EMEND aprepitant 40 mg capsules blister pack

Riik: Austraalia

keel: inglise

Allikas: Department of Health (Therapeutic Goods Administration)

Toimeaine:

aprepitant

Saadav alates:

Merck Sharp & Dohme (Australia) Pty Ltd

INN (Rahvusvaheline Nimetus):

Aprepitant

Volitamisolek:

Registered

Toote omadused

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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
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Aprepitant
has
been
shown
in
animal
models
to
inhibit
emesis
induced
by
cytotoxic
chemotherapeutic agents, such as cisplatin, via central actions.
Pr