# Creatine



## winger (Jul 26, 2003)

Creatine

TRADE NAMES

Creatine is available generically from numerous manufacturers. Branded products include Muscle Power (Mason Vitamins), Creatine Fuel (Twinlab), Creatine Booster (Champion Nutrition), Creatigen (Bricker Labs), CreaVate (Prolab Nutrition), Perfect Creatine (Nature's Best), Xtra Advantage Creatine Serum (Muscle Marketing USA), Micronized Creatine (Met-Rx), Creavescent (GEN), Power Creatine (Champion Nutrition), Phosphagen (GNC), Crea-Tek (Iron Tek), Effervescent Creatine Elite (Muscle Link).

DESCRIPTION

Creatine is a non-protein amino acid found in animals and, in much lesser amounts, plants. Creatine is synthesized in the kidney, liver and pancreas from the amino acids L-arginine, glycine and L-methionine. Following its biosynthesis, creatine is transported to the skeletal muscle, heart, brain and other tissues. Most of the creatine is metabolized in these tissues to phosphocreatine (creatine phosphate). Phosphocreatine is a major energy storage form in the body.

Creatine is known chemically as N-(aminoiminomethyl)-N-methyl glycine and its structural formula is:

Supplemental creatine is typically a synthetic substance. It is a solid and is water-soluble.

ACTIONS AND PHARMACOLOGY

ACTIONS

Supplemental creatine may have an energy-generating action during anaerobic exercise and may also have neuroprotective and cardioprotective actions.

MECHANISM OF ACTION

Since the action of supplemental creatine has yet to be clarified, the mechanism of action is a matter of speculation. Much is known, however, about the biochemistry of endogenous creatine. Creatine is mainly synthesized in the kidney, liver and pancreas. In its synthesis, the guanidino group of L-arginine is transferred to glycine to form guanidinoacetate and ornithine by a transamidinase reaction, a reaction that takes place in the pancreas, liver and kidney. Guanidinoacetate is methylated by S-adenosylmethione (SAMe) to form creatine. About 1 to 2 grams of creatine are biosynthesized daily and another 1 to 2 grams are obtained from diet.

In muscle and nerve, most of the creatine is phosphorylated to phosphocreatine (PCr) in a reaction that is catalyzed by the enzyme creatine kinase (CK). There are three isoforms (isoenzymes) of CK. CK-MM is the skeletal muscle isoform; CK-BB, the brain isoform, and CK-MB, the isoform found in cardiac muscle. Most of the PCr in the body is in skeletal muscle.

Creatine, creatine kinase and phosphocreatine make up an intricate cellular energy buffering and transport system connecting sites of energy production in the mitochondria with sites of energy consumption. CK is a key enzyme involved in cellular energy homeostasis. It reversibly catalyzes the transfer of the high-energy phosphate bond in PCr to adenosine diphosphate (ADP) to form adenosine triphosphate (ATP), and it catalyzes the transfer of the high-energy phosphate bond in ATP to creatine to form PCr. During periods of intense exercise and skeletal muscle contraction, bioenergetic metabolism switches from one in which oxidative phosphorylation is the major pathway of ATP production to one in which so-called anaerobic glycolysis becomes dominant. Much less ATP would be generated during this period if it were not for phosphocreatine (PCr) being the only fuel available to regenerate ATP during this period. Thus the availability of PCr is the limiting factor of skeletal-muscle performance during high intensity and brief bursts (about 10 seconds) of activity. Supplemental creatine may increase PCr levels in skeletal muscle and hypothetically enhance ATP turnover during maximal exercise.

Creatine supplementation of transgenic amyotrophic lateral sclerosis (ALS) mice carrying the superoxide dismutase (SOD)1 mutation has reportedly produced improvement in motor performance and extension of survival, as well as protection against loss of both motor neurons and substantia ***** neurons. Mitochondrial dysfunction is among the earliest features found in these mice models of familial ALS. Creatine administration to these mice appears to stabilize mitochondrial CK and inhibits opening of the mitochondrial transition pores.

Creatine, as well as a creatine analogue called cyclocreatine, inhibit growth of a broad range of solid tumors in rat models of cancer; these tumors express high levels of CK. Although the mechanism of tumor inhibition is unknown, there is speculation about what it may be. Creatine feedback inhibits the transamidination step in its biosynthesis. This results in sparing L-arginine, the limiting precursor in creatine synthesis. More available L-arginine can lead to increased levels of nitric oxide (NO), which is a factor in macrophage activation. Another possibility is that glycolysis is inhibited in these tumors. Phosphocreatine inhibits enzymes in the glycolitic pathway, including glyceraldehyde-3-phosphate dehydrogenase, phosphofructokinase and pyruvate kinase.

PHARMACOKINETICS

Creatine is absorbed from the small intestine and enters the portal circulation and is transported to the liver. The ingested creatine, along with creatine made in the liver, is then transported into the systemic circulation and distributed to various tissues of the body, including muscle and nerves, by crossing the cell membrane via a specific creatine-transporter system against a 200:1 gradient. Chronic creatine supplementation in rats down-regulates creatine transporter protein expression. If this is also the case in humans, then chronic creatine supplementation would lead to lower amounts entering cells at any given time.

Within muscle and nerve cells, about 60 to 67% of the creatine entering the cells gets converted to phosphocreatine via the enzyme creatine kinase. About 2% of creatine is converted to creatinine, and both creatine and creatinine are excreted by the kidneys.

INDICATIONS AND USAGE

There is some evidence that supplemental creatine may enhance performance in a limited number of high-intensity, short-term physical activities, but the data are mixed, and no ergogenic effect has been convincingly demonstrated outside of laboratory settings. Adequate safety data are still lacking. There is some very preliminary data that creatine may be helpful in treating muscular dystrophy and amyotrophic lateral scleroses and may improve skeletal muscle function in some with congestive heart failure and gyrate atrophy of the retina. Creatine has inhibited the growth of some solid tumors in rats, but no human cancer data exist.

RESEARCH SUMMARY

Limited muscle function benefit has been noted in some early studies of creatine. All of these studies have been of short duration (mostly lasting one or two weeks and, in no case, more than eight weeks). Many other studies have found no benefit.

A recent review article summarized the results of 71 trials published between 1993 and 1997. Of those that studied effects of supplemental creatine (usually 20 grams daily for 4 to 21 days) on short term, high-intensity performance, 23 reported positive effects and 20 reported no effect. Studies examining the effects of creatine on oxidative energy systems, muscle isokinetic torque and isometric force produced similarly mixed results. Among the few field tests that have been conducted (all related to swim sprints) none detected any effect on athletic performance. Only among studies of cycle ergometer performance was there any superiority of creatine over placebo (11 trials reported improvement, while six others reported no improvement).

Since this review was published there have been a few more positive than negative reports, but, again, the positive effects are almost entirely seen in laboratory settings and are confined to short-term, high-intensity performance.

One author recently reviewed the creatine data and has concluded that supplemental creatine achieves an ergogenic effect, at least in the laboratory, in repeated stationary cycling sprints. But he found no convincing evidence that it does so in single sprints. He also discerned a possible ergogenic effect in weightlifting, but none in running or swimming sprints of any kind. He and others have speculated that the weight gain that typically accompanies creatine supplementation offsets any ergogenic effect that might otherwise benefit runners and swimmers.

Some have claimed that this weight gain, typically 0.5 to 1.6 kilograms occurring in the first few days to first two weeks of creatine supplementation, is evidence of increased muscle mass. Most researchers, however, believe that this weight gain is accounted for by creatine-induced water retention. The longer-term studies needed to confirm or refute claims that chronic creatine supplementation can result in greater muscle mass have not been conducted.

Another caveat offered by several researchers is that almost all of the positive creatine effects so far noted have been achieved in laboratory tests of elite athletes and were observed only in the sort of maximal intermittent exercise that non-athletes can rarely achieve. No benefit for any aerobic activity has been demonstrated.

In addition, safety data are lacking and are urgently needed, especially for long-term use of creatine and for use among the pediatric population (including adolescents) and among those in poor health. There are some reports that long-term use of creatine may be nephrotoxic. This needs further investigation before long-term creatine supplementation can be recommended under any circumstance.

Possible additional uses for creatine have been suggested by preliminary work. There is some evidence of creatine synthesis in the retina, and supplementation with 1.5 grams of creatine daily for a year has been reported to bring improvement in genetic gyrate atrophy--not in the blindness that results from this condition but in the skeletal muscle abnormalities that also characterize it. Giving 5 grams of creatine four times a day for a period of five days has similarly been reported to improve skeletal muscle function in some with congestive heart failure. The effect was small.

In a mouse model of amyotrophic lateral sclerosis (ALS), supplemental creatine significantly prolonged survival. Improvement was seen on motor-performance tests, and there was histologic evidence of neuron protection associated with creatine supplementation. Because creatine protected neurons in the substantia *****, there is speculation that the supplement could also have positive effects in Parkinson's disease.

These researchers have suggested that creatine may exert the favorable results seen in the mouse model through an intracellular energy-buffering effect that may help prevent the sort of mitochondrial dysfunction that they postulate plays a role in neuronal cell death. More research is needed.

Another recent, preliminary report asserts a positive role for supplemental creatine in the treatment of muscular dystrophy and some other neuromuscular disorders. This study tested 10 grams of creatine daily for five days, followed by 5 grams daily for an additional 5 to7 days, against placebo. Increases were noted in handgrip, ankle and knee strength among those taking creatine. Again, more research is needed.

CONTRAINDICATIONS, PRECAUTIONS, ADVERSE REACTIONS

CONTRAINDICATIONS

Creatine is contraindicated in those with renal failure and renal disorders such as nephrotic syndrome.

PRECAUTIONS

Creatine supplements should be avoided by children, adolescents, pregnant women, nursing mothers and anyone at risk for renal disorders such as diabetics. Those taking creatine should have serum creatinine levels monitored.

ADVERSE REACTIONS

The deaths of three American college wrestlers had been linked to the use of creatine supplements. However, results of post mortem tests led to the conclusion that the deaths were caused by severe dehydration and renal failure, and were not due to creatine. Apparently, the wrestlers were trying to lose enough weight through perspiration to allow them to compete in lower-weight classes. Typical adverse effects are gastrointestinal and include nausea, diarrhea and indigestion. Also common are muscle cramping and strains. Weight gain may occur from water retention. During a five day loading period, weight gains of 1.1 to 3.5 pounds have been reported. There are reports of elevated serum creatinine, a metabolite of creatine and a marker of kidney function, in some who take creatine and have normal renal function. This is reversible upon discontinuation of creatine.

Anecdotal reports of adverse events to FDA have included rash, dyspnea, vomiting, diarrhea, nervousness, anxiety, migraine, fatigue, polymyositis, myopathy, seizures and atrial fibrillation.

INTERACTIONS

There are as yet no known drug, nutritional supplement or herb interactions. Caffeine (in coffee, tea and caffeinated beverages) appears to interfere with any beneficial effects of creatine supplementation.

DOSAGE AND ADMINISTRATION

The typical form of creatine available is a creatine monohydrate powder.

The dosing for those who use creatine to attempt to improve performance in brief, high-intensity activities, is a loading dose of 20 grams or 0.3 grams per kilogram in divided doses four times a day for two to five days, followed by a maintenance dose of no more than 2 grams daily or 0.03 grams per kilogram. Those who use creatine supplements should take them with adequate water, six to eight glasses per day.

HOW SUPPLIED

Capsules - 700 mg, 725 mg, 750 mg, 1200 mg

Effervescent Tablets - 5 gm

Effervescent Powder - 27 gm/packet

Powder - 5 gm/tsp

Wafers - 1000 mg

LITERATURE

Feldman EB. Creatine: a dietary supplement and ergogenic aid. Nutr Rev.1999; 57:45-50.

Greenhoff PL. Creatine and its application as an ergogenic aid. Int J Sport Nutr. 1995; 5:S100-S110.

Juhn MS. Oral creatine supplementation. Phys Sports Med. 1999; 27;47-45..

Klivenyi P, Ferrante RJ, Matthews RT, et al. Neuroprotective effects of creatine in a transgenic animal model of amyotrophic lateral sclerosis, Nat Med. 1999; 5:47-350.

Koshy KM, Griswald E, Sneeberger EE. Interstitial nephritis in a patient taking creatine. N Engl J Med. 1999; 340:814-815.

Miller EE, Evans AE, Cohn M. Inhibitions of rate of tumor growth by creatine and cyclocreatine. Proc Natl Accd Sci USA. 1993; 90:3304-3308.

Poortman JR, Augier H, Renaut V, et al. Effect of short-term creatine supplementation on renal responses in men. Eur J Appl Physiol. 1997; 76:566-567.

Sipila I, Rapola J, Simell O, et al. Supplemental creatine as a treatment for gyrate atrophy of the choroid and retina. N Engl J Med. 1981; 304:867-870.

Tarnopolsky M, Martin J. Creatine monohydrate increases strength in patients with neuromuscular disease. Neurology. 1999; 52:854-857.

Toler SM. Creatine is an ergogenic for anaerobic exercise. Nutr Rev. 1997; 55:21-23.

Vandenberghe K, Gillis N. Van Leemputte M, et al. Caffeine counteracts the ergogenic action of muscle creatine loading. J Appl Physiol. 1996; 80:452-457.

Williams MH, Branch JD. Creatine supplementation and exercise performance: an update. J Am Coll Nutr. 1998; 17:216-234.


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## Great White (Apr 4, 2003)

Cool - About time we had an artile on creatine


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## Guest (Mar 4, 2004)

Wow, a serious post from winger...for once


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## winger (Jul 26, 2003)

> Originally posted by Insanity
> 
> *Wow, a serious post from winger...for once *


That would be one more then the Benmeister.


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## Guest (Mar 4, 2004)

Yeah, you could be right....


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## winger (Jul 26, 2003)

> Originally posted by Insanity
> 
> *Yeah, you could be right.... *


You are one funny man.


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## OnePack (Jan 9, 2004)

Another name for it..Creatine Monodydrate.

I've just noticed on my packet it says "pure pharmaceutical grade" does anyone know what this means?


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## Panthro (Jan 12, 2004)

its just technical jargon to make it sound good. It means f-all.


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## Mobster (Apr 1, 2004)

Simply put there are several grades: 80 mesh is granular and doesn't dissolve easily and 200 mesh is almost 'micronised' (like the MetRx version). You also have several sources and the European (Italy and Germany) is regarded as better than Chinese and Korean sourced creatine. At best *pharmaceutical grade* means it has been tested for purity, source and grain size and could be used by Doctors but in practise it means clean and unsullied.

Re the original article - summerize plllleeeasszee. I ain't wading through that. Just add a bold section at the end and highlight the relevent sections in the text.


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## Jock (Apr 8, 2003)

Prolab is the best stuff in my book.


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## demon (Apr 23, 2003)

My dad asked me on Friday if I took creatine.

He said that he'd heard some doctors on a local radio station talking about what creatine does to the heart. They apparently said that it can cause one of the conditions that can bring about sudden death syndrome (of which there have been a few cases here in n. ireland recently).

He wasn't too sure of the details and I was unable to find anything more about it. Anyone hear anything / know anything about this?


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## Lorian (Apr 9, 2003)

demon said:


> My dad asked me on Friday if I took creatine.
> 
> He said that he'd heard some doctors on a local radio station talking about what creatine does to the heart. They apparently said that it can cause one of the conditions that can bring about sudden death syndrome (of which there have been a few cases here in n. ireland recently).
> 
> He wasn't too sure of the details and I was unable to find anything more about it. Anyone hear anything / know anything about this?


Creatine is one of the most widely researched and safest supplements on the planet. I would be extremely sceptical of any 'research' which claims otherwise.

But that's just my opinion



L


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## demon (Apr 23, 2003)

That's what I said to my dad Lorian.

I haven't stopped taking it and I don't plan to, but I will be 'keeping an ear out'.


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## Jock (Apr 8, 2003)

I agree, scientists and doctors have been studying creatine like maniacs, actually trying to find something wrong with it.

No credible evidence has arisen so far.


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## Aftershock (Jan 28, 2004)

Propably more people had adverse reactions taking Aspirin! Internal beading and all that!!!!

Like a mate once said to me "If u believe it all everything is bad for you mate, breathing, sleeping and eating potatoes" made perfect sence to me at the time.....


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## hackskii (Jul 27, 2003)

Bad rap or misinformation on creatine. I was having a beer in a bar with a guy and he was a furniture mover. He said he suffers from lactic acid buildup while working. I suggested he take some creatine. He said that creatine was steroids and it is bad for you.

Here a guys is arguing with me and he is getting hammered on alcohol and talking trash about creatine. I did not go into it too much with him. But I have read alot about creatine and have yet to see some convincing evedence of health associated problems. Maybe not drinking enough water would be the only thing bad about creatine.

I did read an article on older people that had atrophied muscles. They found that they were deficient in creatine in the muscle. Hmmm


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## Lorian (Apr 9, 2003)

Also, Doctors' are now finding that Creatine can be extremely beneficial for treating a whole host of other issues including: Neuromuscular disorders, Myocardial disease, Traumatic brain injury, and even Type 1 Diabetes (it has been shown to reduce circulating blood sugar concentrations).



L


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## OnePack (Jan 9, 2004)

demon said:


> My dad asked me on Friday if I took creatine.
> 
> He said that he'd heard some doctors on a local radio station talking about what creatine does to the heart. They apparently said that it can cause one of the conditions that can bring about sudden death syndrome (of which there have been a few cases here in n. ireland recently).
> 
> He wasn't too sure of the details and I was unable to find anything more about it. Anyone hear anything / know anything about this?


got me worried for a split second then.

which radio station was this on? what was the program name? does ur dad remember?


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## demon (Apr 23, 2003)

It was a programme called Talkback on Radio Ulster.

I don't think it's anything to be too concerned about, but if I do hear anything in the future about it, I'll let you know.


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## Killerkeane (Nov 9, 2003)

which is the best proven brand of creatine on the market?


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## hackskii (Jul 27, 2003)

It is all proven. I like V12 the best as it has other stuff in it but the stuff that is finer in powder i think might be better.

I think there is some cheap Chineese stuff floating around and stear clear of that.


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## Killerkeane (Nov 9, 2003)

okay, ill buy some creatine form h&b then, no going back now


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## OGX (Aug 29, 2004)

I have tried creatine (Dymatize) for a week and a half because i wanted to see my bodys reaction to supps as i've never tried supps before and just got many nasty spots on my face so stopped taking it! Anyone else have or had this prob? I did notice an increase in strength though!


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## winger (Jul 26, 2003)

Were you loading?


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## OGX (Aug 29, 2004)

yeah 5 days then was on the maintance stage for another 5 or 6 days! Does creatine supps contain any toxins?


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## particleastro (Aug 18, 2004)

Just for my 2 pence worth. I bought some Reflex XXL Matrix, which has Creatine and L-Glutamine. Wonders for PWO recovery, and towards the end of the tub (about three weeks), I had some impressive gains. Lost about 50% after it finished, but have regained about 90%. I thought it was great stuff, although I cant afford to be on it all the time. I got dizzy when I first started on it, but drank plenty of water and that settled down.

One last side effect, every night since I started taking it I have been dreaming about sword fighting...


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## chris jenkins (Aug 14, 2004)

I think your ok with creatine, its the best supplement on the market. Dont believe the hype, I have been using it for years now without any problems.


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## megatron (Apr 21, 2004)

Creatine didn't agree with me when I tried it, that is not to say that it is useless. It just didn't work for me, made me ill - but then I have gut issuees anyway.


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## Tuna_boi (Oct 30, 2004)

Creatine, MUST HAVE CREATINE!!ARGHHHHHHHHHHHHHHHHHHH *sounds of shirt stitching tearing and buttons popping off"..


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## Stu (Jan 22, 2005)

Killerkeane said:


> which is the best proven brand of creatine on the market?


 Vpx's CEX is supposed to be awesome, but its expensive

You could try regular CEE but beware the taste


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## Broady (Aug 10, 2007)

In the initial loading phase, I sometimes, due to work etc cannot spread the intake evenly throughout the day. Over a longer period of time i.e. numerous cycles will this severely effect my kidneys??


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## davey d (Jan 8, 2007)

But creatine is a protein made naturally in the body ..


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## DaPs (Apr 4, 2007)

Do you HAVE to do the loading phase, or can you just take it 5g before and after workout normally without the loading?


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## Chris4Pez1436114538 (Sep 3, 2007)

Bump


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## winger (Jul 26, 2003)

Don't do the loading phase.


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## paulo (Feb 17, 2007)

agreed thegastrointestinal upset shiits are due to loading just do maintenance and will work the same


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## bkotey (Mar 29, 2007)

Lorian said:


> Creatine is one of the most widely researched and safest supplements on the planet. I would be extremely sceptical of any 'research' which claims otherwise.
> 
> But that's just my opinion
> 
> ...


Dont get me wrong, I luv creatine but heard alot recently bout neggative effects, I think Mental effects, all just hearsay but anybody else heard out?


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## Bulk1 (Apr 12, 2007)

DaPs said:


> Do you HAVE to do the loading phase, or can you just take it 5g before and after workout normally without the loading?


Creatine ethyl ester doesn't require the larger doses or loading phase of creatine monohydrate. I have some yet to try so will be interesting to see the benifits (or not) of creatine.


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## winger (Jul 26, 2003)

Creatine didn't do anything for me. God I wish it would. I guess I just have to train and eat that much better.


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## hutchings_18 (Jan 10, 2008)

Reflex Tri-Matrix is pretty good, it contains taurine and caffine, which woke me up for my 7am gym sessions before work :lift:

I also took Norateen Heavyweight II and Reflex Instant Whey over the 3 month period and gained just under a stone. I was well happy! Looked good just before hols abroad... but then got a tooth infection while abroad, couldn't open my mouth to eat and ended up losing quite a bit of it hwell:

Did lose quite a bit of extra body fat though.


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## winger (Jul 26, 2003)

hutchings_18 said:


> . but then got a tooth infection while abroad, couldn't open my mouth to eat and ended up losing quite a bit of it hwell:
> 
> Did lose quite a bit of extra body fat though.


Sorry to hear about the tooth infection mate!

But on the flip side, nice to hear you lost some bf!


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## Greg_dds (Dec 23, 2007)

what is the best creatine to buy on the market then?ie- what brand?thanks guys. i used to do al lot of maximuscle stuff then hit the cheap stuff from holland and barrat, but want to know the absoulte best creatine as im goining into the army in september, i know its a few months awya but i was get to my peak.


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## smithy26 (Sep 8, 2006)

any 1 tryed the syrum, the one u take as droplets under the tonge. if wots was ure gains if any


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## Robbie (Dec 31, 2007)

smithy26 said:


> any 1 tryed the syrum, the one u take as droplets under the tonge. if wots was ure gains if any


Generally considered to be one of THE biggest wastes of cash.

I have a bottle kicking about somewhere...


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## davey d (Jan 8, 2007)

That norateen heavy weight is ****e.....the creatine gives you good enough gains ....


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## Chris4Pez1436114538 (Sep 3, 2007)

> what is the best creatine to buy on the market then?ie- what brand?thanks guys. i used to do al lot of maximuscle stuff then hit the cheap stuff from holland and barrat, but want to know the absoulte best creatine as im goining into the army in september, i know its a few months awya but i was get to my peak


TBH the holland and barret stuff is not that bad even though ppl say it is, it has sugar to spike insulin which is needed "supposedly" after a workout!!!!!

I personally wouldn't use creatine til after a workout no matter which one you choose to use and then have 5-10g!

And like already said dont bother doing the loading phase that is what supplement companies suggest so they can sell more and remember someone who eats a good diet with meat shouldn't need that much creatine supplement anyways!

Just my personal opinion!!!!!!


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## winger (Jul 26, 2003)

Chris4Pez said:


> TBH the holland and barret stuff is not that bad even though ppl say it is, it has sugar to spike insulin which is needed "supposedly" after a workout!!!!!
> 
> I personally wouldn't use creatine til after a workout no matter which one you choose to use and then have 5-10g!
> 
> ...


Well I could not agree more. Me personally, I notice nothing from creatine, but then again, I am a carnivore.


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## Craig N (Jun 25, 2008)

Cnp pro E2 creatine Is easily the best. By bonding an ester to creatine, it gives a lipophilic (fat penetrating) property. This has increased its bio availability over any other form of creatine by a staggering 3900%! This means that any fluid retained will be in muscle cells, not under the skin which enables you to use it up until the day of a competition. Dosages need only be a small percentage of conventional dosing protocols and there is no need to load . There's also no need to add simple sugars to create an "insulin spike", thus none of the potential gains in bodyfat associated with this approach. Best of all, there are none of the unpleasant side effects or damage to performance that can be experienced with existing forms of creatine. Now, all that can be gained from creatine supplementation I think is benefit.


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## dudz (Oct 27, 2008)

Good Read


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