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Tegaserod Pharmacokinetics Are Similar in Patients with Severe Renal Insufficiency and in Healthy Subjects
Author(s) -
Swan Suzanne K.,
Zhou Honghui,
Horowitz Ann,
Alladina Latifa,
Hubert Martine,
AppelDingemanse Silke,
Osborne Stuart,
Lambrecht Larry,
McLeod James F.
Publication year - 2003
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/0091270003251823
Subject(s) - tegaserod , medicine , cmax , pharmacokinetics , tolerability , partial agonist , adverse effect , gastroenterology , hemodialysis , agonist , irritable bowel syndrome , pharmacology , receptor
Tegaserod (HTF 919), a selective 5‐HT 4 receptor partial agonist with promotile activity throughout the gastrointestinal tract, is in development for the treatment of irritable bowel syndrome. In an open‐label, parallel‐group study, the pharmacokinetics of a single 12‐mg oral dose of tegaserod in patients with severe renal insufficiency requiring hemodialysis were compared with data obtained from healthy subjects matched for age, weight, height, and gender (n = 10, both). The pharmacokinetics of tegaserod were similar in both groups (AUC ( 0h‐tz ) , ng • h/ml: 14.6 ± 8.5 vs. 14.3 ± 7.1; C max , ng/ml: 4.6 ± 2.3 vs. 5.1 ± 2.2; t max , h: 1.0, for both). Tegaserod had similar tolerability in renally impaired patients and healthy volunteers, with adverse events largely related to the gastrointestinal pharmacological actions of the drug. Therefore, no dose adjustment of tegaserod is necessary for patients with renal insufficiency.