Glibenclamide 磺醯尿素類 SU Gliben 5mg 中度腎衰竭 eGFR 60 以下不建議使用

商品名: Gliben 5mg 固利康錠

初始劑量 2.5mg QD. 之後根據血糖, 可每周往上調升 2.5mg/D 

最大劑量 20mg QD 

若劑量>10mg. 建議早餐服用 10 mg. 剩下劑量分配在其他時間服用

PEAK 服用5mg之後 2-6 小時到達最大血中濃度

多次服用的血中藥物濃度與單次服用的AUC相似, 代表身體內不會蓄積

禁忌
嚴重肝腎衰竭
eGFR < 60

半衰期

靜脈注射 2 小時
口服 2-5 小時

某些研究發現, 糖尿病患服用之後的半衰期達 8-10 小時
糖尿病患服用單次劑量, 低血糖效果可持續 24 小時

Glibenclamide 在肝臟代謝, 之後由腎臟和腸子排出體外, 有些代謝產物具有生理活性, 在慢性腎病患者會蓄積血中, 雖然肝臟排出也能代償一部分的腎臟排泄下降

Glibenclamide is completely metabolised in the liver. The drug is metabolised at the cyclohexyl ring principally to a 4-trans-hydroxy derivative. A second metabolite, the 3-cis-hydroxy derivative, also occurs. These metabolites contribute some hypoglycaemic action; they are weakly active (0.25% and 2.5%, respectively, as glibenclamide) in rabbits. Glibenclamide is excreted as metabolites in the bile and urine, approximately 50% by each route. In patients with renal insufficiency, depending on the degree of the renal excretion disorder, there is increased elimination of metabolites via the bile. This dual excretory pathway is qualitatively different from that of other sulphonylureas, which are excreted primarily in the urine.

慢性腎病的患者, 服用 glibenclamide 若發生低血糖可能會很嚴重, 持續超過 24 小時

Glibenclamide (glyburide) is metabolized in the liver and excreted by the kidneys equally and intestine. Some metabolites are active and can accumulate in CKD despite the fact that biliary removal partially counteracts the limited renal excretion.

Hypoglycemia may be serious and lasting more than 24 h in CKD.

第一第二期慢性腎病, eGFR 60-90 應減低劑量

eGFR < 60 不建議使用

The use of glibenclamide in subjects with moderate CKD (eGFR 60-90 mL/min) should be limited (reduced dose, frequent monitoring due to increased risk of hypoglycemia). The drug and is contraindicated in stage ≥ 3 CKD (eGFR < 60 mL/min)[17].


不同的磺醯尿素類, 低血糖的機率各有不同

Glimepiride 低血糖機率 2%-4%

Glibenclamide 低血糖機率 20-30%

Glibenclamide (glyburide) is associated with an incidence of hypoglycemia of up to 20–30%, compared to as low as 2% to 4% with glimepiride.