Rezulin (Troglitazone)

ALTERNATIVE STEROID NAMES: Rezulin, Resulin, Romozin
Usual dosages: 100 – 200 mg per day


Rezulin is a very interesting new oral antihyperglycemic medication, approved for U.S. sale in 1997. Specifically we are speaking of the active compound troglitazone, which is classified as a thiazolidinedione antidiabetic agent. This drug was designed for use on patients with Type-II (noninsulin-dependent diabetes mellitus (NIDDM) also known as adult-onset diabetes). Rezulin is useful in this situation because it acts by increasing the body’s sensitivity to insulin, therefore requiring some amount of endogenous insulin to be present in order to have an effect (Type-I diabetics produce no appreciable amount of insulin). The action of this drug is quite advanced from the oral agents we are familiar with like Glucophage (metformin HCL). Rezulin works by increasing the number of active insulin receptor sites, allowing the hormone to have a more pronounced effect. This enables Rezulin to be a much more potent compound, and therefore more useful than Glucophage (which acts via a less direct mechanism). The one worry is that a state of hypoglycemia (low blood sugar) may be easier to produce with Rezulin. Since insulin is needed for the drug to work however, this problem is usually only seen when injectable insulin is used at the same time. Glucophage is perhaps less dangerous if the dosage is misjudged, although most feel it is still a much cruder product and less worth consideration at this time.

In the short time this drug has been available, safety concerns have generated it quite a bit of attention as well. This began in the end of 1997, about the time that Glaxo-Wellcome voluntarily halted production of the Romozin brand (UK) due to the death of five patients receiving treatment. These deaths were due to serious liver complications, brought about by a somewhat toxic nature of this substance. Soon after investigating, Parke-Davis decided not to discontinue their U.S. product, believing the benefits of Rezulin to greatly outweigh any risks. And the risks were certainly made clear in our country as well. By November of 1997 35 people taking it had developed serious liver complications, resulting in two deaths. Parke-Davis promptly issued a warning to medical professionals, urging them to monitor their patients’ liver enzymes during the first year of therapy. Subsequent to the warning, an additional 150 cases of liver difficulty were reported. The manufacturer quickly pointed out that statistically such occurrences we consistent with those found acceptable in clinical trials, noting that only about 2 percent of patients will show elevated liver enzymes and fewer will develop an actual problem. There have also been some lawsuits against Pfizer owned Warner-Lambert company, which followed published Mayo Clinic reports of heart failure and that drug causes fluid buildup in some patients (dangerous for livers). FDA has recalled Rezulin on March 21, 2000.

The use of insulin and insulin enhancing medications for athletic purposes has been increasingly popular in recent years. This is due to the fact that the main action of insulin is to transport carbohydrates (glucose), fatty acids and amino acids into various body cells. This is how blood sugar is lowered, as insulin deposits glucose into the target cells, removing this nutrient from circulation. The negative to this hormone is that fat cells are possible targets for this effect, potentially increasing the athlete’s body fat percentage. But insulin will also store carbohydrates and protein into the body’s muscle tissue cells. During intense periods of weight training (and a diet without excess fat and calories) it has been shown that insulin can display a much greater tendency for storage in muscle cells than fat cells. The result could be a notable anabolic effect, producing a fuller and harder look to the physique. Since injectable insulin carries with it a number of considerable risks, many athletes first choose to experiment with oral diabetes medications.

But Glucophage has received very mixed reviews. Many athletes claimed to have received little or no benefit when taking this drug. Others have reported an anabolic effect, but usually only when higher dosages or longer cycles were utilized. Since Rezulin appears to be much more active in the body than Glucophage, it may prove to be a more potent anabolic for athletes. But this drug is not without its own unique risks. For starters, one cannot ignore the risks for liver damage with this drug. This is especially true with athletes, as most of the individuals who would use Rezulin are probably regular steroid users. Since most would of course be periodically taking c17-alpha alkylated (liver toxic) orals, this risk for liver damage may be amplified with such a combination. The fact that much shorter periods of intake are going to be used by athletes may not provide the most comfort, being that the medical cases in question involved both long and short-term treatment with this compound. Nausea, vomiting, abdominal pain, fatigue, anorexia, jaundice and dark urine are all symptoms that liver trouble may be developing. at which point the drug should be quickly discontinued. Also common with Rezulin is an increase of total, HDL and LDL cholesterol values. Since these values typically rise evenly, leaving the actual HDL/LDL ratio generally unchanged, trouble with cardiac functioning does not commonly result from this effect.

Since Rezulin is so new, it will probably take some time before a standard intake regimen becomes popular. It would seem like the best advice to begin taking the drug with a low dosage, perhaps 100-200 mg. Being that this drug has a very long half life, it is taken only once per day. Food also increases the absorption of Rezulin, so it is always taken with a meal so that the optimal blood level is achieved. The athlete will presumably take the dose one to two hours before a training session, as the drug will take two to three hours to achieve its peak blood level. Afterwards (and throughout the day) a carbohydrate replacement drink like Ultra Fuel may be indispensable when managing the blood sugar level. Creatine monohydrate is also a common adjunct to insulin manipulation therapies, as the hormone will enhance the storing effect of the creatine supplementation by helping to shuttle it into muscle cells. Also, the user will probably have no need to exceed the standard medical dosage of 400 mg-600 mg. Perhaps he/she may even find it most comfortable to stay below this point, as the healthy athlete will not be suffering the same insulin related dysfunction’s as the target patient.

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