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Inositol nicotinate

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Also listed as: Inositol hexaniacinate, Inositol hexanicotinate
Related terms
Background
Evidencetable
Tradition
Dosing
Safety
Interactions
Attribution
Bibliography

Related Terms
  • Hexanicit®, hexanicotinoyl inositol, Hexopal®, inositol hexaniacinate, inositol hexanicotinate, inositol niacinate, m-inositol nicotinate, meso-inositol, meso-inositol hexanicotinate, niacin, niacinamide, nicotinamide, nicotinic acid, no-flush niacin, vitamin B3.
  • Note: Inositol nicotinate consists of six nicotinic acid (niacin) molecules linked with an inositol molecule. When taken by mouth, inositol nicotinate is broken down into nicotinic acid (niacin) and inositol. Therefore, although inositol nicotinate may produce similar effects and adverse effects as niacin, only those effects and adverse effects specific to inositol nicotinate are included in this monograph.

Background
  • Inositol nicotinate, also known as inositol hexaniacinate, consists of six nicotinic acid (niacin) molecules crossed-linked with an inositol molecule. Inositol nicotinate is a form of niacin (vitamin B3) which may decrease flushing, compared to niacin. Inositol nicotinate has been in use in Europe for over 30 years as a no-flush form of niacin.
  • Good scientific evidence supports the use of inositol nicotinate for peripheral artery disease. Inositol nicotinate has also been studied as a treatment for cerebral ischemia (lack of adequate blood flow to the brain), high cholesterol, high blood pressure, Raynaud's disease, and necrobiosis lipoidica (a skin condition associated with diabetes).

Evidence Table

These uses have been tested in humans or animals. Safety and effectiveness have not always been proven. Some of these conditions are potentially serious, and should be evaluated by a qualified healthcare provider. GRADE *


Inositol nicotinate may have beneficial effects in patients with peripheral artery disease. More studies are needed to make any conclusions in this area.

B


Limited research suggests that inositol nicotinate may have beneficial effects in patients with cerebral ischemia. More studies are needed to make any conclusions in this area.

C


Limited research suggests that inositol nicotinate may have beneficial effects in patients with high cholesterol. Additional research is needed before a conclusion can be made.

C


Studies examining the effects of inositol nicotinate alone on high blood pressure are currently lacking. Further research on inositol nicotinate alone for this use is needed.

C


Limited research suggests that inositol nicotinate may have beneficial effects in patients with Raynaud's disease. Additional research is needed in this area.

C


Necrobiosis lipoidica is an inflammatory disorder associated with diabetes mellitus. The cause is unknown and there is a lack of traditional therapies. Additional research is needed to determine if inositol nicotinate may be effective in the treatment of this condition.

C
* Key to grades

A: Strong scientific evidence for this use
B: Good scientific evidence for this use
C: Unclear scientific evidence for this use
D: Fair scientific evidence for this use (it may not work)
F: Strong scientific evidence against this use (it likley does not work)


Tradition / Theory

The below uses are based on tradition, scientific theories, or limited research. They often have not been thoroughly tested in humans, and safety and effectiveness have not always been proven. Some of these conditions are potentially serious, and should be evaluated by a qualified healthcare provider. There may be other proposed uses that are not listed below.

  • Acne, calming, dizziness, improved sleep, migraines (atherosclerosis-related), osteoarthritis, premenstrual syndrome (PMS), psoriasis, restless leg syndrome, schizophrenia, tinnitus (ringing in the ears), tonic (nerve).

Dosing

Adults (18 years and older)

  • For high cholesterol, 600-800 milligrams of inositol nicotinate has been taken by mouth daily.
  • For peripheral artery disease, 2 grams of inositol nicotinate (Hexopal®) has been taken by mouth twice daily for three months. One gram of inositol nicotinate (Hexopal®) has been taken by mouth four times daily for three months.

Children (under 18 years old)

  • There is no proven safe or effective dose for inositol nicotinate in children.

Safety

The U.S. Food and Drug Administration does not strictly regulate herbs and supplements. There is no guarantee of strength, purity or safety of products, and effects may vary. You should always read product labels. If you have a medical condition, or are taking other drugs, herbs, or supplements, you should speak with a qualified healthcare provider before starting a new therapy. Consult a healthcare provider immediately if you experience side effects.

Allergies

  • Avoid with known allergy or sensitivity to inositol nicotinate, niacin, or their constituents.

Side Effects and Warnings

  • Inositol nicotinate may cause breathing problems, dizziness, feeling of warmth, gastrointestinal complaints, high uric acid level in the blood, hives, impaired glucose tolerance, itchy or swollen skin, liver toxicity, skin flushing (redness), rash, or tightness in the throat.
  • Inositol nicotinate may increase blood sugar levels. Caution is advised in patients with diabetes or hypoglycemia, and in those taking drugs, herbs, or supplements that affect blood sugar. Blood glucose levels may need to be monitored by a qualified healthcare professional, including a pharmacist, and medication adjustments may be necessary.
  • Inositol nicotinate may cause changes in blood pressure. Caution is advised in patients taking herbs or supplements that affect blood pressure.
  • Inositol nicotinate may increase the risk of bleeding. Caution is advised in patients with bleeding disorders or taking drugs that may increase the risk of bleeding. Dosing adjustments may be necessary.
  • Use cautiously in patients in patients with cardiovascular conditions, as inositol nicotinate may cause chest pain or changes in blood pressure and heart rhythm, as is observed with niacin.
  • Use cautiously in patients taking lipid or cholesterol lowering agents, as inositol nicotinate may lower blood levels of lipids or cholesterol.
  • Avoid in patients with liver disease or stomach ulcers, as liver problems, stomach ulcers, diarrhea, jaundice, vomiting, or stomach pain may occur.
  • Avoid in patients using carbamazepine, as inositol nicotinate should not be combined with carbamazepine.
  • Avoid in pregnant or breastfeeding women due to a lack of available scientific evidence.
  • Avoid in patients with known allergy to inositol nicotinate, niacin, or any of their constituents.

Pregnancy and Breastfeeding

  • Avoid in pregnant or breastfeeding women due to a lack of available scientific evidence.

Interactions

Interactions with Drugs

  • Inositol nicotinate may increase the risk of bleeding when taken with drugs that increase the risk of bleeding. Some examples include aspirin, anticoagulants ("blood thinners") such as warfarin (Coumadin®) or heparin, antiplatelet drugs such as clopidogrel (Plavix®), and nonsteroidal anti-inflammatory drugs such as ibuprofen (Motrin®, Advil®) or naproxen (Naprosyn®, Aleve®).
  • Inositol nicotinate may increase blood sugar levels. Caution is advised when using medications that may also affect blood sugar. Patients taking insulin or drugs for diabetes by mouth should be monitored closely by a qualified healthcare professional, including a pharmacist. Medication adjustments may be necessary.
  • Inositol nicotinate may cause changes in blood pressure. Caution is advised in patients taking drugs that affect blood pressure, including agents that widen blood vessels.
  • Inositol nicotinate may also interact with alcohol, carbamazepine, cardiovascular agents, lipid or cholesterol lowering agents, or nicotine.

Interactions with Herbs and Dietary Supplements

  • Inositol nicotinate may increase the risk of bleeding when taken with herbs and supplements that are believed to increase the risk of bleeding. Multiple cases of bleeding have been reported with the use of Ginkgo biloba, and fewer cases with garlic and saw palmetto. Numerous other agents may theoretically increase the risk of bleeding, although this has not been proven in most cases.
  • Inositol nicotinate may increase blood sugar levels. Caution is advised when using herbs or supplements that may also affect blood sugar. Blood glucose levels may require monitoring, and doses may need adjustment.
  • Inositol nicotinate may cause changes in blood pressure. Caution is advised in patients taking herbs or supplements that affect blood pressure, including herbs and supplements that widen blood vessels.
  • Inositol nicotinate may also interact with cardiovascular herbs and supplements, lipid or cholesterol lowering herbs and supplements, or nicotine.

Attribution
  • This information is based on a systematic review of scientific literature edited and peer-reviewed by contributors to the Natural Standard Research Collaboration (www.naturalstandard.com).

Bibliography
  1. Belch JJ, Ho M. Pharmacotherapy of Raynaud's phenomenon. Drugs 1996;52(5):682-695.
  2. Cucinotta D, Silvestrini C, Mancini, M, et al. [Experience with the medical treatment of chronic cerebrovascular insufficiency: bamethan and inositol nicotinate versus placebo]. G Clin Med 1981;62(5):339-350.
  3. Dorner V, Fischer FW. The influence of m-inositol hexanicotinate ester on the serum lipids and lipoproteins. Arzneim-Frosch 1961;11:110-113.
  4. Head A. Treatment of intermittent claudication with inositol nicotinate. Practitioner 1986;230(1411):49-54.
  5. Hentzer E. [Treatment of peripheral arterial insufficiency with inositol nicotinate (Hexanicit)]. Nord Med 1966;76(38):1090-1093.
  6. 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(6):473-483.
  7. Hutt V, Wechsler JG, Klor HU, et al. [Effect of a clofibrate-inositol nicotinate combination on lipids and lipoproteins in primary hyperlipoproteinemia of types IIa, IV and V]. Arzneimittelforschung 1983;33(5):776-779.
  8. Kiff RS, Quick CR. Does inositol nicotinate (Hexopal) influence intermittent claudication? A controlled trial. Br J Clin Pract 1988;42(4):141-145.
  9. Kramer KD, Ghabussi P, Hochrein H. [Antihypertensive combination-therapy with inositol nicotinate in essential hypertension]. Med Welt 1977;28(27):1198-1201.
  10. Kramer KD, Ghabussi P, Lehmann HU, et al. [Dose-effect comparison of antihypertensive combinations with and without alpha-methyldopa]. MMW Munch Med Wochenschr. 1975;117(14):579-582.
  11. Momsen AH, Jensen MB, Norager CB, et al. Drug therapy for improving walking distance in intermittent claudication: a systematic review and meta-analysis of robust randomised controlled studies. Eur J Vasc Endovasc Surg 2009;38(4):463-74.
  12. O'Hara J, Jolly PN, Nicol CG. The therapeutic efficacy of inositol nicotinate (Hexopal) in intermittent claudication: a controlled trial. Br J Clin Pract 1988;42(9):377-383.
  13. Rhodes EL. Fibrinolytic agents in the treatment of necrobiosis lipoidica. Br J Dermatol 1976;95:673-674.
  14. 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 1978;73(7):231-239.
  15. Wilke H, Frahm H. [Treatment of hyperlipoproteinaemia types IIa, IIb, IV and V with a combination of clofibrate and inositol nicotinate (author's transl)]. Dtsch Med Wochenschr 1976;101(11):401-405.

Copyright © 2011 Natural Standard (www.naturalstandard.com)


The information in this monograph is intended for informational purposes only, and is meant to help users better understand health concerns. Information is based on review of scientific research data, historical practice patterns, and clinical experience. This information should not be interpreted as specific medical advice. Users should consult with a qualified healthcare provider for specific questions regarding therapies, diagnosis and/or health conditions, prior to making therapeutic decisions.

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