Office of Clinical Pharmacology, Office of Translational Sciences, Center of Drug Evaluation and Research, US Food and Drug Administration, Silver Spring, Maryland, USA.
Clin Pharmacol Ther. 2024 Oct;116(4):976-979. doi: 10.1002/cpt.3340. Epub 2024 Jun 7.
Glucagon was discovered about a hundred years ago and its role in health and disease is under continuous investigation. Glucagon is a counter regulatory hormone secreted by alpha cells of the pancreas in response to multiple stimuli. Although some of glucagon's actions and its clinical application have been described, clinical experience with glucagon has been historically overshadowed by that of insulin. To date, the role of glucagon's actions in pharmacotherapy has been under explored. Glucagon plays a considerable role as a hormonal regulator via its known actions on the liver. The rise in obesity and diabetes mellitus prevalence is bringing focus to glucagon's known physiological roles and possible clinical applications. Six glucagon products and a glucagon analog are approved for use in the United States. Clinical pharmacology studies provide crucial support of glucagon's actions as evident from comprehensive pharmacokinetics and pharmacodynamics evaluations in humans. Here, we briefly describe the established physiological role of glucagon in humans and its known relationship with disease. We later summarize the clinical pharmacology of available glucagon products with different routes of administration.
胰高血糖素大约在一百年前被发现,其在健康和疾病中的作用仍在不断研究中。胰高血糖素是胰腺α细胞在多种刺激下分泌的一种抗调节激素。虽然已经描述了胰高血糖素的一些作用及其临床应用,但胰高血糖素的临床经验在历史上一直被胰岛素所掩盖。迄今为止,胰高血糖素作用在药物治疗中的作用仍未得到充分探索。胰高血糖素通过其对肝脏的已知作用发挥着重要的激素调节作用。肥胖症和糖尿病患病率的上升使人们更加关注胰高血糖素的已知生理作用和可能的临床应用。目前,有六种胰高血糖素产品和一种胰高血糖素类似物在美国获得批准使用。临床药理学研究为胰高血糖素的作用提供了重要支持,从人类全面的药代动力学和药效学评估中可以明显看出这一点。在这里,我们简要描述了胰高血糖素在人类中的既定生理作用及其与疾病的已知关系。随后,我们总结了不同给药途径的现有胰高血糖素产品的临床药理学。