Silkay 125mg Tablet

País: Malàisia

Idioma: anglès

Font: NPRA (National Pharmaceutical Regulatory Agency, Bahagian Regulatori Farmasi Negara)

ingredients actius:

Bosentan Monohydrate

Disponible des:

MEDISPEC (M) SDN.BHD

Designació comuna internacional (DCI):

Bosentan Monohydrate

Unidades en paquete:

60 Tablets; 10 Tablets

Fabricat per:

UNISON LABORATORIES CO.LTD

Informació per a l'usuari

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_CONSUMER MEDICATION INFORMATION LEAFLET (RIMUP) _
SILKAY 125 MG TABLET
Bosentan monohydrate eq. to Bosentan (125 mg) 1
WHAT IS IN THIS LEAFLET
1.
What Silkay 125 is used for
2.
How Silkay 125 works
3.
Before you use Silkay 125
4.
How to use Silkay 125
5.
While you are using it
6.
Side effects
7.
Storage and Disposal
of Silkay 125
8.
Product Description
9.
Manufacturer and Product
Registration Holder
10.
Date of revision
WHAT SILKAY 125 IS USED FOR
Silkay 125 is a prescription medicine
used to treat people with certain types
of
pulmonary
arterial
hypertension
(PAH), which is high blood pressure in
the vessels of the lungs.
HOW SILKAY 125 WORKS
Silkay
125
tablets
contain
Bosentan,
which belongs to the class of medicines
called
“endothelin
receptor
antagonists”.
Bosentan blocks a naturally occurring
hormone
called
endothelin-1
(ET-1),
which causes blood vessels to narrow.
Thus, it acts to reduce abnormally high
blood pressure by widening these blood
vessels.
BEFORE YOU USE SILKAY 125
_- When you must not use it _
Do not take Silkay 125:
•
if you are allergic to bosentan or
any of the other ingredients of this
medicine
•
if
you
have
liver
problems
(ask
your doctor)
•
if you are pregnant, or could get
pregnant because you are not using
reliable
contraceptive
methods.
Please read the information under
“Contraceptives”
and
“Taking
other medicines”
•
if you are taking cyclosporine A (a
medicine used after a transplant)
PREGNANCY AND LACTATION
DO NOT
take Silkay 125 if you are
pregnant
or
planning
to
become
pregnant.
_PREGNANCY TESTS _
Silkay
125
may harm
unborn babies
conceived
before
starting
or
during
treatment.
If
you
are
a
woman
who
could
become
pregnant,
your
doctor
will ask you to take a pregnancy test
before you start taking Silkay 125, and
regularly while you are taking it.
_CONTRACEPTIVES _
If it is possible that you could become
pregnant, use a reliable form of birth
control (contraception) while you are
taking
Silkay
125.
Your
doctor
or
gynecologist
will

Fitxa tècnica

ANTIHYPERTENSIVE
Each film coated tablet contains:
BOSENTAN MONOHYDRATE EQ. TO BOSENTAN 125 MG
PRODUCT DESCRIPTION:
Orange-white, oval, biconvex, film coated tablet with engraved 125 on
one side and plain on the other side
MECHANISM OF ACTION:
_PHARMACOLOGY_
Bosentan is a dual endothelin receptor antagonist (ERA) with affinity
for both endothelin A and B
(ET
A
and ET
B
) receptors. Bosentan decreases both pulmonary and systemic vascular
resistance resulting
in increased cardiac output without increasing heart rate.
The neurohormone endothelin-1 (ET-1) is one of the most potent
vasoconstrictors known and can also
promote fibrosis, cell proliferation, cardiac hypertrophy and
remodelling, and is pro-inflammatory.
These effects are mediated by endothelin binding to ET
A
and ET
B
receptors located in the
endothelium and vascular smooth muscle cells. ET-1 concentrations in
tissues and plasma are increased
in several cardiovascular disorders and connective tissue diseases,
including PAH, scleroderma, acute
and chronic heart failure, myocardial ischemia, systemic hypertension
and atherosclerosis, suggesting
a pathogenic role of ET-1 in these diseases. In PAH and heart failure,
in the absence of endothelin
receptor antagonism, elevated ET-1 concentrations are strongly
correlated with the severity and
prognosis of these diseases.
Bosentan competes with the binding of ET-1 and other ET peptides to
both ET
A
and ET
B
receptors,
with a slightly higher affinity for ET
A
receptors (K
i
= 4.1–43 nanomolar) than for ET
B
receptors
(K
i
= 38–730 nanomolar). Bosentan specifically antagonises ET receptors
and does not bind to other
receptors.
_PHARMACOKINETICS_
Absorption
In healthy individual, the absolute bioavailability of Bosentan is
approximately 50% and is not affected
by food. The maximum plasma concentrations are attained within 3–5
hours.
Distribution
Bosentan is highly bound (> 98%) to plasma proteins, mainly albumin.
Bosentan does not penetrate
into erythrocytes.
A volume of distribution (V
ss
) of about 18 liters w