title: Effect of a single-dose rifampin on the pharmacokinetics of pitavastatin in healthy volunteers.
abstract: OBJECTIVE
  As an inhibitor of HMG-CoA reductase that catalyses the first step of cholesterol synthesis, pitavastatin undergoes little hepatic metabolism; however, it is a substrate of uptake and efflux transporters. Since pitavastatin is potentially co-administered with agents that affect transporter activities, the pharmacokinetics of pitavastatin was investigated on the effects of a single-dose rifampin in healthy volunteers.
  
  
  METHODS
  Twelve Chinese healthy male volunteers took 4 mg pitavastatin orally with 150 ml water or with a single dose of 600 mg rifampin on separate occasions and the plasma concentrations of pitavastatin were measured over 48 h by HPLC-MS/MS.
  
  
  RESULTS
  A single dose of rifampin significantly increased the mean area under the plasma concentration-time curve(AUC)(0-48 h) and Cmax of pitavastatin by 573.5 %(95%CI, 373.3-773.7 %, p < 0.001) and 819.2 %(95 % CI, 515.4-1123.0 %, p < 0.001) respectively, while significantly decreased the t1/2 and CL/F of pitavastatin by 38.8 % (95 % CI, 18.2-59.4 %, p < 0.001) and 81.4 % (95 % CI, 75.0-87.7 %, p < 0.001) respectively.
  
  
  CONCLUSIONS
  Co-administration of pitavastatin with a single dose of rifampin resulted in a significant increase in plasma levels of pitavastatin in Chinese healthy subjects.
authors.affiliation: Institute of Clinical Pharmacology, Central South University, Xiang-Ya School of medicine, 110 Xiang-Ya road, Changsha, Hunan, 410078, People's Republic of China.
authors.forename: Yao
authors.initials: Y
authors.lastname: Chen
authors.forename: Wei
authors.initials: W
authors.lastname: Zhang
authors.forename: Wei-hua
authors.initials: WH
authors.lastname: Huang
authors.forename: Zhi-rong
authors.initials: ZR
authors.lastname: Tan
authors.forename: Yi-cheng
authors.initials: YC
authors.lastname: Wang
authors.forename: Xi
authors.initials: X
authors.lastname: Huang
authors.forename: Hong-Hao
authors.initials: HH
authors.lastname: Zhou
mesh_terms: D000328:Adult; D018592:Cross-Over Studies; D004347:Drug Interactions; D064368:Healthy Volunteers; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000097:blood / Q000493:pharmacokinetics*; D027381:Liver-Specific Organic Anion Transporter 1; D008297:Male; D027361:Organic Anion Transporters / Q000037:antagonists & inhibitors; D011804:Quinolines / Q000097:blood / Q000493:pharmacokinetics*; D012293:Rifampin / Q000494:pharmacology*; D055815:Young Adult
chemical_list: D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D027381:Liver-Specific Organic Anion Transporter 1; D027361:Organic Anion Transporters; D011804:Quinolines; C503999:SLCO1B1 protein, human; C108475:pitavastatin; D012293:Rifampin