What are Alpha-glucosidase Inhibitors?

Alpha-glucosidase Inhibitors are the oral anti-diabetic drugs generally used for diabetes mellitus type-2 that prevent the digestion of carbohydrates. The alpha-glucosidase normally covers carbohydrates into simple sugar and the alpha-glucosidase Inhibitors slow down this step.

What are the common examples of alpha-glucosidase Inhibitors?

The alpha-glucosidase Inhibitors include:-

  • Acarbose –Precose or Glucobay 
  • Migitol – Glyset
  • Voglibose 

The alpha glucose IDs inhibitors show a specific advantage of reducing postprandial glycemia. the dosages of these alpha-glucosidase inhibitors vary such as the dosage of acarbose and miglitol is 25 to 50 milligram whereas that of voglibose is 0.2 -0.3 milligram.

What are the functions of alpha glucoside ace inhibitors?

Alpha glucoside ace inhibitors work by preventing the digestion of carbohydrates such as starch, table sugar, etc.

  • These inhibitors start inhibiting the enzyme alpha glucoside ace in intestinal brush border.
  • The inhibitors prevent absorption and delays the digestion of carbohydrates.
  • It results in to reduced PPBG  excursions.
  • It is very modest in efficacy and it usually takes 6 to 8 weeks.

What are the effects of alpha glucoside ace inhibitors?

The effects include:- 

  • Results in flatulence or abdominal discomfort.
  • Have no effects on lipid or blood pressure.
  • No effect on weight gain or loss.
  • It is contradictory to IBD or cirrhosis.

What are the contraindications of alpha-glucosidase Inhibitors?

The contradictions of alpha-glucosidase Inhibitors include:- 

  • Inflammatory bowel diseases.
  • Gastrointestinal conditions are worsened by gas or distention.
  • In renal diseases.

What is the role of alpha-glucosidase inhibitors in chronic kidney disorder?

  • Several drugs with numerous different mechanisms of action and different pharmacologic profiles are being used with an objective to improve glycemic control in patients diagnosed with type 2 Diabetes.

But the therapeutic advantages for patients with type 2 diabetes and chronic kidney disease (CKD) are actually limited because of the reduced glomerular filtration rate that results In the accumulation of certain drugs or their certain metabolites. 

We also know that diabetes mellitus is a leading cause of chronic kidney disorder and a major cause of morbidity and mortality worldwide.

  • The noted drugs such as sulfonylurea ,a conventional oral hypoglycemic agents are not suitable due to the risks of prolonged hypoglycaemia where as an another drug metformin is also contradicted to patients with moderate to advanced stages of CKD.
  • In order to achieve optimum glycemic control insulin injection therapy always remain the mainstay of treatment in CKD patients with diabetes , particularly to those who are receiving a dialysis therapy. 
  • Some other agents are also used in patients with CKD ,Repaglinide and mitiglinide are some rapid and short acting insulinotropic SU receptor ligands . Sulfonylurea are the old drugs ,widely used. These eases the secretion of insulin and  increases the risk of hypoglycaemia that creates a major issue for CKD patients. But these are some attractive options for the dialysis patients.
  • The alpha glucosidase inhibitors are less accompanied by hypoglycemia and are usually administered without dose adjustments in dialysis patients. The National Kidney Foundation Kidney disease outcomes quality initiative guidelines however, recommends that the alpha glucosidase inhibitors should be generally avoided in patients with advanced stages of CKD or on dialysis. CKD in patients influences glycemic control that makes management of patients quite challenging. 
  • Also, the loss of renal function impairs renal gluconeogenesis where as insulin resistance are worsened by elevated counter regulatory hormones ,altered lipid metabolism, uremic acidosis and the accumulation of uremic toxins. 

Therefore, the effect of renal insufficiency on pharmacokinetics and pharmacodynamics of glucose-lowering drugs is a timely issue, since a reduced GFR may produce some dangerous accumulation of these drugs or the active metabolites, with increased side effects. The selective inhibition of the alpha-glucosidase enzyme consequently reduces postprandial glucose variations without affecting insulin secretion or without increasing the risks of hypoglycemia. 

One of the major alpha-glucosidase inhibitors is Acarbose. 

Acarbose is a complex oligosaccharide having a molecular weight of 645.6 Dalton. Acarbose shows a reversible inhibition of pancreatic enzyme alpha-amylase that metabolize complex starch to oligosaccharides in the lumen of the small intestine. It is orally administered at a dose of 75 to 300 mg/day, before each meal.  Acarbose is almost excreted by the kidneys. Less than 2% of starting dose is recovered in urine as an active drug. In CKD patients, the plasma levels of acarbose and its metabolites are increased by several folds. 

Conclusion

The dosages of drugs in diabetic -CKD patients is a challenging problem. However, a panel of glucose-lowering agents is for the improvement of glycemic control.  One must keep in mind that CKD can potentially trigger the pharmacokinetics of different therapeutic agents through different mechanisms. 

The proper assessment of renal functions in fragile genres is a prerequisite for selecting the best provided therapeutic options. Also, the renal functions should be carefully examined during the treatment to detect certain changes that may affect drug metabolism and its excretion. However, in CKD, the drugs undergoing hepatic metabolism or non-renal excretion should be preferred. 

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