Miglitol (Glyset) is an oral glucosidase inhibitor that inhibits the absorption of dietary carbohydrates. It is used in the management of patients with diabetes mellitus type 2. Compared to most other diabetes medications, it is one of the least potent drugs. It causes significant gastrointestinal side effects. However, it is associated with weight loss and may be used in individuals with prediabetes to prevent the development of diabetes.

Miglitol (Glyset) Uses:

• Diabetes mellitus Type 2:

  • It is used as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus

Acarbose is another oral diabetes medicine that has a similar mechanism of action as miglitol.

Miglitol Dose in Adults:

Miglitol (Glyset) Dose in the treatment of Type 2 Diabetes mellitus:

• Initial: 25 mg orally three times a day with the first bolus of each meal OR
• 25 mg once daily with the major meal and gradually titrating the dose to 25 mg thrice daily to minimize the gastrointestinal side effects.
• The dose may then be titrated to a maintenance dose of 50 mg thrice daily and continued for about three months.
• Patients whose glycemic control is not satisfactory may need to increase the dose to the maximum recommended dose of 100 mg thrice daily.
• However, the lowest effective dose should be used.

• Concomitant use with insulin and/or insulin secretagogues (eg, sulfonylurea):

  • Patients may need to reduce their insulin or other diabetes medications dose to avoid the risk of hypoglycemia.

Use in Children:

Not indicated.

Miglitol (Glyset) Pregnancy Risk Category: B

• Poorly managed diabetics pose a greater risk for maternal and fetal complications.
• Negative maternal and fetal outcomes include preeclampsia and preeclampsia as well as preterm and spontaneous abortions, complications of birth, stillbirths, macrosomia, and preeclampsia.
• Patients with diabetes should plan their pregnancy. The target HbA level should be kept as close to the target as possible and as tight as possible, without increasing the chance of hypoglycemia.
• Pregnancy should be a good time to use insulin and other drugs.

Use of Miglitol while breastfeeding

• It is excreted from breast milk. A 100 mg dose of the drug has resulted in 0.4% infant exposure.
• When the drug is given to lactating mothers, the manufacturer suggests that they avoid breastfeeding.

Miglitol (Glyset) Dose in Kidney Disease:

• • CrCl >=25mL/minute
    • It is not necessary to adjust the dose.
    • The drug is excreted unchanged in its simplest form, but the elevated plasma levels due to renal impairment do not affect the effectiveness of the clinical response. It primarily acts in your gastrointestinal tract.
  • CrCl >25 mL/minute, or SCr >2 mg/dL
    • It is not recommended for use in severe renal disease.

Miglitol (Glyset) Dose in Liver disease:

Adjustment in the dose is not necessary.

Common Side Effects of Miglitol (Glyset):

• Gastrointestinal:

  • Flatulence
  • Diarrhea
  • Abdominal pain

Less Common Side Effects of Miglitol (Glyset):

• Dermatologic:

  • Skin rash

Contraindications to Miglitol (Glyset):

• Allergy reactions to miglitol and any component of the formulation
• Diabetic ketoacidosis
• Inflammatory bowel disease
• Colonic ulceration
• Patients with partial or predisposed to intestinal obstruction.
• An excessive gas formation can lead to chronic gastrointestinal conditions such as malabsorption, maldigestion, or GI problems that are more severe.

Warnings and precautions

• GI side effects:

  • Many patients experience gastrointestinal side effects.
  • With continued treatment, diarrhea and abdominal pain are less common.

• Hypoglycemia:

  • Hypoglycemia is less common with monotherapy. However, it can occur when the drug is combined with insulin or sulfonylurea.
  • Miglitol-treated patients with mild to moderate hypoglycemia should be given oral glucose, instead of sucrose.
  • Sucrose won't be absorbed and will not be hydrolyzed into fructose or glucose.
  • For severe hypoglycemia episodes, intravenous glucose or glucagon may be required.

• Renal impairment:

  • It is not recommended for patients suffering from severe kidney diseases, such as those with a CrCl less than 25ml/minute or creatinine greater than 2mg/dl.

• Stress-related disorders:

  • In cases of stress-related conditions such as surgery, trauma, or severe medical condition, Miglitol could be stopped.
  • In these cases, insulin may be of benefit to patients.

Miglitol: Drug Interaction

Monitoring parameters:

Monitor blood sugars and glycated hemoglobin. Patients who have good glycemic control need to check their HbA at least every six months.

Patients who fail to reach their HbA target should monitor it every three months.

How to administer Miglitol (Glyset)?

It should be administered at the start of each meal, usually with the first bolus of the meal.

Mechanism of action of Miglitol (Glyset):

It acts at the brush border of small intestinal membrane-bound enzymes alpha-glucosidase enzymes, which are normally responsible for hydrolyzing oligosaccharides or disaccharide glucose and other monosaccharides.

The inhibition of the enzyme causes the incomplete and delayed absorption of carbohydrates.

This results in a decrease in post-prandial blood glucose. It is possible to reverse the inhibition of this enzyme. It doesn't cause hypoglycemia, as it doesn't have an effect on insulin secretion like sulfonylurea.

Absorption:

• The dose determines how much absorption is possible (it's saturable at high doses).
• It is fully absorbed when taken at 25 mg.
• Only 50% to 70% of 100 mg doses are absorbed.

Protein binding:

• < 4%

Metabolism:

• It is not metabolized.

Half-life elimination:

• ~2 hours

Time to peak:

• 2-3 hours

Excretion:

• It is excreted in urine as unchanged.

International Brands of Miglitol (Glyset):

• Glyset
• Darlibose
• Diaban
• Diamig
• Diaset
• Diastabol
• Glitol
• Litomen
• Migbose
• Plumarol
• Seibule

Miglitol Brand Names in Pakistan:

No Brands Available in Pakistan.