Can aprepitant used for nausea and vomiting be good gastrointestinal complaints?


UĞAN R. A., Un H., KÖSE D., ÇADIRCI E., Tastan T. B., Yayla M., ...Daha Fazla

NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, cilt.393, sa.12, ss.2463-2472, 2020 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 393 Sayı: 12
  • Basım Tarihi: 2020
  • Doi Numarası: 10.1007/s00210-020-01956-5
  • Dergi Adı: NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Agricultural & Environmental Science Database, BIOSIS, Biotechnology Research Abstracts, CAB Abstracts, Chemical Abstracts Core, Chimica, EMBASE, MEDLINE, Veterinary Science Database
  • Sayfa Sayıları: ss.2463-2472
  • Anahtar Kelimeler: Aprepitant, Rat, Cancer, Gastrointestinal complaints, SUBSTANCE-P, CYCLOOXYGENASE-2 EXPRESSION, GASTRIC HYPEREMIA, RECEPTOR, ULCER, ACID, LOCALIZATION, TACHYKININS, SECRETION, SYSTEM
  • Atatürk Üniversitesi Adresli: Evet

Özet

Aprepitant is a selective SP/NK-1 receptor antagonist and used in postoperative and chemotherapeutics induced emesis and vomiting. The aim of our study is to show aprepitant may have beneficial effects on gastrointestinal complaints in cancer patients undergoing chemotherapeutics by indomethacin-induced gastric ulcer model. A total of 48 rats were fasted 24 h for ulcer experiment. Aprepitant doses of 5, 10, 20, and 40 mg/kg were evaluated for their antiulcer activity. Omeprazole (20 mg/kg) was used as a positive control group. Six hours after 25 mg/kg indomethacin administration, all stomachs were dissected out. After macroscopic analyses, tumor necrosis factor-alpha (TNF-alpha), interleukin-1 beta (IL-1 beta), COX-1, and COX-2 mRNA levels and SOD activity, and GSH and MDA levels of stomachs were determined. Histopathological examinations were evaluated. Aprepitant administration exerted 48.14%, 49.62%, 65.92%, and 76.77% ulcer inhibition effects at 5, 10, 20, and 40 mg/kg, respectively. Aprepitant administration decreased oxidative stress and inflammatory parameters in stomach tissues dose dependently. Aprepitant administration increased stomach COX-2 mRNA levels at 20 and 40 mg/kg doses. Although aprepitant appears to be disadvantageous in terms of treating gastric ulcer due to COX enzyme inhibition according to the previous studies, aprepitant has been shown to have ulcer healing effect in our study. When aprepitant is given as an anti-nausea and vomiting drug to cancer patients undergoing chemotherapy, we can argue that it will not be necessary to add a new gastric protective agent as it also shows beneficial effects in gastrointestinal complaints.