Tag: Nutrient Supplements

Creatine and Exercise

A Quick Overview of Creatine

Published on by Andrew Marshall1 Comment

Introduction

Creatine is a chemical found naturally in the body, and also in red meat and seafood. It is often used to improve exercise performance and muscle mass.

Creatine and Exercise

Creatine is involved in making energy for muscles, with approximately 95% of it being found in skeletal muscle. The majority of sports supplements in the US contain creatine. Individuals who have lower creatine levels when they start taking creatine seem to get more benefit than individuals who start with higher levels.

People commonly use creatine for improving exercise performance and increasing muscle mass, but it is also used for muscle cramps, fatigue, multiple sclerosis (MS), depression, and many other conditions – although there is no good scientific evidence to support most of these uses.

Creatine use is allowed by the International Olympic Committee (IOC) and the US National Collegiate Athletic Association (NCAA).

What is Creatine?

It is a combination of three different amino acids:

  • Glycine;
  • Arginine; and
  • Methionine.

Creatine is involved in a vast number of processes in the body. For example, it is a fundamental component in how your body creates its primary form of energy in muscle cells, the compound adenosine triphosphate (ATP). When muscles contract explosively, or for brief, intense work lasting no longer than 8-12 seconds, creatine (bonded with phosphoric acid as creatine phosphate) is how the muscle creates the energy necessary to do it.

  • It exists in a steady state with a similar compound named creatinine that can be measured in lab tests as a marker of kidney function.
  • It is passed out of your body in your urine.
  • This means your body must release stored creatine each day to keep normal levels, the amount depending on your muscle mass.
  • Although creatine is created naturally in your body, you must keep up your levels and do so through your daily diet.

What is the Role of Creatine?

  • Creatine is a fuel source.
  • Simply put, creatine helps to maintain a continuous supply of energy to working muscles by keep production up in working muscles.
  • Small amounts are also found in your heart, brain and other tissues.
  • The phosphate-bonded form of creatine is your body’s energy of first choice when performing anaerobic activity, for example lifting weights.
  • When your body is trying to create the compound that powers quick muscle contractions, ATP, it does so by ‘borrowing’ a phosphate molecule from phosphocreatine and combining it with another compound, adenosine diphosphate (ADP).
  • Only after a muscle has largely used up its store of phosphocreatine does it start to produce ATP from other sources, like glucose or fats.
  • A secondary function of creatine is to draw water into muscle cells, making them more hydrated.

What are our Sources of Creatine?

  • Most of the creatine in your body is created in the liver and kidneys, but the majority of it is stored in muscle tissue (approximately 95%).
  • As a healthy human body is capable of creating its own creatine – and it can also be easily obtained through a diet that contains animal products – it is not considered an ‘essential’ nutrient.
  • In a normal omnivorous /carnivorous diet, you consume one to two grams/day of creatine.
  • However, as dietary creatine generally comes from animal products, vegan and vegetarian fitness enthusiasts and professional athletes may not get as much creatine in their diet as those who eat dairy products, eggs, and/or meat.
  • This is one reason why creatine is often recommended as an important supplement for vegans and vegetarians.
Sources of Creatine

What is it Used For?

  • Possibly Effective for:
    • Athletic Performance: Taking creatine by mouth seems to somewhat improve rowing, jumping, and soccer performance. It is not clear if it helps with sprinting, cycling, swimming, or tennis.
    • Disorders of Creatine Metabolism or Transport: Taking creatine by mouth daily can increase creatine levels in the brain in children and young adults with conditions called GAMT deficiency or AGAT deficiency. But taking creatine does not seem to improve brain creatine levels in children who have a disorder in which creatine is not transported properly.
      • Guanidinoacetate Methyltransferase (GMAT) deficiency is an inherited disorder that primarily affects the brain and muscles.
      • Arginine: Glycine Amidinotransferase (AGAT) deficiency is an inherited disorder that primarily affects the brain.
    • Muscle Strength: Taking creatine by mouth seems to somewhat improve muscle strength in both younger and older adults. It is not clear if applying creatine to the skin helps.
    • Sarcopenia (Age-Related Muscle Loss): Taking creatine by mouth for up to 12 weeks seems to improve muscle strength in older adults. It seems to work best when used along with exercise to build muscles.
  • Possibly Ineffective for:
    • Lou Gehrig Disease (Amyotrophic Lateral Sclerosis or ALS): Taking creatine by mouth does not seem to slow disease progression or improve survival in people with ALS.
    • An inherited brain disorder that affects movements, emotions, and thinking (Huntington Disease): Taking creatine by mouth does not improve symptoms in people with Huntington disease.
    • Osteopenia (Low Bone Mass): Taking creatine by mouth does not seem to slow or reduce bone loss in people with osteopenia.

There is interest in using creatine for a number of other purposes, but there is not enough reliable information to say whether it might be helpful.

What are the Side Effects?

  • When taken by mouth:
    • Creatine is likely safe for most people.
    • Doses up to 25 grams daily for up to 14 days have been safely used.
    • Lower doses up to 4-5 grams daily for up to 18 months have also been safely used.
    • Creatine is possibly safe when taken long-term.
    • Doses up to 10 grams daily for up to 5 years have been safely used.
    • Side effects might include dehydration, upset stomach, and muscle cramps.
  • When applied to the skin:
    • There is not enough reliable information to know if creatine is safe.
    • It might cause side effects such as redness and itching.

The majority of reported side effects (mild to moderate) are of weight gain, gastrointestinal distress, altered insulin production, inhibition of endogenous creatine synthesis, renal dysfunction, or dehydration in study participants.

Experts generally agree that there is sufficient evidence to be confident that 5 g/day of creatine is generally harmless to healthy adults, but there is not enough evidence to make an informed recommendation in favour or against doses higher than 5 g/day (Shao et al., 2006).

Are There Any Special Precautions or Warnings to Consider?

  • Pregnancy and breast-feeding:
    • Creatine is used as a dietary supplement to increase muscle mass and improve exercise performance.
    • Creatine is a normal component of human milk, supplying about 9% of the infant’s daily requirements.
    • Milk levels of creatine have not been measured after exogenous administration in humans.
    • Creatine is converted into creatinine in the mother’s and infant’s bodies.
    • It may increase the infant’s serum creatinine, which may alter estimations of the infant’s kidney function.
    • Some authors speculate that creatine supplementation of nursing mothers might help avoid creatine deficiency syndromes, but no studies are available that test this hypothesis.
    • Until more data are available, it is probably best to avoid creatine supplementation unless it is prescribed by a healthcare professional.
  • Children:
    • Creatine is possibly safe when taken by mouth, short-term.
    • Creatine 3-5 grams daily for 2-6 months has been taken safely in children 5-18 years of age.
    • Creatine 2 grams daily for 6 months has been taken safely in children 2-5 years of age.
    • Creatine 0.1-0.4 grams/kg daily for up to 6 months has been taken safely in both infants and children.
  • Bipolar disorder:
  • Kidney disease:
    • Creatine might make kidney disease worse in people who already have kidney disease.
    • If you have kidney disease, speak with a healthcare professional before using creatine.
  • Parkinson disease:
    • Caffeine and creatine taken together may make symptoms of Parkinson disease worse.
    • If you have Parkinson disease and take creatine, use caffeine with caution.

What about Dosage?

  • Creatine is found in foods such as meat and seafood. Creatine is also found in many different types of sports supplements.
  • In supplements (discussed below), creatine has most often been used by adults in a one-time loading dose of up to 20 grams by mouth daily for up to 7 days, followed by a maintenance dose of 2.25-10 grams daily for up to 16 weeks.
  • Speak with a healthcare provider to find out what type of product and dose might be best for a specific condition.

Interactions

A total of five (5) drugs are known to interact with creatine:

  • Minor:
    • Cimetidine.
    • Probenecid.
    • Trimethoprim.
    • These are all known to interfere with the kidney’s secretion of creatinine.
  • Moderate:
    • Entecavir: Using entecavir together with creatine may increase the blood levels of one or both medications.
    • Pemetrexed: Creatine may increase the blood levels of Pemetrexed. You may be more likely to develop serious side effects such as anaemia, bleeding problems, infections, and nerve damage when these medications are used together.

What about Creatine Monohydrate?

  • Creatine monohydrate, the most popular form of creatine supplements, is simply creatine with one molecule of water attached to it – hence the name monohydrate.
  • It is usually around 88-90% creatine by weight.
  • It is not a steroid, it is totally different and works in a different manner.
  • Its not a stimulant, although it is sometimes combined with stimulant ingredients (such as caffeine) in pre-workout formulas.

Supplementation and Fitness

  • More Work:
    • Supplementation with creatine serves to increase creatine stores and phosphocreatine availability in the body, resulting in faster ATP formation.
    • The understanding being that the more phosphocreatine you have, the more work you can accomplish before fatigue sets it.
  • Cell Hydration:
    • A secondary function of creatine is to draw water into muscle cells, making them more hydrated.
    • When muscle cells are hydrated a few things happen, the most notable being an increase in protein synthesis. Muscle protein synthesis (MPS) is the driving force behind adaptive responses to exercise and represents a widely adopted proxy for gauging chronic efficacy of acute interventions (i.e. exercise/nutrition).
    • This action of drawing water into the cell can make muscles look bigger or fuller (think weightlifters/bodybuilders).

Supplementation and Bipolar Disorder

  • Negative changes in mood or anxiety following supplementation with creatine have been documented in two human trials (Roitman et al., 2007; Volek et al., 2000) and one animal experiment (Allen et al., 2010).
  • Specifically, in an open-label clinical trial of creatine, Roitman et al. (2007) reported that two patients diagnosed with bipolar disorder exhibited hypomania or mania following daily supplementation with 3-5 g creatine.
  • In a clinical trial examining the effectiveness of creatine to enhance heavy resistance training, Volek et al. (2000) noted that two subjects reported feeling more aggressive and nervous after 1 week of creatine supplementation (25 g/day).
  • In rodents, Allen et al. (2010) observed increased depression-like behaviour in male rats supplemented with 4% creatine for five weeks, although this effect was not replicated in male rats in a follow-up study (Allen et al., in press).
  • Taken together, there remains the possibility that creatine can increase risk of mania or depression in susceptible individuals.
  • It is also possible that long-term high dosing of creatine alters creatine transporter function or creatine kinase activity in a manner that adversely affects emotional regulation.
  • Further research is required before definitive conclusions are drawn, but caution is warranted in at-risk individuals.

For a good outline of creatine metabolism and psychiatric disorders read Patricia Allen’s article here.

An Overview of Magnesium Stearate

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Introduction

Have you ever wondered what coats your medications and vitamin/dietary/nutritional supplements? Well, it is an additive made from magnesium stearate.

“Magnesium stearate is widely used in the production of dietary supplement and pharmaceutical tablets, capsules and powders as well as many food products, including a variety of confectionery, spices and baking ingredients.” (Hobbs et al., 2017, p.554).

Magnesium stearate is a fine, light white powder that sticks to your skin and is greasy to the touch. It is a simple salt made up of two substances:

  • A saturated fat known stearic acid; and
  • The mineral magnesium.

Stearic acid can also be found in many foods, including:

  • Chicken;
  • Eggs;
  • Cheese;
  • Chocolate;
  • Walnuts;
  • Salmon;
  • Cotton seed oil;
  • Palm oil; and
  • Coconut oil.

Magnesium stearate is commonly added to many foods, pharmaceuticals, and cosmetics. In medications and vitamins, its primary purpose is to act as a lubricant. It may be derived from plants as well as animal sources.

What is it Used For?

  • It has been widely used for many decades in the food industry as an emulsifier, binder and thickener, as well as an anticaking, lubricant, release, and antifoaming agent.
  • It is present in many food supplements, confectionery, chewing gum, herbs and spices, and baking ingredients.
  • It is also commonly used as an inactive ingredient in the production of pharmaceutical tablets, capsules and powders.
  • It is useful because it has lubricating properties, preventing ingredients from sticking to manufacturing equipment during the compression of chemical powders into solid tablets; magnesium stearate is the most commonly used lubricant for tablets.
  • However, it might cause lower wettability and slower disintegration of the tablets and slower and even lower dissolution of the drug.
  • It can also be used efficiently in dry coating processes.
  • In the creation of pressed candies, magnesium stearate acts as a release agent and it is used to bind sugar in hard candies such as mints.
  • It is a common ingredient in baby formulas.

It is possible to create capsules without magnesium stearate, but it is more difficult to guarantee the consistency and quality of those capsules.

Other Names

Mangeniusm stearate has number of other names, approximately 45, including:

  • Magnesium Distearate.
  • Magnesium Octadecanoate.
  • Octadecanoic Acid, Magnesium Salt.
  • Dibasic Magnesium Stearate.
  • Stearic Acid, Magnesium Salt.
  • Magnesium Dioctadecanoate.
  • Synpro 90.
  • Petrac MG 20NF.
  • NS-M (Salt).
  • SM-P.
  • Synpro Magnesium Stearate 90.
  • HSDB 713.
  • Rashayan Magnesium Stearate.

How is it Manufactured/Made?

  • Molecular Formula: C36H70MgO4 or Mg(C18H35O2)2, it exists as a salt containing two stearate anions and a magnesium cation.
    • An anion has more electrons than protons, consequently giving it a net negative charge.
    • A cation has more protons than electrons, consequently giving it a net positive charge.
  • Magnesium stearate is produced by:
    • The reaction of sodium stearate (the sodium salt of stearic acid) with magnesium salts; or
    • Treating magnesium oxide with stearic acid.
  • Some nutritional supplements specify that the sodium stearate used in manufacturing magnesium stearate is produced from vegetable-derived stearic acid.

Magnesium stearate is a major component of bathtub rings. When produced by soap and hard water, magnesium stearate and calcium stearate both form a white solid insoluble in water, and are collectively known as soap scum.

What Does My Body Do With Magnesium?

  • Upon ingestion, magnesium stearate is dissolved into magnesium ion and stearic and palmitic acids.
  • Magnesium is absorbed primarily in the small intestine, and to a lesser extent, in the colon.
  • Magnesium is an essential mineral, serving as a cofactor for hundreds of enzymatic reactions and is essential for the synthesis of carbohydrates, lipids, nucleic acids and proteins, as well as neuromuscular and cardiovascular function.
  • The majority of magnesium content in the body is stored in bone and muscle.
  • A small amount (~1%) is present in serum and interstitial body fluid, mostly existing as a free cation while the remainder is bound to protein or exists as anion complexes.
  • The kidney is largely responsible for magnesium homeostasis and maintenance of serum concentration.
  • Excretion occurs primarily via the urine, but also occurs in sweat and breast milk.
  • Stearic and palmitic acids are products of the metabolism of edible oils and fats for which the metabolic fate has been well established.
  • These fatty acids undergo ß-oxidation to yield 2-carbon units which enter the tricarboxylic acid cycle (aka Krebs cycle and citric acid cycle, the second stage of cellular respiration) and the metabolic products are utilised and excreted.

How Much Can I Consume and What are the Risks?

  • The US Food and Drug Administration (FDA) has approved magnesium stearate for use as an additive in food and supplements, being classified (in the US) as generally recognised as safe (GRAS).
  • In the European Union (EU) and European Free Trade Agreement (EFTA) it is listed as food additive E470b.
  • In 1979, the FDA’s Subcommittee on GRAS Substances (SCOGS) reported, “There is no evidence in the available information on … magnesium stearate … that demonstrates, or suggests reasonable grounds to suspect, a hazard to the public when they are used at levels that are now current and in the manner now practiced, or which might reasonably be expected in the future.”
  • It is generally considered to have a “safe toxicity profile”. (Hobbs et al., 2017, p.554).
  • According to PubChem (a part of the The National Library of Medicine’s National Centre for Biotechnology Information), it is considered safe for consumption at amounts below 2,500 milligrams (mg) per kilogram per day. For a 150-pound (68 kg) adult, that equals 170,000 mg per day.
  • Capsule manufacturers typically use only small amounts of magnesium stearate in their products. When you take their products at the recommended dose, they do not contain enough magnesium stearate to cause negative side effects.

“Stearic acid typically ranges between 0.5-10 percent of the tablet weight while magnesium stearate typically represents 0.25-1.5 percent of the tablet weight. Therefore, in a 500 mg tablet, the amount of stearic acid would probably be about 25 mg, and magnesium stearate about 5 mg.” (Bruno, 2013, p.53).

What are the Health Risks of Magnesium Stearate?

  • Toxicology data from animal studies relevant to evaluation of magnesium stearate are lacking (e.g. doses that will not lead to a dietary imbalance, known composition of material tested, appropriate administration route, etc.).
  • There are also no human data related to magnesium stearate toxicity.
  • It has been noted that infants are particularly sensitive to the sedative effects of magnesium salts and that individuals with chronic renal impairment retained 15-30% of administered magnesium, which may cause toxicity.
  • Moreover, diarrhoea and other gastrointestinal effects have been observed with excessive magnesium intake resulting from use of various magnesium salts for pharmacological/medicinal purposes.
  • Many magnesium-containing food additives have been evaluated individually, but not collectively, for laxative effects.
  • With this in mind, it is important to understand what effect cumulative exposure to magnesium via food additives may have, although studies indicate a lack of genotoxic risk posed specifically by magnesium stearate consumed at current estimated dietary exposures.
  • PubChem also notes that it can be an irritant which may cause skin, eye, and respiratory irritation, as well as potentially causing long lasting harmful effects to aquatic life (although relates to the powder form and not capsule form).
  • Some people report having negative reactions to magnesium stearate and feel much better when they eliminate it. These people might have a sensitivity to it. It is possible to be allergic to magnesium stearate, and it can be difficult to avoid this food additive.

Alleged Health Risks Not Borne Out by the Science

  • Some people (mainly on the internet) claim that magnesium stearate suppresses your immune T-cell function and causes the cell membrane integrity in your helper T cells to collapse.
    • However, there is no scientific evidence to support those claims.
    • Generally, these claims have been made based on a single mouse study that was related to stearic acid, not magnesium stearate (Tebbey & Buttke, 1990).
    • Mice lack an enzyme in their T cells that humans have. This makes stearic acid safe for us to ingest. Human T-cells have the delta-9 desaturase enzyme required to convert stearic acid into oleic acid to avoid a toxic build-up.
    • Another factor to consider is that the study was conducted by bathing the mouse T-cells in stearic acid.
    • It is impossible to consume stearic acid in such humongous amounts through supplements.
  • Some people have also claimed that magnesium stearate might interfere with your body’s ability to absorb the contents of medication capsules.
    • Studies have found that although magnesium stearate may slow down dissolution and absorption in some cases, it does not affect the overall bioavailability of nutrients.
  • Gene Bruno (MS, MHS), writing in Vitamin Retailer in March 2013, gives a good outline on why the above two points are not borne out by the science.
  • Another claim is that magnesium stearate can form a biofilm in the intestines just as soaps containing calcium and magnesium stearates form soap scum in sinks and bathtubs.
    • The Human gut environment is completely different to that of a bathroom.
    • Human intestines have acids and enzymes that do not allow soap scum to accumulate.
    • And, soap scum is nothing like a biofilm – If anything, magnesium stearate can actually prevent the formation of biofilms.

What are the Alternatives to Magnesium Stearate?

Magnesium stearate and stearic acid are the most common lubricants used in pharmaceutical processes. However, there are other lubricants, including fatty acid esters, inorganic materials, and polymers.

  • Metallic Salts of Fatty Acids:
    • They are still the most dominant class of lubricants.
    • Magnesium stearate, calcium stearate, and zinc stearate are the three common metallic salts of fatty acids used.
    • Of these three lubricants, magnesium stearate is one of the most frequently used.
  • Fatty Acids:
    • These are also common lubricants, with stearic acid being the most popular one.
    • Chemically, stearic acid is a straight-chain saturated monobasic acid found in animal fats and in varying degrees in cotton seed, corn, and coco.
    • The commercial material of stearic acid has other minor fatty acid constituents such as myistic acid and palmitic acid.
  • Fatty Acid Esters:
    • Fatty acid esters, including glyceride esters (glyceryl monostearate, glyceryl tribehenate, and glyceryl dibehenate) and sugar esters (sorbitan monostearate and sucrose monopalmitate), are often used as lubricants in the preparation of solid dosage forms.
    • In particular, Compritol® 888 ATO is an effective lubricant to replace magnesium stearate when the latter causes delay of dissolution and other compatibility issues.
  • Inorganic Materials and Polymers:
    • Are used as lubricants when magnesium stearate is not appropriate.
    • In terms of inorganic materials, talc (a hydrated magnesium silicate (Mg3Si4O10(OH)2)), is often used as a lubricant or a glidant in formulations.
    • Similarly, polymers, such as PEG 4000, are occasionally used as lubricants in solid dosage forms when the use of magnesium stearate displays compression and chemical incompatibility issues.

Besides the conventional lubricants, manufacturers are also using natural-based lubricants (such as rice extract) or excipient premixes (such as cellulose/rice extract/oil/wax).

Summary

The benefits of using magnesium stearate in supplements far outweigh the potential risks. And, apart from ensuring a homogenous mixture of active ingredients and accurate, consistent dosage, magnesium stearate has several health benefits of its own. As an essential mineral, magnesium is crucial for more than 300 enzyme reactions occurring in the human body. Stearic acid is known to lower LDL cholesterol and improve heart function.

References and Further Reading

Book: SNAP Matters

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Book Title:

Snap Matters – How Food Stamps Affect Health And Well-Being (Studies in Social Inequality).

Author(s): Judith Bartfield, Craig Gundersen, Timothy Smeeding, and James P. Ziliak (Editors).

Year: 2015.

Edition: First (1st).

Publisher: Stanford University Press.

Type(s): Hardcover, Paperback, and Kindle.

Synopsis:

In 1963, President Kennedy proposed making permanent a small pilot project called the Food Stamp Programme (FSP). By 2013, the programme’s fiftieth year, more than one in seven Americans received benefits at a cost of nearly $80 billion. Renamed the Supplemental Nutrition Assistance Programme (SNAP) in 2008, it currently faces sharp political pressure, but the social science research necessary to guide policy is still nascent.

In SNAP Matters, Judith Bartfeld, Craig Gundersen, Timothy M. Smeeding, and James P. Ziliak bring together top scholars to begin asking and answering the questions that matter. For example, what are the antipoverty effects of SNAP? Does SNAP cause obesity? Or does it improve nutrition and health more broadly? To what extent does SNAP work in tandem with other programmes, such as school breakfast and lunch? Overall, the volume concludes that SNAP is highly responsive to macroeconomic pressures and is one of the most effective antipoverty programmes in the safety net, but the volume also encourages policymakers, students, and researchers to continue examining this major pillar of social assistance in America.

Book: How to Use Herbs, Nutrients, and Yoga in Mental Health Care

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Book Title:

How to Use Herbs, Nutrients, and Yoga in Mental Health Care.

Author(s): Richard P. Brown, Patricia L. Gerberg, and Phillip R. Muskin.

Year: 2012.

Edition: Reprint Edition.

Publisher: W.W. Norton & Co.

Type(s): Hardcover, Paperback and Kindle.

Synopsis:

Many physicians and therapists agree that herbs and mind-body practices enhance health, but many more are reluctant to integrate them into their clinical work because of a lack of training or, given how long it takes to master the use of hundreds of different herbs, a lack of time.

But the trend is clear: clients and consumers alike want control over their health care choices, making the time ripe for a practical resource that guides both the clinician and the consumer on complementary and alternative medicine (CAM). This book answers that call.

Three noted experts in integrative medicine, Drs. Brown, Gerbarg, and Muskin, demystify the complexities of alternative mental health care, giving readers a comprehensive yet accessible guidebook to the best treatment options out there.

From mood, memory, and anxiety disorders to ADD, sexual enhancement issues, psychotic disorders, and substance abuse, every chapter covers a major diagnostic category.

The authors then present a range of complementary and alternative treatments-including the use of herbs, nutrients, vitamins, nootropics, hormones, and mind-body practices that they have found to be beneficial for various conditions within each category.

For example, B complex vitamins and folate have been shown to help with depression; omega-3 fatty acids can offer relief for bipolar sufferers; coherent and resonant breathing techniques-used by Buddhist monks-induce healthy alpha rhythms in the brain to relieve anxiety; the elderly can boost their memory by taking the ancient medicinal herb Rhodiola rosea; and those with chronic fatigue syndrome can find comfort in acupuncture and yoga.

Focusing on evidence-based approaches, the research, the authors’ clinical experience, and the potential risks and benefits of each treatment are carefully examined.

Brown, Gerbarg, and Muskin have distilled an otherwise daunting field of treatment down to its basics: their overriding approach is to present the CAM methods that are most practical in a clinical setting, easy to administer, and low in side effects.

With helpful summary tables at the end of each chapter, clinical pearls, and case vignettes interspersed throughout, this is a must-have resource for all clinicians and consumers who want the best that alternative medicine has to offer.