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Monday, November 22, 2004
Dumaguing: Diamicron stops blood sugar on the run
By Dr. Vic Dumaguing
ONE hundred fifty million diabetics in 2000 and probably more than 300 million diabetics in the year 2025. These are the staggering figures released by the International Diabetics Federation to emphasize the rise of diabetes in epidemic proportions. Indeed, the implications are enormous, considering the personal suffering and cost to health care systems which are increasingly faced with both the serious macrovascular and microvascular complications of diabetes.
In the general population, the prevalence of coronary artery disease is about 4 percent but there may be a fourfold increase in adult diabetic patients, compared with non-diabetic individuals of the same age. The risk of heart failure has been shown to increase two-fold for diabetic men and five-fold for diabetic women. Thirty percent of patients with myocardial infarction suffer from clinically diagnosed type 2 diabetes. Since type 2 DM accounts for 90 percent of all diabetes cases and 80 percent of deaths in type 2 DM are cardiovascular related, it is not surprising that cardiovascular disease has replaced kidney disease as the leading cause of death among diabetic patients.
Clinical Type 2 DM arises when pancreatic beta cells fails to compensate for decreased sensitivity of receptors to insulin. It is widely believed that beta cell-failure is genetically determined. Now in patients with adequate beta cell function in whom dietary and lifestyle modification have proved to be insufficient, sulfonylurea have been recommended as first-line therapy and successfully used in the treatment of type 2 DM for almost 40 years.
Apparently, not all sulfonylureas are the same. Diamicron MR is a new once-daily formulation of the sulfonylurea gliclazide. It has a hydrophilic matrix of a hypromellose-based polymer that expands to form a gel when it comes in contact with gastrointestinal fluid, which progressively release gliclazide. It has an impressive bioavailability of 97%. Moreover, the release of gliclazide over a 24-hour period parallels the typical circadian glycemic profile of type 2 DM patients. In one study, after 10 weeks on Diamicron MR, fasting and postprandial (after meals), blood sugar values were significantly reduced.
Diamicron MR treatment also increase sensitivity of the receptors in target organs, particularly skeletal muscles cells, to insulin. It was also shown that Diamicron is able to suppress the excessive production of glucose by the liver in type 2 DM patients. Research endeavors along this line show that this suppression is independent of the drug on pancreatic hormones like insulin, thus it is postulated that Diamicron exerts a direct effect on liver glucose metabolism. It is now an established fact that the effect of oxidative stress on pancreatic beta-cell contributes to the progressive deterioration of beta cell function. Kimoto et. al showed in this context that Diamicron can protect beta-cells from the toxic effects of reactive oxygen species in diabetes.
Another cutting-edge advantage of Diamicron MR over the other sulfonylureas is its selective binding to sulfonylurea receptors, (the so-called ATP sensitive potassium channels) in the beta-cells of the pancreas and not affecting the other sulfonylurea receptors that could lead to cardiovascular abnormalities. Furthermore, the binding of Diamicron MR to the sulfonylurea receptor is very rapidly reversible and these properties explain the very low incidence of the much-dreaded side effect of anti-diabetes treatment - hypoglycemia or a sudden fall in blood sugar.
Aside from neuropathy, nephropathy complications of uncontrolled diabetes, retinopathy that could lead to blindness is a very serious concern among patients. The Japanese Diabetic Retinopathy Program studied the effects of Diamicron, other sulfonylureas and placebo on the progression of retinopathy in diabetic patients. After five year, the incidence of retinopathy was significantly lower in patients taking Diamicron.
The tolerability and safety of Diamicron MR was assessed in a 12-month, randomized double-blind study which showed that only few adverse events were reported, the most common of which is arthralgia or joint pain, followed by arthritis, back pain and bronchitis, which were mild to moderate. It is of particular interest that, in contrast to the enormous body weight-gain in long-term treatment with sulfonylureas, the body weight of Diamicron users remained stable. Lipid profile was also good with slight reduction in total cholesterol and low-density lipoproteins (bad cholesterol).
So, if your blood sugar is like a wayward train, on a wild run, don't despair, there is Daimicron MR.
(November 22, 2004 issue)
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