title: Population pharmacokinetics and prophylactic anti-emetic efficacy of ramosetron in surgical patients.
abstract: This study characterized the pharmacokinetics of ramosetron and compared prophylactic anti-emetic efficacy with that of ondansetron in a large population.
  
  
  
  Fifty-eight patients consented to the pharmacokinetic analysis and were assigned randomly to receive 0.3, 0.45 or 0.6 mg ramosetron after induction of anaesthesia. Blood samples were acquired at preset intervals. Non-compartmental and population pharmacokinetic analyses were performed. In total, 1102 patients consented to the evaluation of prophylactic anti-emetic efficacy and were allocated randomly to receive 0.3 mg ramosetron or 4 mg ondansetron at the end of surgery. An additional 16 mg ondansetron were mixed in the intravenous patient-controlled analgesia pump of the ondansetron group. Post-operative nausea and vomiting (PONV) were evaluated 6, 24 and 48 h post-operatively using the Rhodes index of nausea, vomiting and retching (RINVR). Administration of rescue anti-emetics and adverse events were evaluated.
  
  
  
  The pharmacokinetic parameter estimates were V1 (l) = 5.12, V2 (l) = 108, CL (l⋅min(-1) ) = 0.08 + (59⋅age(-1) ) × 0.09, Q (l⋅min(-1) ) = 1.42. The incidences of PONV in the ramosetron and ondansetron groups were 77 (13.9%) and 113 (20.6%) and 44 (7.9%) and 66 (12.0%) at 24 and 48 h post-operatively, respectively (P = 0.004, 0.030). RINVR was significantly lower in the ramosetron than the ondansetron group 24 and 48 h post-operatively (P = 0.003, 0.025). Use of rescue anti-emetics and incidence of adverse events were comparable.
  
  
  
  A two compartment mammillary model was used to describe ramosetron pharmacokinetics. Prophylactic anti-emetic efficacy of ramosetron was significantly better 24 and 48 h post-operatively than that of ondansetron, particularly when the Apfel score was ≥ 3.
authors.affiliation: Department of Anaesthesiology and Pain Medicine, Asan Medical Centre, University of Ulsan College of Medicine, Seoul.
authors.forename: Yong-Hun
authors.initials: YH
authors.lastname: Lee
authors.affiliation: Intern, Asan Medical Centre, Seoul.
authors.forename: Jae-Hyeon
authors.initials: JH
authors.lastname: Seo
authors.affiliation: Department of Anaesthesiology and Pain Medicine, Severance Hospital, Yonsei University College of Medicine, Seoul.
authors.forename: Kyung-Tae
authors.initials: KT
authors.lastname: Min
authors.affiliation: Department of Anaesthesiology and Pain Medicine, Seoul National University Hospital, Seoul National University College of Medicine, Seoul.
authors.forename: Young-Jin
authors.initials: YJ
authors.lastname: Lim
authors.affiliation: Department of Anaesthesiology and Pain Medicine, Chonnam National University Hwasun Hospital, Chonnam National University Medical School, Gwangju.
authors.forename: Seong-Wook
authors.initials: SW
authors.lastname: Jeong
authors.affiliation: Department of Statistics, Ewha Woman's University, Seoul.
authors.forename: Eun-Kyung
authors.initials: EK
authors.lastname: Lee
authors.affiliation: Department of Anaesthesiology and Pain Medicine, Asan Medical Centre, University of Ulsan College of Medicine, Seoul.
authors.forename: Byung-Moon
authors.initials: BM
authors.lastname: Choi
authors.affiliation: Department of Anaesthesiology and Pain Medicine, Department of Clinical Pharmacology and Therapeutics, Asan Medical Centre, University of Ulsan College of Medicine, Seoul, South Korea.
authors.forename: Gyu-Jeong
authors.initials: GJ
authors.lastname: Noh
mesh_terms: D000932:Antiemetics / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics / Q000627:therapeutic use; D001562:Benzimidazoles / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D004311:Double-Blind Method; D005260:Female; D006801:Humans; D008297:Male; D008875:Middle Aged; D008954:Models, Biological; D017294:Ondansetron / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics / Q000627:therapeutic use; D020250:Postoperative Nausea and Vomiting / Q000097:blood / Q000517:prevention & control*
chemical_list: D000932:Antiemetics; D001562:Benzimidazoles; D017294:Ondansetron; C071315:ramosetron
keywords: anti-emetics; pharmacokinetics; post-operative nausea and vomiting; ramosetron