261
Views
6
CrossRef citations to date
0
Altmetric
Drug Safety Evaluations

Safety and tolerability of extended-release niacin with laropiprant

, MRCP, , MD, , , MD & , MSc FRCP MD
Pages 151-159 | Published online: 01 Dec 2011

Bibliography

  • Ridker PM, Genest J, Boekholdt SM, HDL cholesterol and residual risk of first cardiovascular events after treatment with potent statin therapy: an analysis from the JUPITER trial. Lancet 2010;11:333-9
  • Panel AP. Reducing residual cardiovascular risk: the relevance of raising high-density lipoprotein cholesterol in patients on cholesterol-lowering treatment. Diab Vasc Dis Res 2006;3:S1-S12
  • Durrington P. Hyperlipidaemia Diagnosis and Management. 3rd edition. Hodder Arnold; London: 2007
  • Castelli WP, Garrison RJ, Wilson PW, Incidence of coronary heart disease and lipoprotein cholesterol levels. The Framingham Study. JAMA 1986;256:2835-8
  • Stamler J, Wentworth D, Neaton JD. Is relationship between serum cholesterol and risk of premature death from coronary heart disease continuous and graded? findings in 356,222 primary screenees of the Multiple Risk Factor Intervention Trial (MRFIT). JAMA 1986;256:2823-8
  • Shah PK, Kaul S, Nilsson J, Exploiting the vascular protective effects of high-density lipoprotein and its apolipoproteins: an idea whose time for testing is coming, part I. Circulation 2001;104:2376-83
  • Soran H, Younis NN, Charlton-Menys V, Variation in paraoxonase-1 activity and atherosclerosis. Curr Opin Lipidol 2009;20:265-74
  • Navab M, Reddy ST, Van Lenten BJ, HDL and cardiovascular disease: atherogenic and atheroprotective mechanisms. Nat Rev Cardiol 2011;8:222-32
  • Third Report of the National Cholesterol Education Program (NCEP). Expert Panel on detection, evaluation, and treatment of high blood cholesterol in adults (Adult Treatment Panel III) final report. Circulation 2002;106:3143-421
  • Brown G, Albers JJ, Fisher LD, Regression of coronary artery disease as a result of intensive lipid-lowering therapy in men with high levels of apolipoprotein B. N Engl J Med 1990;323:1289-98
  • Brown BG, Zhao XQ, Chait A, Simvastatin and niacin, antioxidant vitamins, or the combination for the prevention of coronary disease. N Engl J Med 2001;345:1583-92
  • Taylor AJ, Sullenberger LE, Lee HJ, Arterial Biology for the Investigation of the Treatment Effects of Reducing Cholesterol (ARBITER) 2: a double-blind, placebo-controlled study of extended-release niacin on atherosclerosis progression in secondary prevention patients treated with statins. Circulation 2004;110:3512-17
  • Taylor AJ, Lee HJ, Sullenberger LE. The effect of 24 months of combination statin and extended-release niacin on carotid intima-media thickness: ARBITER 3. Curr Med Res Opin 2006;22:2243-50
  • Taylor AJ, Villines TC, Stanek EJ, Extended-release niacin or ezetimibe and carotid intima-media thickness. N Engl J Med 2009;361:2113-22
  • Lee JM, Robson MD, Yu LM, Effects of high-dose modified-release nicotinic acid on atherosclerosis and vascular function: a randomized, placebo-controlled, magnetic resonance imaging study. J Am Coll Cardiol 2009;54:1787-94
  • Carlson LA, Oro L, Ostman J. Effect of a single dose of nicotinic acid on plasma lipids in patients with hyperlipoproteinemia. Acta Med Scand 1968;183:457-65
  • Parsons WB Jr, AchorRW, BergeKG, . Changes in concentration of blood lipids following prolonged administration of large doses of nicotinic acid to persons with hypercholesterolemia: preliminary observations. Proc Staff Meet Mayo Clin 1956;31:377-90
  • Parsons WB Jr, Flinn JH. Reduction of serum cholesterol levels and beta-lipoprotein cholesterol levels by nicotinic acid. AMA Arch Intern Med 1959;103:783-90
  • NIH stops clinical trial on combination cholesterol treatment: lack of efficacy in reducing cardiovascular events prompts decision. National Institute of Health News 2011. Available from: http://www.nih.gov/news/health/may2011/nhlbi-26.htm
  • Whelan AM, Price SO, Fowler SF, The effect of aspirin on niacin-induced cutaneous reactions. J Fam Pract 1992;34:165-8
  • Gleim G. Efficacy and safety profile of co-administered ER niacin/laropiprant and simvastatin in dyslipidaemia. Br J Cardiol 2009;16:90-7
  • Shah S, Ceska R, Gil-Extremera B, Efficacy and safety of extended-release niacin/laropiprant plus statin vs. doubling the dose of statin in patients with primary hypercholesterolaemia or mixed dyslipidaemia. Int J Clin Pract 2010;64:727-38
  • Maccubbin D, Bays HE, Olsson AG, Lipid-modifying efficacy and tolerability of extended-release niacin/laropiprant in patients with primary hypercholesterolaemia or mixed dyslipidaemia. Int J Clin Pract 2008;62:1959-70
  • Karpe F, Frayn KN. The nicotinic acid receptor–a new mechanism for an old drug. Lancet 2004;363:1892-4
  • Ganji SH, Tavintharan S, Zhu D, Niacin noncompetitively inhibits DGAT2 but not DGAT1 activity in HepG2 cells. J Lipid Res 2004;45:1835-45
  • Jin FY, Kamanna VS, Kashyap ML. Niacin decreases removal of high-density lipoprotein apolipoprotein A-I but not cholesterol ester by Hep G2 cells. Implication for reverse cholesterol transport. Arterioscler Thromb Vasc Biol 1997;17:2020-8
  • Acton S, Rigotti A, Landschulz KT, Identification of scavenger receptor SR-BI as a high density lipoprotein receptor. Science 1996;271:518-20
  • Martinez LO, Jacquet S, Esteve JP, Ectopic beta-chain of ATP synthase is an apolipoprotein A-I receptor in hepatic HDL endocytosis. Nature 2003;421:75-9
  • Rubic T, Trottmann M, Lorenz RL. Stimulation of CD36 and the key effector of reverse cholesterol transport ATP-binding cassette A1 in monocytoid cells by niacin. Biochem Pharmacol 2004;67:411-19
  • van der Hoorn JW, de Haan W, Berbee JF, Niacin increases HDL by reducing hepatic expression and plasma levels of cholesteryl ester transfer protein in APOE*3Leiden.CETP mice. Arterioscler Thromb Vasc Biol 2008;28:2016-22
  • Ganji SH. Niacin inhibits LDL oxidation and redox-sensitive VCAM-1 and MCP-1 expression in human aortic endothelial cells. Arterioscler Thromb Vasc Biol 2004;24:125
  • Ganji SH, Qin S, Zhang L, Niacin inhibits vascular oxidative stress, redox-sensitive genes, and monocyte adhesion to human aortic endothelial cells. Atherosclerosis 2009;202:68-75
  • Mrochek JE, Jolley RL, Young DS, Metabolic response of humans to ingestion of nicotinic acid and nicotinamide. Clin Chem 1976;22:1821-7
  • Cayen MN. Disposition, metabolism and pharmacokinetics of antihyperlipidemic agents in laboratory animals and man. Pharmacol Ther 1985;29:157-204
  • Miller ON, Hamilton JG, Goldsmith GA. Investigation of the mechanism of action of nicotinic acid on serum lipid levels in man. Am J Clin Nutr 1960;8:480-90
  • Knopp RH, Ginsberg J, Albers JJ, Contrasting effects of unmodified and time-release forms of niacin on lipoproteins in hyperlipidemic subjects: clues to mechanism of action of niacin. Metabolism 1985;34:642-50
  • Birjmohun RS, Hutten BA, Kastelein JJ, Increasing HDL cholesterol with extended-release nicotinic acid: from promise to practice. Neth J Med 2004;62:229-34
  • Illingworth DR, Stein EA, Mitchel YB, Comparative effects of lovastatin and niacin in primary hypercholesterolemia. A prospective trial. Arch Intern Med 1994;154:1586-95
  • Mills E, Prousky J, Raskin G, The safety of over-the-counter niacin. A randomized placebo-controlled trial [ISRCTN18054903]. BMC Clin Pharmacol 2003;3:4-12
  • Kamal-Bahl SJ, Burke T, Watson D, Discontinuation of lipid modifying drugs among commercially insured United States patients in recent clinical practice. Am J Cardiol 2007;99:530-4
  • Kamal-Bahl SJ, Burke TA, Watson DJ, Dosage, titration, and gaps in treatment with extended release niacin in clinical practice. Curr Med Res Opin 2008;24:1817-21
  • Benyo Z, Gille A, Bennett CL, Nicotinic acid-induced flushing is mediated by activation of epidermal langerhans cells. Mol Pharmacol 2006;70:1844-9
  • Benyo Z, Gille A, Kero J, GPR109A (PUMA-G/HM74A) mediates nicotinic acid-induced flushing. J Clin Invest 2005;115:3634-40
  • Maciejewski-Lenoir D, Richman JG, Hakak Y, Langerhans cells release prostaglandin D2 in response to nicotinic acid. J Invest Dermatol 2006;126:2637-46
  • Sturino CF, O'Neill G, Lachance N, Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocy clopenta[b]indol-3-yl]-acetic acid (MK-0524). J Med Chem 2007;50:794-806
  • MSD. Summary of product characteristics TREDAPTIVE 1000 mg/20 mg modified release tablets. 2011. Available from: http://www.medicines.org.uk/EMC/medicine/22227/SPC/TREDAPTIVE+1000+mg+20+mg+modified+release+tablets/
  • Dallob A, Luo WL, Luk JM, The effects of laropiprant, a selective prostaglandin D(2) receptor 1 antagonist, on the antiplatelet activity of clopidogrel or aspirin. Platelets 2011;22:495-503
  • Lai E, Schwartz JI, Dallob A., Effects of extended release niacin/laropiprant, laropiprant, extended release niacin and placebo on platelet aggregation and bleeding time in healthy subjects. Platelets 2010;21:191-8
  • Bays HE, Dujovne CA, McGovern ME, Comparison of once-daily, niacin extended-release/lovastatin with standard doses of atorvastatin and simvastatin (the ADvicor Versus Other Cholesterol-Modulating Agents Trial Evaluation [ADVOCATE]). Am J Cardiol 2003;91:667-72
  • Bays HE, McGovern ME. Once-daily niacin extended release/lovastatin combination tablet has more favorable effects on lipoprotein particle size and subclass distribution than atorvastatin and simvastatin. Prev Cardiol 2003;6:179-88
  • Managing Dyslipidemias in Patients With Chronic Kidney Disease - Guidelines. 2003, The National Kidney Foundation KDOQI
  • Increased myopathy with combination use of ER niacin/laropiprant (Tredaptive®) and simvastatin 40 mg in Chinese patients. Results from interim analysis of HPS2-THRIVE study. Safety alerts 2010. Available from: http://www.hsa.gov.sg/publish/hsaportal/en/health_products_regulation/safety_information/product_safety_alerts/safety_alerts_2010/increased_myopathy.html
  • Tato F, Vega GL, Grundy SM. Effects of crystalline nicotinic acid-induced hepatic dysfunction on serum low-density lipoprotein cholesterol and lecithin cholesteryl acyl transferase. Am J Cardiol 1998;81:805-7
  • Capuzzi DM, Guyton JR, Morgan JM, Efficacy and safety of an extended-release niacin (Niaspan): a long-term study. Am J Cardiol 1998;82:74U-81U; discussion 5U-6U
  • Vaccari CS, Hammoud RA, Nagamia SH, Revisiting niacin: reviewing the evidence. J Clin Lipidol 2007;1:248-55
  • Guyton JR. Extended-release niacin for modifying the lipoprotein profile. Expert Opin Pharmacother 2004;5:1385-98
  • Henkin Y, Oberman A, Hurst DC, Niacin revisited: clinical observations on an important but underutilized drug. Am J Med 1991;91:239-46
  • Schwartz ML. Severe reversible hyperglycemia as a consequence of niacin therapy. Arch Intern Med 1993;153:2050-2
  • Grundy SM, Vega GL, McGovern ME, Efficacy, safety, and tolerability of once-daily niacin for the treatment of dyslipidemia associated with type 2 diabetes: results of the assessment of diabetes control and evaluation of the efficacy of niaspan trial. Arch Intern Med 2002;162:1568-76
  • Maccubbin D, Koren MJ, Davidson M, Flushing profile of extended-release niacin/laropiprant versus gradually titrated niacin extended-release in patients with dyslipidemia with and without ischemic cardiovascular disease. Am J Cardiol 2009;104:74-81
  • Guyton JR, Bays HE. Safety considerations with niacin therapy. Am J Cardiol 2007;99:22C-31C
  • Paolini JF, Mitchel YB, Reyes R, Effects of laropiprant on nicotinic acid-induced flushing in patients with dyslipidemia. Am J Cardiol 2008;101:625-30
  • Lai E, Wenning LA, Crumley TM, Pharmacokinetics, pharmacodynamics, and safety of a prostaglandin D2 receptor antagonist. Clin Pharmacol Ther 2008;83:840-7
  • McKenney J, Bays H, Koren M, Safety of extended-release niacin/laropiprant in patients with dyslipidemia. J Clin Lipidol 2010;4:105-12
  • Lauring B, Dishy V, Luo WL, Laropiprant in combination with extended-release niacin does not alter urine 11-dehydrothromboxane B2, a marker of in vivo platelet function, in healthy, hypercholesterolemic, and diabetic subjects. J Clin Pharmacol 2009;49:1426-35
  • Norquist JM, Watson DJ, Yu Q, Validation of a questionnaire to assess niacin-induced cutaneous flushing. Curr Med Res Opin 2007;23:1549-60
  • Maclean A. Efficacy and safety of extended-release niacin/laropiprant in patients with type 2 diabetes mellitus. Br J Cardiol 2011;18:37-45
  • Birjmohun RS, Hutten BA, Kastelein JJ, Efficacy and safety of high-density lipoprotein cholesterol-increasing compounds: a meta-analysis of randomized controlled trials. J Am Coll Cardiol 2005;45:185-97

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.