Glucophage (Metformin HCL)
SHORT GLUCOPHAGE DESCRIPTION:
Glucophage is generally used in the management of mature onset (Type-II) diabetes. The drug will make its way to circulation slowly, over a period of about six hours. The general intake schedule among bodybuilders is to take 850 mg (one tablet) twice per day. The user will be sure to additionally supplement with a carbohydrate replacement (such as Ultra Fuel) and with creatine monohydrate, particularly after periods of training.
LONG GLUCOPHAGE DESCRIPTION:
Glucophage is a trade name for the oral anti-hyperglycemic agent metformin HCL. This type of drug is generally used in the management of mature onset (Type-II) diabetes. It is utilized when dietary management and exercise alone have not been able to control the disease, yet injectable insulin is not appropriate since this hormone is still present in the body. While the main activity of metformin HCL is the increased utilization of glucose, it does not directly mimic the action of insulin. The precise mode of action is actually unknown, but it is believed to increase insulin sensitivity through some peripheral process. Use of this agent will certainly lower the patient’s blood sugar, but its activity makes it unlikely to cause a state of hypoglycemia if the dosage is accidentally misjudged (a major concern with injectable insulin).
The concept of harnessing insulin for performance enhancement has been catching on in recent years. As you may know, insulin is considered a “storage hormone”. It transports amino acids, fatty acids and carbohydrates (glucose) into various cells of your body. This process includes the storage of protein in skeletal muscle cells, equating to a possible anabolic effect. But insulin is a little tricky because it can also direct storage to fat cells, obviously an unwanted result. It is however possible to “guide” insulin in the right direction. Athletes have found that during periods of intense weight training, and a diet without excess caloric intake, insulin can show a much greater affinity for protein and carbohydrate storage in muscle cells. By manipulating insulin levels (or insulin sensitivity) under these conditions, we can see notable growth. Implemented correctly, the result should be a fuller, more defined look to the muscles. Injectable insulin can be extremely risky however, an incorrect dosage or insufficient carbohydrate intake having grave consequences to the user’s health. In extreme cases, hypoglycemia (low blood sugar) can lead to coma or even death. Since this effect is rare with Glucophage, it is considered by many athletes to be an introduction to insulin manipulation.
When administered, the absorption rate of metformin HCL is very slow. The drug will make its way to circulation slowly, over a period of about six hours. The general intake schedule among bodybuilders is to take 850 mg (one tablet) twice per day. The user will be sure to additionally supplement with a carbohydrate replacement (such as Ultra Fuel) and with creatine monohydrate, particularly after periods of training. The result of this treatment will probably not be as dramatic as when using insulin, but a notable anabolic effect can be achieved nonetheless. Most athletes opt to use this drug for a limited duration, cycles of Glucophage usually lasting only a couple of months. This would be followed by an equally long break (at a minimum).
While Glucophage is considered much safer than insulin, it is not without its own unique risks. The most serious complication is the possible development of lactic acidosis. This is an often-fatal metabolic disorder involving (among other factors) an increase in lactate levels (lactic) and a pronounced decrease in blood pH (acidosis). The package insert displays the additional warning: the administration of oral hypoglycemics may be associated with increased cardiovascular mortality as compared to treatment with diet alone or diet with insulin. The risk for severe side effects are increased in people suffering from liver dysfunction or who drink excessive alcohol. Or those with renal dysfunction, noting impaired creatine clearance (a serum concentration above 1,2 mg per 100 ml is considered the cut-off point for treatment). A number of other “minor” side effects may include, but are not limited to, anorexia, nausea, vomiting, diarrhea, metallic taste, fatigue, weakness and malabsorbtion of vitamin B12. Quite often these effects will subside if the dosage is lowered, stubborn cases requiring the drug to be discontinued. If vomiting occurs, the athlete will usually discontinue the drug immediately for fear this may be an early symptom of lacticacidosis.
Glucophage belongs to the same family of antidiabetic agents (biguanide derivatives) as Debeone (Phenformin HCL). Debeone was removed from the U.S. market (and others) in the late 70’s, exhibiting a high tendency for lacticacidosis. While this compound is still available in Mexico, it is really too risky to justify using for performance enhancement. Since Glucophage has a much more reliable safety record, it is the preferred agent of the two (and usually never substituted). The reports on this drug have actually been mixed, with many bodybuilders being very disappointed with the results. Those looking for a more pronounced effect than this drug can provide will generally. avoid stronger oral agents, and instead advance to injectable insulin. Others might first wish to give Rezulin a try, which is another recently developed oral agent. This drug appears to have a more intense effect (through a different mechanism) than Glucophage, but does present a number of unique risks to the user as well.