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Diabetes Medications 101: Oral Perspectives

Diabetes is rapidly becoming an epidemic worldwide because of the change in diet and lifestyle. And the Philippines is not spared. The number of diabetics and patients with diabetes-related complications has increased despite measures and advocacies to modify lifestyle.

The mainstays of treatment are lifestyle and behavioral modification thru regular exercise and proper diet. However, if these measures fail, the oral anti-diabetes drugs should be initiated.

Oral anti-diabetes drugs are commonly prescribed to patients diagnosed to have type 2 diabetes with mellitus (T2DM). These pills lower blood sugar levels in diabetes patients who are still able to produce insulin. Anti-diabetes medications were not designed to cure diabetes, but were designed to control sugar levels near normal to prevent diabetes-related complications.

In the treatment of diabetes, we should be aware how diabetes appears in an apparently healthy patient (knowing the pathophysiology of diabetes), thereby addressing the basic defect causing the problem of high blood sugar.

One basic problem that leads to uncontrolled sugar (glucose) in the blood stream is impaired insulin secretion by the pancreatic beta-cells. At the time of diagnosis, T2DM patients develop the so-called “beta-cell failure” where at least 50-60 percent of the pancreas is not able to make enough insulin to move glucose inside the cell where it should be. Secondly, insulin does not work as it should, or the cells (muscle and fat) don’t take glucose as they should in patients with T2DM (insulin resistance).

There are currently six available classes and examples of oral anti-diabetes medications in the Philippines, namely:

  • Biguanides (Metformin)
  • Thiazolidinediones (Pioglitazone)
  • Sulfonylureas (Gliclazide, Glibenclamide, Glimepiride, Glipizide)
  • Meglitinides (Nateglinide, Repaglinide)
  • Alpha-glucosidase inhibitors (Acarbose, Voglibose)
  • DDP-4 inhibitors (Sitagliptin, Vildagliptin, Saxagliptin)

BIGUANIDES

  • Function:
    • Decrease the amount of sugar (glucose) produced by the liver and help the body use insulin better
    • Improve insulin’s ability to move sugars into the cells
    • Prevent the liver from releasing stored sugars
  • Benefits:
    • Do not cause hypoglycemia and weight gain while controlling blood sugarssome studies show a decrease in triglycerides (16%), LDL-cholesterol (8%), total cholesterol (5%), and increase in HDL-cholesterol (2%)
  • Side effects:
    • Upset stomach (nausea, vomiting, diarrhea, metallic taste, sickness with alcohol, tiredness, or dizziness)

THIAZOLIDINEDIONES

  • Function:
    • Help the body use insulin more efficiently and help decrease the amount of glucose produced by the liver
    • Increase insulin sensitivity
  • Benefits:
    • Useful in patients with renal dysfunction or in cases where metformin is contraindicated
    • Generally well-tolerated
  • Side effects:
    • Rare, but may include elevated liver enzymes, weight gain, headache, fluid retention, anemia, bone fracture in females

SULFONYLUREAS

  • Function:
    • Lower blood sugar by stimulating the pancreatic beta-cells to release more insulin
  • Side effects:
    • Hypoglycemia (low sugar), upset stomach (5%), skin rash, itching, weight gain, liver changes (rare)

MEGLITINIDES

  • Function:
    • Like sulfonylureas, meglitinides stimulate the pancreas to secrete more insulin but act more quickly (they are short-acting agents) – Effects depend on the carbohydrate load taken during the meal
  • Side effects:
    • hypoglycemia, upset stomach, weight gain

a-GLUCOSIDASE INHIBITORS

  • Function:
    • Lower blood sugar after a meal
    • Delay absorption/digestion of complex carbohydrates to absorbable monosacharides at the gut level thru the inhibition of the a-glucosidase enzyme
    • Do not have an effect on insulin resistance
  • Benefits:
    • Do not cause hypoglycemia Side effects: stomach upset (bloating, flatulence, diarrhea, nausea, cramps)

DPP-4 INHIBITORS

  • Function:
    • Work to lower blood sugar by increasing insulin secretion when sugars are high, signal the liver to stop producing sugar when there is an excess of sugar in the blood
  • Benefits:
    • Lower potential for hypoglycemia Side effects: Upper respiratory tract infection, sore throat, headache, nausea

There is NO best pill for the treatment of diabetes. Management of diabetes should be individualized based on the patient’s diet, activity and culture (e.g., muslim). But as educators, we should reiterate that the 3 factors important in good sugar control are lifestyle change thru regular exercise, proper diet and regular intake of anti-diabetes medications. Without one of these, it will be difficult to achieve near-normal sugar levels.

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