Epalrestat is a carboxylic acid derivative and a noncompetitive and reversible aldose reductase inhibitor used for the treatment of diabetic neuropathy, which is one of the most common long-term complications in patients with diabetes mellitus. The structure of epalrestat is showed in Figure 1.
Diabetic neuropathy is nerve damage that is caused by diabetes. Over time, high blood glucose levels, also called
blood sugar, and high levels of fats, such as triglycerides, in the blood from diabetes can damage your nerves.
Symptoms depend on which type of diabetic neuropathy you have.
Four main types of neuropathy can impact on the nervous system including:
The types of is showed in figure 2.
Diabetic neuropathy is one of the most common long-term complications in patients with diabetes mellitus, with a prevalence of 60-70% in the United States. Treatment options include antidepressants, anticonvulsants, tramadol, and capsaicin. These agents are modestly effective for symptomatic relief, but they do not affect the underlying pathology nor do they slow progression of the disease.
Epalrestat is an aldose reductase inhibitor that is approved for the improvement of subjective neuropathy symptoms, abnormality of vibration sense, and abnormal changes in heartbeat associated with diabetic peripheral neuropathy.
The sorbitol (polyol) metabolic pathway, an alternative glucose reduction pathway involving the enzymes aldose reductase and sorbitol dehydrogenase, is thought to be activated by hyperglycaemic conditions. Intracellular accumulation of sorbitol during hyperglycaemia is considered to be at least partially responsible for the pathogenesis of late-onset complications of diabetes mellitus.
Epalrestat, an uncompetitive aldose reductase inhibitor, significantly reduces intracellular sorbitol accumulation in sciatic nerve, erythrocytes and ocular tissues from animal models, and in erythrocytes in humans, with diabetes mellitus, without affecting glucose levels. Epalrestat also increased sodium-dependent myoinositol uptake into sciatic nerve tissue in rats and skin fibroblasts from patients with diabetes, and attenuated nerve conduction velocity and retinal changes commonly seen in patients with diabetic neuropathy and retinopathy, respectively.
Epalrestat has been available in Japan for the treatment of diabetic neuropathy since 1992. Up to now, there are lots of related products used in the treatment of diabetic neuropathy. Here we list several epalrestat medications companies.
|Brand||Country of Origin||Company|
|Alrista||India||Macleods Pharmaceuticals Pvt Ltd|
|Epalrest-50||India||Johnlee Pharmaceuticals Pvt. Ltd|
|Eparel||India||Micro Labs Ltd.|
|Aldorin||Bangladesh||Eskayef Bangladesh Ltd|
|Tanglin||China||Yangtze River Pharmaceutical Group|
|Epalrestat 50||Japan||Sawai Pharmaceutical|
|Takata||Japan||Sanwa kagaku Co., Ltd.|
Table 1. Epalrestat tablets company list
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