Acarbose

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Acarbose.jpg

[edit] MECHANISM OF ACTION

Acarbose, a complex oligosaccharide, 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 Acarbose delays the digestion of ingested carbohydrates, and thus prevent the formation of absorbable monosaccharides (glucose, fructose), thereby lowering postprandial glucose levels. Acarbose also inhibits pancreatic alpha-amylase an enzyme that hydrolyzes complex starches to oligosaccharides in the lumen of the small intestine. As a consequence of plasma glucose reduction, Acarbose reduces levels of glycosylated hemoglobin (HbA1c) in patients with type 2 diabetes mellitus. In contrast to sulfonylureas, Acarbose does not enhance insulin secretion and when administered alone should not cause hypoglycemia in the fasted or postprandial state. Because its mechanism of action is different, the effect of Acarbose to enhance glycemic control is additive to that of sulfonylureas, insulin or metformin when used in combination. Data from clinical trials indicate that acarbose lowers postprandial and fasting blood glucose levels in by about 20 and 10%, respectively and reduces glycosylated hemoglobin levels (0.6%) in type 2 diabetes patients.

[edit] INDICATIONS

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

[edit] DOSAGE

Acarbose 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 Acarbose is 25 mg given orally three times daily at the start (with the first bite) of each main meal
  • Maintenance Dosage: Acarbose should be adjusted at 4–8 week intervals based on one-hour postprandial glucose or glycosylated hemoglobin levels, and on tolerance. The dosage can be increased from 25 mg three times daily to 50 mg three times daily. Some patients may benefit from further increasing the dosage to 100 mg three times daily.
  • Maximum Dosage : The maximum recommended dose for patients < 60 kg is 50 mg three times daily. The maximum recommended dose for patients > 60 kg is 100 mg three times daily

[edit] CONTRAINDICATIONS

  • Patients with diabetic ketoacidosis or cirrhosis.
  • 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] INTERACTIONS

  • Sulfonylureas or Insulin: Acarbose 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 Acarbose 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 Acarbose, instead of table sugar (Acarbose prevents the breakdown of table sugar)
  • Metformin: No increased incidence of hypoglycemia was observed in patients when Acarbose was added to metformin therapy.

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category B (US). The safety of Acarbose 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.
  • It is not known whether Acarbose is excreted in human milk. Because many drugs are excreted in human milk, Acarbose should 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, and generally diminish in frequency and intensity with time.

  • Jaundice (rarely)

[edit] RELATED LINKS

Understanding Alpha-glucosidase inhibitors
Understanding Type 2 Diabetes
A simple explanation of what diabetes is

[edit] BIBLIOGRAPHY

[edit] REFERENCES

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)