GLURENOR

Indications

• Type 2 diabetes mellitus
• Non-insulin dependent diabetes mellitus (NIDDM)

Dosage

Children: Safety and efficacy in children have not been established; refer to the BNF for Children for guidance.

Adults: The usual starting dose is 30 mg once daily, which can be adjusted based on blood glucose levels. Maximum daily dose should not exceed 120 mg.

Mechanism of action

Gliquidone lowers blood glucose by stimulating insulin release from functioning pancreatic beta cells and increasing peripheral tissue sensitivity to insulin. It likely binds to ATP-sensitive potassium channel receptors on pancreatic cells, leading to reduced potassium conductance and membrane depolarization. This depolarization causes calcium ion influx through voltage-sensitive calcium channels, ultimately inducing insulin secretion.

Pharmacodynamics

As a sulfonylurea, gliquidone acts primarily by enhancing insulin secretion in individuals with type 2 diabetes, where there is a deficiency of insulin. It effectively reduces blood sugar levels by stimulating the pancreas to produce and release more insulin, while also promoting glucose uptake by cells, which is crucial for maintaining normal blood glucose levels.

Pharmacokinetics

Gliquidone is absorbed from the gastrointestinal tract and reaches peak plasma concentrations within 1 to 3 hours after oral administration. It is metabolized in the liver, primarily via cytochrome P450 enzymes, and has a half-life that allows for once or twice daily dosing. The metabolites are excreted primarily through the urine.

Contra-indications

• Hypersensitivity to gliquidone or any of its components
• Diabetic ketoacidosis
• Type 1 diabetes mellitus
• Severe renal impairment
• Severe hepatic impairment

Adverse effects

• Hypoglycemia
• Weight gain
• Gastrointestinal disturbances (nausea, vomiting, diarrhea)
• Skin reactions (rash, pruritus)
• Hematological reactions (leukopenia, thrombocytopenia)
• Liver function abnormalities

Interactions

• Other antidiabetic medications (may increase risk of hypoglycemia)
• CYP2C9 inhibitors (may increase gliquidone levels)
• CYP2C9 inducers (may decrease gliquidone levels)
• Beta-blockers (may mask symptoms of hypoglycemia)
• Alcohol (may potentiate hypoglycemic effect)

Precautions

• Monitor blood glucose levels regularly
• Use with caution in patients with hepatic or renal impairment
• Adjust dose in elderly patients due to potential for altered pharmacokinetics
• Consider potential for drug interactions with concomitant medications

Pregnancy

Gliquidone should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Glycemic control is crucial in pregnancy, and insulin is the preferred treatment.

Breast-feeding

It is not known whether gliquidone is excreted in human milk. Caution should be exercised when administering to nursing women.

Storage

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

Formulations

• Tablets: 30 mg, 60 mg

Mechanism of action

The mechanism of action of gliquidone in lowering blood glucose appears to be dependent on stimulating the release of insulin from functioning pancreatic beta cells, and increasing sensitivity of peripheral tissues to insulin. Gliquidone likely binds to ATP-sensitive potassium channel receptors on the pancreatic cell surface, reducing potassium conductance and causing depolarization of the membrane. Membrane depolarization stimulates calcium ion influx through voltage-sensitive calcium channels. This increase in intracellular calcium ion concentration induces the secretion of insulin.

Pharmacodynamics

Gliquidone is an anti-diabetic drug in the sulfonylurea class. In patients with diabetes mellitus, there is a deficiency or absence of a hormone manufactured by the pancreas called insulin. Insulin is the main hormone responsible for the control of sugar in the blood. Gliquidone is an antidiabetic medication which is used in those patients with adult maturity onset or non-insulin dependent diabetes (NIDDM). It works by lowering blood sugar levels by stimulating the production and release of insulin from the pancreas. It also promotes the movement of sugar from the blood into the cells in the body which need it.