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Pain & Inflammation

Tags: pain, inflammation

Chronic Pain

Pain affects more Americans than diabetes, heart disease and cancer combined. 1 Millions suffer from chronic pain every year and the effects of this type of recurring pain exact a tremendous toll in health care costs, lost worker productivity, as well as the emotional and financial burden it places on patients and their families. According to a recent Institute of Medicine Report, pain is a significant public health problem that costs society at least $560-$635 billion annually, an amount equal to about $2,000.00 for every man, woman and child living in the U.S.2

Unfortunately, the conventional prescription and over-the-counter pain killers available are fraught with dangerous adverse effects. Conservative calculations estimate that approximately 107,000 patients are hospitalized annually for nonsteroidal anti-inflammatory drug (NSAID)-related gastrointestinal (GI) complications and at least 16,500 NSAID-related deaths occur each year among arthritis patients alone.3 COX-2 inhibitors like Vioxx®, Bextra®, Celebrex®, etc. were launched with great expectations regarding their benefits, but soon thereafter it was discovered that the benefits experienced were greatly offset by the fact that these anti-inflammatories caused myocardial infarctions (heart attacks) and cerebrovascular accidents (strokes). The risks were so great that the Food and Drug Administration (FDA) went so far as to take both Vioxx and Bextra off the market.

But what if you could offer your patients an anti-inflammatory product that would inhibit COX-2 (cyclooxygenase-2) and 5-LOX (5-lipoxygenase), without any side effects? Common herbs from India – turmeric and boswellia – hold the answer to inflammation and chronic pain. As research demonstrates, these natural ingredients are superior to conventional drugs in efficacy and have the additional benefit of not putting your patient’s health at risk.

Background & Evidence

Curcumin

The plant turmeric (Curcuma longa) is very well known in India. The root is harvested, cleaned, dried, and powdered to be used as a spice (turmeric gives curry its beautiful golden yellow color). The key to turmeric’s health effects lies in the compound known as curcumin. Turmeric contains only 2-5% curcumin content, so prescribing an unstandardized, powdered turmeric root product means that your patients are going to need to ingest very large amounts to get even a modest amount of curcumin into the bloodstream. For medicinal effects, turmeric powder cannot provide the physiological effects of curcumin.

Curcumin is extremely effective in relieving inflammation, which is a key causative factor in 80-90% of all chronic disease, including chronic pain. Rather than influencing a single pathway, as most conventional prescription and over-the-counter pain killers do, curcumin simultaneously influences multiple pathways on multiple levels. For example, research has shown curcumin has the ability to suppress the activation of the NF-kB, as well as down-regulate COX-2, inhibit 5-LOX, and inhibit the activity of TNF.4,5 Curcumin is also a potent antioxidant, able to neutralize unstable, reactive free radicals.

Unfortunately, standard curcumin extracts are poorly absorbed, and any curcumin that does reach the bloodstream quickly converts into other compounds. This means that patients have to ingest large doses in order to realize any health benefits. In some studies, patients took as many as 16-24,capsules a day, which can be problematic, expensive, and makes compliance difficult.

Scientists in India have created a curcuminoid complex (curcumin is one kind of curcuminoid) which is better absorbed than standard curcumin. In comparison tests, this specialized curcumin, which is ground into a very fine powder and mixed with turmeric essential oils, was up to 10 times better absorbed than plain curcumin, and it stayed active in the bloodstream at meaningful levels for much longer.6 Because of its enhanced absorption, this blend is extremely effective in reducing inflammation. It not only inhibits COX-2, but does it in such a way as not to block it completely since some COX-2 is necessary for other body functions. This modulation means that the COX-2 inflammatory pathway is quieted without any significant side effects.

To date, there have been 12 published studies (6 of which are human clinical trials) on the role of this special, highly absorbable form of curcumin in treating rheumatoid and osteoarthritis, Alzheimer’s Disease, precancerous conditions, depression, blood lipids and cardiovascular health, as well as absorption and retention.6, 7-12

In one double-blind study, this highly absorbable curcumin was shown to work as well as an NSAID as a pain reliever and anti-inflammatory in rheumatoid arthritis, but without the dangerous side effects.10 The study looked at the effects of 500 mg of a specialized highly absorbable curcumin extract taken twice daily compared with the prescription drug diclofenac sodium (one brand name is Voltaren®) 50 mg taken twice daily, or a combination of the two in patients with rheumatoid arthritis. The group receiving the highly absorbable curcumin had the greatest reduction in joint pain and swelling with no adverse effects. In contrast, 14% of the participants in the drug group stopped the test because of the adverse effects they experienced.

Additional studies are currently underway in the U.S., Australia, Canada, and Asia for a variety of health concerns, including Alzheimer’s disease and lung cancer. Researchers cite their selection of this form of curcumin because of its absorption, retention, human safety profile, purity and use of only approved class 3, food-grade solvents in its extraction process.

While curcumin is a potent anti-inflammatory and antioxidant in its own right, there are additional natural ingredients that can support and work synergistically with curcumin to further relieve both acute and chronic pain.

Boswellia

Boswellia (Boswellia serrata) is another traditional herb that can effectively reduce inflammation and relieve pain.13 It does this by inhibiting 5-LOX, an enzyme that activates leukotrienes, which in turn induce inflammation. The majority of boswellia’s anti-inflammatory activity is linked to the array of boswellic acids in the extract, the most active of which is AKBA (Acetyl-11-keto-β-boswellic acids). However, there are challenges to using boswellia as an effective natural medicine. Unstandardized boswellia can have as little as 1% AKBA. Additionally, there is a pro-inflammatory compound in boswellia called beta boswellic acid (BBA) that interferes with the overall anti-inflammatory effects of this herb. BBA can account for over 20% of the boswellic acids.

A unique and patented form of boswellia has been shown to have a higher level of efficacy. This specialized boswellia extract has higher naturally occurring levels of AKBA (not spiked) and is standardized to a minimum of 10% AKBA. This means it can have up to 10 times the amount of plain boswellia’s most active compound. It’s also purified to reduce beta boswellic acid. By screening out most of these undesirable boswellic acids, this specialized extract is able to provide much greater clinical benefit than standard boswellia extracts.

A combination of this high absorption curcumin and purified boswellia was judged superior to the prescription arthritis drug, celecoxib (brand name Celebrex®) in a clinical study of osteoarthritis.9 Celecoxib is the best-selling prescription drug for arthritis in the United States. Subjects in this 12 week study were randomized to two groups. One group received 100 mg of celecoxib twice daily, while the second group received a 500 mg blend of this unique curcumin and boswellia twice daily. Symptom scoring and clinical evaluation demonstrated superior results on pain relief and distance walked without pain for the curcumin and boswellia blend compared to celecoxib. The combination was shown to be equal to celecoxib on measures of joint flexibility.

Curcumin and boswellia form the foundation of any effective pain-relieving formula because of their ability to reduce the activity of the two most significant inflammation pathways in the body – COX-2 and 5-LOX.

DLPA

The pain reliever DLPA (D,L-phenylalanine) contains two forms of the amino acid phenylalanine. The “D” form of phenylalanine appears to block a nervous system enzyme (enzyme carboxypeptidase A) that intensifies pain signals.14-17 The “L” form improves mood-elevating chemicals in the brain, such as dopamine, epinephrine and norepinephrine.14-16 According to current theory, DLPA prevents the breakdown of one of the brain’s natural pain-killing substances, enkephalins, which are in the same family as endorphins. DLPA supplements combine the “L” and “D” forms of phenylalanine, which work synergistically to reduce chronic pain and improve mood—two concerns that are interconnected.18,19

Nattokinase

This enzyme from fermented soybean increases microcirculation, enabling other compounds that are carried in the bloodstream (such as curcumin, boswellia, and pain-killing endorphins) to reach the areas where they are needed the most.20,21 It also decreases fibrinogen in the body, a compound that is associated with muscle damage and muscle fiber stiffness.22

Summary

Curcumin, boswellia, DLPA and nattokinase provide one of the most powerful anti-inflammatory and pain relieving combinations you can offer your patients. These ingredients, which have been proven to be highly effective and safe for extended use, will benefit anyone who is suffering from pain, whether it is acute, sudden pain such as trauma,  overexertion, sprains, bone damage and burns, or chronic pain from arthritis, migraine headaches, bursitis, back pain, or any type of recurring pain. Research shows these ingredients are as effective as synthetic drugs and have no significant adverse effects.

Formula

Consider adding the following formula to your dispensary:

Proprietary Complex                                                                                                    727 mg

DLPA (dl Phenylalanine), Boswellia (Boswellia serrata) Gum Resin Extract (BosPure®) standardized to contain >70% Total Organic and Boswellic Acids with AKBA >10%, with less than 5% beta-boswellic acids, Curcumin (Curcuma longa)   Rhizome Extract (BCM-95®) standardized for curcuminoid complex (curcumin, demethoxycurcumin and bisdemethoxycurcumin), Nattokinase

 

Recommendations: Initial dosing is one capsule three times daily. Many integrative practitioners recommend using up to 3 capsules three times daily.

References:

  1. AAPM Facts and Figures on Pain. The American Academy of Pain Medicine website. Located at: http://www.painmed.org/PatientCenter/Facts_on_Pain.aspx. Accessed on January 21, 2013.
  2. Institute of Medicine Report from the Committee on Advancing Pain Research, Care, and Education: Relieving Pain in America, A Blueprint for Transforming Prevention, Care, Education and Research. The National Academies Press, 2011.
    http://books.nap.edu/openbook.php?record_id=13172&page=1.
  3. Singh G. Recent considerations in nonsteroidal anti-inflammatory drug gastropathy. Am J Med. 1998;105(1B):31S-38S
  4. Jurenka JS. Anti-inflammatory properties of curcumin, a major constituent of Curcuma longa: a review of preclinical and clinical research. Altern Med Rev. 2009;14(2):141-53.
  5. Jacob A, Wu R, Zhou M, Wang P. Mechanism of the Anti-inflammatory Effect of Curcumin: PPAR-gamma Activation. PPAR Res. 2007;89369.
  6. Antony B, Merina B, Iyer VS, Judy N, Lennertz K, Joyal S. A pilot cross-over study to evaluate human oral bioavailability of BCM-95 CG (Biocurcumax™) a novel bioenhanced preparation of curcumin. Ind J Pharm Sci. 2008:445-449.
  7. Benny B, Antony B. Bioavailability of Biocurcumax (BCM-95). Spice India. 2006:11-15.
  8. Baum L et al. Six-Month Randomized Placebo-Controlled, Double-Blind, Pilot Clinical Trial of Curcumin in Patients with Alzheimer’s Disease. J Clin Psychopharmacol. 2008; 28(10):110-14.
  9. Antony B, Kizhakedath R, Benny M, Kuruvilla BT. Clinical Evaluation of a herbal product (Rhulief™) in the management of knee osteoarthritis. Abstract 316. Osteoarthritis Cartilage. 2011;19(S1):S145-S146.]
  10. Chandran B, Goel A. A Randomized, Pilot Study to Assess the Efficacy and Safety of Curcumin in Patients with Active Rheumatoid Arthritis. Phytother Res. 2012;26(11):1719-25
  11.  Baum L, Cheung SK, Mok VC, Lam LC, et al. Curcumin effects on blood lipid profile in a 6-month human study. Pharmacol Res. 2007;56(6):509-14.
  12. Deepa Das A, Balan A, Sreelatha KT. Comparative Study of the Efficacy of Curcumin and Turmeric as Chemopreventative Agents in Oral Submucous Fibrosis: A Clinical and Histopathological Evaluation. JIAOMR. 2012;22(2):88-92
  13. Ammon HP. Boswellic acids in chronic inflammatory diseases. Planta Med. 2006;72(12):1100-16.
  14. Ehrenpreis S. Analgesic properties of enkephalinase inhibitors: animal and human studies. Prog Clin Biol Res. 1985;192:363-370.
  15. Ehrenpreis S. D-phenylalanine and other enkephalinase inhibitors as pharmacological agents: implications for some important therapeutic application. Acupunct Electrother Res. 1982;7(2-3):157-72.
  16. DPLA. In: Hendler SS, ed. PDR for Nutritional Supplements. 2nd ed. Montvale, NJ: Physician’s Desk Reference; 2008:189.
  17. Russell AL, McCarty MF. DL-phenylalanine markedly potentiates opiate analgesia –- and example of nutrient/pharmaceutical up-regulation of the endogenous analgesia system. Med Hypotheses. 2000;55(4):283-8.
  18. Beckmann H, Strauss MA, Ludolph E. DL-phenylalanine in depressed patients: an open study. J Neural Transm. 1977;41(2-3):123-34.
  19. Beckmann H, Athen D, Oltheanu M, et al. DL-phenylalanine versus imipramine: a double-blind controlled study. Arch Psychiatr Nervenkr. 1979;227(1):49-58.
  20. Hsia CH, Shen MC, Lin JS, et al. Nattokinase decreases plasma levels of fibrinogen, factor VII, and factor VIII in human subjects. Nutr Res. 2009;29(3):190-6.
  21. Fujita M, Hong K, Ito Y, Fujii R, Kariya K, Nishimuro S. Thrombolytic effect of nattokinase on a chemically-induced thrombosis model in rat. Biol Pharm Bull. 1995;18(10):1387-91.
  22. Ribeiro J, Almeida-Dias A, Oliveira AR, Mota J, Appell HJ, Duarte JA. Exhaustive exercise with high eccentric components induces prothrombotic and hypofibrinolytic responses in boys. Int J Sports Med. 2007;28(3):193-6.