Clinical Pharmacokinetics of Metformin

  title={Clinical Pharmacokinetics of Metformin},
  author={Garry G Graham and Jeroen M Punt and Manit Arora and Richard Osborne Day and Matthew P. Doogue and Janna K Duong and Timothy J. Furlong and Jerry R. Greenfield and Louise C. Greenup and Carl M J Kirkpatrick and John E. Ray and Peter Timmins and Kenneth Mapson Williams},
  journal={Clinical Pharmacokinetics},
Metformin is widely used for the treatment of type 2 diabetes mellitus. [] Key Result The population mean renal clearance (CLR) and apparent total clearance after oral administration (CL/F) of metformin were estimated to be 510 ± 130 mL/min and 1140 ± 330 mL/min, respectively, in healthy subjects and diabetic patients with good renal function.

Pharmacokinetics of metformin in the rat: assessment of the effect of hyperlipidemia and evidence for its metabolism to guanylurea.

Hyperlipidemia by itself did not affect the pharmacokinetics of metformin, and comparative chromatographic elution times and mass spectra suggested that one of the predominant metabolites was guanylurea.

Effect of plasma membrane monoamine transporter genetic variants on pharmacokinetics of metformin in humans

The genetic variation of c.883-144A>G SNP in PMAT significantly affects the renal clearance of metformin in healthy Korean male subjects, and the role of PMAT genetic variations on the pharmacokinetic characteristics of metforms in a Korean population is evaluated.

Mechanism of Metformin: A Tale of Two Sites

Surprising results from their clinical trials suggest the primary effect of metformin resides in the human gut, as well as counteracting the cardiovascular complications of type 2 diabetes.

Clinical Pharmacokinetics of Metformin

  • T. Sheleme
  • Medicine, Biology
    Metformin - Pharmacology and Drug Interactions
  • 2021
The elimination half-life of Metformin during multiple dosages in patients with good renal function is approximately 5 hours, and it is rapidly distributed following absorption and does not bind to plasma proteins.

Population pharmacokinetics and dosing optimization of metformin in Chinese patients with type 2 diabetes mellitus

The results of the simulation showed that patients with type 2 diabetes mellitus administered metformin twice a day require higher total daily doses than those with a regimen of 3 times a day at each stage of kidney function, and eGFR had a significant impact on meetformin pharmacokinetics.

Metformin Sinusoidal Efflux from the Liver Is Consistent with Negligible Biliary Excretion and Absence of Enterohepatic Cycling

It is demonstrated that despite similar magnitude of metformin liver and kidney distribution, met formin biliary excretion is negligible due to predominant sinusoidal efflux from the liver.

Metformin and its gastrointestinal problems: A review

It is used clinically in diabetes, polycystic ovary syndrome, and in obese for weight reduction and has cardioprotective effect and its use is recently being studied in cancer and HIV associated metabolic abnormalities.

Population Pharmacokinetics of Metformin in Mexican Patients with Type 2 Diabetes Mellitus

In the PPM of metformin in Mexican patients with T2DM here described, the covariates, LBW and CLcr had a significant influence on interindividual variability of V/F and CL/F.

Investigation of possible pharmacokinetic interaction of metformin with sugar replacement sweeteners in rats.

Investigation of possible effects of two types of sweeteners; stevia and aspartame on the pharmacokinetic parameters of metformin in rats showed that administration of these two sweeteners did not have high effect on pharmacokinetics of meetformin.

Pharmacokinetic interaction between telithromycin and metformin in diabetes mellitus rats

  • J. H. LeeH. KangM. Lee
  • Biology, Medicine
    Xenobiotica; the fate of foreign compounds in biological systems
  • 2010
After the oral and intravenous administration of both drugs together, the total area under the plasma concentration–time curve (AUC) of metformin was comparable possibly due to the increased intestinal metabolism of met formin by telithromycin.



Pharmacokinetics of metformin after intravenous and oral administration to man

The kinetics of14C-metformin have been studied in five healthy subjects after oral and intravenous administration, which resulted in a plasma concentration profile of “flip-flop” type for oral metformin.

Involvement of Organic Cation Transporter 1 in Hepatic and Intestinal Distribution of Metformin

It is suggested that Oct1 is responsible for the hepatic uptake as well as playing a role in the intestinal uptake of metformin, whereas the renal distribution and excretion are mainly governed by other transport mechanism(s).

Kidney Function and Age Are Both Predictors of Pharmacokinetics of Metformin

Both creatinine clearance (CLcr*; corrected for body surface area) and age are predictors of metformin clearance, with the following model best fitting the data: CL/F [or (CL/F)b, CLR, CLR] = α + β·CLCr* + γ · CLcr*·age.

Effect of Cephalexin on the Pharmacokinetics of Metformin in Healthy Human Volunteers

It is concluded that cephalexin inhibits the renal tubular secretion of metformin resulting in higher circulating serum concentrations and is responsible for the increase in Cmax and AUC in healthy human volunteers.

Effect of food on the pharmacokinetics of a vildagliptin/metformin (50/1000 mg) fixed-dose combination tablet in healthy volunteers

The vildagliptin/metformin (50/1000 mg) fixed-dose combination tablet can be administered in the same manner as metformin, and can be recommended to be taken with meals to reduce the gastrointestinal symptoms associated with metformIn.

Disposition of metformin (N,N‐dimethylbiguanide) in man

Kinetic parameters ol metformin (N,N‐dimethylbiguanide), an anti‐diabetic reported to be associated with a lower number of episodes of lactic acidosis than phenformin, were determined in volunteers with normal renal function and in patients with different degrees ol renal impairment, to help explain the lower incidence of toxic effects.

Metformin kinetics in healthy subjects and in patients with diabetes mellitus.

Plasma metformin concentrations measured throughout the seventh and fourteenth days of continuous 0.5 g twice daily treatment were accurately predicted from single dose data, although a discrepancy between observed and predicted trough levels reflected the existence of a slow elimination phase.

Clinical Pharmacokinetics and Pharmacodynamics of Allopurinol and Oxypurinol

Measurement of plasma concentrations of oxypurinol in selected patients, particularly those with renal impairment, may help to decrease the risk of toxicity and improve the hypouricaemic response.