【藥品庫存】 藥品安全警訊 (藥品回收)：本品2批號因產品持續安定性試驗之溶離度試驗結果未能符合規格，於2022/12/21 經食藥署公告回收，院內使用非回收批號。 更新日期：2022/12/22。 #高警訊藥品 #特殊劑型：不建議磨粉、管灌藥品

糖尿病 (Sulfonylurea) Type 2 diabetes mellitus

Sulfonylurea antidiabetic agent
Gliclazide is a second-generation sulfonylurea oral hypoglycemic agent closely related to glyburide. At the cellular level, sulfonylureas bind to a sulfonylurea receptor on the pancreatic beta-cell which inhibits the adenosine triphosphate-dependent potassium channel (K-ATP). However, sulfonylureas only stimulate phase I (initial rapid peak) release of insulin and have no effect on phase II (prolonged insulin release). Gliclazide also appears to increase the sensitivity of the liver and peripheral tissues to insulin.

Absorption
1. Effects of Food：clinically insignificant
Distribution
1. Protein Binding：85% to 99%　
2. Vd：13 to 24 L
Metabolism
1. via hydroxylation, oxidation, and glucuronidation to 7 metabolites　
2. Metabolites: Carboxy derivative, (inactive), Hydroxymethyl derivative (inactive), Hydroxyazabicyclo-octyl derivatives (inactive), Glururonide derivatives (inactive)
Excretion
1. Renal(60-80%), Feces(20%)
2. Gliclazide is eliminated primarily as metabolites. The amount of unchanged drug eliminated in the urine varies from less than 1% to 20%
Pharmacodynamics
1. Elimination Half-life: 8-12 hours (In some studies, the half-life was longer in women than in men; tends to be longer in elderly)
2. Renal Clearance (rate)：0.5 mL/minute

1. Diabetic ketoacidosis
2. Hypersensitivity to gliclazide or other sulfonylureas
3. Type I diabetes as sole therapy
4. Stress conditions (eg, serious infection, trauma, surgery)
5. Pregnancy, breastfeeding

Contraindicated: Fetal risk has been demonstrated

Contraindicated: Infant risk has been demonstrated.

Common
Hypoglycemia, Gastrointestinal discomfirt(Diarrhea, constipation, gastroenteritis, abdominal pain , gastritis, nausea)
Rare
Dermatological disease(dermatitis, skin rash, pruritus), increased AST or ALT, hepatitis, visual disturbance

Administration
Should be taken with meals
Dosage
1. Initial: 30 mg once daily
2. Titration: If adequate glycemic control is not obtained, may increase the dose in 30 mg increments every 2 weeks.
3. Maximum dose: 120 mg once daily.
Conversion from insulin
1. May consider conversion from insulin to gliclazide therapy in patients receiving <40 units/day insulin.
2. Prior to conversion, discontinue insulin for 48 to 72 hours with close monitoring ((3 times/day) of urine for glucose and ketones. Patients with ketonuria and glycosuria 12 to 24 hours after discontinuing insulin should not be converted to gliclazide therapy and should remain on insulin therapy.

1. Mild to moderate impairment: No dosage adjustment required; adjust dose cautiously
2. Severe impairment: Use is contraindicated

Mild to moderate impairment: Refer to adult dosing
Severe impairment: Use is contraindicated