EMEND aprepitant 80mg & 125mg tri-pack capsule blister pack

Country: Australia

Language: English

Source: Department of Health (Therapeutic Goods Administration)

Active ingredient:

aprepitant

Available from:

Merck Sharp & Dohme (Australia) Pty Ltd

Authorization status:

Registered

Patient Information leaflet

EMEND
®
_Aprepitant_
CONSUMER MEDICINE INFORMATION
WHAT IS IN THIS LEAFLET
This leaflet answers some common
questions about EMEND. It does not
contain all the available information.
It does not take the place of talking to
your doctor or pharmacist.
All medicines have risks and
benefits. Your doctor has weighed
the risks of you taking EMEND
against the benefits they expect it
will have for you.
IF YOU HAVE ANY CONCERNS ABOUT
TAKING THIS MEDICINE, ASK YOUR
DOCTOR OR PHARMACIST.
KEEP THIS LEAFLET WITH THE MEDICINE.
You may need to read it again.
WHAT EMEND IS USED
FOR
_CHEMOTHERAPY INDUCED_
_NAUSEA AND VOMITING_
EMEND, in combination with other
medicines, is used to prevent nausea
(feeling sick) and vomiting
associated with cancer
chemotherapy.
_POST-OPERATIVE NAUSEA AND_
_VOMITING_
EMEND is used to prevent nausea
(feeling sick) and vomiting which
can occur after surgery.
EMEND belongs to a group of
medicines called neurokinin 1 (NK1)
receptor antagonists. It works by
blocking the actions of substances in
your brain, called substance P
neurokinins, that cause nausea and
vomiting.
Your doctor may have prescribed
EMEND for another reason. Ask
your doctor if you have any questions
about why EMEND has been
prescribed for you.
The safety and effectiveness of
EMEND in children and teenagers
under the age of 18 years have not
been established.
EMEND is not addictive.
BEFORE YOU TAKE
EMEND
_WHEN YOU MUST NOT TAKE IT_
DO NOT TAKE EMEND IF YOU HAVE
AN ALLERGY TO EMEND OR ANY OF THE
INGREDIENTS LISTED AT THE END OF THIS
LEAFLET.
DO NOT TAKE EMEND IF YOU ARE
TAKING:
•
cisapride, used to treat stomach
reflux
•
pimozide, used to treat psychotic
conditions
•
terfenadine (Teldane*) and
astemizole (Hismanal*),
antihistamines used for allergic
conditions, including hayfever
* not available in Australia
•
St Johns Wort - a herb used to
treat depression
Taking EMEND with these
medicines may cause serious or life-
threatening reactions.
DO NOT TAKE EMEND IF YOU HAVE A
RARE HEREDITARY PROBLEM OF
FRUCTOSE INTOLERANCE, GLUCOSE-
G

Summary of Product characteristics

A140917
Page 1 of 28
PRODUCT INFORMATION
EMEND CAPSULE
NAME OF THE MEDICINE
aprepitant
CHEMICAL STRUCTURE
Aprepitant is chemically described as
5-[[(2_R_,3_S_)-2-[(1_R_)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-
3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3_H_-1,2,4-triazol-3-one.
Molecular formula:
C
23
H
21
F
7
N
4
O
3
Molecular mass: 534.43
CAS NUMBER
CAS number: 170729-80-3
DESCRIPTION
EMEND is a substance P neurokinin 1 (NK1) receptor antagonist.
Aprepitant is a white to off-white crystalline solid. It is
practically insoluble in water. Aprepitant is
sparingly soluble in ethanol and isopropyl acetate and slightly
soluble in acetonitrile.
Each capsule of EMEND for oral administration contains 40 mg, 80 mg,
125 mg or 165 mg of
aprepitant.
Each capsule of EMEND contains the following inactive ingredients:
sucrose, microcrystalline
cellulose, hydroxypropyl cellulose and sodium lauryl sulfate. The hard
gelatin capsules contain the
following inactive ingredients: gelatin and titanium dioxide CI 77891,
and may also contain sodium
lauryl sulfate and silicon dioxide. The 40-mg capsule shell also
contains iron oxide yellow CI 77492,
the 125-mg capsule shell also contains iron oxide red CI 77491 and
iron oxide yellow CI 77492, and
the 165-mg capsule shell also contains indigo carmine. The capsules
are printed with ink containing
iron oxide black CI 77499.
PHARMACOLOGY
MECHANISM OF ACTION
Aprepitant
is
a
selective
high
affinity
antagonist
at
human
substance-P
neurokinin-1
(NK
1
)
receptors. Aprepitant showed at least 3,000-fold selectivity for the
NK
1
receptor over other enzyme,
transporter, ion-channel and receptor sites, including the dopamine
and serotonin (5HT
3
) receptors
that are targets for existing chemotherapy-induced nausea and vomiting
(CINV) and postoperative
nausea and vomiting (PONV) therapies.
N
O
O
CF
3
CF
3
F
N
NH
NH
O
CH
3
A140917
Page 2 of 28
Aprepitant
has
been
shown
in
animal
models
to
inhibit
emesis
induced
by
cytotoxic
chemotherapeutic agents, such as cisplatin, via central actions.
Pr