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The latest in stimulants, joint pain (including CBD) and strength

The never ending search to replace DMAA, CBD and the latest ingredients for joint pain. Plus: can anything replace creatine for strength?

For weightlifters, the search for the next great stimulant, the next big strength booster or the best pain reliever is never ending. But with industry regulations on OTC (over the counter) ingredients becoming tighter it may prove to be more difficult for future generations of supplements to replace some of the ingredients we will discuss in this article. So this information will be key to ensuring you are using the best ingredients available to maximize your training/performance. We will discuss more innovations for similar categories: stimulants (cognitive function), joints (inflammation) and strength (sort of).

Stimulants:

Out- banned synthetic stimulants

In- Alpha GPC, CDP Choline

Just a few years ago, use of the synthetic stimulant 1,3 DMAA (1,3-dimethylamylamine, chemically similar to ephedrine) was a popular synthetic stimulant used in many pre-workout and energy products. Its safety had been called into question by the FDA and it was subsequently banned by many sports organizations. It rose in popularity due to amphetamine like effects that boosted energy, focus and fat metabolism. Due to the upcoming guidance for new raw materials under the FDA’s NDI (New Dietary Ingredients notification process) which we mentioned in part one, this synthetic ingredient which did not exist as a dietary supplement before 1996 (it was a drug for nasal decongestion in the 1940’s(1)). Similar synthetic stimulants which are also banned have appeared on the market since then (ex: DMHA, 2-Aminoisoheptane). Due to the lack of long term safety data (it has been named in multiple cases of adverse events and even death (2)), effects on athletes (does the stimulation of the central nervous system reduce CNS performance over time?) and most importantly its legality in sport. This popular stimulant must have a replacement in the market for athletes who are looking to get the most out of their nervous system while training/competing.

So far, the underground sports nutrition market has brought the extracts juglans-regia-extract aka 2-amino-5-methylheptane or Octodrine (supposed to be a natural source of DMHA) and Eria Jarensis Extract aka n-phenethyl dimethylamine citrate (supposedly a natural source phenylethylamine) to the forefront. However, as extracts that aren’t standardized, well researched, or well regulated, it’s impossible to tell how much of the target compound an extract will yield per serving. Most extracts that aren’t standardized yield miniscule amounts of key compounds which leads companies to adulteration tactics to make the ingredients effective.

This occurred shortly after DMAA was banned and an ingredient called Dendrobium said to yield phenylthylamines strong enough to pickup where DMAA left off. What ended up occurring was reliable sources of Dendrobium did nothing and products like Craze that featured Dendrobium ended up being spiked with amphetamines. Take into consideration that an effective dose of phenylthylamines can be anywhere between 500mg and 1,000mg and their effect is prolonged by a monoamine oxidase inhibitor like hordenince Hcl at a few hundred mg. Those amounts alone should tell you that there’s something fishy about an herbal extract of just a few hundred milligrams having substantial effects if the pure amine’s themselves have higher dosages.

Fortunately, the mass market has already begun to respond to the need for improved cognitive function in athletes safely and effectively. Many pre-workouts and focus promoting products have responded by turning to cholinergic compounds like Alpha GPC or CDP Choline that are better absorbed than regular choline and have been on the market for decades. Choline is the precursor to the neurotransmitter acetylcholine which plays a major role in memory and brain function. Cholinergic compounds work by increasing acetylcholine levels in the brain.

Alpha GPC (L-Alpha glycerylphosphorylcholine) is a natural choline compound that has been shown to improve power output in men with at least two years of resistance training experience (3) and even reduce cognitive decline in the elderly (4). Its chief competitor as a nootropic (supplement to enhance memory or cognitive function) is CDP Choline which has been shown to improve attention (5) and memory in older subjects (6). These compounds when combined with caffeine can provide athletes with the cognitive and energy boost necessary to support improvements in performance while meeting the regulatory standards of all sports and FDA regulations.

Joints pain and inflammation:

Out-Omega 3

In- Curcumin, EPA, Endocannabinoid system (including CBD)

When many athletes begin to feel the joint pain that comes with inflammation, we’re tempted to reach for our NSAIDS (over the counter Non Steroidal Anti-Inflammatory Drugs ) from one of a few major brands. However, research has shown that this can inhibit the muscle recovery and growth process (7). Adequate post-exercise protein or protein supplementation and use of BCAAs before or during exercise can help reduce delayed onset muscle soreness in untrained lifters (those who may suffer the most from delayed onset muscle soreness)(8). Which means this method should be adequate for recovery for trained athletes who typically don’t experience DOMS as often. However, when it comes to inflammation and pain in your joints, protein and BCAA’s won’t quite cut it.

This is where Omega 3 supplementation for athletes came in. While supplements like Glucosamine and Chondroitin or UC-II (covered in part 1) improve joint comfort with consistent long term use, supplements like Omega 3’s were supported by evidence for reducing acute joint pain. More specifically they are reported to and have evidence showing that they may reduce arthritic pain in joints similar to NSAIDs (9). Omega 3’s are primarily composed of two long-chain fatty acids: EPA and DHA. While DHA is important in the growth and development of children, EPA becomes more important for cognitive function and inflammation control later in life (10).

As a result, the future of Omega 3 supplementation in athletes will revolve around high end Omega 3 supplements (+80% Omega 3 content within fish oil) that are processed to focus on EPA content (5:1 ratio of EPA to DHA or higher). And there are many on the market already as these products have positioned themselves as being superior to standard Omega 3’s. The controversy in the industry however was that up until 2016, no one had really compared EPA directly to DHA for markers of inflammation in a study without using a mixture of some kind. So researchers conducted a study published in the American Society for Nutrition doing just that and low and behold, EPA actually lost to DHA…confused? Don’t be, one thing the researchers left out was the fact that EPA converts to DHA easily in adults and an adults demand for EPA supplementation increases after childhood. So if you use an Omega 3 supplement with greater EPA, not only is the mechanism of action for EPA proven to reduce inflammation (EPA is an inhibitor of the enzyme delta-5-desaturase (D5D) that produces arachidonic acid a pro inflammatory Omega 6), but it can also convert to DHA in the adult body when necessary.

The next great supplement for joint pain is the multifunctional and increasingly popular Turmeric/Curcumin. While this supplement has a host of health and wellness benefits, Turmeric has been found through research to alleviate symptoms of joint arthritis (11). But just like with Omega 3’s, there is a specific constituent of Turmeric that is responsible for its anti-inflammatory properties. That constituent is Curcumin. Now not all Curcumin’s are created equal, bioavailability is a limiting factor with Curcumin supplementation and notable companies have combined Curcumin with soy lecithin in a specific ratio, high concentration curcuminoid complex with turmeric essential ois (BCM-95 brand), curcumin with a phospholipid complex (Meriva brand) or multiple curcuminoids with a black pepper extract for better absorption. The research for bioavailable curcumins like these has been astounding with studies showing they may be as efficacious as prescribed methods for controlling arthritis (12).

The dark horse in this category is of course any ingredient that acts upon the endocannabinoid system for pain and inflammation relief. The most notable ingredient in this category is of course CBD, which is NOT banned by WADA (World Anti-Doping Association) and has tons of anecdotal feedback supporting its effectiveness for pain relief. The risk is that the market for this ingredient is expanding so quickly that ingredient regulation is sub optimal and the risk of using a supplement with THC levels that exceed the allowable 0.03% is possible. The alternative is an ingredient that has been on the market for a long time but has only recently received GRAS (and FDA designation for ‘Generally recognized as safe’) status so it is now readily available for supplement use. It is called palmitoylethanolamide (PEA) and it also acts on the endocannabinoid system to support pain and inflammation control but without the THC. This could prove to be a safer alternative for athletes in sports (13).

Strength:

Out- Creatine Monohydrate

In- Who are you kidding? Creatine Monohydrate is king

Despite the new technologies for creatine hitting the market, creatine monohydrate is still the pound for pound king when it comes to creatine supplementation. The most effective new technologies for creatine technology however do improve upon its water solubility at a higher price. But an increase in water solubility is not supported by any human research to be an increase in effectiveness. So taking a smaller dose of a more water soluble creatine (which the marketing for these types of creatines will promote) is not likely to provide you with the benefits of a full serving of regular monohydrate.

Forms of creatine that are touted to be superior in solubility (the real advantage is that it will mix better in water) would be creatine-di-malate or creatine HCl which is reported to reduce the bloating and cramping which can result from creatine monohydrate use. However it is also not supported by independent research to be any more effective than monohydrate. My concern with alternate forms of creatine is also the reduction in creatine per serving that they are recommending. There are also forms of creatine that have been bonded with minerals like magnesium (magnesium creatine chelate) that claim greater abosrption, but they still show similar effects to regular monohydrate (14).

There have even been buffered forms of creatine that have been promoted to be better protected against stomach acid than creatine monohydrate. Not only have buffered creatines fallen short in terms of efficacy and providing superior safety (15) but other novel forms of creatine on the market (like the debunked creatine ethyl ester) have shown to be inferior to monohydrate in terms of stability (16).

  1. Col John Lammie et al. Report of the Department Of Defense: 1,3 Dimethylamylamine (Dmaa) Safety Review Panel. June 3, 2013

  2. Singer, Natasha, et al. F.D.A. Issues Warning on Workout Supplement. New York Times. Retrieved April 16, 2013.

  3. Tim Ziegenfuss, et al. Acute supplementation with alpha-glycerylphosphorylcholine augments growth hormone response to and peak force production during, resistance exercise. JISSN (Suppl 1):P15DOI: 10.1186/1550-2783-5-S1-P15

  4. De Jesus Moreno, et al. Cognitive improvement in mild to moderate Alzheimer's dementia after treatment with the acetylcholine precursor choline alfoscerate: a multicenter, double-blind, randomized, placebo-controlled trial. Clin Ther. 2003 Jan;25(1):178-93

  5. McGlade E,Agoston, et al. Cognizin® Citicoline Increases Motor Speed and Attention in Healthy Adolescent Males. Journal of Attention Disorders. 15 July 2015, 1557-1246.

  6. Alvarez XA, et al. Citicoline Improves Memory Performance in Elderly Subjects. Methods & Findings in Experimental & Clinical Pharmacology. 19(3):201-10,1997 Apr.

  7. Q.A. Soltow, et al. Ibuprofen inhibits skeletal muscle hypertrophy in rats. Medicine and Science in Sports & Exercise, 38(5): 840-46, 2006.

  8. Song-Gyu Ra, et al. Combined effect of branched-chain amino acids and taurine supplementation on delayed onset muscle soreness and muscle damage in high-intensity eccentric exercise. Journal of the International Society of Sports Nutrition2013

  9. Maroon JC, et al. Omega-3 fatty acids (fish oil) as an anti-inflammatory: an alternative to nonsteroidal anti-inflammatory drugs for discogenic pain. Surg Neurol. 2006 Apr;65(4):326-31

  10. Kiecolt-Glaser JK, et al. Omega-3 supplementation lowers inflammation in healthy middle-aged and older adults: a randomized controlled trial. Brain Behav Immun. 2012 Aug;26(6):988-95. doi: 10.1016/j.bbi.2012.05.011. Epub 2012 May 26

  11. James W. Daily, et al. Efficacy of Turmeric Extracts and Curcumin for Alleviating the Symptoms of Joint Arthritis: A Systematic Review and Meta-Analysis of Randomized Clinical Trials. J Med Food. 2016 Aug 1; 19(8): 717–729. Published online 2016 Aug 1. doi: 10.1089/jmf.2016.3705

  12. Binu Chandran, et al. A Randomized, Pilot Study to Assess the Efficacy and Safety of Curcumin in Patients with Active Rheumatoid Arthritis. Phytotherapy research. Published March 8, 2012. Doi: 10.1002/ptr.4639

  13. Linda G, et al. Palmitoylethanolamide for the treatment of pain: pharmacokinetics, safety and efficacy. Br J Clin Pharmacol. 2016 Oct; 82(4): 932–942.

  14. Selsby JT, et al. Mg2+-creatine chelate and a low-dose creatine supplementation regimen improve exercise performance. J Strength Cond Res. 2004 May;18(2):311-5..

  15. Andrew R Jagim, et al. A buffered form of creatine does not promote greater changes in muscle creatine content, body composition, or training adaptations than creatine monohydrate. J Int Soc Sports Nutr. 2012; 9: 43. Published online 2012 Sep 13. doi: 10.1186/1550-2783-9-43

  16. Ralf Jäger, et al. Analysis of the efficacy, safety, and regulatory status of novel forms of creatine. Amino Acids. 2011 May; 40(5): 1369–1383. Published online 2011 Mar 22. doi: 10.1007/s00726-011-0874-6

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