Laropiprant is the Bad One; Niacin is/was/will always be the Good One
by W. Todd Penberthy, PhD
(OMNS July 25, 2014) Niacin has been used for
over 60 years in tens of thousands of patients with tremendously favorable
therapeutic benefit (Carlson 2005). In the first-person NY Times best
seller, "8 Weeks to a Cure for Cholesterol," the author describes his journey
from being a walking heart attack time bomb to a becoming a healthy individual.
He hails high-dose niacin as the one treatment that did more to correct his poor
lipid profile than any other (Kowalski 2001). Many clinical studies have shown
that high doses of niacin (3,000-5,000 mg plain old immediate release niacin
taken in divided doses spread out over the course of a day) cause dramatic
reductions in total mortality in patients that experienced previous strokes
(Creider 2012). High dose niacin has also been clinically proven to provide
positive transformational relief to many schizophrenics in studies involving
administration of immediate release niacin in multi-thousand-milligram
quantities to greater than 10,000 patients (Hoffer 1964; Osmond 1962). Most
importantly, after 60 years of use the safety profile for niacin (especially
immediate release niacin) remains far safer than the safest drug (Guyton
2007).
Bad Reporting
So why has the media suddenly presented the
following niacin alarmist headlines in response to the most recent study in the
New England Journal of Medicine?
"Niacin drug causes serious side effects, study
says" - Boston Globe, 7/16/14
"Niacin safety, effectiveness questioned in new
heart study" - Healthday News, 7/17/14
"Doctors say cholesterol drug risky to take" -
Times Daily, 7/16/14
"Niacin risks may present health risks claim
scientists" - Viral Global News, 7/17/14
"Studies reveal new niacin risks" - Drug
Discovery and Development, 7/17/14
"No love for niacin" - Medpage Today,
7/17/14
"Niacin could be more harmful than helpful" -
Telemanagement, 7/18/14
The truth of the matter is that the study quoted
and used laropiprant (trade names: Cordaptive and Tredaptive). Laropiprant is a
questionable drug and the results say next to nothing about niacin. The study
compared over 25,000 patients treated with either niacin along with laropiprant,
or placebo. The patients in this study had previous history of myocardial
infarction, cerebrovascular disease, peripheral arterial disease, or diabetes
mellitus with evidence of symptomatic coronary disease. The side effects
observed in those who took the laropiprant-niacin combination were serious and
included an increase in total mortality as well as significant increases in the
risk for developing diabetes.
For responsible reporters, this should have
raised the question of which compound, the drug laropiprant, or the vitamin
niacin, is the culprit.
Such side effects have not been seen in over 10
major clinical trials of niacin involving tens of thousands of patients, not in
over 60 years of regular usage of niacin in clinics across the country. However,
niacin causes a warm flush on the skin. Some people find the warm niacin flush
uncomfortable, although many people enjoy this temporary sensation. In this
study, niacin was given in combination with laropiprant, a drug that prevents
the niacin flush. By including a dose of laropiprant along with the niacin to
eliminate the flush, the thought was that more patients could benefit from
niacin without complaint. But in fact the niacin flush is healthy. A reduced
flush response to niacin is a diagnostic for increased incidence of
schizophrenia, and this assay is now widely available (Horrobin 1980; Messamore,
2003; Liu 2007; Smesny, 2007).
Problems with Laropiprant
So what about the other half of the combo, the
drug laropiprant?
- Laropiprant has never been approved by the FDA for use in the USA and when taken alone has been shown to increase gastrointestinal bleeding. *
- Laropiprant interferes with a basic prostaglandin receptor pathway that is important for good health.
- Last year Merck announced it would withdraw laropiprant worldwide due to complaints from continental Europe. Therefore the clinical trials in this most recent study could only be performed in the UK, Scandinavia, and China.
So why did so many media outlets and even some
MDs conclude that niacin was the problem? Simple: none of the headlines
mentioned laropiprant, which is quite clearly the real culprit that caused the
side effects reported. The simplest way to put it is to say that sensational
stories promulgated by the media are quite often completely wrong. This suggests
a hidden agenda.
Confusing and fantastical headlines can increase
readership for hysteria-based business models. Which headline is likely to
garner the greatest attention: "Laropiprant is a Dangerous Medication that has
Not Been Approved by the FDA" or "Niacin Causes Serious Side Effects"? The
correct headline would be, "Niacin doesn't cause serious side effects; drugs
do."
Why the B Vitamins Are So Important
The B vitamins were discovered due to terrible
nutritional epidemics: pellagra (niacin/vitamin B3 deficiency) and beriberi
(thiamine/vitamin B1 deficiency). We are very sensitive to a deficiency of
niacin. Over 100,000 people died in the American south in the first two decades
of the 20th century due to a lack of niacin in their diet. It was perhaps the
worst nutritional epidemic ever observed in modern times, and was a ghastly
testimony to how vulnerable the human animal is to niacin deficiency. The
pellagra and beriberi epidemics took off shortly after the introduction of
processed foods such as white rice and white flour. Poor diets, mental and
physical stresses, and certain disease conditions have all been proven to
actively deplete nicotinamide adenine dinucleotide (NAD) levels, causing
patients to respond favorably to greater than average niacin dosing.
How is it possible that niacin can be useful for
many different conditions? It seems too good to be true. The reason is that
niacin is necessary for more biochemical reactions than any other
vitamin-derived molecule: over 450 different gene-encoded enzymatic reactions
(UniproKB database of the Swiss Institute of Bioinformatics; (Penberthy 2013)).
That is more reactions than any other vitamin-derived co-factor! Niacin is
involved in just about every major biochemical pathway. Some individuals, who
have a genetically encoded amino acid polymorphism within the NAD binding domain
of an enzyme protein, will have a lower binding affinity for NAD that can only
be treated by administering higher amounts of niacin to make the amount of NAD
required for normal health. Genetic differences such as these are why many
individuals require higher amounts of niacin in order for their enzymes to
function correctly (Ames 2002).
It is a deadly shame that the media so often
ignores this information. Fortunately, many physicians will see through the
recent headlines that give misinformation about niacin, having already
personally witnessed how effective high dose niacin therapy is for preventing
cardiovascular disease.
Nutrients are the Solution, Not the Problem
So what is the solution? At the end of the day
the data on patients with problem cholesterol/LDL levels still support
3,000-5,000 milligrams of immediate-release niacin as the best clinically-proven
approach to maintaining a healthy lipid profile. Niacin in 250mg to 1000mg doses
can be purchased inexpensively from many sources. Extended-release niacin is the
form of niacin that is most frequently sold by prescription, but it has more
side effects than immediate release (plain old) niacin. . . and it costs much
more.
Tangential to niacin but pointed to
cardiovascular disease, conventional medicine is finally beginning to respect
chelation therapy as an approach owing to the recent unparalleled positive
clinical results for cardiovascular disease patients with diabetes - up to 50%
prevention of recurrent heart attacks and 43% reduction in death rate from all
causes (Avila 2014). Some times chelation therapy can be expensive. However,
there are other inexpensive approaches include high dose IP6 therapy that are
yet to be conventionally appreciated. Other supplements desirable for any ideal
cardiovascular disease: a nutritional regimen include additional vitamin C,
magnesium, coenzyme Q, fat soluble vitamins (A, D, E, and K2), and grass-fed
organic butter. Your ideal intake varies with your individuality.
Nutrients such as niacin you need. Media
misinformation you don't.
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