Wednesday, November 28, 2007

Blackwater Mercenaries Accused of Steroid Abuse

A civil lawsuit filed on behalf of the families of the individuals killed in the shooting incident on Sept. 16 in Nusoor Square, Baghdad, alleges that Blackwater guards were abusing steroids. The lawsuit, “Estate of Himoud Saed Atban, et al. v. Blackwater USA, et al.” (C.A. No. 07-1831), which was filed on October 11th in Washington DC by four families of persons killed in the shooting incident. However, the suit was amended on Monday Nov. 26th that included the allegations of steroid usage and "other judgment-altering substances". Page 8, Section 35 of the complaint states:

Blackwater routinely sends heavily-armed "shooters" into the streets of Baghdad with the knowledge that some of those "shooters" are chemically influenced by steroids and other judgment-altering substances. Reasonable discovery will establish that Blackwater knew that 25 percent or more of its "shooters" were ingesting steroids or other judgment-altering substances, yet failed to take effective steps to stop the drug use. Reasonable discovery will establish that Blackwater did not conduct any drug-testing of its "shooters" before sending them equipped with heavy weapons into the streets of Baghdad.
Blackwater spokesperson, Anne Tyrell told CNN that "All Blackwater personnel are drug tested during the screening process, before ever working for the company, and are subject to random testing, which is performed quarterly." She continued "Steroids and performance enhancing drugs (both illegal and prescribed) are absolutely in violation of our policy." Ms. Tyrell refused to comment on the lawsuit further. However, this comment could be true in both respects, yet still fails to address the question of whether Blackwater security personnel are tested directly for steroids. The most commonly used drug test used by most any group who performs them, is known as the NIDA-5, which only tests for marijuana, cocaine, amphetamines, opiates, PCP and some of their analogues and metabolites, but not any type of steroids. Normally, a test for steroids must be specifically ordered and is much more expensive than a typical test for commonly abused psychoactive drugs. Steroid tests are normally administered to athletes and in places where steroid abuse may be common, but is almost never used in a common workplace screening. Unfortunately, neither the document of the lawsuit nor Blackwater themselves identify publicly how and what type of drug tests they use. It appears that Blackwater's employee screening process is quite rigorous, at least currently. On Blackwater USA's corporate web site, there are job listing for "Contract Opportunities", one of which is listed as "Personal Security Specialist(PSS)". Requirements are listed as:

# Must be willing and able to deploy for 6 months.
# Must have solid experience in the US Military or Sworn Law Enforcement
# Must be a U.S. Citizen, proof of citizenship is required.
# Weight must be proportionate to height.
# Must maintain a neat and clean appearance.
# Must be in good health and pass a physical test.
# Most positions require ability to obtain/maintain a secret or higher clearance.
# No history of major illness or mental disorder.
# Must have an Honorable Discharge and DD-214.
# No felony, violent crimes, spouse or child abuse convictions(NO WAIVERS)
# No personal bankruptcy or significant credit problems with past seven (7) years.

Susan Burke, of Burke O’Neil LLC, one of the lawyers for the defendants, stated to CNN:

"The reality is that Blackwater has indeed fired people for steroid use, so they're on clear notice that there's steroid use," Burke said. She said Blackwater has marketed the idea "that their people are kind of tougher and bigger than anybody else," and has turned a blind eye toward "serious, repeated situations of excessive use of force."
However, as most familiar with steroid usage know, and as previously discussed on Pogue's Blog, the link between steroids and violence is more of an urban legend than reality, and studies have shown that there is little to no causative link between the use of testosterone and aggression in mentally stable males. But, there are several other interesting allegations made in the lawsuit that security personnel of Blackwater may not only be predisposed to violence, but chosen and trained for it. Page 10 and 11 of the amended lawsuit claim that Blackwater hired individuals who were previously associated with the Chilean military, presumably those who served under former dictator, Augusto Pinochet, as well as other third world countries run by dictators or military juntas. The lawsuit also mentions other previous incidents were Blackwater personnel were involved with acts of violence and killing in Iraq that went unpunished.

Blackwater itself has been under much scrutiny almost from the start of the war in Iraq. On March 31, 2004, four Blackwater American security contractors were killed in Fallujah, their bodies burned and then hung from a bridge, in what became a very well known international incident that some viewed as resulting in negligence on the part of Blackwater. Families of the contractors have also sued Blackwater, in the case Helvenston et al. v. Blackwater Security. This incident, as well as the use of military contractors in Iraq was profiled in the documentary by Brave New Films titled Iraq for Sale: The War Profiteers. The film alleges that after the incident in Fallujah, Blackwater went on to profit $221.4 million in US contracts in 2004 alone. The current lawsuit filed against Blackwater for the Nusoor Square incident alleges that they have made more than one billion dollars for their contracts with the United States. It's a very interesting film, and it is available to watch in it's entirety on Google Video through the link above.

What else, if any, "judgment-altering substances" that Blackwater employees may have been using has yet to come to light. The American public can only hope that this case, however long it may take, will go all the way through a court process to determine what mistakes and possible cover-ups Blackwater and their associates may have been involved with. But, unfortunately, as with most cases, it is likely to be settled out of court with no resolution or closure being reached for anyone except for the lawyers.

Saturday, November 03, 2007

How to Syndicate my blog or Subscribe for Updates

This article describes several simple methods of how to syndicate the content of my blog to your website, including specific categories of posts. I also discuss how you can subscribe to my content yourself so you can be notified if I post a new article.

Syndicating my RSS Feed

I provide RSS feed of my sites post through Feedburner. The URL of my feed is http://feeds.feedburner.com/pogue972 By clicking on that URL (depending on your browser settings) you will be taken to my feed page where you can subscribe to my feed in your default RSS reader. If you are using Firefox 2 or IE7, it should give you the option of adding my feed to your internal browser feed reader through the bookmarks function. Otherwise, you can add the feed however you choose.

If you wish to publish my feed on your website, you are welcome to do so, as I provide this function to anyone who wants to under a Creative Commons license to use it freely, even in commercial projects, although it is still copywritten and you may not copy and paste my entire articles for usage. No modification or sale of my material is allowed either.

Depending on what type of web site you have, you may be able to do this through an internal RSS feed syndicater that is provided with the software, such as most content management systems (CMS) provide. Alternately, you can try and find an addon for your system or install a reader such as Magpie RSS through your web site's control panel (contact your hosting service for more information on this if you aren't familiar or don't know how). If you are unable to do this, the simplest way to to syndicate an RSS feed is by using Feed2JS, or Feed to JavaScript, which you can install as a PHP script, or use one of their many free mirror servers to do this. Using this method is the quickest and the easiest for anyone. Here quick overview of how to do it.

On the mirrors page, pick a mirror closest to your web servers location or just use the default one. One there, click the "Build" link at the top of the page. The first field is "URL Enter the web address of the RSS Feed" which is where you will enter my Feedburner URL. The next option is "Show channel?". If you choose yes or title, it will cause "Pogue's Blog" to show up as the first link if you choose title. If you choose no, it will only show the articles. The third option is "Number of items to display". This lets you choose how many of the articles you want to display from my blog. If you leave it at 0, it will display the 7 most recent articles, which is what I currently have as my limit. I keep mine at only three (see the news section on the side of my blog) so I can publish more than one feed without taking up too much space.

Next is "Show/Hide item descriptions?". Choosing 0 will just show the article's title, and 1 will show the first 500 characters of the article. You can also tweak this if you wish to show less than 500 characters. "Use HTML in item display?" depends on how you have your site setup and how you want the output to be. Try no and then hit the preview button to see how it looks, if you don't like it or it doesn't work on your site, try yes. After that is the option to "Show posting date" and then choose the time zone. If you choose yes, it will show the time and date the post was published, and then using the time zone option you can leave it as "feed" for my time zone or -6, for example, would be Central Standard Time. "Target links in the new window?" simply causes each article link to use the target="_blank" to open the link in a new window (or tab) if you want visitors to stay on your page and visit the article in a new window. "UTF-8 Character Encoding" allows the feed output in Unicode, which is the character set I use, so it's a good idea to enable this. "Podcast enclosures" should be no, and "Custom CSS" is optional for your site. After this, hit preview and a popup window will open with what the feed will look like in the settings you've chosen, if you don't like it, change one or more of the options and click Generate JavaScript and just copy and paste the code into your page where ever you would like it to go.

Feedburner also provides some very nice animated GIFs which display my Headlines. Here is the code for an image in 468x60 with the default color set. If you would like any other sizes or colors, please let me know and I will be happy to provide them for you.

Syndicating Categories

I use del.icio.us to tag all my posts for categories. The link to my categories on my blog is http://del.icio.us/pogue24 If you wanted to use delicious to syndicate my feed, just look for the orange RSS button at the bottom of the page which will link you to the feed output for that specific tag or category. So, for example, if you just wanted to syndicate all my articles for supplements you would go to http://del.icio.us/rss/pogue24/supplements
Each time I publish a new article on supplements, I tag it with the supplements tag and it will show up on delicious and on any RSS feed that is reading it.

Subscribe by Email

For email subscriptions, I use FeedBlitz which is owned and operated by Feedburner. Every time I publish a new article, you will receive an email. The emails are only sent once per day, so if I published five articles in one day (I wish) you would still only receive one email. No spam is sent and neither I nor FeedBlitz share, sell or rent your email address for any other purpose than to be automatically notified when a new post is made to my blog. To subscribe, there is a link on the right side where you can fill in your email address, and there is a link at the bottom of all my posts where you can also click to make a comment. You can also click here and subscribe and get updates to your email, Skype, AOL or Twitter.

If you have any questions or need some help syndicating my feed, feel free to leave a comment or contact me (see the link on the right just above the recommended services box).

Monday, October 22, 2007

Archive: Information on Lithium Orotate

This article was originally written and posted on a now defunct website which discussed topics involving incentive sites. Many incentive sites at the time had a trial offer for a product called Feel Serenity, which was a dietary supplement that contained lithium orotate. In order to receive a credit on these incentive sites to earn your prize, the member had to complete one of the trial offers, and there were a limited number to choose from. So, in order to reach your goal of getting the prize you had selected, a member had to complete an offer and then refer a certain number of people to also complete an offer under them. Since there were a limited number of offers, people would eventually have to pick some that they might not be interested in or understand. At the time, Feel Serenity allowed a person to pay around $5.00 to receive a 30 day trial of the product (I'm not sure if this is still indeed how the terms work) and then needed to contact the company to cancel the subscription, otherwise the person would be billed in monthly installments of $40/month and automatically be shipped it each month. So, because many people at the time were receiving a sample of the lithium product, I felt that people should understand what it was and how it worked, since lithium is sold in other forms as a powerful anti-depressant drug. Also, please note that I advise against purchasing the product from Feel Serenity and it's parent company, Urban Nutrition, as they have an extremely bad track record of continuing to bill people even after they have canceled. More information can be seen on the BBB and RoR.

Much of the information below is disorganized and may be hard to follow. However, I have attempted to recreate the forum thread as it was originally posted. Only the first portion of the article is mine, and parts of it have been updated for various reasons (broken links, new information, etc). Please also note that this article is incomplete and not a full description of the overview of lithium and lithium orotate. The facts and opinions of the information that was reposted by other individuals on the original thread, as reproduced here, are not entirely mine and have not been completely checked for facts. If you find a mistake anywhere here, please feel free to leave a comment or contact me regarding it. Always consult with a doctor before taking any dietary supplement, especially if you are on any prescription drugs and in particular if you are using any compounds for mood alteration as lithium orotate, along with it's usage and dosage would be best discussed with a medical doctor.

Information on Lithium Orotate

Many have you have probably seen, or even done the offer for "Feel Serenity" on some of these incentive sites. I wanted to go over briefly what the ingredients of this dietary supplement is, and how it works.

Feel Serenity is lithium orotate, or lithium bound to orotic acid; a salt of lithium. Lithium is an element, number 3 on the periodic table and labeled as Li. Lithium is a natural element, which can be found in our daily diets, and is also used to power certain types of batteries, amongst other things.

As a medication, lithium carbonate and lithium citrate is used to treat manic and bipolar depression. Lithium appears to be used in the brain to manufacture a number of neurotransmitters, including seretonin, dopamine and norephinepherine. Although scientists still are not completely sure how lithium treats depression, it is still the gold standard used to treat certain severe cases of bipolar disorder, and manic depression, in lieu of newer anti-psychotic drugs.
Lithium orotate is similar to lithium carbonate, except that there is more lithium mg to mg when compared to carbonate. It can be sold over the counter as a dietary supplement, because it is found in nature and is not regulated by the FDA as a drug, although it's technical legal status is not clearly defined. It is also not patented by anyone for use as a treatment for depression. Only the lithium carbonate & citrate versions are available by prescription. The other difference is that there are fewer studies supporting lithium orotate as treatment for depression, as well as it's safety (more on this below, than lithium carbonate, although one would expect them to be similar.
If you decide to try the sample of Feel Serenity, it would be a good idea to start off with one tablet daily. The typical dosage of lithium orotate is a dosage of 200mg per day. If you are taking any other types of medication, especially medication for depression, it would be wise to speak with a physician before using this supplement. Some of the most common side effects of lithium use can be headaches, and other odd physical sensations. Some individuals can already have sufficient lithium in their blood from dietary sources, and increasing consumption of lithium can have adverse effects on their health. However, lithium in small doses, for most people will have little effects, and may improve mood and outlook, and can normally be used without problems. Unfortunately, lithium itself can be toxic in large doses. The clinical dose of lithium in the form of carbonate and citrate is close to the toxic dosage. There have only been a few studies on the safety of lithium orotate itself, and two studies show contradicting evidence regarding it's safety as being harmful to the kidneys (please see the link at the bottom of the page to the Lithium Orotate Project for more information on this topic).

Over the counter lithium can be purchased by many manufacturers. GRL Lithium Orotate contains 64mg per serving and Nutrient Carriers contains 120mg. Solaray sells Lithium Aspartate, which is lithium bound to aspartic acid (a common amino acid) in a 5mg dosage. Since each of these forms of lithium is bound to another compound for whatever reason (such as increased stability, better bioavailbility, etc.) it will cause the total amount of lithium that is actually absorbed by the body less than what is on the label. Unique Nutrition sells lithium orotate bulk powder with one serving size being 100mg (I presume it comes with a scoop), and Beyond a Century sells it in power form as well.

Articles

Books

Note: Consuming lithium may deplete your bodies stores of inositol, a B vitamin. You may want to consider supplementing with extra amounts of inositol if you plan to, or already use lithium.

Supplement Minimizes Common Lithium Side Effect

By Alan R. Gaby, MD

Healthnotes Newswire (February 3, 2005)—Supplementing with inositol can reduce the severity of psoriasis, a common side effect in people taking lithium medication, reports a study in the British Journal of Dermatology (2004;150:966–9). Psoriasis affects the skin, appearing as red patches covered by a silvery, flaky surface. Fingers and toenails may also be affected, with the lesions appearing as white-colored pits, ridges down the nail, yellowish spots, or thickness at the cut end.

Lithium carbonate is widely used to stabilize mood in people suffering from bipolar disorder (manic depression). It has also been used with some success to treat cluster headaches (a condition related to migraine), alcoholism, and selected cases of asthma. Although lithium is probably the most effective treatment available for bipolar disorder, it can cause a number of side effects, including tremor, kidney problems, visual impairment, and psoriasis. In most cases, these side effects can be prevented or minimized by carefully monitoring the dosage. Nevertheless, many people develop psoriasis or experience a worsening of pre-existing psoriasis when they take lithium.

Inositol is a member of the B-complex group of vitamins. Previous studies have shown that supplementing with inositol can reduce some of the negative side effects of lithium (such as excessive urination), without reducing its beneficial effects. Researchers therefore investigated whether taking inositol might also have a positive effect on lithium-induced psoriasis.

Fifteen people with psoriasis who were taking lithium participated in the new study. They were randomly assigned to receive 6 grams of inositol per day or a placebo for ten weeks. After a four-week "washout period" in which no treatment was given, the treatments were reversed, so that those initially taking inositol were given the placebo, and vice versa. The severity of psoriasis decreased by approximately 35% during inositol treatment, whereas the psoriasis worsened by about 60% during the placebo period. Thirteen of 15 people improved while taking inositol, but only 7 of 15 improved while taking placebo. In a separate group of people with psoriasis who were not taking lithium, inositol was found to be of no benefit; in fact, people fared somewhat worse with inositol than with placebo, although the difference was not statistically significant.

Inositol has also been shown to be an effective treatment for obsessive-compulsive disorder, panic attacks, and some cases of depression. According to one study, however, inositol supplementation appeared to cause abnormal elevations of mood (mania) in some people. To be on the safe side, people with mental disorders and those taking prescription medications should seek medical advice before taking inositol.

Alan R. Gaby, MD, an expert in nutritional therapies, testified to the White House Commission on CAM upon request in December 2001. Dr. Gaby served as a member of the Ad-Hoc Advisory Panel of the National Institutes of Health Office of Alternative Medicine. He is the author of Preventing and Reversing Osteoporosis (Prima, 1994), and co-author of The Natural Pharmacy, 2nd Edition (Healthnotes, Three Rivers Press, 1999), the A–Z Guide to Drug-Herb-Vitamin Interactions (Healthnotes, Three Rivers Press, 1999), Clinical Essentials Volume 1 and 2 (Healthnotes, 2000), and The Patient’s Book of Natural Healing (Prima, 1999). A former professor at Bastyr University of Natural Health Sciences, in Kenmore, WA, where he served as the Endowed Professor of Nutrition, Dr. Gaby is the Chief Medical Editor for Healthnotes, Inc.

Copyright © 2005 Healthnotes, Inc. All rights reserved.


Other supplements to look into to help with depression include:





Lithium Orotate Studies:

Human

Alcohol. 1986 Mar-Apr;3(2):97-100.

Lithium orotate in the treatment of alcoholism and related conditions.

Sartori HE.

The subjects were 42 alcoholic patients (33 males and 9 females) who were treated with lithium orotate during an alcohol rehabilitation program in a private clinical setting for at least six months. They derive from a total number of 105 patients who received this treatment initially, while the remainder discontinued the treatment within six months. The data were collected from a private practice record and the follow-up varied between six months and 10 years. The 42 patients studied displayed a multitude of complaints in addition to chronic alcoholism. These included liver dysfunction, seizure disorders, headaches, hyperthyroidism, affective disorders. Meniere's syndrome, liver and lung cancers. Thirty-six of the 42 patients studied had been hospitalized at least once for the management of their alcoholism. Lithium orotate was given, 150 mg daily, with a diet low in simple carbohydrates and containing moderate amounts of protein and fat. In addition, calcium orotate (for hepatic involvement), magnesium orotate, bromelaine, and essential phospholipids (for cardiac problems), and supportive measures were instituted, if required. Lithium orotate proved useful as the main pharmacologic agent for the treatment of alcoholism. Ten of the patients had no relapse for over three and up to 10 years, 13 patients remained without relapse for 1 to 3 years, and the remaining 12 had relapses between 6 to 12 months. Lithium orotate therapy was safe and the adverse side effects noted were minor, i.e., eight patients developed muscle weakness, loss of appetite or mild apathy. For these patients, the symptoms subsided when the daily dose was given 4 to 5 times weekly.

Animal

J Pharm Pharmacol. 1979 Mar;31(3):161-3.

Kidney function and lithium concentrations of rats given an injection of lithium orotate or lithium carbonate.


Smith DF, Schou M.

A recent study by Kling et al (1978) noted the finding of higher lithium concentrations in serum and brain of rats after an intraperitoneal injection (2 mmol lithium kg-1) of lithium orotate as a slurry than of lithium carbonate in solution. The authors suggested that lithium orotate might offer advantages in the treatment of patients. We repeated the experiments of Kling et al but in addition examined the kidney function of the rats. Glomerular filtration rate and urine flow were markedly lower in rats given lithium orotate than in rats given lithium carbonate, sodium chloride or a sham injection. The renal lithium clearance was significantly lower, the kidney weight and the lithium concentrations in serum, kidney and heart significantly higher after injection of lithium orotate than after injection of lithium carbonate. The higher lithium concentrations could be accounted for by the lower kidney function. It seems inadvisable to use lithium orotate for the treatment of patients.

J Pharm Pharmacol. 1978 Jun;30(6):368-70.

Rat brain and serum lithium concentrations after acute injections of lithium carbonate and orotate.

Kling MA, Manowitz P, Pollack IW.

Eight hours after intraperitoneal injections of 1.0, 2.0, and 4.0m equiv Li kg-1, the serum and brain lithium concentrations of rats were significantly greater after lithium orotate than after lithium carbonate. While little serum lithium remained at 24 h after injection of 2.0 m equiv kg-1 lithium carbonate, two-thirds of the 2 h serum lithium concentration was present 24h after lithium orotate. Furthermore, the 24 h brain concentration of lithium after lithium orotate was approximately three times greater than that after lithium carbonate. These data suggest the possibility that lower doses of lithium orotate than lithium carbonate may achieve therapeutic brain lithium concentrations and relatively stable serum concentrations.


The article below was posted in the original thread where this information appeared. It was posted by a user whose name was lost in the database. The article below was written by Michael Motter and was originally posted on a site called dr-bob.org in 2003. No modifications to the original article have been made. All credit for this article goes to Mr. Motter (or perhaps Dr. Motter by now).

What is Lithium Orotate?
By Michael Motter
Pre-Doc Psychology Student
James Madison University

About Lithium Orotate

Lithium orotate is a popular nutritional supplement that has been marketed in the United States under such names as "Serenity" (www.findserenitynow.com), "Advanced Research" (www.betterlife.com), and "Life Link" (www.nubrain-store.com) to name a few of the many brands that can be found via the internet. Many of these websites claim that lithium orotate is a natural alternative to mood stabilizer and antidepressant medication without any side effects. They claim that lithium orotate can benefit anyone who has migraine headaches, alcoholism, bipolar disorder, depression, or epilepsy.

These claims are backed by the research of Dr. Hans A. Nieper, a German physician, who first studied the use of lithium orotate for migraine headaches, alcoholism, depression, and epilepsy. Dr. Nieper’s article The Clinical Applications of Lithium Orotate: A Two Years Study (1973) concluded that lithium orotate is an effective treatment for migraine headaches, alcoholism, depression, and epilepsy. However, caution should be exercised when interpreting these conclusions. His findings are based on correlation studies and the subjective reports of his patients. Dr. Nieper simply administered lithium orotate to 64 patients that had been diagnosed with the various disorders discussed and used their subjective accounts as evidence of its effectiveness. There is no control group in which he made a comparison to or mention of how he went about controlling for extraneous variables that could have also accounted for their improvement. Thus, we have no idea if it was the lithium orotate or some other factor that accounted for his patient’s improvement. Other research by Satori (1986) suffers from the same flaws. His work supports Nieper's claim that lithium orotate is an effective treatment for alcoholism and migraine headaches. Again all evidence is based on subjective report and there is no control group in which he compares his findings.

What is Lithium:

Lithium is a mineral or more specifically an alkali metal that is present in the human diet in ultratrace quantities and is also found in some natural mineral waters (Physicians Desk Reference, 2003). The typical daily dietary intake of lithium is approximately 200 to 600 micrograms. Fish, processed meat, milk, milk products, eggs, potatoes and vegetables are rich sources of this mineral. In the United States lithium carbonate and lithium citrate are approved by the FDA for the clinical treatment of bipolar disorder (Food & Drug Administration, 2003). Carbonate (carbonic acid) and citrate (citric acid) are mineral carriers that transport lithium throughout the body. According to Yung (1984) many physicians have also begun to prescribe lithium carbonate and citrate for the "off label" treatment of migraine headaches, seizure disorders, and psychosis. It is important to note that "off label" usage is generally considered an option only after all traditional treatment methods have failed and it is not approved by the FDA.

How it Works:

Lithium is administered orally and is generally taken with food, although its absorption is not markedly affected by the presence of food (Physicians Desk Reference, 2003). According to McKim (2003) lithium carbonate, citrate, and orotate is administered orally and therefore it passes through the stomach into the gastrointestinal tract where it is absorbed by the capillaries into the blood stream. These minerals are then absorbed rapidly into the blood stream (80-100%). Peak levels in the blood occur between a half-hour and two hours with citrate and carbonate. Once in the blood it travels to the brain where it must cross the cell membrane or blood brain barrier. Lithium carbonate and citrate cross the blood brain barrier via active transport. Lithium levels in the blood need to be elevated so that there is enough of it to pass through the membrane in order to be therapeutic. Mckim (2003), reports that no one knows for certain but it is theorized that lithium ions concentrate outside of the membrane causing the potential to become less negative and causing depolarization. The voltage gated ion channels open which allow the sodium ions to rush in. It is hypothesized that the lithium ions replace sodium ions and cross through the blood brain barrier resulting in neutralization of the resting potential.

According to McKim (2003) lithium carbonate and citrate therapy requires reaching serum concentrations of lithium that are close to the toxic concentration. Lithium Carbonate and Citrate therapy requires serum levels of 1.0-1.5 mEq/L for acute mania and 0.6 – 1.2mEq/L for maintenance. During treatment lithium serum concentrations should not usually exceed 1.5 mEq/L. Mild to moderate toxic reactions may occur at lithium concentrations from 1.5 to 2 mEq/L, and moderate to severe reactions at concentrations above 2 mEq/L. Serum lithium concentrations should usually be monitored 3 times weekly and blood studies and urinalysis weekly during the initial period of administration and periodically as required thereafter.

Lithium orotate is administered orally and therefore it passes through the stomach into the gastrointestinal tract where it is absorbed by the capillaries into the blood stream. According to Nieper (1973) digestion breaks off the lithium mineral from the lithium compound when lithium is attached to carbonate and citrate which is then absorbed rapidly into the blood stream. Therefore, lithium orotate is coated with a special coating which supposedly protects the lithium orotate while it passes through the stomach acids. This coating protects the compound and allows it to be absorbed by the capillaries into the bloodstream with most of the lithium still bound to the orotate. According to Nieper (1973) the orotate carriers show a special affinity for tissues in which metabolism involves the blood brain barrier. Orotate supposedly uses passive transport to cross through the blood brain barrier. Because the lithium is still mostly attached to the orotate carrier, it diffuses across the membrane releasing the lithium to the other side and leaving little left in the blood stream.

Nieper (1973) reports that a mineral analysis of his patients whole blood and blood serum found that lithium orotate does not cause the approximate level of 0.02 ppm lithium in normal blood or serum to be exceeded by more than 30% (0.026 ppm). Lithium carbonate contains 18.8mg of elemental lithium per 100mg per 100mg (57mg per 300mg, 113mg per 600mg). Most lithium orotate compounds contains 3.83mg of elemental lithium per 100mg (4.8mg per 120mg). Lithium carbonate can cause serum to rise an average of 0.2 to 0.4 mEq/L after intake of 300 mg and 0.3 to 0.6 mEql/L after intake of 600 mg of lithium carbonate. It appears that lithium orotate does not contain enough elemental lithium per recommended dosage to cause lithium serum concentrations to rise beyond toxic levels. This may explain why they claim that lithium blood serum monitoring is unnecessary. It also raises the questions whether there is even enough lithium to cause any type of therapeutic effect.

Nieper (1973) claims that lower elemental doses of lithium can be administered when attached to orotate because most of the lithium doesn’t dissolve from the carrier until it passes through the blood brain barrier. Therefore, all of the lithium (theoretically enough to be therapeutic) goes to the brain and a minimal amount gets left behind in the blood. Thus the amount of lithium that enters into the bloodstream doesn’t reach toxic levels and doesn’t need to be monitored.
Lithium is excreted via the kidneys (renally). It is excreted rapidly and several daily doses are needed to maintain the therapeutic level. It is not metabolized; approximately 95% is renally excreted (saliva, sweat, feces 5%). Lithium is excreted unchanged in the urine. Renal excretion is biphasic, with rapid clearance of up to two-thirds within 6-12 hours followed by a slower elimination over the next twelve hours. The overall half-life is between 12 and 24 hours. The excretion rate varies considerably among individuals and increases with age. Half-life in geriatric patients and patients with impaired renal function is increased to 36 to 50 hours.

What Are The Side Effects:

Nieper (1973) claims that because of the low amount of lithium in the blood serum, the common side effects of lithium carbonate and citrate which include: diarrhea, frequent urination, dehydration, lethargy, nausea, skin rashes, tremor, thyroid dysfunction, and weight gain supposedly do not occur. The low levels also claim to make it safe for use with antithyroid, asthma, bronchitis, cystic fibrosis, emphysema, non-steroidal anti-inflammatory drugs (NSAID's), and sinusitis medication and diuretics which may cause interactions with lithium carbonate or citrate. It gives no mention of antipsychotic medication which can have interactions with lithium carbonate and citrate (McKim, 2003).

Nieper (1973) claims that lithium orotate does not have renal side effects because of its low dose. However, research conducted by Smith and Schou (1979) found that kidney functioning and urine flow were markedly lower in rats given a intraperitoneal injection (2 mmol lithium kg-1) of orotate than rats given carbonate, sodium chloride, or a sham injection. Renal lithium clearance was significantly lower. Kidney weight and lithium concentrations in serum kidney and heart were significantly higher in the orotate group which may be caused by the lower kidney functioning. Smith and Schou concluded that lithium orotate was not recommended as safe for humans. Smith (1976) reports that the pharmacokinetics of the lithium ion given as lithium orotate do not differ from lithium chloride or lithium carbonate when administered in rats. Though excessive secretion of urine and excessive thirst developed more slowly in rats given lithium orotate than in those given lithium carbonate or lithium chloride. Lithium orotate is recommended to be unsafe during pregnancy and breast feeding. Lithium passes into milk and its use should be avoided during lactation as concentrations are 33 to 50% of those in the mother's serum (McKim, 2003). Several anecdotal accounts of lithium orotate were found on internet chat rooms claiming that lithium orotate caused depression.

Comparison of the Different Forms of Lithium:

An overall comparison of the differences in costs, research efficacy, and side effects between lithium orotate and lithium carbonate or citrate shows that there is considerable difference in these three areas. The cost of lithium orotate varies depending on the website where it is purchased. For ninety 120mg tablets of Serenity the monthly cost is $39.99 per month or approximately $0.44 per pill. Two-hundred 120mg tablets of Advanced Research costs $12.99 per month or approximately $0.06 per ill. One hundred 135mg tablets of Life Link totals $12.00 per months or approximately $0.12 per pill. One hundred and fifty 300mg tablets of lithium carbonate or citrate on the other costs approximately $25.00 per month or almost $0.17 per pill.

Dr. Nieper and Dr. Sartori's claims are based only on subjective case study reports. A search on the National Library of Medicine’s (2003) website indicate that there have been no double-blind controlled studies on the effects of lithium orotate for any medical or health related purposes. Thus the claims made by Dr. Nieper and Dr. Satori are based on weak scientific evidence. Smith (1976) reports that pharmacokinetics of the lithium orotate do not differ from lithium chloride or lithium carbonate when administered in rats. Furthermore, according to Garbutt, West, Carey, Lohr, & Crews (1999) suggestions that it might be useful in treating alcoholism are unfounded. Lithium is not useful for treating patients who have alcohol dependence without other psychiatric conditions. There is limited research on the effects of lithium in primary alcoholics without comorbid mood disorders. According to Picket & O’Dell (1992) there is no credible research to support the supplemental or medically unsupervised use of lithium for any purpose. There are no indications for the supplemental use of lithium. If lithium dosage is too low, you will derive no benefit. There is little research on the claims that lithium orotate is absent of the side effects that accompany lithium carbonate or citrate. What research has been done by Smith and Schou (1979) indicates that the renal side effects of lithium orotate may be more severe than carbonate or citrate in rats.
Lithium orotate is not regulated by the FDA. It is marketed as a "dietary supplement". According to Dietary Supplement Health and Education Act (DSHEA) of 1994 (Food & Drug Administration, 2003) a dietary supplement is a product taken by mouth that contains a dietary ingredient intended to supplement the diet. The dietary ingredients in these products may include: vitamins, minerals, herbs or other botanicals, amino acids, and substances such as enzymes, organ tissues, glandulars, and metabolites. Dietary supplements can also be extracts or concentrates, and may be found in many forms such as tablets, capsules, softgels, gelcaps, liquids, or powders (page 1).
Because it is not regulated by the FDA the claims that the various companies make about it’s effectiveness are not regulated by the government but instead by the company. A company is responsible for determining that its products are safe and that claims they make about them are substantiated by adequate evidence to show that they are not false or misleading. This means that the supplements do not need approval from FDA before they are marketed. Companies do not have to provide the FDA with the evidence it relies on to substantiate safety or effectiveness before or after it markets its products. In addition it is also interesting to note that Dr. Nieper has a history with the federal government. The 1994 FDA Import Alert states that Dr. Nieper was accused of importing numerous drugs into the United States without FDA approval (FDA, 1994).

Conclusion:

In conclusion there is some of anecdotal evidence that lithium orotate is an effective treatment for the various health concerns it claims to help. However, there have been no controlled research studies that validate these claims. Why Dr. Nieper never followed up his patients claims with more rigorous research remains a mystery. Is it possible that he was merely a "snake-oil" salesman trying to make a quick buck or is there something we are missing? It appears that many in the complementary and alternative healing community believe that there is something missing in modern medicine that does not fully address our health concerns. But even if this is the case and lithium orotate is beneficial, then it would seem logical to pursue further research. This would not only validate their claims but also reduce the risk of harm. Harm that has all too often occurred in the absent minded world of nutritional supplements, see ephedra and phen/fen.

References

Food and Drug Administration (1994). Automatic Detention of New Drugs Promoted by
Dr. Hans Nieper of West Germany. Retrieved June 26, 2003 from www.fda.gov/ora/fiars/ora_import_ia6628.html

Food and Drug Administration (2003). Dietary Supplement Health and Education Act (DSHEA) of 1994. Retrieved June 26, 2003 from www.cfsan.fda.gov

Garbutt, J.C., West, S.L., Carey, T.S., Lohr, K.N., & Crews, F.T. (1999).
Pharmacological treatment of alcohol dependence: a review of the evidence. JAMA, 281(14), 1318-25.

McKim, W. A. (2003). Drugs & Behavior: An Introduction to Behavioral
Pharmacology (5th ed.). Upper Saddle River, New Jersey: Prentice Hall.

Nieper, H. A. (1973). The clinical applications of lithium orotate: A two year study. Agressologie, 14(6), 407-411.

Physicians Desk Reference (2003). Lithium. Retrieved June 25, 2003 from
www.pdrhealth.com

Pickett, E.E., & O'Dell, B.L. (1992). Evidence for dietary essentiality of lithium in the rat. Biol Trace Elem Res, 34, 299-319.

Satori, H.E. (1986). Lithium orotate in the treatment of alcoholism and related conditions. Alcohol, 3(2), 97-100.

Smith, D. F. (1976). Lithium orotate, carbonate and chloride: pharmacokinetics, polyuria in rats. British Journal of Pharmacology, 56, 399-402.

Smith, D. F., Schou, M. (1979). Kidney function and lithium concentrations of rats given an injection of lithium orotate or lithium carbonate. Journal of Pharmaceutical Pharmacology, 31(3), 161-163.

Yung, C.Y. (1984). A review of clinical trials of lithium in neurology. Pharmacology, Biochemistry, & Behavior. 21, 1, 57-64.

Further Readings

Kling, M. A., Manowitz, P., Pollack, I.W. (1978). Rat brain and serum lithium concentrations after acute injections of lithium carbonate and orotate. Journal of Pharmaceutical Pharmacology, ;30(6), 368-70.

Nieper, H. A. (1999). The Curious Man. Avery Publishing Group.



The information below was also posted by another individual, whose name and information has also been lost. However, it seems likely that this person is the owner of the website mentioned in this short op-ed piece.

Kidney study for lithium orotate had a flawed conclusion
Taken from the Lithium Orotate Works! website

*Note* The website above contains many pages of information about lithium orotate on various subjects.

Kidney Dangers of Lithium Orotate?

Is using lithium orotate dangerous? An Internet search will bring up a list of sites stating that it is. In every instance (found to date), this supposition is based solely on a single study done on lithium orotate in 1978. There is no other research or study of any kind which concludes that lithium orotate is dangerous to use.

And the much-quoted conclusion of the 1978 study is INCORRECT for the reasons explained below.

Flawed Conclusion of Kidney Study and Lithium Orotate

When researching for any problems or concerns regarding lithium orotate use, an abstract of a study done by Smith and Schou in 1978 can be found at PubMed.

This study compared the effects on kidney function of lithium carbonate and lithium orotate. Groups of rats were injected with equal amounts of lithium carbonate and lithium orotate (and a neutral injection of sodium chloride for the control group) and then examined.

The study found that renal lithium clearance was significantly lower, and kidney weight and the lithium concentrations in serum significantly higher after the injection of lithium orotate than after the injection of lithium carbonate.

The conclusion the study drew because of this lowered kidney function was that it seemed inadvisable to use lithium orotate for the treatment of patients.

However, a highly significant point which is completely unaddressed by this study is that the same amounts of lithium orotate and lithium carbonate were used. But people DON'T USE the same enormous amounts required for lithium carbonate when using lithium orotate.

An effective dose of lithium orotate typically contains 15 mg of elemental lithium compared to 126 mg of elemental lithium from lithium carbonate. More than 700% more lithium is used with lithium carbonate. Based on the information in the study stating that equal amounts of each item was used, THE STUDY ADMINISTERED 700% TOO MUCH LITHIUM OROTATE!

This conclusion of this study is skewed because it completely disregards the way lithium orotate is administered in actual use.

Ironically, this study which concluded that lithium orotate was inadvisable for treatment of patients was done as a direct follow-up study to one performed by Kling, Manowitz and Pollack in 1978. Their study suggested that lithium orotate could be used in lower amounts than required of lithium carbonate to achieve therapeutic results.

Other links on Lithium Orotate

  • The Lithium Orotate Project - one of the best, most recent and up to date sites with information on lithium orotate with overview's of all the studies conducted on it, it's safety and it's legality as a supplement.
  • Lithium: Profile of a Mood Stabilizer by HowStuffWorks.com - some good basic info on the compound lithium itself and how it works to treat bipolar depression and other conditions.
  • About Hans Nieper, M.D. - considered to be, if not the "discoverer" of lithium orotate, then it's biggest proponent. Dr. Nieper also bonded orotic acid to many other compounds to try and increase their worth as dietary ingredients and drugs. However, some other people have a less positive view of the doctor, including Quackwatch for some of his purported cancer treatments - although the site doesn't discuss lithium orotate specifically.
Please visit the discussion at bodybuilding.com for more information on this topic.

Tuesday, September 04, 2007

Toxic Popcorn

An ingredient used to create the butter flavor in microwave popcorn, diacetyl, has been causing some concerns for workers in plants who make the product, as it has been shown to have a causative link between the ingredient and bronchiolitis obliterans - a debilitating lung disease. However, a question that has not been addressed is whether or not the diacetyl ingredient is toxic when used in a household setting. Are consumers at risk when microwaving their artificial buttery concoctions? No one really knows, but some manufacturers, such as Pop Weaver (PDF) (HTML), have already removed the ingredient from their product line.



Friday, August 03, 2007

Archive: Methyl Hydroxy Nandrolone (MOHN)

My article for Methyl Hydroxy Nandrolone (M4OHN) was written for the same company that I wrote my Methyl Hydroxy Testosterone (M4OHT) article for. It was also written in 2004 in a period leading up to the banning of prohormones, when manufacturers were bringing out all sorts of new compounds that were either active steroids or precursors to them. Most all of them had never been tested and were able to be created due to the new found access to a book by Julius Vida, a scientist who synthesized every possible modification of male sex steroids and then published them in a book, entitled "Androgens and Anabolic Agents, Chemistry and Pharmacology", in 1969. Although the book had been long out of date, an individual finally was able to find a copy of it and scanned it, converted it into PDF format, and sold it. This, along with the availability of Chinese companies to synthesize almost anything requested, allowed supplement companies to sell steroids that were never manufactured or widely used - and hence, not scheduled - a legal loophole that is still exploited to this day. Although for some reason, both M4OHN and M4OHT were banned by California state law, they were not banned in any other state, and as such, they were manufactured and sold until finally banned by the Anabolic Steroid Control Act of 2004.


Hydroxy Nandrolone, like its counterpart, Hydroxy Testosterone, is a steroid which is quite obscure and not much is written about it in medical literature. Hydroxy Nandrolone was produced commercially in Italy under the name Steranabol. However, it was sold as an injectable product, as opposed to an oral one, with cypionate ester attached. It is chemically known as oxabolone.

Nandrolone is the base steroid of Hydroxy Nandrolone. Nandrolone deconate is a popular anabolic steroid, commonly known as Deca Durabolin. Deca is well known for being a strong anabolic compound, with fewer androgenic properties. This is due to the fact that nandrolone is missing a carbon atom at the 19 position, giving it overall more affinity for the androgen receptor than testosterone. [1] However, unlike Hydroxy Nandrolone, nandrolone can aromatize into estrogen, which is another factor involved in it's strong anabolic effects.

Like Hydroxy Testosterone, Hydroxy Nandrolone also has a hydroxyl group at the 4 position on the molecule. This makes it incapable of interacting with the aromatese and 5 alpha reductase enzymes. However, since regular nandrolone typically reduces into a much weaker androgen, DHN (dihydronandrolone) via 5AR, this would make Hydroxy Nandrolone more androgenic. In the body nandrolone reduces to DHN through the same pathway that testosterone reduces to DHT. But, in this case, DHN is weaker and less androgenic than DHT, which is responsible for most of testosterone's androgenic effects (acne, androgenic alopecia, prostate issues, etc). So, with Hydroxy Nandrolone, we are left with a more potent androgen since it cannot convert through the same pathway. [2]

When we look at the information on Steranabol, we see that it is overall less potent than its parent, nandrolone. [3] Although not structurally similar, Methyl Hydroxy Nandrolone is probably closer in action to another popular steroid, oxandrolone. Oxandrolone, commonly known for its trade name, Anavar, a very mild oral steroid, even though it's a 17-alpha-alkylated (methylated) compound that's based on DHT. Oxandrolone is well known for for it's safety and low potential for HTPA shutdown. It is usually incorporated into cutting or lean mass cycles, as it will not aromatize because of it's DHT base.

Because of it being derived from DHT, oxandrolone can be somewhat androgenic in higher doses, and this will probably not be as pronounced with Hydroxy Nandrolone. This is because the hydroxyl group reduces androgen receptor binding affinity. There is also a question of progesterone related activity with this compound. It is well known that nandrolone and its derivatives can bind to the progesterone receptor. [4] However, it is thought that progesterone requires the presence of estrogen in order to cause gyno. Therefore, those prone to gyno may not want to use Hydroxy Nandrolone with another aromatizing compound like 4AD, while others might simply just use an anti-estrogen, such as tamoxifen citrate (Nolvadex) - a SERM, or an AI like ATD while on a cycle. However, it is unknown what affinity Hydroxy Nandrolone has for the progesterone receptor, so taking precaution is not unwarranted.

With Methyl Hydroxy Nandrolone, or MOHN, we end up with a very interesting compound. Using MOHN, one would expect increases in lean muscle mass, as well as a noticeable increase in strength. Since MOHN doesn’t aromatize, you would not notice water retention, or other estrogenic side effects typically associated with Deca. MOHN would work well during bulking cycles with the addition of 4AD and 1-testosterone or 1,4andro, and probably work even better on cutting cycles with a lower dose of 4AD. MOHN should be well tolerated by people concerned about side effects, and even women. Being a methylated compound, it will increase strain on the liver, so it would be best not to stack it with other methylated substances. As with MOHT, supplements that assist in liver function, such as ALA, NAC and Milk Thistle would be a welcome addition to the stack.

1. Bergink EW, Janssen PS, Turpijn EW, van der Vies J. Comparison of the receptor binding properties of nandrolone and testosterone under in vitro and in vivo conditions. J Steroid Biochem 1985 Jun;22(6):831-6

2. Van Mol, Peter. Steranabol. Bodybuilding.com

3. Llewellyn, William. Anabolics 2004. Molecular Nutrition, Jupiter FL, 2004.

4. Reel JR, Humphrey RR, Shih YH, Windsor BL, Sakowski R, Creger PL, Edgren RA. Competitive progesterone antagonists: receptor binding and biologic activity of testosterone and 19-nortestosterone derivatives. Fertil Steril. 1979 May;31(5):552-61.

Wednesday, August 01, 2007

Archive: Methyl Hydroxy Testosterone (MOHT)

My two articles on Methyl Hydroxy Testosterone (M4OHT) and Methyl Hydroxy Nandrolone (M4OHN) were written for a supplement manufacturer who was selling the two compounds. When these articles were written in 2004, both of these were brand new compounds on the then still legal prohormone market. Unfortunately, shortly after M4OHT was released, it was discovered it wasn't just illegal in California, but actually scheduled in the Steroid Control Act of 1990 and removed from the market before very many people had a chance to try it. A slightly weaker version of the non-methylated version was also sold encapsulated in oil and bound to an ester. Neither M4OHT or M4OHN are legally available as a supplement and were permanently scheduled with the passing of the Anabolic Steroid Control Act of 2004.

Hydroxy Testosterone is a relatively new steroid on the supplement scene. William Llewellyn of Molecular Nutrition first brought the compound to the sports world's attention when he discussed its discovery on a popular bodybuilding forum. However, Hydroxy Testosterone did not see the light of day for quite some time after it was initially discussed.

Hydroxy Testosterone is an active metabolite of the European anti-aromatese drug, Formestane (4-hydroxy androstenedione). It was also investigated by the pharmaceutical firm Searle during the steroid hayday of the middle of the last century. However, it was never marketed as an anabolic, probably because of their more potent discovery oxandrolone. Being that it was never produced by a pharmaceutical, and never being included in the Anabolic Steroid Control Act of 1990, it can be considered legal (for the time being at least) to sell as a dietary supplement. However, hydroxy testosterone and its counterpart hydroxy nandrolone are not legal to sell in California, where it is a scheduled drug.

Hydroxy Testosterone is similar to the obscure anabolic steroid, Clostebol (sold commercially as Megagrisevit Mono). Clostebol has been marketed in the past, in parts of Europe and Asia, where it is used as a transdermal and injectable preparation. Clostebol has a chloro group on the 4 position of the molecule, making it incapable of interacting with both the 5 alpha reductase and aromatese enzymes. [1] Hydroxy Testosterone shares this feature by having a hydroxyl group at the same 4 position, it is also incapable of forming DHT and estrogen. This makes it an ideal drug for individuals looking to avoid the common side effects associated with other steroid and prohormone products. Hydroxy Testosterone also has the very interesting feature of acting as a mild aromatese inhibitor and 5 alpha reductese inhibitor. This means that it would act in a similar, albeit weaker, fashion to both the anti-aromatese drug anastrozole and the 5-AR inhibitor finasteride. [2]

According to standard assays of potency, Hydroxy Testosterone shows to have an RBA (relative binding affinity) of 75. When compared to testosterone propionate, hydroxyl testosterone acetate was shown to be 0.65 times as anabolic and 0.25 times as androgenic by injection. [3] This would make it a very mild androgen in nature, and very easy for individuals who are concerned about common side effects of steroidal compounds. Since it does not convert to estrogen or DHT, it would not be an ideal drug for bulking or strength gains, but more suited for lean muscle gains or even fat reduction. Women would most likely tolerate this drug very well.

Now, there is a new version of Hydroxy Testosterone available, which has been methylated. Methylating a drug makes an alteration at the C17 position of the molecule, allowing it to avoid liver breakdown. Two drugs which are methylated are the well known and popular illegal steroids, Winstrol and Dianabol. Although Methyl Hydroxy Testosterone, or MOHT, is not anywhere near as potent as those two compounds, it does have the same methyl alteration, increasing bioavailability and changing the action of the drug in the body. Generally, methylating a compound decreases the binding affinity towards the androgen receptor, making it less potent overall. However, since it greatly increases the half life, bioavailability and has other possible mechanisms, such as decreasing SHBG binding affinity, it would most likely make MOHT more favorable to use.

When we look for comparable drugs known to athletes, only one other comes to mind. Oral Turnibol (OT) is an exotic steroid developed for secret use by East German athletes. Currently, only one known underground lab is known to make it, and it is questionable whether or not it is legitimate. Recently, a prohormone has been sold by various companies of Oral Turnibol labeled as them chemical 4-chloro-17a-methyl-1,4-diene-3,17 diol. It is currently being sold as the supplement Halovar, which converts directly to OT. Oral Turnibol was East Germany's answer to the androgenic structure of Dianabol. [4] With a structure very similar to Methyl Hydroxy Testosterone, with the exception of a hydroxyl group in place of Turnibol's 4-chloro group, it has the same attributes. Turnibol cannot aromatize or convert to DHT. We could generally expect a similar result with MOHT, seen as significant gains in lean mass and mild increases in strength, without the negative side effects of Dianabol. [5] A very interesting account of the use of Oral Turnibol by female swimmers in the former communist East Germany is detailed in the book Faust's Gold by Dr. Steven Ungerleider.

Methyl Hydroxy Testosterone would stack well with just about anything. For bulking, it would stack very well with 4AD and possibly an oralgel or transdermal form of 1-testosterone, 1AD or 1,4andro. For cutting, it would stack well with 1-testosterone or 5AA. In both cases it would work well to help keep the other side effects minimal, by decreasing overall DHT and estrogen, as well as causing a positive hardening effect on the muscle. It would be wise not to stack it with another methylated compound, such as MOHN or Methyl-1-Test for fear of elevating liver enzymes too greatly. For individuals concerned with protecting their liver, supplementing with Milk Thistle or N-Acetyl-L-Cysteine (NAC) would be wise option.

The dosage of MOHT would probably be in the range of 5-15mg daily. It would be advisable to start off at a low dosage to find out how well it's tolerated, and then work up to a higher dosage. MOHT would be best taken with a meal.

1. Van Mol, Peter. Megagrisevit Mono. Bodybuilding.com.

2. Davies JH, Shearer RJ, Rowlands MG, Poon GK, Houghton J, Jarman M, Dowsett M. Effects of 4-hydroxyandrost-4-ene-3,17-dione and its metabolites on 5 alpha-reductase activity and the androgen receptor. J Enzyme Inhib. 1992;6(2):141-7.

3. Vida, J.A. Androgens and Anabolic Agents, Chemistry and Pharmacology. Academic Press, Inc, New York, 77-91, 1969.

4. Montana, Nelson. Johnny, We Hardly Knew Ye. Testosterone Nation.

5. Llewellyn, William. Anabolics 2004. Molecular Nutrition, Jupiter FL, 2004.

Monday, June 18, 2007

New Lab Studies Show Creatine Ethyl Ester & Kre-Alkalyn Ineffective

At the recent International Society of Sports Nutrition, two new studies were released showing that both Creatine Ethyl Ester (CEE) and Kre-Alkalyn were ineffective in vitro. The studies were conducted by The Division of Sport Sciences at Northumbria University, Newcastle UK and Kingston University London, Department of Life Sciences by Dr. MJ. Tallon Dr. R. Child.

Both studies used similar methods to compare the rates of conversion of CEE and Kre-Alkalyn to the waste by-product creatinine when compared to Creapure brand micronized creatine monohydrate. "Each product was incubated in 900ml of pH 1 HCL [hydrochloric acid] at 37º +/- 1ºC and samples where drawn at 5, 30 and 120 minutes and immediately analyzed by HPLC [high-performance liquid chromatography] (UV) for creatine and creatinine." [1,2] This occured in both product studies. Although this test was conducted in a laboratory, it was meant to mimic conditions that would be present in the human stomach.

Creatine Ethyl Ester

"Creatine ethyl ester is merely creatine monohydrate with an added ester attached to make the creatine molecule more lipophilic [having an ability to be absorbed by lipids, or fats]." [3] Adding an ester to compounds is nothing new, but until this point, there has been no real data indicating that creatine ethyl ester was any better than any other form of creatine on the market - particularly the most studied form, creatine monohydrate. By adding an ester to a compound for oral consumption, it attempts to allow it to pass through the harsh acidic stomach content and be taken up by lymphatic absorption. Esterification is the process that allows an acid molecule to combine with an alcohol molecule, which removes water from the equation. This makes it more soluble in an oil or fat - similar to esterfied steroids.

Creatine Ethyl Ester has a long history - longer than I actually imagined, with studies dating back to the 1920s. [3] However, this most recent form, which was originally conceived to be used as a dietary supplement was first introduced by The University of Nebraska, which holds patent #6897334: Production of creatine esters using in situ acid production. This patent does not specify the usage of CEE, but only it's production and manufacturer. Initially, CEE was submitted to the FDA for review to market it as an OTC dietary supplement, CE2™, it was rejected by the FDA (PDF) following safety concerns. However, that didn't stop every other supplement company on the planet from picking up the ingredient and selling it, despite the lack of pre-market approval by the FDA of from its patent holders.

The new study involving CEE uses two products, SAN CM2 Alpha - a blended product that includes Di-L-Arginine-L-Malate, Beta-Alanine, and CEE HCL. SAN previously sold a version of CEE that was methylated, a molecular change to the creatine in an attempt to enhance absorption by avoiding breakdown in the stomach and liver. However, this version was removed at concerns about it's potential conversion to methanol. The second brand tested was MRI CE2, which is the original Medical Research Institute that requested approval to market CEE from the FDA. MRI is the company that was founded by Ed Byrd, who also popularized NO2 products. CE2 contains only creatine ethyl ester HCl.

Creatine ethyl ester rapidly degrades to creatinine in stomach acid

Child R and Tallon MJ

Department of Life Sciences, Kingston University, Penrhyn Rd, Kingston-upon-Thames, United Kingdom. University of Northumbria, Sport Sciences, Northumbria University, Northumberland Building, Newcastle upon Tyne, United Kingdom, DrChild@CR-Technologies.net

Creatine ethyl ester (CEE) is a commercially available synthetic creatine that is now widely used in dietary supplements. It comprises of creatine with an ethyl group attached and this molecular configuration is reported to provide several advantages over creatine monohydrate (CM). The Medical Research Institute (CA, USA) claim that the CEE in their product (CE2) provides greater solubility in lipids, leading to improved absorption. Similarly San (San Corporation, CA, USA) claim that the CEE in their product (San CM2 Alpha) avoids the breakdown of creatine to creatinine in stomach acids. Ultimately it is claimed that CEE products provide greater absorption and efficacy than CM. To date, none of these claims have been evaluated by an independent, or university laboratory and no comparative data are available on CEE and CM.

This study assessed the availability of creatine from three commercial creatine products during degradation in acidic conditions similar to those that occur in the stomach. They comprised of two products containing CEE (San CM2 Alpha and CE2) and commercially available CM (Creapure™). An independent laboratory, using testing guidelines recommended by the United States Pharmacopeia (USP), performed the analysis. Each product was incubated in 900ml of pH 1 HCL at 37º +/- 1ºC and samples where drawn at 5, 30 and 120 minutes and immediately analyzed by HPLC (UV).

After 30 minutes incubation only 73% of the initial CEE present was available from CE2, while the amount of CEE available from San CM2 Alpha was even lower at only 62%. In contrast, more than 99% of the creatine remained available from the CM product. These reductions in CEE availability were accompanied by substantial creatinine formation, without the appearance of free creatine. After 120 minutes incubation 72% of the CEE was available from CE2 with only 11% available from San CM2 Alpha, while more than 99% of the creatine remained available from CM.

CEE is claimed to provide several advantages over CM because of increased solubility and stability. In practice, the addition of the ethyl group to creatine actually reduces acid stability and accelerates its breakdown to creatinine. This substantially reduces creatine availability in its esterified form and as a consequence creatines such as San CM2 and CE2 are inferior to CM as a source of free creatine.
As indicated by the study, the products tested in the sample under performed that of regular micronized creatine monohydrate. In real world terms this would equate to purchasing a product that itself advertises to be superior to "regular" creatine by withstanding breakdown in the stomach and other common problems, yet it turns out that it does not perform as advertised, at least in the lab. The conversion of creatine into creatinine is an unwanted effect of the compound, as creatine needs to make it's way into skeletal muscle cells to be effective. Creatinine is not effective at anything, and high levels in individuals with kidney problems can be hazardous. In fact, creatinine is one of the markers doctors check for when doing routine blood tests to determine if renal failure is occurring.

Kre-Alkalyn

Kre-Alkalyn [KA] is not a modification to creatine itself, but an alternative delivery system for the compound. However, the claims made for Kre-Alkalyn have generally been viewed with skepticism due to the fact that there has been no clinical research performed on it, and the claims made about KA are similar to those made in the past by products such as the well known and bunk liquid creatine.

Here is a partial description taken from an advertisement for a KA product:

Kre-Alkalyn...a patented Creatine in a pharmaceutical delivery system providing maximum stability and absorption. Creatine Monohydrate has been proven through a decade and more of research to enhance strength, endurance, and subsequent athletic performance. The only disadvantages of traditional Creatine Monohydrate are the extremely short term stability, rapid conversation into the bi-product Creatinine when exposed to liquid, and subsequent poor absorption into the bloodstream. Kre-Alkalyn...which is buffered for maximum absorption and stability, solves this dilemma. Kre-Alkalyn...offers the athlete Creatine which is 100% stable, will not break down into Creatinine, and will absorb efficiently into the bloodstream. In fact, each 1 gram of Kre-Alkalyn is equivalent to ingesting 10 grams of Creatine powder allowing the athlete to take far less product while experiencing even more explosive results.
Kre-Alkalyn is covered under several patents for it's usage as a creatine supplement delivery system. Patent #6,399,661 details some of the inner workings of KA:

Abstract
The present invention relates to an oral creatine supplement and the method of making this supplement which includes mixing an alkaline powder with a powdered creatine until the pH of the mixture is in the range between 7-14. A powdered additive is added to the mixture for improving sweetness and taste. Finally, a further alkaline powder is added to the mixture to adjust the pH of the mixture to a range between 7-14. This mixture is then mixed with water prior to ingestion.

What is claimed is:

1. A process for producing a creatine mixture for ingestion comprising the steps of:

mixing an alkaline powder with a powdered creatine to adjust the pH of the mixture to a range between 7-14;
adding a powdered additive to the mixture for improving sweetness and taste; and
adding a further alkaline powder to the mixture to adjust the pH of the mixture to a range between 7-14.
2. The method according to claim 1 wherein the alkaline powder is comprised of soda ash.

3. The method according to claim 1 wherein the alkaline powder is comprised of magnesium glycerol phosphate.

4. The method according to claim 1 wherein the alkaline powder is selected from a hydroxide, carbonate, bicarbonate, chloride, tree latex or a phosphate.

5-8. The method according to claim 1 wherein the creatine powder is comprised of creatine monohydrate, creatine phosphate, creatine pyruvate, creatine citrate.
The patent itself includes tests demonstrating KA's ability to defeat conversion to creatinine and the reasoning behind how it works. Like CEE, Kre-Alkalyn is a higher priced creatine product that has less total creatine per dose than standard the monohydrate version. Unfortunately, as with the previous study for CEE, this new study, using the same methods, successfully demonstrates that KA doesn't live up to it's claims and that micronized creatine monohydrate still wins out.

Kre-alkalyn® supplementation has no beneficial effect on creatine-to-creatinine conversion rates.

Tallon MJ and Child R

University of Northumbria, Sport Sciences, Northumbria University, Northumberland Building, Newcastle upon Tyne, United Kingdom, Department of Life Sciences, Kingston University, Penrhyn Rd, Kingston-upon-Thames, United Kingdom. DrTallon@CR-Technologies.net

All American Pharmaceutical and Natural Foods Corp. (Billings, MT, USA) claim that Kre-alkalyn® (KA) a "Buffered" creatine, is 100% stable in stomach acid and does not convert to creatinine. In contrast, they also claim that creatine monohydrate (CM) is highly pH labile with more than 90% of the creatine converting to the degradation product creatinine in stomach acids. To date, no independent or university laboratory has evaluated the stability of KA in stomach acids, assessed its possible conversion to creatinine, or made direct comparisons of acid stability with CM.

This study examined whether KA supplementation reduced the rate of creatine conversion to creatinine, relative to commercially available CM (Creapure™). Creatine products were analyzed by an independent commercial laboratory using testing guidelines recommended by the United States Pharmacopeia (USP). Each product was incubated in 900ml of pH 1 HCL at 37º +/- 1ºC and samples where drawn at 5, 30 and 120 minutes and immediately analyzed by HPLC (UV) for creatine and creatinine.

In contrast to the claims of All American Pharmaceutical and Natural Foods Corp., the rate of creatinine formation from CM was found to be less than 1% of the initial dose, demonstrating that CM is extremely stable under acidic conditions that replicate those of the stomach. This study also showed that KA supplementation actually resulted in 35% greater conversion of creatine to creatinine than CM. In conclusion the conversion of creatine to creatinine is not a limitation in the delivery of creatine from CM and KA is less stable than CM in the acid conditions of the stomach.
Conclusions

Both studies demonstrate that two new and very highly-touted creatine products do not live up to their claims in lab conditions. Contrary to claims made by both products that they can withstand the supposed problems of regular creatine conversion to creatinine in the body, the in fact work less well than the regular versions. However, it should be emphasized that both of these test are performed in vitro and more studies need to be done, especially on male athletes and weight lifters, to see how they stack up in real world conditions. It is also important to make the determination as to whether or not they have a real effect on strength and body composition. Another factor that is noticeable is the email addresses of the two doctors that conducted the study. Although I am not personally familiar with either of them or their ties to CR-Technologies.net, it does appear that the web page for that domain sells a product called Creasafe™, which claims to be "the worlds safest and most advance [sic] creatine", bringing up the possibility of a conflict of interest. UPDATE: Dr. Tallon has responded to this criticism.

Still, for now, it appears that the best bet for people supplementing with creatine is what has been recommended all along - micronized creatine monohydrate.

References

Thanks to Anssi Manninen for clearing up some confusion in the studies text.

1. Child R and Tallon MJ. Creatine ethyl ester rapidly degrades to creatinine in stomach acid. Department of Life Sciences, Kingston University, Penrhyn Rd, Kingston-upon-Thames, United Kingdom. University of Northumbria, Sport Sciences, Northumbria University, Northumberland Building, Newcastle upon Tyne, United Kingdom, DrChild@CR-Technologies.net

2. Tallon MJ and Child R. Kre-alkalyn® supplementation has no beneficial effect on creatine-to-creatinine conversion rates. University of Northumbria, Sport Sciences, Northumbria University, Northumberland Building, Newcastle upon Tyne, United Kingdom, Department of Life Sciences, Kingston University, Penrhyn Rd, Kingston-upon-Thames, United Kingdom. DrTallon@CR-Technologies.net

NOTE: The original abstracts of these studies have been posted online at NPICenter. The abstracts which are in this blog were copied and after Layne Norton (str8flexed) posted them on bodybuilding.com, which lead to some of the characters showing up incorrectly.

3. Creatine Ethyl Ester…Reviewing the Literature by Deserusan
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