epalrestat

Action and Spectrum

Actions and Spectrum 

epalrestat works by inhibiting aldose reductase, an enzyme that converts glucose to sorbitol in nerve cells. In diabetic neuropathy, the accumulation of sorbitol can cause osmotic stress and damage to nerve cells.  

It reduces the accumulation of sorbitol and helps alleviate nerve damage and associated symptoms.  

Drug Interaction

Adverse Reaction

Frequency not defined  

Nausea 

Vomiting 

Abnormal liver function 

Numbness or tingling 

Diarrhea 

Gastrointestinal discomfort 

Black Box Warning

Black Box Warning 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• epalrestat should not be used in individuals with known hypersensitivity or allergic reaction to its components. 

Caution: 

• Patients with significant liver impairment should use with caution. 

Pregnancy / Lactation

Pregnancy consideration: 

Pregnancy category: N/A 

Lactation: Excretion into human milk is unknown  

Pregnancy Categories:         

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.  

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women. 

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 

Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology  

epalrestat is an aldose reductase inhibitor. In diabetic neuropathy, excess glucose can lead to the accumulation of sorbitol in nerve cells, causing osmotic stress and damage.  

epalrestat reduces the conversion of glucose to sorbitol, thereby preventing or slowing down the buildup of sorbitol in nerve cells. 

Pharmacodynamics 

epalrestat disrupts the polyol pathway, a biochemical process that is implicated in the development of diabetic neuropathy. This pathway converts glucose to sorbitol and then to fructose.  

Pharmacokinetics 

Absorption   

epalrestat is well-absorbed from the gastrointestinal tract. 

Distribution 

epalrestat is distributed throughout the body. 

Metabolism 

epalrestat undergoes hepatic metabolism in the liver. 

Elimination and excretion 

epalrestat is eliminated from the body through the urine. 

Adminstartion

Administration 

epalrestat is taken orally in the form of tablets.

Patient Information Leaflet

Patient information leaflet 

Generic Name: epalrestat 

Why do we use epalrestat? 

epalrestat is indicated for the treatment of diabetic neuropathy.   

It is used to improve the quality of life for individuals with this condition by reducing the symptoms and complications associated with nerve damage caused by diabetes.