nicotinic acid (niacin, vitamin B3, Niaspan)

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Pathology

  • deficiency of nicotinic acid (niacin) is pellagra

Indications

* may not be useful as adjunct therapy in patients with hyperlipidemia

* lowers risk of non-fatal myocardial infarction or non-fatal stroke in patients not taking statins[17]

* does not lower risk of fatal myocardial infarctions, fatal stroke or all-cause mortality in patients taking statins[17]

Contraindications

* sustained-release niacin[14][16] combined with laropriant[16]

pregnancy category = c

safety in lactation = ?

Dosage

-..........-

 Schedule A:
    1st week:  100 mg PO TID
    2nd week:  200 mg PO TID
    3rd week:  300 mg PO TID
    4th week:  400 mg PO TID
    5th week:  500 mg PO TID
    6th week:  600 mg PO TID
    7th week:  700 mg PO TID
    8th week:  800 mg PO TID
    9th week:  900 mg PO TID
   10th week: 1000 mg PO TID
 Schedule B:
    1st week:  200 mg PO TID
    2nd week:  400 mg PO TID
    3rd week:  600 mg PO TID
    4th week:  800 mg PO TID
    5th week: 1000 mg PO TID
    6th week: 1200 mg PO TID
    7th week: 1400 mg PO TID
    8th week: 1600 mg PO TID

Average effective dose: 2.0-2.5 g/day

Max dose: 8 g/day

Capsules: 100 mg, 500 mg

Tablets: 50 mg, 100 mg, 250 mg, 500 mg

Niaspan:

  • sustained release (over 8-12 hours) (QHS)[6]
  • less hepatotoxic than other sustained-release forms[7]
  • may have benefits similar to immediate-release niacin[10]

Pharmacokinetics

elimination via kidney

elimination via liver

1/2life = 45 minutes

Monitor

Adverse effects

* less frequent with sustained-release forms may be minimized by giving 325 mg of aspirin or 200 mg of ibuprofen 30 minutes before niacin

# if dizziness occurs, avoid sudden changes in posture

% niaspan may be less heptatoxic than other sustained-release forms[6]

Drug interactions

Test interactions

Mechanism of action

More general terms

More specific terms

Additional terms

Component of

References

  1. Kaiser Permanente prescriber guidelines, 1999
  2. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  4. Prescriber's Letter 7(2):8, Feb. 2000
  5. Jump up to: 5.0 5.1 5.2 5.3 5.4 5.5 Medical Knowledge Self Assessment Program (MKSAP) 11, 14, 17. American College of Physicians, Philadelphia 1998, 2006, 2015
  6. Jump up to: 6.0 6.1 6.2 Prescriber's Letter 11(5):27 2004 Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=200504&pb=PRL (subscription needed) http://www.prescribersletter.com
  7. Jump up to: 7.0 7.1 Prescriber's Letter 11(5):27 2004 What You Should Know About Niacin Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=211207&pb=PRL (subscription needed) http://www.prescribersletter.com
  8. Jump up to: 8.0 8.1 Prescriber's Letter 14(6): 2007 Niacin Abuse in the Attempt to Alter Urine Drug Tests Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=230606&pb=PRL (subscription needed) http://www.prescribersletter.com
  9. Prescriber's Letter 14(8): 2007 New Niaspan Formulation Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=230808&pb=PRL (subscription needed) http://www.prescribersletter.com
  10. Jump up to: 10.0 10.1 Vogt A et al, Prolonged-release nicotinic acid for the management of dyslipidemia: an update including results from the NAUTILUS study. Vasc Health Risk Manag. 2007;3(4):467-79. PMID: https://www.ncbi.nlm.nih.gov/pubmed/17969377
  11. Prescriber's Letter 16(12): 2009 COMMENTARY: Ezetimibe vs. Niacin for Atherosclerosis: The ARBITER 6-HALTS Study PATIENT HANDOUT: What You Should Know About Niacin Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=251212&pb=PRL (subscription needed) http://www.prescribersletter.com
  12. Prescriber's Letter 17(1): 2010 Second-Line Therapy of Dyslipidemia RESOURCE: Niacin Titration Schedule PATIENT HANDOUT: What You Should Know About Niacin COMMENTARY: Ezetimibe vs. Niacin for Atherosclerosis: The ARBITER 6-HALTS Study CHART: Non-Statin Lipid-Lowering Agents Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=260101&pb=PRL (subscription needed) http://www.prescribersletter.com
  13. Jump up to: 13.0 13.1 13.2 Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Liver Function Test Scheduling Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=260704&pb=PRL (subscription needed) http://www.prescribersletter.com
  14. Jump up to: 14.0 14.1 14.2 NIH News: Thursday, May 26, 2011 NIH stops clinical trial on combination cholesterol treatment Lack of efficacy in reducing cardiovascular events prompts decision http://www.nih.gov/news/health/may2011/nhlbi-26.htm
    Prescriber's Letter 18(7): 2011 Niacin Plus Statin to Reduce Cardiovascular Risk: AIM-HIGH Study Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=270701&pb=PRL (subscription needed) http://www.prescribersletter.com
    The AIM-HIGH Investigators. Niacin in patients with low HDL cholesterol levels receiving intensive statin therapy. N Engl J Med 2011 Nov 15 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/22085343 <Internet> http://www.nejm.org/doi/full/10.1056/NEJMoa1107579
  15. Deprecated Reference
  16. Jump up to: 16.0 16.1 16.2 16.3 The HPS2-THRIVE Collaborative Group. Effects of extended-release niacin with laropiprant in high-risk patients. N Engl J Med 2014 Jul 17; 371:203. <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/25014686 <Internet> http://www.nejm.org/doi/full/10.1056/NEJMoa1300955
    Anderson TJ et al. Safety profile of extended-release niacin in the AIM-HIGH trial. N Engl J Med 2014 Jul 17; 371:288. <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/25014706 <Internet> http://www.nejm.org/doi/full/10.1056/NEJMc1311039
  17. Jump up to: 17.0 17.1 17.2 Keene D et al. Effect on cardiovascular risk of high density lipoprotein targeted drug treatments niacin, fibrates, and CETP inhibitors: Meta-analysis of randomised controlled trials including 117,411 patients. BMJ 2014 Jul 18; 349:g4379 PMID: https://www.ncbi.nlm.nih.gov/pubmed/25038074
  18. Jump up to: 18.0 18.1 18.2 Yancey JR, Rey JB. Use of Niacin for Primary or Secondary Prevention of Cardiovascular or Cerebrovascular Events. Am Fam Physician. 2018 Apr 1;97(7):436-437. PMID: https://www.ncbi.nlm.nih.gov/pubmed/29671561 Medscape https://www.medscape.com/viewarticle/895259_2
  19. Ferral M, Wang Z, Anderson JT et al A terminal metabolite of niacin promotes vascular inflammation and contributes to cardiovascular disease risk. Nature Medicine 2024 volume 30, pages 424-234 PMID: https://www.ncbi.nlm.nih.gov/pubmed/38374343 https://www.nature.com/articles/s41591-023-02793-8

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