Miglitol

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Miglitol.jpg

[edit] MECHANISM OF ACTION

Miglitol is an alpha-glucosidase inhibitor.
Alpha-glucosidases is an intestinal enzyme that hydrolyze oligosaccharides, trisaccharides, and disaccharides to glucose and other monosaccharides in the brush border of the small intestine.
Therefore, Alpha-glucosidase inhibition by Miglitol delays the digestion of ingested carbohydrates, and thus prevent the formation of absorbable monosaccharides (glucose, fructose), thereby lowering postprandial glucose levels. Long-term studies show that a moderate average reduction of HbA1c of 0.3-0.7% point from baseline can be achieved. [1]

In contrast to sulfonylureas, Miglitol does not enhance insulin secretion and when administered alone, it has no or a very small effect on fasting blood glucose levels and does not cause hypoglycemia in the postprandial state. Because its mechanism of action is different, the effect of Miglitol to enhance glycemic control is additive to that of sulfonylureas, insulin or metformin when used in combination.

[edit] INDICATIONS

Miglitol is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

[edit] DOSAGE

Miglitol should be started at a low dose, with gradual dose escalation as described below, both to reduce gastrointestinal side effects and to permit identification of the minimum dose required for adequate glycemic control of the patient:

  • Starting dosage: The recommended starting dosage of Miglitol is 25 mg given orally three times daily at the start (with the first bite) of each main meal
  • Maintenance Dosage: After 4 - 8 weeks of the 25 mg 3 times daily regimen, the dosage should be increased to 50 mg 3 times daily for approximately three months, following which a glycosylated hemoglobin level should be measured to assess therapeutic response. If, at that time, the glycosylated hemoglobin level is not satisfactory, the dosage may be further increased to 100 mg 3 times daily, the maximum recommended dosage

[edit] CONTRAINDICATIONS

  • Patients with diabetic ketoacidosis.
  • Patients with inflammatory bowel disease (ulcerative colitis or Crohn’s disease), partial intestinal obstruction or in patients predisposed to intestinal obstruction.
  • Patients who have chronic intestinal diseases associated with marked disorders of digestion or absorption.

[edit] PRECAUTIONS

[edit] INTERACTIONS

  • Sulfonylureas or Insulin: Miglitol given in combination with a sulfonylurea or insulin will cause a further lowering of blood glucose and may increase the potential for hypoglycemia. To treat symptoms of low blood sugar when taking Miglitol in combination with a sulfonylurea or insulin, patient should have a readily available source of glucose (dextrose, D-glucose), whose absorption is not inhibited by Miglitol, instead of table sugar (Miglitol prevents the breakdown of table sugar)

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category B (US). The safety of Miglitol in pregnant women has not been established, therefore it should be used during pregnancy only if clearly needed. Because current information strongly suggests that abnormal blood glucose levels during pregnancy are associated with a higher incidence of congenital anomalies as well as increased neonatal morbidity and mortality, most experts recommend that insulin be used during pregnancy to maintain blood glucose levels as close to normal as possible.
  • Miglitol has been shown to be excreted in human milk to a very small degree. Total excretion into milk accounted for 0.02% of a 100-mg maternal dose. The estimated exposure to a nursing infant is approximately 0.4% of the maternal dose. Although the levels of miglitol reached in human milk are exceedingly low, it is recommended that Miglitol not be administered to a nursing woman.

[edit] SIDE EFFECTS

Most common reactions are mild-to-moderate gastrointestinal effects, such as flatulence, diarrhea, or abdominal discomfort. The incidence of diarrhea and abdominal pain tended to diminish considerably with continued treatment.

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES

  1. http://www.ncbi.nlm.nih.gov/pubmed/11249557
Diabetes (Antidiabetic drugs)
Insulin Secretagogues (drugs that increase insulin release from pancreas) Sulfonylureas Chlorpropamide (Diabinese)   Glibenclamide or Glyburide (Diabeta, Micronase, Glynase, Daonil, Euglycon)   Gliclazide (Diamicron)   Glimepiride (Amaryl, Solosa)   Glipizide (Glucotrol, Minidiab, Glibenese)   Gliquidone (Glurenorm)
Meglitinides Repaglinide (Prandin, Novonorm)   Nateglinide (Starlix)
Dipeptidyl peptidase-4 inhibitors Linagliptin (Trajenta)   Saxagliptin (Onglyza)   Sitagliptin (Januvia)   Vildagliptin (Galvus)
Incretin mimetics (GLP-1 agonists and analogs) Exenatide (Byetta)   Liraglutide (Victoza)   Lixisenatide (Lyxumia)   Dulaglutide (Trulicity)
Insulin Sensitizers (drugs that decrease insulin resistance)
Biguanides Metformin (Glucophage)
Thiazolidinediones Pioglitazone (Actos)
Drugs that retard the digestion and absorption of carbohydrates in the small intestine
Alpha-glucosidase inhibitors Acarbose (Glucobay, Precose)
Drugs that reduce glucose absorption in the kidney and increase glucose excretion in the urine
Sodium glucose cotransporter 2 (SGLT2) inhibitors Canagliflozin (Invokana)   Dapagliflozin (Farxiga)   Empagliflozin (Jardiance, Glyxambi, Synjardi)
Insulin and insulin analogs
Intermediate acting insulins Insulin lispro protamine (Humalog BASAL)   Isophane human insulin : Human insulin protamine (NPH) (Humulin I, Protaphane)
Long-acting insulins‎ Insulin detemir (Levemir)   Insulin glargine (Lantus)
Fast-acting insulins‎ Regular insulin : Insulin (Human recombinant) (Actrapid, Humulin R)
Ultra-rapid-acting insulins‎‎ Insulin aspart (Novorapid)   Insulin glulisine (Apidra)   Insulin lispro (Humalog)   Insulin human (Inhalation Powder) (Afrezza)
Premixed insulin‎‎‎ (ultra-rapid-acting + intermediate acting Insulin aspart / Insulin aspart protamine (Novomix)   Insulin lispro / Insulin lispro protamine (Humalog Mix)
Inhaled Insulin Insulin human (Inhalation Powder) (Afrezza)
Combination therapy
Sulfonylurea + Metformin Glibenclamide / Metformin (Bieuglicon M, Diaglimet, Glibomet, Gliconorm, Glicorest, Suguan M)
Thiazolidinedione + Metformin Pioglitazone / Metformin (Competact, Glubrava)
Thiazolidinedione + Sulfonylurea Pioglitazone / Glimepiride (Tandemact)
Dipeptidyl peptidase-4 inhibitors + Metformin Linagliptin / Metformin (Jentadueto)   Sitagliptin / Metformin (Efficib, Janumet, Velmetia)   Vildagliptin / Metformin (Eucreas)