UPTRAVI FILM-COATED TABLET 200MCG

Country: Singapore

Language: English

Source: HSA (Health Sciences Authority)

Active ingredient:

Selexipag

Available from:

JOHNSON & JOHNSON INTERNATIONAL (SINGAPORE) PTE LTD

ATC code:

B01AC27

Pharmaceutical form:

TABLET, FILM COATED

Composition:

Selexipag 0.2 mg

Administration route:

ORAL

Prescription type:

Prescription Only

Manufactured by:

ALLPACK GROUP AG (Primary and Secondary Packager)

Authorization status:

ACTIVE

Authorization date:

2017-07-06

Summary of Product characteristics

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PRODUCT INFORMATION
UPTRAVI
®
(SELEXIPAG)
200, 400, 600, 800, 1000, 1200, 1400 AND 1600
MICROGRAMS FILM COATED TABLETS
NAME OF THE MEDICINE
Active: selexipag
UPTRAVI
®
(selexipag) is a selective non-prostanoid prostacyclin IP receptor
agonist.
The chemical name of selexipag is 2-{4-[(5,6-diphenylpyrazin-2-
yl)(isopropyl)amino]butoxy}-
_N_
-(methylsulfonyl) acetamide.
_ _
_Structural formula: _
_ _
The molecular formula: C
26
H
32
N
4
O
4
S
The molecular weight: 496.62 mg/mol
CAS: 475086-01-2
Pharmacotherapeutic group: Platelet aggregation inhibitors excl.
heparin
ATC code: B01AC27.
DESCRIPTION
Selexipag is a pale yellow crystalline powder that is practically
insoluble in water. In
the solid state selexipag is very stable, is not hygroscopic, and is
not light sensitive.
Each
round
film-coated
tablet
contains
200
micrograms
or
multiples
thereof
(respectively 400, 600, 800, 1000, 1200, 1400, or 1600 micrograms)
selexipag. The
tablets include the following inactive ingredients: mannitol, maize
starch, hyprolose,
and magnesium stearate. The tablets are film coated with a coating
material containing
hypromellose, propylene glycol, titanium dioxide, and carnauba wax. In
addition,
tablets may contain iron oxide red, iron oxide yellow, or iron oxide
black. The film-
coated tablets are not light sensitive.
PHARMACOLOGY
MECHANISM OF ACTION
The vasculo-protective effects of prostacyclin (PGI
2
) are mediated by the prostacyclin
receptor (IP receptor). Decreased expression of IP receptors and
decreased synthesis of
prostacyclin contribute to the pathophysiology of pulmonary arterial
hypertension
(PAH).
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Selexipag is an oral, selective, IP prostacyclin receptor agonist, and
is structurally and
pharmacologically distinct from prostacyclin and its analogues.
Selexipag is hydrolysed
by carboxylesterase to yield its active metabolite, which is
approximately 37-fold more
potent than selexipag. Selexipag and the active metabolite are high
affinity IP receptor
agonists with a high selectivity for the IP receptor versus oth