Inositol Nicotinate

OTHER NAME(S): Hexaniacinate d'Inositol, Hexanicotinate d'Inositol, Hexanicotinate de Meso-Inositol, Hexanicotinoyl Inositol, Inositol Hexaniacinate, Inositol Hexanicotinate, Inositol Niacinate, Meso-Inositol Hexanicotinate, Niacinate d'Inositol, Niacine Sans Rougissement, Nicotinate d'Inositol, No-Flush Niacin, Hexanicotinyl cis-1,2,3-5-trans-4,6-cyclohexane, Myo-inositol hexa-3-pyridine-carboxylate, Nicotinate d’Inositol, Nicotinato de Inositol

Overview

Inositol nicotinate is a compound made of niacin (vitamin B3) and inositol. Inositol occurs naturally in the body and can also be made in the laboratory.

Inositol nicotinate is used for blood circulation problems, including a painful response to cold, especially in the fingers and toes (Raynaud syndrome). It is also used for high cholesterol, high blood pressure, and many other conditions, but there is no good scientific evidence to support these uses.

Inositol nicotinate releases niacin, or vitamin B3, when it is processed by the body. Niacin can widen blood vessels, lower blood levels of fats such as cholesterol, and break up a protein needed for the clotting of blood.

Inositol nicotinate releases niacin, or vitamin B3, when it is processed by the body. Niacin can widen blood vessels, lower blood levels of fats such as cholesterol, and break up a protein needed for the clotting of blood.

References
  1. McEvoy GK, ed. AHFS Drug Information. Bethesda, MD: American Society of Health-System Pharmacists, 1998.
  2. Anon. Inositol hexaniacinate. Altern Med Rev 1998;3:222-3.
  3. Sunderland GT, Belch JJ, Sturrock RD, et al. A double-blind, randomized, placebo-controlled trial of hexopal in primary Raynaud's disease. Clin Rheumatol 1988;7:46-9.
  4. Hutt V, Wechsler JG, Klor HU, Ditschuneit H. [Effect of a clofibrate-inositol nicotinate combination on lipids and lipoproteins in primary hyperlipoproteinemia of types IIa, IV and V]. Arzneimittelforschung 1983;33:776-9.
  5. Holti G. An experimentally controlled evaluation of the effect of inositol nicotinate upon the digital blood flow in patients with Raynaud's phenomenon. J Int Med Res 1979;7:473-83.
  6. Ring EF, Bacon PA. Quantitative thermographic assessment of inositol nicotinate therapy in Raynaud's phenomena. J Int Med Res 1977;5:217-22.
  7. Wilke H, Frahm H. [Treatment of hyperlipoproteinaemia types IIa, IIb, IV and V with a combination of clofibrate and inositol nicotinate]. [Article in German]. Dtsch Med Wochenschr 1976;101:401-5.
  8. Knodel LC, Talbert RL. Adverse effects of hypolipidaemic drugs. Med Toxicol 1987;2:10-32.
  9. Gibbons LW, Gonzalez V, Gordon N, Grundy S. The prevalence of side effects with regular and sustained-release nicotinic acid. Am J Med 1995;99:378-85.
  10. Crouse JR III. New developments in the use of niacin for treatment of hyperlipidemia: new considerations in the use of an old drug. Coron Artery Dis 1996;7:321-6.
  11. Garg A, Grundy SM. Nicotinic acid as therapy for dyslipidemia in non-insulin-dependent diabetes mellitus. JAMA 1990;264:723-6.
  12. American Society of Health-System Pharmacists. ASHP Therapeutic Position Statement on the safe use of niacin in the management of dyslipidemias. Am J Health Syst Pharm 1997;54:2815-9.
  13. Guyton JR, Goldberg AC, Kreisberg RA, et al. Effectiveness of once-nightly dosing of extended-release niacin alone and in combination for hypercholesterolemia. Am J Cardiol 1998;82:737-43.
  14. Food and Nutrition Board, Institute of Medicine. Dietary Reference Intakes for Thiamin, Riboflavin, Niacin, Vitamin B6, Folate, Vitamin B12, Pantothenic Acid, Biotin, and Choline (2000). Washington, DC: National Academy Press, 2000. Available at: https://books.nap.edu/books/0309065542/html/.
  15. Brown BG, Zhao XQ, Chait A, et al. Simvastatin and niacin, antioxidant vitamins, or the combination for the prevention of coronary disease. N Engl J Med 2001;345:1583-93.
  16. Bays HE, Dujovne CA. Drug interactions of lipid-altering drugs. Drug Saf 1998;19:355-71.
  17. Figge HL, Figge J, Souney PF, et al. Nicotinic acid: a review of its clinical use in the treatment of lipid disorders. Pharmacotherapy 1988;8:287-94.
  18. Raising HDL and Niacin Use. Pharmacist's Letter/Prescriber's Letter 2004;20(5):200504.
  19. McKenney J. New perspectives on the use of niacin in the treatment of lipid disorders. Arch Intern Med 2004;164:697-705.
  20. Dorner V, Fischer FW. [The influence of m-inositol hexanicotinate ester on the serum lipids and lipoproteins]. Arzneim-Forsch 1961;11:110-13.
  21. Meyers CD, Car MC, Park S, Brunzell JD. Varying cost and free nicotinic acid content in over-the-counter niacin preparations for dyslipidemia. Ann Intern Med 2003;139:996-1002.
  22. Reaven P, Witztum JL. Lovastatin, nicotinic acid and rhabdomyolysis (letter). Ann Int Med 1988;109:597-8.
  23. Ito MK. Advances in the understanding and management of dyslipidemia: using niacin-based therapies. Am J Health-Syst Pharm 2003;60(suppl 2):s15-21.
  24. O'Brien T, Silverberg JD, Nguyen TT. Nicotinic acid-induced toxicity associated with cytopenia and decreased levels of thyroxine-binding globulin. Mayo Clin Proc. 1992;67(5):465-8.
  25. Garnett WR. Interactions with hydroxymethylglutaryl-coenzyme A reductase inhibitors. Am J Health Syst Pharm. 1995;52(15):1639-45.
  26. Cashin-Hemphill L, Spencer CA, Nicoloff JT, et al. Alterations in serum thyroid hormonal indices with colestipol-niacin therapy. Ann Intern Med. 1987;107(3):324-9.
  27. Drinka PJ. Alterations in thyroid and hepatic function tests associated with preparations of sustained-release niacin. Mayo Clin Proc. 1992;67(12):1206.
  28. Shakir KM, Kroll S, Aprill BS, Drake AJ 3rd, Eisold JF. Nicotinic acid decreases serum thyroid hormone levels while maintaining a euthyroid state. Mayo Clin Proc. 1995;70(6):556-8.
  29. Andersson RG, Aberg G, Brattsand R, Ericsson E, Lundholm L. Studies on the mechanism of flush induced by nicotinic acid. Acta Pharmacol Toxicol (Copenh). 1977 Jul;41(1):1-10.
  30. Brown WV. Niacin for lipid disorders. Indications, effectiveness, and safety. Postgrad Med. 1995 Aug;98(2):185-9, 192-3.
  31. Schwartzkopff W, Zschiedrich M. [Combination or monotherapy of hyperlipoproteinemia typus IIb, IV, V with clofibrate and m-inositolnicotinate or clofibrinic acid (author's transl)]. Med Klin. 2-17-1978;73:231-239.
  32. Kiff, R. S. and Quick, C. R. Does inositol nicotinate (Hexopal) influence intermittent claudication? A controlled trial. Br.J.Clin.Pract. 1988;42(4):141-145.
  33. O'Hara, J., Jolly, P. N., and Nicol, C. G. The therapeutic efficacy of inositol nicotinate (Hexopal) in intermittent claudication: a controlled trial. Br.J.Clin.Pract. 1988;42(9):377-383.
  34. Kramer, K. D., Ghabussi, P., and Hochrein, H. [Antihypertensive combination-therapy with inositol nicotinate in essential hypertension]. Med.Welt. 7-8-1977;28(27):1198-1201.
  35. Head, A. Treatment of intermittent claudication with inositol nicotinate. Practitioner 1986;230(1411):49-54.
  36. Hentzer, E. [Treatment of peripheral arterial insufficiency with inositol nicotinate (Hexanicit)]. Nord.Med. 9-22-1966;76(38):1090-1093.
  37. Cucinotta, D., Silvestrini, C., Mancini, M., Maini, C., and Passeri, M. [Experience with the medical treatment of chronic cerebrovascular insufficiency: bamethan and inositol nicotinate versus placebo]. G.Clin.Med. 1981;62(5):339-350.
  38. Kramer, K. D., Ghabussi, P., Lehmann, H. U., and Hochrein, H. [Dose-effect comparison of antihypertensive combinations with and without alpha-methyldopa]. MMW.Munch.Med Wochenschr. 4-4-1975;117(14):579-582.
  39. Belch, J. J. and Ho, M. Pharmacotherapy of Raynaud's phenomenon. Drugs 1996;52(5):682-695.
  40. Domer, V. and Fischer, F. W. The influence of m-inositol hexanicotinate ester on the serum lipids and lipoproteins. Arzneim-Frosch 1961;11:110-113.
  41. Rhodes, E. L. Fibrinolytic agents in the treatment of necrobiosis lipoidica. Br J Dermatol 1976;95:673-674.
  42. Aramwit P, Srisawadwong R, Supasyndh O. Effectiveness and safety of extended-release nicotinic acid for reducing serum phosphorus in hemodialysis patients. J Nephrol. 2012 May-Jun;25(3):354-62.
  43. He YM, Feng L, Huo DM, Yang ZH, Liao YH. Benefits and harm of niacin and its analog for renal dialysis patients: a systematic review and meta-analysis. Int Urol Nephrol. 2014 Feb;46(2):433-42.
  44. Lakey WC, Greyshock N, Guyton JR. Adverse reactions of Achilles tendon xanthomas in three hypercholesterolemic patients after treatment intensification with niacin and bile acid sequestrants. J Clin Lipidol. 2013 Mar-Apr;7(2):178-81.
  45. Schandelmaier S, Briel M, Saccilotto R, Olu KK, Arpagaus A, Hemkens LG, Nordmann AJ. Niacin for primary and secondary prevention of cardiovascular events. Cochrane Database Syst Rev. 2017 Jun 14;6:CD009744.
  46. Niaspan [package insert]. Barcelona, Spain: AbbVie LTD; 2015.