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Niacin available drugs
- Niacin (generic and sustained-release generic)
- Niaspan (extended release niacin)
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Indication & Role
- Best to increase HDLs 30-40%
- Lowers LDLs 20-30%
- Lowers triglycerides 35-45%
- Only drug that reduces LPa by 40%
- Reduces Cardiovascular events
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MoA
- Inhibits adipose cells triglycerides (TGCs) lipolysis, decreasing hepatic glyceride synthesis.
- May inhibit rate limiting enzyme in TGCs synthesis
- In liver inhibits synthesis & esterification of FAs.
- Decreases clearance of apoAI in HDL increasing HDLs
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RoA
Orally in short acting or sustained release preps.
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1. Absorption
2. Distribution
3. Metabolism
4. Elimination
- 1. Well absorbed orally
- 2. Peak [plasma] (PPC) 30-60 min.
- 3. 1/2 life 60 min.
- 4. Taken up by liver, excess excreted in urine
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Common SEs
- Hepatotoxicity indicated by >50% reduction in LDLs
- Cutaneous effects flushing and pruritis of the face
- Upper trunk
- Skin rashes
- Acanthosis nigricans
- Flushing and associated pruritis are prostaglandin mediated thus concomitant aspirin usage may alleviate it.
- Dyspepsia
- Rarely nausea, vomiting, and diarrhea (N/V/D)
- DM pts niacin can induce insulin resistance with resultant hyperglycemia.
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Clinical Use
- Pts that don't tolerate statins.
- Increase dose slowly.
- Monitor w/in a few weeks for signs of hepatic toxicity or hyperglycemia.
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