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by James LaValle, R.Ph., NMD, CCN
Safe Approaches to
Inflammation and Pain
 Inflammationit's now a front-page
headline. Many people suffer from
arthritis and other painful inflammatory
conditions, but little did they know that
inflammation inflicts many devastating
effects, even beyond the outward effects
of pain and swelling. Although this story
has been developing for several years,
the picture is now very clear . . . inflammation
is known to be a factor in most of
our chronic diseases, including heart disease
(high cholesterol levels, stroke,
angina and heart attacks), cancer, diabetes,
even Alzheimer's and Parkinson's
disease. In fact, nutrition experts have
been warning for years that inflammation
is the common thread to these seemingly
unrelated diseases of aging.
Another reason inflammation is capturing
headlines is that the common
medical treatments for inflammation and
inflammatory conditions, non-steroidal
anti-inflammatory drugs (NSAIDs), can
have unwanted and dangerous side
effects. VioxxR(rofecoxib), one of the drugs
in the non-steroidal anti-inflammatory
drug category, was recently pulled from
the market because it appears to increase
the risk of blood clots, heart attack and
stroke. Over the counter NSAIDS, such as
ibuprofen and naproxen, can cause
stomach and gastrointestinal irritation.
Acetaminophen is a pain reliever that is
not an NSAID, but it also has side effects;
it can be toxic to the liver or kidneys in
high doses or even in lower doses in
those who drink alcohol, even moderately.
This begs the question, are there
other options?
Fortunately, there are several steps
one can take for relief of pain and inflammation
that are free of these side effects,
and actually have significant heart benefits
such as lowering cholesterol in addition
to decreasing inflammation (see
below). In order to understand how these
natural substances work, it is helpful to
first understand exactly what inflammation
is and how it leads to chronic diseases.
What exactly is inflammation? It is a
vascular and cellular response to illness
or injury that causes pain, redness,
swelling and tissue damage. Inflammation
can be driven by diet and lifestyle; it can
manifest itself in diseases such as arthritis,
or it can be occurring silently inside until it
finally results in heart disease or
Alzheimer's.
The various compounds in the body
that cause inflammation, such as histamine,
cytokines and prostaglandins, are
called the mediators of inflammation.
Cytokines are released from activated
white blood cells and include interleukin-
6 (IL-6), interleukin-1B (IL-1B), leukotriene
B4 (LT-B4) and tumor necrosis factor
alpha (TNF-a). All of these cytokines are
known to be elevated in those who suffer
from rheumatoid arthritis, and they can
be a factor in osteoarthritis. These substances
also cause increased production
of fibrinogen and are the connection
between inflammation and heart disease.
Fibrinogen is a protein that assists in
the formation of blood clots. Increase
your body's tendency to form blood clots,
and you are increasing your risk of heart
attack and stroke. Some researchers
believe that the serious cardiovascular
side effects of the drug Vioxx are the
result of its increasing the tendency to
form blood clots by causing platelets to
aggregate, or stick together. Fortunately,
there is one natural anti-inflammatory/
pain reliever available that has the opposite
effect, i.e., it keeps platelets from
sticking together (see below).
Ways to Stop Excess Inflammation
Fighting inflammation can be done on
different levels. Dietary and lifestyle
measures can be used to prevent inflammation
from occurring in the first place.
However, they may not be enough for
someone who already has elevated
inflammatory cytokines, and generally
lifestyle measures alone will not be
enough to stop inflammatory pain.
With existing inflammation, dietary
supplements or drugs may be used to
reduce the levels of inflammatory
cytokines. However, drug therapies may
not be the safest first option due to
the known side effects. The NSAIDs
discussed earlier work by inhibiting the
enzymes (COX 1 and COX 2 enzymes) that
are responsible for converting prostaglandins
to inflammatory cytokines. COX 1 enzymes
are needed for prostaglandin production in
the stomach; without them the mucosal linings
of the stomach begin to breakdown,
and ulcers can form. The primary side effect
of NSAIDs is gastrointestinal upset, GI
bleeding and ulcers.
Selective COX 2 inhibitors are another
drug option; they are so-named because
they affect only the COX 2 enzyme and
thereby inhibit inflammation without significantly
affecting the COX 1 enzyme. The
prescription drug Vioxx was claimed to
be a selective COX 2 inhibitor. But after a
short time on the market, the FDA
required that the gsafer on the stomachh
claim be removed from its advertising. In
addition, the drug turned out to have
fatal cardiovascular side effects. A recent
article, however, has revealed that other
COX 2 inhibitors do not have the risks that
Vioxx did, indicating that not all COX 2
medications work in the same way.
A Natural Agent Takes Center Stage
One herbal extract in particular has been
demonstrated to be an effective antiinflammatory.
NexrutineŽ is a patentpending
plant extract developed from
the Phellodendron tree (Phellodendron
amurense). (www.nexrutine.com). Nexrutine
was shown in one clinical trial to reduce
pain and improve physical functioning
and mental status in osteoarthritis
patients as evidenced by improved
scores on the SF-36, a questionnaire
widely used in clinical studies to evaluate
physical and mental pain and function.
As always, with any product, whether
from plants or synthetic drugs, if the
mechanism of action is suspected to be
somewhat inhibitory of COX 2 enzymes,
safety must always be considered. The
plant source of Nexrutine has been used
safely for thousands of years for various
conditions in traditional medicine.
Animal and human clinical trials have
been conducted to verify the safety of this
herbal extract, and no significant side
effects have been noted. While some
other anti-inflammatory products have
been shown to increase the risk for cardiovascular
problems by causing
platelets to aggregate (blood clotting),
Nexrutine's safety is further enhanced by
the fact that the major anti-inflammatory
compound in Nexrutine has the opposite
effect. In fact, a study published in 2002
Thrombosis Research reported that the
primary active ingredient in Nexrutine
significantly inhibited platelet aggregation.
Another study reported in Nature
Medicine this year found that this same
active ingredient lowered total cholesterol
in test subjects anywhere from 18 to
25 percent without affecting HDL. The
anti-platelet and the cholesterol-lowering
capabilities of Nexrutine with its efficacy
for pain and inflammation certainly combine
to make this an extremely beneficial
and promising natural anti-inflammatory
option.
Other herbal agents that have shown
promise as anti-inflammatory agents are
curcumin, boswellia and green tea,
though human trails on the efficacy of
boswellia and curcumin as an antiinflammatory
are limited. Green tea is
better known for its cancer prevention
and thermogenic properties than its antiinflammatory
properties.
Lifestyle and dietary intake have a profound
effect on either promoting or
inhibiting inflammation. Several lifestyle
measure and dietary changes can also be
made to reduce or prevent inflammation.
Stop smokingCigarette smoke introduces
irritants into the lung linings and
bloodstream that induce an inflammatory
response in the tissues.
Control the stress responseStress can
cause cortisol levels to elevate. Cortisol
stimulates the production of TNF alpha
and IL-6 directly. Chronically elevated cortisol
is linked with obesity and increased
belly fat, a known source of inflammatory
cytokine production. Consider taking
ReloraR for stress. Relora (www.relora.com) is
a proprietary natural product, containing
patented ingredients extracted from two
plant species used in Traditional Chinese
Medicine for over 1500 yearsPhellodendron amurense and Magnolia
officinalis. Studies on Relora indicate it
may help to relieve stress, lower cortisol
and prevent weight gain.
Eat a healthy dietEat plenty of fruit,
vegetables, some fish and make sure
your meals are low in saturated fat. Fruits
and vegetables provide antioxidants that
help neutralize free radicals produced by
inflammation and therefore help prevent
the further inflammation that can be a
result of free radical damage to cells. Fish
oils are known to inhibit inflammation by
turning off the pathways that lead to the
production of inflammatory substances.
If you are reluctant to eat fish because of
contamination concerns, take a daily
dose of fish oil, at least 1.8 grams per day.
Trans fats contained in margarines and
partially hydrogenated oils promote
inflammatory pathways. Avoid trans fats
and foods that contain them.
Exercise and control your weightFat
cells are efficient factories for producing
inflammatory cytokines, and burning
calories shrinks those cells reducing sites
of inflammation.
Get adequate sleepGetting enough
sleep is known to be an important factor
in pain management. Studies are also
revealing that sleep deprivation increases
inflammatory factors. Eliminating caffeine
is one measure that improves sleep.
In addition, supplements like 5HTP,
Seditol. (www.seditol.com) and melatonin
help promote restful sleep.
Oral hygieneBacteria that can be
present in the gums may be a source of
inflammation in the body. Therefore,
good oral hygiene is another way to
reduce internal inflammation.
Other dietary supplements that may
help in controlling the excessive release
of cortisol and chronic inflammation
include:
A quality multiple vitamin/mineral
dailyE vitamins get used up at accelerated
rates during times of stress. In addition,
other vitamins and minerals are
important for maintaining overall health
and immunity. Some have specific antiinflammatory
action; for instance, zinc is
known to help control the over production
of nitric oxide, a free radical that can
damage cells when excesses occur in the
body.
Selected references:
Vgontzas, A., et al. Circadian Interleukin-6 Secretion and Quantity and Depth of Sleep, J Clin Endo and Met. (Aug. 1999).
Thrombosis Research 106 (2002). pp 2237
James B. LaValle, R.Ph., NMD, CCN is the
author of The Cox-2 Connection: Breakthrough
Treatment of Arthritis, Alzheimer's and Cancer.
Published by Healing Arts Press, Rochester,
Vermont. He is a faculty member at the
British Institute of Homeopathy and the
University of Cincinnati College of Pharmacy.
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