Population pharmacokinetics of metformin in healthy subjects and patients with type 2 diabetes mellitus: Simulation of doses according to renal function

Clinical Pharmacokinetics

Volumn 52, Issue 5, 2013, Pages 373-384

  Duong, Janna K ^a,b   Kumar, Shaun S ^a,b   Kirkpatrick, Carl M ^c   Greenup, Louise C ^b   Arora, Manit ^a   Lee, Toong C ^d   Timmins, Peter ^e   Graham, Garry G ^a,b   Furlong, Timothy J ^b   Greenfield, Jerry R ^b,f   Williams, Kenneth M ^a,b   Day, Richard O ^a,b  

^a UNIVERSITY OF NEW SOUTH WALES   (Australia)

^b ST VINCENT S HOSPITAL   (Australia)

^c MONASH UNIVERSITY   (Australia)

^d SCHOOL OF PHYSICS   (Malaysia)

^e BRISTOL MYERS SQUIBB   (United States)

^f GARVAN INSTITUTE OF MEDICAL RESEARCH   (Australia)

Author keywords

[No Author keywords available]

Indexed keywords

CREATININE; METFORMIN; ANTIDIABETIC AGENT; CARRIER PROTEIN;

ADULT; AGED; ARTICLE; BODY WEIGHT; CAUCASIAN; CONTROLLED STUDY; CREATININE CLEARANCE; DIABETES CONTROL; DRUG FORMULATION; HUMAN; KIDNEY FUNCTION; LEAN BODY WEIGHT; MAJOR CLINICAL STUDY; NON INSULIN DEPENDENT DIABETES MELLITUS; PLASMA CONCENTRATION-TIME CURVE; PRIORITY JOURNAL; SINGLE NUCLEOTIDE POLYMORPHISM; ADOLESCENT; BIOLOGICAL MODEL; COMPARATIVE STUDY; CONTROLLED CLINICAL TRIAL; DELAYED RELEASE FORMULATION; DOSE RESPONSE; GENETICS; KIDNEY FAILURE; MALAYSIA; MIDDLE AGED; NONLINEAR SYSTEM; PATHOPHYSIOLOGY; TISSUE DISTRIBUTION; VERY ELDERLY;

ADOLESCENT; ADULT; AGED; AGED, 80 AND OVER; DELAYED-ACTION PREPARATIONS; DIABETES MELLITUS, TYPE 2; DOSE-RESPONSE RELATIONSHIP, DRUG; EUROPEAN CONTINENTAL ANCESTRY GROUP; HUMANS; HYPOGLYCEMIC AGENTS; MALAYSIA; MEMBRANE TRANSPORT PROTEINS; METFORMIN; MIDDLE AGED; MODELS, BIOLOGICAL; NONLINEAR DYNAMICS; POLYMORPHISM, SINGLE NUCLEOTIDE; RENAL INSUFFICIENCY; TISSUE DISTRIBUTION; YOUNG ADULT;

EID: 84886992019     PISSN: 03125963     EISSN: 11791926     Source Type: Journal    
DOI: 10.1007/s40262-013-0046-9     Document Type: Article

References (41)

1. World Health Organization. Diabetes fact sheet no. 312. 2012. http://www.who.int/mediacentre/factsheets/fs312/en/index.html. Accessed 19 Feb 2012
2. Hundal RS, Krssak M, Dufour S, et al. Mechanism by which metformin reduces glucose production in type 2 diabetes. Diabetes. 2000;49(12):2063-9.
3. Effect of intensive blood-glucose control with metformin on complications in overweight patients with type 2 diabetes (UKPDS 34). UK Prospective Diabetes Study (UKPDS) Group. Lancet. 1998;352(9131):854-65.
4. Diabex tablets. Carole Park, Australia: Alphapharm Pty Ltd; 2012
5. Bruijstens LA, van Luin M, Buscher-Jungerhans PM, et al. Reality of severe metformin-induced lactic acidosis in the absence of chronic renal impairment. Neth J Med. 2008;66(5):185-90.
6. Graham GG, Punt J, Arora M, et al. Clinical pharmacokinetics of metformin. Clin Pharmacokinet. 2011;50(2):81-98.
7. Tzvetkov MV, Vormfelde SV, Balen D, et al. The effects of genetic polymorphisms in the organic cation transporters OCT1, OCT2, and OCT3 on the renal clearance of metformin. Clin Pharmacol Ther. 2009;86(3):299-306.
8. Zhou M, Xia L, Wang J. Metformin transport by a newly cloned proton-stimulated organic cation transporter (plasma membrane monoamine transporter) expressed in human intestine. Drug Metab Dispos. 2007;35(10):1956-62.
9. Bardin C, Nobecourt E, Larger E, et al. Population pharmacokinetics of metformin in obese and non-obese patients with type 2 diabetes mellitus. Eur J Clin Pharmacol. 2012;68(6):961-8.
10. Tucker GT, Casey C, Phillips PJ, et al. Metformin kinetics in healthy subjects and in patients with diabetes mellitus. Br J Clin Pharmacol. 1981;12(2):235-46.
11. Timmins P, Donahue S, Meeker J, et al. Steady-state pharmacokinetics of a novel extended-release metformin formulation. Clin Pharmacokinet. 2005;44(7):721-9.
12. Shu Y, Brown C, Castro RA, et al. Effect of genetic variation in the organic cation transporter 1, OCT1, on metformin pharmacokinetics. Clin Pharmacol Ther. 2008;83(2):273-80.
13. Sambol NC, Chiang J, O'Conner M, et al. Pharmacokinetics and pharmacodynamics of metformin in healthy subjects and patients with noninsulin-dependent diabetes mellitus. J Clin Pharmacol. 1996;36(11):1012-21.
14. Hong Y, Rohatagi S, Habtemariam B, et al. Population exposure-response modeling of metformin in patients with type 2 diabetes mellitus. J Clin Pharmacol. 2008;48(6):696-707.
15. Christensen MM, Brasch-Andersen C, Green H, et al. The pharmacogenetics of metformin and its impact on plasma metformin steady-state levels and glycosylated hemoglobin A1c. Pharmacogenet Genomics. 2011;21(12):837-50.
16. Lalau JD, Lemaire-Hurtel AS, Lacroix C. Establishment of a database of metformin plasma concentrations and erythrocyte levels in normal and emergency situations. Clin Drug Investig. 2011;31(6):435-8.
17. Duong JK, Roberts DM, Furlong TJ, et al. Metformin therapy in patients with chronic kidney disease. Diabetes Obes Metab. 2012;15(10):963-5.
18. Zarghi A, Foroutan SM, Shafaati A, et al. Rapid determination of metformin in human plasma using ion-pair HPLC. J Pharm Biomed Anal. 2003;31(1):197-200.
19. Boeckman A, Sheiner A, Beal S. NONMEM 6. Ellicott City: GloboMax, ICON Development Solutions; 2007.
20. Wang Y. Derivation of various NONMEM estimation methods. J Pharmacokinet Pharmacodyn. 2007;34(5):575-93.
21. Cullberg M, Eriksson UG, Larsson M, et al. Population modelling of the effect of inogatran, at thrombin inhibitor, on ex vivo coagulation time (APTT) in healthy subjects and patients with coronary artery disease. Br J Clin Pharmacol. 2001;51(1):71-9.
22. Janmahasatian S, Duffull SB, Chagnac A, et al. Lean body mass normalizes the effect of obesity on renal function. Br J Clin Pharmacol. 2008;65(6):964-5.
23. Janmahasatian S, Duffull SB, Ash S, et al. Quantification of lean bodyweight. Clin Pharmacokinet. 2005;44(10):1051-65.
24. Cockcroft DW, Gault MH. Prediction of creatinine clearance from serum creatinine. Nephron. 1976;16(1):31-41.
25. Hooker AC, Staatz CE, Karlsson MO. Conditional weighted residuals (CWRES): a model diagnostic for the FOCE method. Pharm Res. 2007;24(12):2187-97.
26. Brendel K, Comets E, Laffont C, et al. Metrics for external model evaluation with an application to the population pharmacokinetics of gliclazide. Pharm Res. 2006;23(9):2036-49.
27. Henderson AR. The bootstrap: a technique for data-driven statistics. Using computer-intensive analyses to explore experimental data. Clin Chim Acta. 2005;359(1-2):1-26.
28. Wigginton JE, Cutler DJ, Abecasis GR. A note on exact tests of Hardy-Weinberg equilibrium. Am J Hum Genet. 2005;76(5):887-93.
29. Roos JF, Kirkpatrick CM, Tett SE, et al. Development of a sufficient design for estimation of fluconazole pharmacokinetics in people with HIV infection. Br J Clin Pharmacol. 2008;66(4):455-66.
30. Lalau JD, Lacroix C. Measurement of metformin concentration in erythrocytes: clinical implications. Diabetes Obes Metab. 2003;5(2):93-8.
31. Sambol NC, Chiang J, Lin ET, et al. Kidney function and age are both predictors of pharmacokinetics of metformin. J Clin Pharmacol. 1995;35(11):1094-102.
32. Bonate PL. The effect of collinearity on parameter estimates in nonlinear mixed effect models. Pharm Res. 1999;16(5):709-17.
33. Bricker NS, Morrin PA, Kime SW Jr. The pathologic physiology of chronic Bright's disease. An exposition of the "intact nephron hypothesis". Am J Med. 1960;28:77-98.
34. Nies AT, Koepsell H, Winter S, et al. Expression of organic cation transporters OCT1 (SLC22A1) and OCT3 (SLC22A3) is affected by genetic factors and cholestasis in human liver. Hepatology. 2009;50(4):1227-40.
35. Aoki M, Terada T, Kajiwara M, et al. Kidney-specific expression of human organic cation transporter 2 (OCT2/SLC22A2) is regulated by DNA methylation. Am J Physiol Ren Physiol. 2008;295(1):F165-70.
36. Kamber N, Davis WA, Bruce DG, et al. Metformin and lactic acidosis in an Australian community setting: the Fremantle Diabetes Study. Med J Aust. 2008;188(8):446-9.
37. Nye HJ, Herrington WG. Metformin: the safest hypoglycaemic agent in chronic kidney disease? Nephron Clin Pract. 2011;118(4):c380-3.
38. Rossi S. Australian medicines handbook 2011. Adelaide: Australian Medicines Handbook Pty Ltd; 2011.
39. Frid A, Sterner GN, Londahl M, et al. Novel assay of metformin levels in patients with type 2 diabetes and varying levels of renal function: clinical recommendations. Diabetes Care. 2010;33(6):1291-3.
40. Kamber N, Davis WA, Bruce DG, et al. Metformin and lactic acidosis in an Australian community setting: the Fremantle Diabetes Study. Med J Aust. 2008;188(8):446-9.
41. Briet C, Saraval-Gross M, Kajbaf F, et al. Erythrocyte metformin levels in patients with type 2 diabetes and varying severity of chronic kidney disease. Clin Kidney J. 2012;5(1):65-7.