A pharmacological overview of aprepitant for the prevention of postoperative nausea and vomiting

ABSTRACT

Introduction

Post-operative nausea and vomiting (PONV) affects 30% of all patients undergoing surgery and up to 80% of high-risk patients. Antiemetics for PONV prophylaxis target a variety of receptor systems, with varying degrees of efficacy and side effect profile. Neurokinin −1 receptor antagonists are the most recent class of compounds investigated for PONV prophylaxis, with aprepitant being the only one currently approved for this indication.

Areas covered

This review covers the pathophysiology of PONV, current recommendations for PONV prophylaxis, pharmacokinetics, and pharmacodynamics of aprepitant, and the evidence for its efficacy in the management of PONV as a single agent and in combination therapy.

Expert opinion

Aprepitant is effective for PONV prophylaxis. It has superior antivomiting efficacy, long half-life, and favorable side effect profile. Data on antiemetic combinations involving aprepitant are limited, and it is not clear if the addition of other antiemetics to aprepitant results in improved PONV prophylaxis. The oral route of administration of aprepitant is a potential limitation in a busy clinical practice. However, the recent approval of an intravenous formulation could provide a more convenient route of administration. Aprepitant remains more expensive than other antiemetics, and there are no studies assessing the cost effectiveness of its use.

KEYWORDS:

• Aprepitant
• Antiemetics
• Fosaprepitant
• NK-1 antagonist
• PONV

Article highlights

• Aprepitant is an NK-1 receptor antagonist approved for PONV prophylaxis

• Aprepitant is approved in a dose of 40 mg to be administered orally 1-3 hours before surgery

• Recently, an intravenous formulation was approved in a dose of 32 mg to be administered over 30 seconds

• Advantages of aprepitant include its superior antivomiting efficacy compared to other antiemetics along with a prolonged duration of action and favorable side effect profile

• Aprepitant’s antinausea efficacy is modest and comparable to that of 5-HT3 receptor antagonists

Declaration of interest

A Habib has received research funding from Haisco U.S.A, Pacira Pharmaceuticals and Heron Therapeutics and has acted on the advisory boards of Heron Therapeutics, MDoloris and Vertex Pharmaceuticals. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

Information resources

For further information on PONV prophylaxis in clinical practice we recommend the Fourth Consensus Guidelines from Gan, T.J., et al., 2020. For further information on important clinical studies of aprepitant we recommend Gan, T.J., et al. 2007; Diemunsch, P., et al. 2007; Habib, A.S., et al. 2011. Lastly, for an overview of all clinical evidence we recommend the recent network meta-analysis from Weibel, S., et al. 2021.

Reviewer disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This paper was not funded.