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Oral Diabetes Medications

Oral diabetes medicines help control blood glucose levels in people whose bodies still produce some insulin, such as some people with type 2 diabetes. These medicines are prescribed along with specific dietary changes and regular exercise. Many oral diabetes medications may be used in combination to achieve optimal blood glucose control. This guide provides general information about the different oral medicines for diabetes. It will help you learn more about your medication. Always take your medicine exactly as prescribed by your doctor. Discuss your specific questions and concerns with your health care provider. The following are various categories of oral medicines.

Second generation sulfonylurea (Glucotrol®, Amaryl®, and DiaBeta®)

These medications lower blood glucose by stimulating Beta cells in the pancreas to release more insulin

Biguanide (Glucophage®)

This medication works primarily by decreasing the amount of glucose produced by the liver. It also improves insulin’s actions in the body and slows the conversion of carbohydrates into sugar.

Sulfonylurea and biguanide combination (Glucovance®, Metaglip®)

This combination stimulates the pancreas to release more insulin, improves insulin's action in the body and lowers the amount of glucose produced by the liver.

Thiazolidinedione (Actos®, Avandia®)

This medication improves insulin sensitivity in the body, which increases the uptake of glucose into muscle, fat, and liver tissue.

Thiazolidinedione and biguanide combination (Avandamet®, Actoplusmet®)

This combination improves insulin sensitivity at receptors in fat, muscle, liver, and peripheral tissues and lowers the amount of glucose produced by the liver and absorbed by the intestines.

Alpha-glucosidase inhibitor (Precose®, Glyset®)

This medication lowers blood glucose by delaying the breakdown of carbohydrates, thereby reducing glucose absorption in the small intestine. This medication blocks certain enzymes to slow down the digestion of some starches.

Meglitinide, Repaglinide (Prandin®),Nateglinide (Starlix®) —Not chemically a meglitinide, but has similar characteristics

These medications lower blood glucose by stimulating the pancreas to release more insulin. However, it is necessary to take this medication before meals, otherwise the insulin that is released is blocked and will not lower blood glucose.

DPP-4 inhibitors (Januvia®)

For Type 2 diabetes, affects the incretin system, which helps to control blood sugar by affecting alpha and beta cells. Works only when the blood sugar is elevated.

Second Generation Sulfonylurea

Medication Name Tablet Form Recommended Dosage Range
Glipizide (Glucotrol®, Glucotrol XL®) 5 mg, 10 mg
2.5 mg, 5 mg, 10 mg
5-20 mg (once a day)
2.5-20 mg (once a day)
Glyburide (DiaBeta®, Micronase®)
Micronized glyburide (Glynase PresTab®)
1.25 mg, 2.5 mg, 5 mg
1.5 mg, 3 mg, 6 mg
1.25 mg-20 mg
0.75-12 mg
Glimepiride (Amaryl®) 1 mg, 2 mg, 4 mg 1-8 mg (once a day)
How it works:
  • Stimulates beta cells in the pancreas to release more insulin
Side effects:
  • Hypoglycemia
  • Stomach upset
  • Skin rash or itching
  • Weight gain
Comments/special instructions:
  • Take ½ hour to 1 hour before meals.

Glimepiride is taken with the first meal of the day.

Biguanide

Medication Name Tablet form Recommended dosage range
Metformin, (Glucophage®), (Glucophage® XR) 500 mg, 850 mg, 1,000 mg
500 mg, 750 mg
500-2,550 mg
500-2,000 mg
How it works:
  • Improves insulin sensitivity in the peripheral tissues
  • Lowers the amount of glucose produced by the liver and absorbed by the intestines
Side effects:
  • Stomach upset (nausea, diarrhea). This can be minimized by starting at a low dose and increasing the dosage slowly.
  • Metallic taste in mouth
  • Decreased serum B12 level
Comments/special instructions:
  • This does not cause hypoglycemia when prescribed as the only diabetes medication.
  • This medicine usually does not cause weight gain.
  • This medication should be temporarily stopped before hospitalization, surgery, or when getting certain X-ray tests using contrast material (dye).

Regular tests are needed to detect liver and/or kidney problems, which contraindicates the use of this medicine.

Sulfonylurea and Biguanide

Medication name Tablet form Recommended dosage range
Glyburide and metformin (Glucovance®) (Glyburide/metformin)
1.25 mg/250 mg
2.5 mg/500 mg
5 mg/500 mg
1.25 mg—250 mg
20 mg—2,000 mg
Glipizide and metformin (Metaglip®) (Glyburide/metformin)
2.5 mg/250 mg
2.5 mg/500 mg
5 mg/500 mg
2.5 mg—250 mg
20 mg—2,000 mg
How it works:
  • Stimulates the pancreas to release more insulin
  • Improves insulin sensitivity in the peripheral tissues
  • Lowers the amount of glucose produced by the liver
Side effects:
  • Stomach upset (nausea, diarrhea)
  • Metallic taste in mouth
  • Hypoglycemia
  • Skin rash or itching
  • Weight gain
Comments/special instructions:
  • This medication usually does not cause weight gain.
  • This medication should be temporarily stopped before hospitalization, surgery, or X-ray tests using contrast material (dye).

Regular tests are needed to detect liver and/or kidney dysfunction

Thiazolidinedione

Medication name Tablet form Recommended dosage range
Rosiglitazone (Avandia®) 4 mg, 8 mg 4-8 mg
Pioglitozone (Actos®) 15 mg, 30 mg, 45 mg 15-45 mg (once a day)
How it works:
  • Increases insulin sensitivity at receptors in fat, muscle, and liver tissues
Side effects:
  • Edema (swelling)
  • Weight gain
Comments/special instructions:
  • This medication does not cause hypoglycemia when prescribed as the only diabetes medication.
  • Rosiglitizone and pioglitizone can be taken with or without food.
  • The patient should have regular liver tests to detect liver dysfunction. Tests should be done every 2 months for the first year and periodically thereafter.

The most common side effects include upper respiratory infection, sinusitis, fluid retention, and weight gain.

Thiazolidinedione and Biguanide

Medication name Tablet form Recommended dosage range
Rosiglitazone maleate and Metformin (Avandamet®) (Rosiglitazone/Metformin)
1 mg/500 mg
2 mg/500 mg
4 mg/500 mg
1 mg/500 mg-8 mg/1000 mg
Pioglitazone Hcl and Metformin
Hcl (Actoplus Met®)
(Pioglitazone/Metformin®)
15 mg/500 mg
15 mg/850 mg
15 mg/500 mg - max
Dose 45 mg/2550 mg Daily
How it works:
  • Improves insulin sensitivity in fat, muscle, liver, and peripheral tissues
  • Lowers the amount of glucose produced by the liver and absorbed by the intestine
Side effects:
  • Edema (swelling)
  • Weight gain
  • Stomach upset (nausea, diarrhea)
  • Metallic taste in mouth
Comments/special instructions:
  • This does not cause hypoglycemia when prescribed as the only diabetes medication.
  • This medication should be temporarily stopped before hospitalization, surgery, or x-ray tests using contrast material (dye.)

Regular tests are needed to detect liver and/or kidney dysfunction.

Thiazolidinedione and Sulfonylurea

Medication name Tablet form Recommended dosage range
Pioglitazone and Glimepiride (Duetact®) Pioglitazone/Glimepiride
30 mg/2 mg
30 mg/4 mg
30 mg/2 mg-30 mg/4 mg one tablet daily
Rosiglitazone and Glimepiride (Avandaryl®) Rosiglitazone/Glimepiride
4 mg/1 mg
4 mg/2 mg
4 mg/4 mg
Max daily for either is 8 mg
How it works:
  • Stimulates the cells in the pancreas to release more insulin
  • Increases insulin sensitivity at receptors in fat, muscle and liver tissues
Side effects:
  • Hypoglycemia
  • Stomach upset
  • Skin rash or itching
  • Edema (swelling)
Comments/special instructions:
  • Take approximately ½ to 1 hour before a meal at the same time each day

Alpha-Glucosidase Inhibitor


Medication name Tablet form Recommended dosage range
Acarbose (Precose®) 25 mg, 50 mg, 100 mg 75-300 mg
Miglitol (Glyset®) 25 mg, 50 mg, 100 mg 75-300 mg
How it works:
  • Blocks enzymes that help to digest starches, which will slow the absorption of glucose from the intestinal tract into the bloodstream.
Side effects:
  • Stomach upset (gas, diarrhea, nausea, cramps)
Comments/special instructions:
  • This does not cause hypoglycemia when prescribed as the only diabetes medication.
  • It should be taken with the first bite of a meal.

If prescribed in combination with sulfonylurea, treat low blood glucose with glucose tablet or gel, not sugar

Meglitinide


Medication name Tablet form Recommended dosage range
Repaglinide (Prandin®) 0.5 mg, 1 mg, 2 mg 1.5-16 mg
Nateglinide (Starlix®)* 0.5 mg, 1 mg, 2 mg 180-360 mg
How it works:
  • Stimulates the pancreas to release more insulin. (The release of insulin is less effective at low glucose levels.)
Side effects:
  • Hypoglycemia
  • Stomach upset
Comments/special instructions:
  • This medicine is taken before meals. If the meal is missed, the medication for that meal is skipped.

*Not chemically a meglitinide, but has similar characteristics

DPP-4 inhibitors


Medication name Tablet form Recommended dosage range
Sitagliptin (Januvia®) 25 mg, 50 mg, and 100 mg 100 mg once a day, alone or in combination with metformin or a thiazolidinedione
How it works:
  • Affects the incretin system, which helps to control blood sugar by affecting alpha and beta cells.
Side effects:
  • Upper respiratory infection
  • Stuffy or runny nose
  • Sore throat
  • Headache

Comments/special instructions:

  • This medication can be taken alone or in combination with metformin or a thiazolidinedione.
  • This medication works only when the blood sugar is elevated.
  • This medication can be taken with our without food.
  • Before starting this medication, the patient should have his or her kidney function tested, and should have kidney function tested on a regular basis while taking the medication.

This information is provided by the Cleveland Clinic and is not intended to replace the medical advice of your doctor or health care provider. Please consult your health care provider for advice about a specific medical condition. This document was last reviewed on: 1/10/2008...#12070