has been licensed for prevention
of nausea and vomiting associated
with MEC and HEC chemotherapy
in children, toddlers and infants
from the age of six months to 12
years. 33
Intravenous formulation
Two intravenous formulations of
aprepitant are available; however,
both formulations are not
interchangeable (see Table 1). 7
Fosaprepitant
As aprepitant has a low water
solubility, fosaprepitant, its
intravenously administered
water-soluble phosphoryl prodrug,
has been approved for CINV in
prevention in combination with
other antiemetics. 30 Fosaprepitant
is rapidly converted (within 30
minutes of infusion) to aprepitant
by a nearly complete conversion.
Fosaprepitant is a prodrug of
aprepitant and its pharmacological
activity mirrors that of aprepitant. 30
However, as used in several drug
formulations to fully solubilise
the drug, the fosaprepitant
formulation includes the
surfactant polysorbate 80, which
has been associated with systemic
hypersensitivity and infusion-site
adverse reactions including pain,
erythema and swelling. 7,34–36
The latter can be reduced by
using a more dilute fosaprepitant
preparation and 30 minutes’
infusion duration when
administering via a peripheral
intravenous line. 34,35
The labelling of fosaprepitant
includes a warning regarding
serious systemic hypersensitivity
reactions such as anaphylaxis and
anaphylactic shock, during or after
infusion. 30,37
The prescribing information for
IV fosaprepitant reports incidence
rates of 2.2% (MEC) and 3.0%
(HEC) for infusion-site reactions
associated with IV fosaprepitant
treatment; moreover, more
recently studies have reported
appreciably higher rates of 34.7% 38
in patients receiving AC-based
chemotherapy and 7.4% 39 in
patients receiving cisplatin-based
chemotherapy
Aprepitant injectable emulsion
Recently, a new injectable
polysorbate 80 and synthetic
surfactant-free emulsion of IV
hospitalpharmacyeurope.com | 2019 | 57