INOSITOL NICOTINATE

OTHER NAME(S):

Hexaniacinate d'Inositol, Hexanicotinate d'Inositol, Hexanicotinate de Meso-Inositol, Hexanicotinyl cis-1,2,3-5-trans-4,6-cyclohexane, Hexanicotinoyl Inositol, Inositol Hexaniacinate, Inositol Hexanicotinate, Inositol Niacinate, Meso-Inositol Hexanicotinate, Myo-inositol hexa-3-pyridine-carboxyalte, Niacinate d'Inositol, Niacine Sans Rougissement, Nicotinate d'Inositol, Nicotinato de Inositol, No-Flush Niacin.

Overview

Overview Information

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.

How does it work?

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.

Uses

Uses & Effectiveness?

Possibly Effective for

  • Painful response to cold especially in the fingers and toes (Raynaud syndrome). Some research shows that taking a specific product of inositol nicotinate (Hexopal) by mouth for several weeks modestly improves symptoms of Raynaud syndrome.

Insufficient Evidence for

More evidence is needed to rate the effectiveness of inositol nicotinate for these uses.

Side Effects

Side Effects & Safety

When taken by mouth: Inositol nicotinate is POSSIBLY SAFE for most people. It can cause some side effects such as stomach upset, intestinal gas, and nausea. It might also cause liver damage like other niacin products in some people.

Some inositol nicotinate products are promoted as "no-flush" niacin because some people think they don't cause as much flushing as regular niacin. But this possible benefit has not been proven in research studies.

Special Precautions & Warnings:

Pregnancy and breast-feeding: There isn't enough reliable information to know if inositol nicotinate is safe to use when pregnant or breast-feeding. Stay on the safe side and avoid use.

Allergies: Niacin, a chemical that is released when inositol nicotinate breaks down in the body, might make allergies worse by releasing histamine. This is the chemical that triggers allergy symptoms.

Bleeding disorder: Inositol nicotinate might slow blood clotting. In theory, inositol nicotinate might increase the risk of bleeding and make bleeding disorders worse.

Heart disease/heart-related chest pain (unstable angina): Large amounts of niacin, a chemical that is released when inositol nicotinate breaks down in the body, can increase the risk of irregular heartbeat. If you have a heart condition, check with your healthcare provider before using inositol nicotinate.

Diabetes: Niacin, a chemical that is released when inositol nicotinate breaks down in the body, can interfere with blood sugar control. This might require an adjustment in the dose of medicines needed to control diabetes. Increased blood sugar monitoring may be necessary, particularly at the beginning of treatment. If you have diabetes, check with your healthcare provider before using inositol nicotinate.

Gallbladder disease: Niacin, a chemical that is released when inositol nicotinate breaks down in the body, might make gallbladder problems worse. Use with caution.

Gout: Large amounts of niacin, a chemical that is released when inositol nicotinate breaks down in the body, might trigger gout. Use with caution.

Low blood pressure: Niacin, a chemical that is released when inositol nicotinate breaks down in the body, can cause low blood pressure. Use with caution.

Kidney disease: Niacin, a chemical that is released when inositol nicotinate breaks down in the body, might accumulate in people with kidney disease and make their condition worse. Don't use inositol nicotinate if you have kidney problems.

Liver disease: Niacin, a chemical that is released when inositol nicotinate breaks down in the body, can cause liver damage. Don't use inositol nicotinate if you have liver disease.

Sensitivity to niacin: Niacin is released when inositol nicotinate is processed by the body. If you are sensitive to niacin, don't use inositol nicotinate.

Stomach ulcers: Large amounts of niacin, a chemical that is released when inositol nicotinate breaks down in the body, might make peptic ulcer disease worse. Don't use inositol nicotinate if you have ulcers.

Surgery: Inositol nicotinate might slow blood clotting. There is some concern that it might increase the risk of bleeding during and after surgery. Stop taking inositol nicotinate at least 2 weeks before a scheduled surgery.

Interactions

Interactions?

Moderate Interaction

Be cautious with this combination

!
  • Medications for diabetes (Antidiabetes drugs) interacts with INOSITOL NICOTINATE

    Chronic use of inositol nicotinate might increase blood sugar. Diabetes medications are used to lower blood sugar. By increasing blood sugar, inositol nicotinate might decrease the effectiveness of diabetes medications. Monitor your blood sugar closely. The dose of your diabetes medication might need to be changed.
    Some medications used for diabetes include glimepiride (Amaryl), glyburide (DiaBeta, Glynase PresTab, Micronase), insulin, pioglitazone (Actos), rosiglitazone (Avandia), chlorpropamide (Diabinese), glipizide (Glucotrol), tolbutamide (Orinase), and others.

  • Medications that slow blood clotting (Anticoagulant / Antiplatelet drugs) interacts with INOSITOL NICOTINATE

    Inositol nicotinate might slow blood clotting. Taking inositol nicotinate along with medications that also slow clotting might increase the chances of bruising and bleeding. Some medications that slow blood clotting include aspirin, clopidogrel (Plavix), diclofenac (Voltaren, Cataflam, others), ibuprofen (Advil, Motrin, others), naproxen (Anaprox, Naprosyn, others), dalteparin (Fragmin), enoxaparin (Lovenox), heparin, warfarin (Coumadin), and others.

  • Medications used for lowering cholesterol (Statins) interacts with INOSITOL NICOTINATE

    Inositol nicotinate is changed in the body to niacin. Niacin can affect the muscles. Some medication used for lowering cholesterol can also affect the muscles. Taking niacin along with some medications used for lowering high cholesterol might increase the risk of muscle problems.
    Some medications used for high cholesterol include cerivastatin (Baycol), atorvastatin (Lipitor), lovastatin (Mevacor), pravastatin (Pravachol), simvastatin (Zocor), and others.

  • Nicotine patch (Transdermal nicotine) interacts with INOSITOL NICOTINATE

    Inositol nicotinate is broken down in the body to niacin. Niacin can sometimes cause flushing and dizziness. The nicotine patch can also cause flushing and dizziness. Taking inositol nicotinate and using a nicotine patch can increase the possibility of becoming flushed and dizzy.

Dosing

Dosing

The following doses have been studied in scientific research:

BY MOUTH:

  • General: Some dietary supplement products might not list inositol nicotinate separately on the label. Instead, it might be listed under niacin. Niacin is measured in niacin equivalents (NE). 1 mg of inositol nicotinate is the same as 1 mg NE.
  • Painful response to cold especially in the fingers and toes (Raynaud syndrome): 4 grams daily has been used. It might take several weeks before effects are seen.

View References

REFERENCES:

  • Belch, J. J. and Ho, M. Pharmacotherapy of Raynaud's phenomenon. Drugs 1996;52(5):682-695. View abstract.
  • 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. View abstract.
  • 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.
  • Head, A. Treatment of intermittent claudication with inositol nicotinate. Practitioner 1986;230(1411):49-54. View abstract.
  • Hentzer, E. [Treatment of peripheral arterial insufficiency with inositol nicotinate (Hexanicit)]. Nord.Med. 9-22-1966;76(38):1090-1093. View abstract.
  • 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. View abstract.
  • 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. View abstract.
  • 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. View abstract.
  • 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. View abstract.
  • Rhodes, E. L. Fibrinolytic agents in the treatment of necrobiosis lipoidica. Br J Dermatol 1976;95:673-674.
  • 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. View abstract.
  • 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. View abstract.
  • Anon. Inositol hexaniacinate. Altern Med Rev 1998;3:222-3. View abstract.
  • 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. View abstract.
  • Brown WV. Niacin for lipid disorders. Indications, effectiveness, and safety. Postgrad Med. 1995 Aug;98(2):185-9, 192-3. View abstract.
  • 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. View abstract.
  • Dorner V, Fischer FW. [The influence of m-inositol hexanicotinate ester on the serum lipids and lipoproteins]. Arzneim-Forsch 1961;11:110-13.
  • 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. View abstract.
  • 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/.
  • Garg A, Grundy SM. Nicotinic acid as therapy for dyslipidemia in non-insulin-dependent diabetes mellitus. JAMA 1990;264:723-6. View abstract.
  • 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. View abstract.
  • 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. View abstract.
  • 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. View abstract.
  • 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. View abstract.
  • 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. View abstract.
  • Knodel LC, Talbert RL. Adverse effects of hypolipidaemic drugs. Med Toxicol 1987;2:10-32. View abstract.
  • McKenney J. New perspectives on the use of niacin in the treatment of lipid disorders. Arch Intern Med 2004;164:697-705. View abstract.
  • 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. View abstract.
  • Ring EF, Bacon PA. Quantitative thermographic assessment of inositol nicotinate therapy in Raynaud's phenomena. J Int Med Res 1977;5:217-22. View abstract.
  • 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. View abstract.
  • 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. View abstract.
  • 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. View abstract.
  • 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. View abstract.
  • Ziliotto GR, Lamberti G, Wagner A, et al. [Comparative studies of the response of normolipemic and dyslipemic aged subjects to 2 forms of delayed-action nicotinic acid polyesters. Pentaerythrotol tetranicotinate and inositol hexanicotinate. Results of a controlled cross-over trial]. Arch Sci Med (Torino) 1977;134:359-94. View abstract.

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