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Prophylactic use of anti‐emetic medications reduced nausea and vomiting associated with exenatide treatment: a retrospective analysis of an open‐label, parallel‐group, single‐dose study in healthy subjects
Author(s) -
Ellero C.,
Han J.,
Bhavsar S.,
Cirincione B. B.,
DeYoung M. B.,
Gray A. L.,
Yushmanova I.,
Anderson P. W.
Publication year - 2010
Publication title -
diabetic medicine
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.474
H-Index - 145
eISSN - 1464-5491
pISSN - 0742-3071
DOI - 10.1111/j.1464-5491.2010.03085.x
Subject(s) - medicine , exenatide , vomiting , nausea , anesthesia , retrospective cohort study , surgery , diabetes mellitus , type 2 diabetes , endocrinology
Diabet. Med. 27, 1168–1173 (2010) Abstract Aims Transient nausea and, to a lesser extent, vomiting are common adverse effects of exenatide that can be mitigated by dose titration and usually do not result in treatment discontinuation. This retrospective analysis of data from a phase 1, open‐label, parallel‐group, single‐dose study in healthy subjects evaluated the effect of oral anti‐emetics on exenatide‐associated nausea and vomiting and on the pharmacokinetics of exenatide. Methods A single subcutaneous dose (10 μg) of exenatide was administered to 120 healthy subjects (19–65 years, BMI 23–35 kg/m 2 ). Incidences of nausea and vomiting were compared between 60 subjects premedicated with two oral anti‐emetics 30 min before the exenatide dose and 60 non‐premedicated subjects. Similarly, the area under the concentration‐time curve (AUC) and the maximum observed concentration (C max ) of plasma exenatide concentrations over 8 h post‐dose were compared. Results Among all subjects [61% male, 32 ± 12 years, body mass index (BMI) 29.1 ± 3.4 kg/m 2 (mean ± sd )], mild to moderate nausea was the most frequent adverse event after exenatide dosing. Vomiting was also observed. Subjects premedicated with anti‐emetics experienced significantly less nausea and vomiting (16.7 and 6.7%, respectively) vs. non‐premedicated subjects (61.7 and 38.3%, respectively; P ‐value < 0.0001 for both nausea and vomiting). The mean area under the concentration‐time curve and the maximum observed concentration AUC and C max of plasma exenatide concentrations during 8 h post‐dose were not significantly different between groups. Conclusion Administration of oral anti‐emetics before a single 10‐μg exenatide dose was associated with significant reductions in treatment‐emergent nausea and vomiting, with no discernible effect on the pharmacokinetics of exenatide. Use of anti‐emetic therapy may provide a short‐term strategy to minimize the nausea and vomiting associated with exenatide treatment.