hypertriglyceridemia
- niacin, fibrates, and atorvastatin
- in txing hyper-TGs, avoid ___ in diabetics and ___ in high LDL pts
- niacin; fibrates
- stop HMG-CoA reductase inhibitor medication if LFT levels go to ___x the normal upper limit
- 3x