Pharmacokinetics and Pharmacodynamics of Glyburide: Insights for Optimizing Treatment in Type 2 Diabetes
Abstract
Glyburide is a widely used oral antidiabetic agent for managing type 2 diabetes. Despite its long history, evolving insights into its pharmacokinetics (PK) and pharmacodynamics (PD) have highlighted knowledge gaps, especially in the context of genetic variability, drug-drug interactions, and use in special populations. This narrative scoping review synthesizes recent evidence to provide a comprehensive and updated understanding of glyburide’s PK/PD profiles. A thorough literature search of studies published in English, including manual reference checks, was conducted. Glyburide exhibits complex pharmacokinetics, extensive absorption throughout the gastrointestinal tract, significant plasma protein binding, hepatic metabolism via CYP2C9 and CYP3A4 enzymes, and predominantly renal elimination. Its pharmacodynamic effects involve stimulating insulin secretion and enhancing peripheral insulin sensitivity. Common side effects include hypoglycemia and weight gain, while drug-drug interactions and monitoring are crucial for safe and effective use. Understanding glyburide's pharmacokinetics and pharmacodynamics is key to optimizing diabetes management. Tailoring dosages based on patient factors can improve efficacy, minimize adverse effects, and enable personalized care. Further research on genetic influences, drug interactions, and its use in special populations is needed to refine treatment strategies and enhance safety and effectiveness.
Keywords
Full Text:
PDFReferences
Ahmed AM. History of diabetes mellitus. Saudi Med J. 2002 Apr;23(4):373–8. PMID: 11953758. 2002.
Olokoba AB, Obateru OA, Olokoba LB. Type 2 Diabetes Mellitus: A Review of Current Trends. Oman Medical Journal. 2012;27(4):269.
Alfaqeeh M, Alfian SD, Abdulah R. Factors associated with diabetes mellitus among adults: Findings from the Indonesian Family Life Survey-5. Endocrine and Metabolic Science. 2024;14:100161.
Subhashini B, Srinivas Ashok Kumar B, Mouna AA, Nawaz B. A review on type-2 diabetes mellitus and it’s management. World Journal of Pharmaceutical Research. 2023;12(5).
Patlak Scientific Advisor M, Hansen BC, Naider FR, Brautigan DL, Grossman J, Washington G, Hugli TE, Richard Lynch MG, Horwitz BA. Acknowledgments New Weapons to Combat an Ancient Disease: Treating Diabetes Breakthroughs in Bioscience Production Team. 2002.
Chen L, Magliano DJ, Zimmet PZ. The worldwide epidemiology of type 2 diabetes mellitus—present and future perspectives. Nature Reviews Endocrinology 2011 8:4. 2011;8(4):228–236.
Chiniwala N, Jabbour S. Management of diabetes mellitus in the elderly. Current Opinion in Endocrinology, Diabetes and Obesity. 2011;18(2):148–152.
Rambiritch V, Maharaj B, Naidoo P. glibenclamide in patients with poorly controlled type 2 diabetes: a 12-week, prospective, single-center, open-label, dose-escalation study. Clinical Pharmacology: Advances and Applications. 2014:6–63.
Sola D, Rossi L, Schianca GPC, Maffioli P, Bigliocca M, Mella R, Corlianò F, Fra GP, Bartoli E, Derosa G. State of the art paper Sulfonylureas and their use in clinical practice. Archives of Medical Science. 2015;4.
Jaber LA, Antal EJ, Slaughter RL, Welshman IR. Comparison of Pharmacokinetics and Pharmacodynamics of Short-and Long-Term Glyburide Therapy in NIDDM.; 1994.
Alfaqeeh M, Zakiyah N, Suwantika AA, Shabrina Z. Evaluation of Global Post-Outbreak COVID-19 Treatment Interventions: A Systematic Review and Bibliometric Analysis of Randomized Controlled Trials. Journal of Multidisciplinary Healthcare. 2023;16:4193–4209.
Galia E, Nicolaides E, Hörter D, Löbenberg R, Reppas C, Dressman JB. Evaluation of various dissolution media for predicting In vivo performance of class I and II drugs. Pharmaceutical Research. 1998;15(5):698–705.
Patterson JE, James MB, Forster AH, Lancaster RW, Butler JM, Rades T. The Influence of Thermal and Mechanical Preparative Techniques on the Amorphous State of Four Poorly Soluble Compounds. Journal of Pharmaceutical Sciences. 2005;94(9):1998–2012.
Brockmeier D, Grigoleit HG, Leonhardt H. Absorption of glibenclamide from different sites of the gastro-intestinal tract. European Journal of Clinical Pharmacology. 1985;29(2):193–197.
Löbenberg R, Krämer J, Shah VP, Amidon GL, Dressman JB. Dissolution testing as a prognostic tool for oral drug absorption: Dissolution behavior of glibenclamide. Pharmaceutical Research. 2000;17(4):439–444.
Niopas I, Daftsios AC. A validated high-performance liquid chromatographic method for the determination of glibenclamide in human plasma and its application to pharmacokinetic studies. Journal of Pharmaceutical and Biomedical Analysis. 2002;28(3–4):653–657.
Albu F, Georgiţǎ C, David V, Medvedovici A. Determination of glibenclamide in human plasma by liquid chromatography and atmospheric pressure chemical ionization/MS-MS detection. Journal of Chromatography B. 2007;846(1–2):222–229.
Rashid A, Ahmad M, Usman Minhas M, Javed Hassan I, Zubair Malik M. Pharmacokinetic studies of metformin and glibenclamide in normal human volunteers. Pak. J. Pharm. Sci. 2014;27(1):153–159.
Jönsson A, Rydberg T, Sterner G, Melander A. Pharmacokinetics of glibenclamide and its metabolites in diabetic patients with impaired renal function. European Journal of Clinical Pharmacology. 1998;53(6):429–435.
Niemi M, Cascorbi I, Timm R, Kroemer HK, Neuvonen PJ, Kivistö KT. Glyburide and glimepiride pharmacokinetics in subjects with different CYP2C9 genotypes. Clinical Pharmacology & Therapeutics. 2002;72(3):326–332.
Hirota T, Eguchi S, Ieiri I. Impact of Genetic Polymorphisms in CYP2C9 and CYP2C19 on the Pharmacokinetics of Clinically Used Drugs. Drug Metabolism and Pharmacokinetics. 2013;28(1):28–37.
Squassina A, Manchia M, Manolopoulos VG, Artac M, Lappa-Manakou C, Karkabouna S, Mitropoulos K, Zompo M Del, Patrinos GP. Realities and Expectations of Pharmacogenomics and Personalized Medicine: Impact of Translating Genetic Knowledge into Clinical Practice. Pharmacogenomics. 2010;11(8):1149–1167.
Zhou L, Naraharisetti SB, Liu L, Wang H, Lin YS, Isoherranen N, Unadkat JD, Hebert MF, Mao Q. Contributions of human cytochrome P450 enzymes to glyburide metabolism. Biopharmaceutics & Drug Disposition. 2010;31(4):228–242.
D’Souza MR. Traditional Indian Herbs for the Management of Diabetes Mellitus and their Herb–Drug Interaction Potentials: An Evidence-Based Review. Structure and Health Effects of Natural Products on Diabetes Mellitus. 2021:279–296.
Scheen AJ. Pharmacokinetic and toxicological considerations for the treatment of diabetes in patients with liver disease. Expert Opinion on Drug Metabolism & Toxicology. 2014;10(6):839–857.
Snyder RW, Berns JS. Reviews: Use of Insulin and Oral Hypoglycemic Medications in Patients with Diabetes Mellitus and Advanced Kidney Disease. Seminars in Dialysis. 2004;17(5):365–370.
Helal KF, Badr MS, Rafeek MES, Elnagar WM, Lashin MEB. Can glyburide be advocated over subcutaneous insulin for perinatal outcomes of women with gestational diabetes? A systematic review and meta-analysis. Archives of Gynecology and Obstetrics. 2020;301(1):19–32.
Eliasson L, Renström E, Ämmälä C, Berggren PO, Bertorello AM, Bokvist K, Chibalin A, Deeney JT, Flatt PR, Gäbel J, Gromada J, Larsson O, Lindström P, Rhodes CJ, Rorsman P. PKC-Dependent Stimulation of Exocytosis by Sulfonylureas in Pancreatic β Cells. Science. 1996;271(5250):813–815.
Luzi L, Pozza G. Glibenclamide: An old drug with a novel mechanism of action? Acta Diabetologica. 1997;34(4):239–244.
Su J, Xu J, Hu S, Ye H, Xie L, Ouyang S. Advances in small-molecule insulin secretagogues for diabetes treatment. Biomedicine & Pharmacotherapy. 2024;178:117179.
Rodríguez E, Pulido N, Romero R, Arrieta F, Panadero A, Rovira A. Phosphatidylinositol 3-Kinase Activation Is Required for Sulfonylurea Stimulation of Glucose Transport in Rat Skeletal Muscle. Endocrinology. 2004;145(2):679–685.
Meneilly GS, Bryer-Ash M, Elahi D. The Effect of Glyburide on β-Cell Sensitivity to Glucose-Dependent Insulinotropic Polypeptide. Diabetes Care. 1993;16(1):110–114.
Lorenzati B, Zucco C, Miglietta S, Lamberti F, Bruno G. Oral Hypoglycemic Drugs: Pathophysiological Basis of Their Mechanism of ActionOral Hypoglycemic Drugs: Pathophysiological Basis of Their Mechanism of Action. Pharmaceuticals. 2010;3(9):3005–3020.
Rorsman P, Ashcroft FM. Pancreatic β-cell electrical activity and insulin secretion: Of mice and men. Physiological Reviews. 2018;98(1):117–214.
Campbell JE, Newgard CB. Mechanisms controlling pancreatic islet cell function in insulin secretion. Nature Reviews Molecular Cell Biology 2021 22:2. 2021;22(2):142–158.
Hamnvik OPR, McMahon GT. Balancing Risk and Benefit with Oral Hypoglycemic Drugs. Mount Sinai Journal of Medicine: A Journal of Translational and Personalized Medicine. 2009;76(3):234–243.
Garber AJ, Donovan DS, Dandona P, Bruce S, Park JS. Efficacy of Glyburide/Metformin Tablets Compared with Initial Monotherapy in Type 2 Diabetes. The Journal of Clinical Endocrinology & Metabolism. 2003;88(8):3598–3604.
Fonseca V. Effect of thiazolidinediones on body weight in patients with diabetes mellitus. The American Journal of Medicine. 2003;115(8):42–48.
Gangji AS, Cukierman T, Gerstein HC, Goldsmith CH, Clase CM. A Systematic Review and Meta-Analysis of Hypoglycemia and Cardiovascular EventsA comparison of glyburide with other secretagogues and with insulin. Diabetes Care. 2007;30(2):389–394.
Raee MR, Nargesi AA, Heidari B, Mansournia MA, Larry M, Rabizadeh S, et al. All-Cause and Cardiovascular Mortality following Treatment with Metformin or Glyburide in Patients with Type 2 Diabetes Mellitus. Arch Iran Med. 2017;20(3):141–146.
Hedrington MS, Davis SN. The care of pregestational and gestational diabetes and drug metabolism considerations. Expert Opinion on Drug Metabolism & Toxicology. 2017;13(10):1029–1038.
Song R, Chen L, Chen Y, Si X, Liu Y, Liu Y, Irwin DM, Feng W. Comparison of glyburide and insulin in the management of gestational diabetes: A meta-analysis. PLoS ONE. 2017;12(8).
Tsakiridis I, Mamopoulos A, Athanasiadis A, Kourtis A, Dagklis T. Management of pregestational diabetes mellitus: a comparison of guidelines. Journal of Maternal-Fetal and Neonatal Medicine. 2022;35(3).
Guo L, Ma J, Tang J, Hu D, Zhang W, Zhao X. Comparative Efficacy and Safety of Metformin, Glyburide, and Insulin in Treating Gestational Diabetes Mellitus: A Meta-Analysis. Journal of Diabetes Research. 2019;2019.
Butalia S, Gutierrez L, Lodha A, Aitken E, Zakariasen A, Donovan L. Short- and long-term outcomes of metformin compared with insulin alone in pregnancy: a systematic review and meta-analysis. Diabetic Medicine. 2017;34(1):27–36.
Blumer I, Hadar E, Hadden DR, Jovanovič L, Mestman JH, Murad MH, Yogev Y. Diabetes and Pregnancy: An Endocrine Society Clinical Practice Guideline. The Journal of Clinical Endocrinology & Metabolism. 2013;98(11):4227–4249.
Wulf NR, Matuszewski KA. Sulfonamide cross-reactivity: Is there evidence to support broad cross-allergenicity? American Journal of Health-System Pharmacy. 2013;70(17):1483–1494.
Lebovitz HE. Glipizide: A Second-generation Sulfonylurea Hypoglycemic Agent; Pharmacology, Pharmacokinetics and Clinical Use. Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy. 1985;5(2):63–77.
Baciewicz AM, Chrisman CR, Finch CK, Self TH. Update on rifampin, rifabutin, and rifapentine drug interactions. Current Medical Research and Opinion. 2013;29(1):1–12.
May M, Schindler C. Clinically and pharmacologically relevant interactions of antidiabetic drugs. Therapeutic Advances in Endocrinology and Metabolism. 2016;7(2):69–83.
Sola D, Rossi L, Schianca GPC, Maffioli P, Bigliocca M, Mella R, Corlianò F, Paolo Fra G, Bartoli E, Derosa G. Sulfonylureas and their use in clinical practice. Archives of Medical Science. 2015;11(4):840–848.
Mansouri D, Khayat E, Khayat M, Aboawja M, Aseeri A, Banah F, et al. Self-monitoring of blood glucose and hypoglycemia association during fasting in ramadan among patients with diabetes. Diabetes, Metabolic Syndrome and Obesity. 2020;13:1035–1041.
Inzucchi SE, Bergenstal RM, Buse JB, Diamant M, Ferrannini E, Nauck M, Peters AL, Tsapas A, Wender R, Matthews DR. Management of Hyperglycemia in Type 2 Diabetes: A Patient-Centered Approach: Position Statement of the American Diabetes Association (ADA) and the European Association for the Study of Diabetes (EASD). Diabetes Spectrum. 2012;25(3):154–171.
Alfaqeeh M, Alfian SD, Abdulah R. Factors Associated with Hypertension Among Adults: A Cross-Sectional Analysis of the Indonesian Family Life Survey. Vascular Health and Risk Management. 2023;19:827–836.
Chakraborty C, J. Hsu M, Agoramoorthy G. Drug Metabolizing Enzymes in Type II Diabetes and their Pharmacogenetics During Therapy of Anti-Diabetes Drugs. 2015.
Fodor A, Cozma A, Suharoschi R, Sitar-Taut A, Roman G. Clinical and genetic predictors of diabetes drug’s response. Drug Metabolism Reviews. 2019;51(4):408–427.
Venkatachalapathy P, Padhilahouse S, Sellappan M, Subramanian T, Kurian SJ, Miraj SS, Rao M, Raut AA, Kanwar RK, Singh J, Khadanga S, Mondithoka S, Munisamy M. Pharmacogenomics and personalized medicine in type 2 diabetes mellitus: Potential implications for clinical practice. Pharmacogenomics and Personalized Medicine. 2021;14:1441–1455.
Manitpisitkul P, Curtin CR, Shalayda K, Wang SS, Ford L, Heald DL. An open-label drug-drug interaction study of the steady-state pharmacokinetics of topiramate and glyburide in patients with type 2 diabetes mellitus. Clinical drug investigation. 2013;33(12):929–938.
Kristin K. Clemens. Antihyperglycemic Medications and Hypoglycemia in Older Adults with Diabetes - ProQuest.
Cappon G, Vettoretti M, Sparacino G, Facchinetti A. Continuous Glucose Monitoring Sensors for Diabetes Management: A Review of Technologies and Applications. Diabetes & Metabolism Journal. 2019;43(4):383.
Alomar MJ. Factors affecting the development of adverse drug reactions (Review article). Saudi Pharmaceutical Journal. 2014;22(2):83–94.
Castillo WC, Boggess K, Stürmer T, Brookhart MA, Benjamin DK, Funk MJ. Association of Adverse Pregnancy Outcomes With Glyburide vs Insulin in Women With Gestational Diabetes. JAMA Pediatrics. 2015;169(5):452–458.
Malek R, Davis SN. Pharmacokinetics, efficacy and safety of glyburide for treatment of gestational diabetes mellitus. Expert Opinion on Drug Metabolism & Toxicology. 2016;12(6):691–699.
Armstrong K. Methods in comparative effectiveness research. Journal of Clinical Oncology. 2012;30(34):4208–4214.
Gao R, Yang T, Xu W. Enemies or weapons in hands: investigational anti-diabetic drug glibenclamide and cancer risk. Expert Opinion on Investigational Drugs. 2017;26(7):853–864.
DOI: https://doi.org/10.15416/ijcp.2024.13.2.48713
Refbacks
- There are currently no refbacks.
Indonesian Journal of Clinical Pharmacy is indexed by
