第二代胰島素類似物 Insulin Glargine 300U/mL簡稱 Gla-300, insulin degludec (簡稱IDeg-100)
Tresiba Insulin degludec U100
Tresiba Insulin degludec U100
第一代胰島素 insulin glargine 100U/mL 簡稱 Gla-100
IDeg-100 活性長達 42 小時, IDeg-100相較於 Gla-100 的降血糖能力, 可減少一天之內的血糖波動變化, 以及每天的血糖波動,
Gla-300 與 IDeg-100比較, 當給予每天每公斤 0.4 u 的劑量, 一天之內 Gla-300 的代謝活性變化比 IDeg-100減少 20%.
Second-generation basal insulin analogues (insulin glargine 300 U/mL [Gla-300; Sanofi, Paris, France] and insulin degludec [IDeg; Novo Nordisk, Bagsværd, Denmark]) have demonstrated similar efficacy in reducing HbA1c to first-generation insulin therapy (e.g. insulin glargine 100 U/mL [Gla-100; Sanofi]).18 However, the newer agents have longer and more stable pharmacokinetic (PK) and pharmacodynamic (PD) profiles than first-generation treatments.19–23 Gla-300 is associated with low within-day variability and high reproducibility (low betweenday variability) in insulin exposure,19,24 with predictable and stable glycaemic control well beyond 24 hours.25 Similarly, IDeg has demonstrated activity for up to 42 hours with four times lower day-to-day within-patient variability in glucose reduction compared with Gla-100.20 A comparison of the steady state PK/PD profiles of Gla300 and IDeg revealed that Gla-300 provided 20% less within-day fluctuation of metabolic activity than IDeg over 24 hours at a dose of 0.4 U/kg/day (Figure 1).
第二代胰島素類似物可達成與第一代胰島素 Gla-100相似的血糖控制效果, 但第二代胰島素的作用時間 > 24 小時, 血中藥物濃度可維持在較平穩的狀態, 因此可減少血糖波動, 注射時間也比較彈性化, 因此第二代基礎胰島素類似物適合做為一天一次的選擇
Second-generation basal insulin analogues (insulin glargine 300 U/mL [Gla-300; Sanofi, Paris, France] and insulin degludec [IDeg; Novo Nordisk, Bagsværd, Denmark]) have demonstrated similar efficacy in reducing HbA1c to first-generation insulin therapy (e.g. insulin glargine 100 U/mL [Gla-100; Sanofi]).18 However, the newer agents have longer and more stable pharmacokinetic (PK) and pharmacodynamic (PD) profiles than first-generation treatments.19–23 Gla-300 is associated with low within-day variability and high reproducibility (low betweenday variability) in insulin exposure,19,24 with predictable and stable glycaemic control well beyond 24 hours.25 Similarly, IDeg has demonstrated activity for up to 42 hours with four times lower day-to-day within-patient variability in glucose reduction compared with Gla-100.20 A comparison of the steady state PK/PD profiles of Gla300 and IDeg revealed that Gla-300 provided 20% less within-day fluctuation of metabolic activity than IDeg over 24 hours at a dose of 0.4 U/kg/day (Figure 1).
第二代胰島素類似物可達成與第一代胰島素 Gla-100相似的血糖控制效果, 但第二代胰島素的作用時間 > 24 小時, 血中藥物濃度可維持在較平穩的狀態, 因此可減少血糖波動, 注射時間也比較彈性化, 因此第二代基礎胰島素類似物適合做為一天一次的選擇
第二代胰島素類似物發生低血糖機率較低
在調整劑量的期間, Gla-300 造成的夜間低血糖機率較低
These advances have translated into the clinically meaningful benefit of providing similar glycaemic control to Gla-100, but with an ultra-long duration (>24-hour coverage), a more stable PK profile (resulting in reduced glycaemic variability), and greater injection time flexibility. These factors make second-generation basal insulin analogues suitable for once-daily treatment.19–23 In addition to effectively reducing HbA1c, the second-generation basal insulin analogues are associated with a lower risk of hypoglycaemia (both nocturnal hypoglycaemia and also, for Gla-300, all-day hypoglycaemia) compared with Gla-100 (Figure 2).18,27,28 For Gla-300, the benefit of lower incidence of hypoglycaemia is especially pronounced in the titration period.
結論
These advances have translated into the clinically meaningful benefit of providing similar glycaemic control to Gla-100, but with an ultra-long duration (>24-hour coverage), a more stable PK profile (resulting in reduced glycaemic variability), and greater injection time flexibility. These factors make second-generation basal insulin analogues suitable for once-daily treatment.19–23 In addition to effectively reducing HbA1c, the second-generation basal insulin analogues are associated with a lower risk of hypoglycaemia (both nocturnal hypoglycaemia and also, for Gla-300, all-day hypoglycaemia) compared with Gla-100 (Figure 2).18,27,28 For Gla-300, the benefit of lower incidence of hypoglycaemia is especially pronounced in the titration period.
結論
第二代基礎胰島素類似物可做為控制血糖的新療法, 第二代胰島素類似物降低 A1C 效果與第一代相似, 第二代基礎胰島素類似物還有其他臨床效益, 包括更穩定更長時間的作用, 一天施打一次即可. 任何時間都可以注射. 低血糖機率也降低.
Concluding remarks
The second-generation basal insulin analogues provide physicians with new treatment options for achieving targeted glycaemic control. While providing similar efficacy in lowering HbA1c to first-generation insulin analogues, the newer insulin treatment options provide additional clinical benefits, including a more stable, ultra-long duration of action that enables once-daily administration with flexibility in daily injection time, together with a lower risk of hypoglycaemia.
Concluding remarks
The second-generation basal insulin analogues provide physicians with new treatment options for achieving targeted glycaemic control. While providing similar efficacy in lowering HbA1c to first-generation insulin analogues, the newer insulin treatment options provide additional clinical benefits, including a more stable, ultra-long duration of action that enables once-daily administration with flexibility in daily injection time, together with a lower risk of hypoglycaemia.
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