Effect of cephalexin on the pharmacokinetics of metformin in healthy human volunteers.
The purpose of this study was to assess the effect of a single dose of cephalexin on the pharmacokinetics of metformin in healthy human volunteers. A 2 x 2 double blind randomized crossover study was conducted in 12 healthy human volunteers. Each subject received orally either 500 mg of metformin with a placebo or a combination of 500 mg of metformin and 500 mg of cephalexin. Serum and urine levels of metformin were estimated by a validated HPLC method. The systemic disposition of metformin was altered by the co-administration of cephalexin. Cephalexin increased Cmax and AUC by an average of 34% and 24%, respectively, and reduced renal clearance to 14%. The renal clearance of metformin was reduced in a time-dependent manner in the presence of cephalexin. Hence, it is concluded that cephalexin inhibits the renal tubular secretion of metformin resulting in higher circulating serum concentrations.
Jayasagar
G
G
University College of Pharmaceutical Sciences, Kakatiya University, Warangal, AP, India.
Krishna Kumar
M
M
Chandrasekhar
K
K
Madhusudan Rao
C
C
Madhusudan Rao
Y
Y
D019540:Area Under Curve; D002506:Cephalexin / Q000494:pharmacology*; D002511:Cephalosporins / Q000494:pharmacology*; D002851:Chromatography, High Pressure Liquid; D018592:Cross-Over Studies; D004311:Double-Blind Method; D004347:Drug Interactions; D006801:Humans; D007004:Hypoglycemic Agents / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D007668:Kidney / Q000378:metabolism; D008297:Male; D008687:Metformin / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine
D002511:Cephalosporins; D007004:Hypoglycemic Agents; D008687:Metformin; D002506:Cephalexin