Mitiglinide

Mitiglinide is a drug used for the treatment of Type 2 diabetes. It belongs to the class of drugs known as meglitinides, and is marketed under the trade names Glufast, Glufast L, and Glufast M in Japan by Kissei Pharmaceutical Co., Ltd.

Mechanism of Action

Mitiglinide works by stimulating the release of insulin from the pancreas. It does this by binding to ATP-sensitive potassium channels on the surface of the pancreatic beta cells. This binding causes the channels to close, leading to depolarization of the cell membrane and subsequent opening of voltage-gated calcium channels. The influx of calcium into the cell triggers the release of insulin.

Pharmacokinetics

Mitiglinide is rapidly absorbed and eliminated, making it suitable for mealtime use. It reaches peak plasma concentrations within an hour of oral administration and has a half-life of approximately two hours. The drug is metabolized in the liver, primarily by the cytochrome P450 enzyme CYP2C8, and to a lesser extent by CYP3A4. The metabolites are excreted in the urine and feces.

Side Effects

The most common side effects of mitiglinide are hypoglycemia, weight gain, and gastrointestinal disturbances such as diarrhea and nausea. Less common side effects include dizziness, headache, and joint pain.

Contraindications

Mitiglinide is contraindicated in patients with Type 1 diabetes or diabetic ketoacidosis. It should be used with caution in patients with liver disease, as it is metabolized in the liver.

Interactions

Mitiglinide may interact with other drugs, including other antidiabetic agents, beta-blockers, and calcium channel blockers. It may also interact with drugs that inhibit or induce the cytochrome P450 enzymes CYP2C8 and CYP3A4.

See Also

• Meglitinides
• Type 2 diabetes
• Insulin
• ATP-sensitive potassium channel
• Cytochrome P450

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