VOGLINORM

Indications

• Type 2 diabetes mellitus
• Impaired glucose tolerance

Dosage

Children: Refer to the BNF for Children for specific dosing recommendations.

Adults: The usual starting dose is 0.2 mg three times daily, taken with the first bite of each main meal. This may be increased to a maximum of 0.6 mg three times daily based on individual response.

Mechanism of action

Voglibose acts as a competitive inhibitor of alpha-glucosidase enzymes located in the brush border of the small intestines. These enzymes are responsible for breaking down oligosaccharides, trisaccharides, and disaccharides into glucose and other monosaccharides. By inhibiting these enzymes, voglibose decreases the rate of carbohydrate digestion and glucose absorption, thereby helping to lower blood glucose levels after meals. Additionally, it may also inhibit pancreatic alpha-amylase, which further reduces carbohydrate breakdown.

Pharmacodynamics

As an alpha-glucosidase inhibitor, voglibose exhibits significant effectiveness in managing blood glucose levels in patients with type 2 diabetes mellitus. The drug not only decreases immediate postprandial glucose levels but also contributes to a gradual reduction in hemoglobin A1c levels over time, which reflects long-term glycemic control. It is particularly useful in preventing the spikes in blood glucose that occur after meals by delaying carbohydrate absorption.

Pharmacokinetics

Voglibose is absorbed after oral administration, but its systemic bioavailability is limited due to its local action in the intestines. It undergoes minimal metabolism, and its effects are predominantly exerted within the gastrointestinal tract. The elimination half-life and specific details on excretion routes remain less clearly defined, but the drug is primarily excreted unchanged in the faeces, reflecting its mechanism of action as a local inhibitor rather than a systemic agent.

Contra-indications

• Hypersensitivity to voglibose or any of its components
• Diabetic ketoacidosis
• Intestinal obstruction or other gastrointestinal diseases that may be aggravated by increased gas production
• Severe renal impairment
• Inflammatory bowel disease

Adverse effects

• Flatulence
• Diarrhea
• Abdominal pain
• Nausea
• Hypoglycemia when used in combination with other antidiabetic medications

Interactions

• May enhance the hypoglycemic effect of other antidiabetic agents such as sulfonylureas or insulin
• Antacids may interfere with the absorption of voglibose
• Caution is advised when used with gastrointestinal agents that may affect motility

Precautions

• Monitor blood glucose levels regularly
• Use with caution in patients with renal impairment
• Patients should be advised on dietary measures to control carbohydrate intake

Pregnancy

There is limited data on the use of voglibose during pregnancy. It should only be used if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Voglibose is excreted in breast milk. Caution should be exercised when prescribing to breastfeeding women.

Storage

Store at room temperature, away from moisture and heat. Keep out of reach of children.

Formulations

• Tablets: 0.2 mg, 0.3 mg

Mechanism of action

Alpha-glucosidase inhibitors are saccharides that act as competitive inhibitors of enzymes needed to digest carbohydrates: specifically alpha-glucosidase enzymes in the brush border of the small intestines. The membrane-bound intestinal alpha-glucosidases hydrolyze oligosaccharides, trisaccharides, and disaccharides to glucose and other monosaccharides in the small intestine. Acarbose also blocks pancreatic alpha-amylase in addition to inhibiting membrane-bound alpha-glucosidases. Pancreatic alpha-amylase hydrolyzes complex starches to oligosaccharides in the lumen of the small intestine. Inhibition of these enzyme systems reduces the rate of digestion of complex carbohydrates. Less glucose is absorbed because the carbohydrates are not broken down into glucose molecules. In diabetic patients, the short-term effect of these drugs therapies is to decrease current blood glucose levels: the long term effect is a small reduction in hemoglobin-A1c level. (From Drug Therapy in Nursing, 2nd ed)

Pharmacodynamics

Voglibose, an alpha-glucosidase inhibitor, is a synthetic compound with potent and enduring therapeutic efficacies against disorders of sensory, motor and autonomic nerve systems due to diabetes mellitus. The drug was approved in Japan in 1994 for the treatment of diabetes, and it is under further investigation by Takeda for the treatment of impaired glucose tolerance. Alpha-glucosidase inhibitors are oral anti-diabetic drugs used for diabetes mellitus type 2 that work by preventing the digestion of complex carbohydrates (such as starch). Complex carbohydrates are normally converted into simple sugars (monosaccharides) which can be absorbed through the intestine. Hence, alpha-glucosidase inhibitors reduce the impact of complex carbohydrates on blood sugar.