No flush = No effect

13. November 2006 William Davis (3)


"Inositol Hexanicotinate is the true 'flushless niacin.' Unlike 'sustained-release' niacin, which is just regular niacin in a pill which dissolves more slowly, Inositol Hexanicotinate is a niacin complex, formed with the B-vitamin-like inositol. When you take an IHN supplement, the central inositol ring gradually releases niacin molecules, one at a time delivering true niacin. This, like “sustained-release” niacin, allows you to take niacin at clinically-proven doses without going crazy with the itch."


That above bit of nonsense adorns one manufacturers sales pitch for its no-flush niacin. No-flush niacin is one of the biggest scams in the health food store.

Ordinarily, I love health food stores. There's lots of fun and interesting things available that pack real power for your health program. Unfortunately, there's also outright nonsense. No-flush niacin is absolute nonsennse.

No-flush niacin is inositol hexaniacinate, or an inositol molecule complexed with 6 niacin molecules. So it really does contain niacin. However, although it works in rats, it exerts no known effect in humans.

Just Friday, a 41-year old woman came to my office for consultation because her doctor didn't know what to do with lipoprotein(a). She had seen a cardiologist who told her to take no-flush niacin. Both the cardiologist and the patient were therefore puzzled when lipoprotein(a) showed no drop and, in fact, was slightly higher on the no-flush preparation.

The lack of any observable effect and no studies whatsoever showing a positive effect (there is one study demonstrating no effect), manufacturers continue to manufacture it and health food stores continue to push it as an alternative to niacin that causes the flush. It's quite expensive, commonly costing $30-$50 for 100 tablets.

Don't fall for this gimmick. Niacin is among the most helpful of treatments for gaining control over coronary plaque. It raises HDL, corrects small LDL, reduces triglycerides (along with its friend, fish oil, of course), reduces lipoprotein(a), and dramatically contributes to reduced heart attack risk. No-flush niacin does none of this. Track Your Plaque Members: For a thorough discussion of niacin--how to use it, what preparations work and which do not, read Niacin: Ins and outs, ups and downs on the www.cureality.com website.
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Comments (3) -

  • Hoop

    7/4/2007 8:38:00 AM |

    Then again it maybe this patient was using too low a dose?
    And what else was the patient ingesting? And there is the issue of which class lipid abnormality this patient had.

    In my comments below I've included some abstracts of some human based studies that suggest inositol hexanicotinate isn't useless for altering serum lipid levels.


    If we assume for a moment the validity of your anecdote,
    I won't call inositol hexanicotinate worthless rather I would suggest it might have has narrower scope of uses not including the altering
    blood lipids.  Not everyone (me) takes large doses niacin for it lipid altering properties. Consider Kaufman's work with niacinamide in patients
    with degenerative arthritis. He used doses of 1.5 to 4 grams and
    claimed increased joint mobility after a couple of months.
    In my experience, niacin also works as well as niacinamide
    against my pains in and around my joints. Its benefits against the pain come about gradually but
    nonetheless are quite effective for me.

    The flush can be pretty nasty if one isn't careful about the dose.
    I know when I mixed niacinamide and niacin in the past I seemed
    to have somewhat more flushing. I took niacin for several years
    until it started to be trigger atrial premature beats.
    I'll comment further in this posting on a way around these adverse effects of niacin.


    Inositol hexanicotinate maybe superior provided one chooses
    the right patients? Please see the second abstract below.
    ----------------------------------------------------


    1: Eur. J. Clin. Pharmacol. 1979 Aug;16(1):11-5.


    Nocturnal inhibition of lipolysis in man by nicotinic acid and derivatives.


    Kruse W, Kruse W, Raetzer H, Heuck CC,
    Oster P, Schellenberg B, Schlierf G.


    The effect of nicotinic acid and several derivatives
    on the nocturnal level of free fatty acids was studied
    in 12 healthy young women and men. Free fatty acids
    are an important precursor of plasma triglycerides
    and their concentration is highest at night.
    The drugs used were nictinic acid, beta-pyridyl-carbinol,
    mesoinositol hexanicotinate and xantinol nicotinate.
    The highest plasma nicotinic acid level was observed
    with beta-pyridyl-carbinol, but significant reduction in
    free fatty acids during the entire night was only
    achieved with inositolhexanicotinate and
    xantinol nicotinate. There was no correlation between
    the plasm levels of free fatty acids and nicotinic
    acid at any sampling time. If prolonged reduction
    in free fatty acid concentration is desired in the therapy of
    hyperlipidemias, the inositol and xantinol esters of
    nicotinic acid appear to be superior to the other preparations.


    PMID: 499296 [PubMed - indexed for MEDLINE]
    ========================================


    Inositol hexanicotinate seems to work to lower some
    blood lipids in this next human study and granted
    another drug is also involved.
    -------------------------------------------------------------
    1: Arzneimittelforschung. 1979;29(10):1621-4.


    [Treatment of various types of hyperlipoproteinaemia with
    a combination of Mg-chlorophenoxy-isobutyrate and
    mesoinositol-hexanicotinate (author's transl)]


    [Article in German]


    Bolzano K, Krempler F, Haslauer F.


    50 patients with different types of hyperlipoproteinaemia
    were treated with a combination of Mg-chlorophenoxyisobutyrate
    (700 mg) and mesoinositol-hexanicotinate (500 mg) (Atroplex)
    twice daily. 7 patients had type IIa, 39 patients type IIb
    or IV and 4 patients type V. After a period of one
    month without any treatment the patients were treated
    during two months. While the effects of this combination
    on cholesterol of type IIa patients was poor, the
    drug had an excellent lipid-lowering effect in the patients
    with type IIb, IV and V. After 14 days' treatment the
    plasma cholesterol and triglyceride levels in
    patients of type IIb or IV were significantly lowered.
    This effect became even more pronounced after
    one-month treatment. There was no significant difference
    between the effect of one-month treatment and
    that of two-month treatment. About two-thirds of the
    patients of type IIb or IV were responders. No serious side
    effects could be observed during our study.


    Publication Types:
        English Abstract


    PMID: 583231 [PubMed - indexed for MEDLINE]
    --------------------------------------------------
    So could it have been that this patient had one of the classes
    of hyperlipidemic disorders such as type 1, type
    2-a or type 3 for which inositol hexanicotinate
    maybe ineffective?


    =====================================================
    It may have other uses see next paper.
    -------------------------------------


    1: Clin. Rheumatol. 1988 Mar;7(1):46-9.


    A double blind randomised placebo controlled trial
    of hexopal in primary Raynaud's disease.


    Sunderland GT, Belch JJ, Sturrock RD,
    Forbes CD, McKay AJ.


    University Department of Surgery,
    Glasgow Royal Infirmary, Scotland.


    The peripheral vasospastic symptoms associated
    with Raynaud's disease continue to
    be an unsolved clinical problem. Hexopal
    (Hexanicotinate inositol) has shown
    promise in uncontrolled studies and its use in
    patients with Raynaud's disease may reduce such
    vasospasm. This study examines the effects of
    4 g/day of Hexopal or placebo, during cold weather,
    in 23 patients with primary Raynaud's disease.
    The Hexopal group felt subjectively better and
    had demonstrably shorter and fewer attacks of
    vasospasm during the trial period.
    Serum biochemistry and rheology was
    not significantly different between the
    two groups. Although the mechanism of
    action remains unclear Hexopal is safe
    and is effective in reducing the vasospasm
    of primary Raynaud's disease during the winter months.


    Publication Types:
        Clinical Trial
        Randomized Controlled Trial
        Research Support, Non-U.S. Gov't


    PMID: 3044673 [PubMed - indexed for MEDLINE]
    ====================================================
    : J. Int. Med. Res. 1979;7(6):473-83.


    An experimentally controlled evaluation of the effect
    of inositol nicotinate upon the digital blood flow
    in patients with Raynaud's phenomenon.


    Holti G.


    The vaso-active effects of inositol nicotinate (Hexopal)
    were investigated in thirty patients with primary and
    secondary Raynaud's phenomenon using several
    non-invasive experimental techniques under
    controlled conditions. The earlier formed impression
    that this drug requires a prolonged 'build-up' period was
    confirmed. Recording the time required to induce
    Raynaud's phenomenon as well as assessments of total
    and nutrient digital blood flow showed significant
    beneficial therapeutic effects upon the skin's
    microcirculation by inositol nicotinate. This study
    suggests that the therapeutic effect of this drug is not
    merely due to vasodilation but that other mechanisms
    such as enhanced fibrinolysis and lowering of
    serum lipids may play a significant part in its
    overall effect. Smokers responded slower than non-smokers,
    but even elderly patients with longstanding vasospastic
    disease showed measurably improved digital circulation.
    Unlike some other drugs in this field inositol nicotinate was found
    to be effective orally and to be devoid of unwanted side-effects.
    However, in the majority of patients it failed to
    abolish their increased vascular spasm although
    it diminished it significantly in most. It appears
    to be a safe and well tolerated drug, which,
    together with other symptomatic measures, merits
    to be used in the management of vasospastic
    disease of the extremities even in the
    presence of partial obliteration of the microcirculation.


    Publication Types:
        Clinical Trial
        Randomized Controlled Trial


    PMID: 391622 [PubMed - indexed for MEDLINE]
    =======================================


    Perhaps what is needed is a larger dose in comparison
    to other forms of niacin?

    ---------------------------------------------
    Now to expand the topic to plain old TR niacin and betaine.
    ---------------------------------------------

    Timed release niacin as I recall is twice a effective
    as simple niacin in lowering lipids and twice as toxic.
    So it seems come out about even if one takes a half
    the dose of TR niacin.

    Of course, what I'd love to test is niacin in its various forms
    along with trimethylglycine (TMG) aka betaine. And I won't  
    just consider lipid level effects but also the effects on
    osteoarthritis and other joint pains.

    Why do I mention betaine? I know from personal experience
    high doses of betaine along with niacin pretty well blocks
    the flushing effect as well as completely
    blocking the atrial premature beats (AVB) that I would get
    when taking either high dose niacin or niacinamide.
    I had taken niacin at a rather high doses for about 5 or 6 years
    back a couple of decades ago and then I started
    to get the AVBs when I tried to
    resume the use of doses above 100 milligrams.
    Now of course provided I take the betaine I don't have
    this problem. However, I do get AVBs if I don't use the
    betaine and only take the niacin.
    Granted some suggest niacin lowers the lipid levels
    by "stressing" the liver so if betaine blocks
    this effect it maybe contraindicated for the purpose
    of changing lipid levels.
    Here are Pubmed ID numbers, for some papers that
    reflect similar thinking using betaine to reduce
    the toxicity of high dose B-3.
    PMID: 10985907
    PMID: 17156888

    --------------------------------------------

    I'd be interested in your comments on the points of
    theory and science. I am not looking for personal
    advice. A number of people including myself
    are discussing the niacin topic on the
    Usenet forum....sci.life-extension (which
    is also available by way of the Google Group
    Archive for free provided you have a throw away email address).
    Someone else referred to your blog comments and yet
    another person proposed contacting you for a comment.
    I was elected Wink to contact you.
    The group/forum members were interested as to whether there is
    more to your anecdote concerning the possible ineffectiveness
    of inositol hexanicotinate as a lipid lower agent.

    Thank You.

  • Dr. Davis

    7/4/2007 1:36:00 PM |

    Thanks for your insightful comments.

    My experience is based on the experiences of about 10 patients on the no-flush preparation in doses of 1000-4000 mg per day.

    If the rationale for the no-flush preparation is that it provides niacin in such a way as to avoid the flush, we should see rises in HDL, reductions in triglycerides, small LDL, and lipoprotein(a), regardless of the type of hyperlipidemia present (IIa, IIb, III, etc.).

    After using no-flush for up to one year, I have seen absolutely no effect, accepting my relatively small experience.

    Please also understand that my focus is prevention and reversal of coronary heart disease, something that the Track Your Plaque approach does exceptionally well, so I try not to stray off too far from our focus. But why would no-flush have any beneficial effects on arthritis, etc.,as an alternative method of delivering niacin when niacin itself does not possess these effects? I'm not sure I follow the rationale. To be included in a program of coronary atherosclerotic regression, we would have to see substantial effects, as we do with plain old niacin.

    Nonetheless, I encourage your continuing interesting thoughts.

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    11/3/2010 12:29:51 PM |

    Just Friday, a 41-year old woman came to my office for consultation because her doctor didn't know what to do with lipoprotein(a). She had seen a cardiologist who told her to take no-flush niacin. Both the cardiologist and the patient were therefore puzzled when lipoprotein(a) showed no drop and, in fact, was slightly higher on the no-flush preparation.

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