Elimination half-life | Glycemic efficacy (reduction in A1C in percentage points)* | Cardiovascular outcomes ASCVD/HF | Nephropathy¶ | RetinopathyΔ | Cardiovascular/ Overall mortality | |
Long-acting GLP-1 receptor agonists (more pronounced effect on fasting glucose) | ||||||
Dulaglutide Initial dose: 0.75 mg SubQ once weekly.If not meeting glycemic goals after 4 weeks, increase dose as tolerated every 4 weeks as follows: 1.5 mg SubQ once weekly, then 3 mg SubQ once weekly, then 4.5 mg SubQ once weekly. | 5 days | –1 to –1.5 | Benefit/Neutral | Benefit | Neutral | Benefit/Benefit |
Efpeglenatide (investigational, doses represent those used in phase II and III trials) Initial dose:4 or 6 mg SubQ once weekly or 8, 12, or 16 mg SubQ once monthly. | 6 to 7 days | –1 to –1.11 | Benefit/? | Benefit | ? | ?/? |
Exenatide, extended release Initial dose: 2 mg SubQ once weekly. | 8 to 14 days | –1.5 to –1.6 | Neutral/Neutral | ? | Neutral | Benefit/Benefit |
Liraglutide Initial dose: 0.6 mg SubQ once daily for 1 week and then increase to 1.2 mg SubQ once daily.If not meeting glycemic goals after another 1 to 2 weeks, increase dose as tolerated to 1.8 mg SubQ once daily. | 11 to 15 hours | –0.8 to –1.5 | Benefit/Neutral | Benefit | Neutral | Benefit/Benefit |
Semaglutide | ||||||
SubQ formulation Initial dose: 0.25 mg SubQ once weekly for 4 weeks, then increase to 0.5 mg SubQ once weekly; if not meeting glycemic goals after at least 4 weeks, increase dose as tolerated every 4 weeks as follows: 1 mg SubQ once weekly, then 2 mg SubQ once weekly◊. | 6 to 7 days | –1.5 to –2 | Benefit/Neutral | Benefit | Unexpected increase in retinopathy outcomes◊ | Benefit/Benefit |
Oral formulation, take fasting, at least 30 mins before breakfast or other oral medications, with no more than 4 oz of plain water. Initial dose: 3 mg once daily for 30 days and then increase to 7 mg once daily.If not meeting glycemic goals after 30 days on 7 mg dose, increase dose as tolerated to 14 mg once daily. | 6 to 7 days | –0.7 to –2 | Neutral/Neutral | ? | Neutral | Benefit/? |
Short-acting GLP-1 receptor agonists (more pronounced effect on postprandial glucose) | ||||||
Exenatide Initial dose: 5 mcg SubQ twice daily (within 1 hour before the 2 main meals of the day, at least 6 hours apart).If not meeting glycemic goals after 4 weeks, increase dose as tolerated to 10 mcg SubQ twice daily. | 2 to 3 hours | –1 | ?/? | ? | ? | ?/? |
Lixisenatide Initial dose: 10 mcg SubQ once daily, within 1 hour prior to any meal of the day.After 2 weeks, increase dose as tolerated to 20 mcg SubQ once daily. | 3 to 5 hours | –0.8 to –1 | Neutral/Neutral | Neutral | ? | Benefit/Benefit |
Dual-acting GLP-1 and GIP receptor agonists | ||||||
Tirzepatide Initial dose: 2.5 mg SubQ once weekly for 4 weeks, then increase to 5 mg SubQ once weekly. If not meeting glycemic goals after at least 4 weeks, increase dose as tolerated in 2.5 mg increments every 4 weeks as needed to achieve glycemic goals. Maximum dose 15 mg SubQ once weekly. | 5 days | –2 to –2.5 | ?/?§ | ? | ? | ?/? |
GLP-1: glucagon-like peptide 1; A1C: glycated hemoglobin; ASCVD: atherosclerotic cardiovascular disease; HF: heart failure; SubQ: subcutaneously; ?: inadequate data; GIP: glucose-dependent insulinotropic polypeptide; eGFR: estimated glomerular filtration rate.
* Reduction in A1C is dependent upon a number of factors, such as baseline A1C and background therapy. In trials directly comparing shorter- versus longer-acting GLP-1 receptor agonists, longer-acting had better glycemic efficacy.
¶ Nephropathy is defined as elevated albuminuria, reduced eGFR (usually <60 mL/min/1.73 m2), or both.
Δ Retinopathy outcomes were not systematically evaluated or adjudicated.
◊ The higher rate of retinopathy complications with subcutaneous semaglutide was unexpected and may be a consequence of rapid glycemic control similar to that seen in other settings. If subcutaneous semaglutide is prescribed to a patient with diabetic retinopathy, titrate slowly to avoid rapid declines in A1C and perform retinal screening within 6 months of drug initiation to detect progression of retinopathy.
§ In preliminary trials, tirzepatide did not increase the risk of major cardiovascular events.آیا می خواهید مدیلیب را به صفحه اصلی خود اضافه کنید؟