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Endocrine Drugs

GLP-1 Receptor Agonists

    Byetta (daily), Bydureon (weekly) 


    • Mechanism of Action

    • Directly agonise GLP-1 receptors, resulting in glucose-dependant insulin secretion.
  • The incretin hormones, glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic hormone (GIP), are released from the gastrointestinal tract. The incretins stimulate insulin secretion and inhibit glucagon secretion only under hyperglycaemic conditions, with additional effects of delayed gastric emptying, appetite suppression and weight loss.
  • These hormones normally have a short half-life as they are degraded by the enzyme dipeptidyl peptidase-4 (DPP-4).
    • Effects

    • Stimulation of insulin secretion in hyperglycaemia
    • Inhibition of glucagon secretion in hyperglucagonaemia
    • Slowed gastric emptying
    • Appetite suppression
    • Weight loss

Clinical Use

    • Indications

    • Glycaemic control for type II diabetics
    • Adjunctive therapy for weight loss
    • Adverse Effects

    • Hypoglycaemia
    • Headache
    • Reflux
    • Nausea / vomiting
    • Pancreatitis
Last updated on January 1st, 2017


The information in this section has been adapted in part from the Australian Therapeutic Goods Association website's repository of product information documents, which are available at https://www.ebs.tga.gov.au/ebs/picmi/picmirepository.nsf/PICMI.
 Bodenner D, Redman C, Riggs A. Teriparatide in the management of osteoporosis. Clinical Interventions in Aging. 2007;2(4):499-507. Brandi ML. Indications on the use of vitamin D and vitamin D metabolites in clinical phenotypes. Clinical Cases in Mineral and Bone Metabolism. 2010;7(3):243-250. Briet M, Schiffrin EL. Aldosterone: effects on the kidney and cardiovascular system. Nature Reviews Nephrology. 2010 May 1;6(5):261-73. Charles M Clark Jr. Oral therapy in type 2 diabetes: Pharmacological properties and clinical use of currently available agents. Diabetes Spectrum. 1998;11:211. Chisholm DJ. Thiazolidinediones - mechanisms of action. Australian prescriber. 2004; 27(3): 67. Crofton KM. Thyroid disrupting chemicals: mechanisms and mixtures. Int J Androl. 2008; 31: 209-223. Donner T. Insulin – Pharmacology, Therapeutic Regimens and Principles of Intensive Insulin Therapy. [Updated 2015 Oct 12]. In: De Groot LJ, Beck-Peccoz P, Chrousos G, et al., editors. Endotext [Internet]. South Dartmouth (MA): MDText.com, Inc.; 2000-. Available from: http://www.ncbi.nlm.nih.gov/books/NBK278938/ Drury DR. Mechanism of insulin action. Diabetes. 1955 May; 4(3): 203. Fonseca JE, Brandi ML. Mechanism of action of strontium ranelate: what are the facts? Clinical Cases in Mineral and Bone Metabolism. 2010;7(1):17-18. Frampton JE. Empagliflozin: a review in type 2 diabetes. Drugs. 2018 Jul 1;78(10):1037-48. Garber AJ. Long-acting glucagon-like peptide 1 receptor agonists: a review of their efficacy and tolerability. Diabetes care. 2011;34 Suppl 2:S279-S284. Gong L, Goswami S, Giacomini KM, Altman RB, Klein TE. Metformin pathways: pharmacokinetics and pharmacodynamics. Pharmacogenetics and Genomics. 2012;22:820-827. Grzybowska M. Metformin - mechanisms of action and use for the treatment of type 2 diabetes mellitus. Post?py higieny i medycyny do?wiadczalnej. 2011; 65: 277. Hanley DA, Adachi JD, Bell A, Brown V. Denosumab: mechanism of action and clinical outcomes. International Journal of Clinical Practice. 2012;66:1139-1146. Hardee JT, Barnett AL, Thannoun A, Eghtesad B, Wheeler D, Jamal MM. Propylthiouracil-induced hepatotoxicity. West J Med. 1996; 165: 144-147. John R. White J. Dipeptidyl Peptidase-IV Inhibitors: Pharmacological Profile and Clinical Use. Clinical Diabetes. 2008;26:53-57. Lebovitz HE. Sulfonylurea drugs: mechanism of antidiabetic action and therapeutic usefulness. Diabetes care. 1978 May; 1(3): 189. Martin T, Grill V. Bisphosphonates - mechanisms of action. Australian Prescriber. 2000; 23: 130. Reginster J. Strontium ranelate in osteoporosis.Current pharmaceutical design. 2002;8:1907. Russell RGG. Bisphosphonates: Mode of Action and Pharmacology. Pediatrics. 2007;119:S150-S162. Taurog A. The mechanism of action of the thioureylene antithyroid drugs. Endocrinology. 1976; 98(4): 1031-46.