RELESTAT OPHTHALMIC SOLUTION 0.5 mgml

Country: Singapore

Language: English

Source: HSA (Health Sciences Authority)

Active ingredient:

Epinastine HCl

Available from:

ALLERGAN SINGAPORE PTE. LTD.

ATC code:

S01GX10

Dosage:

0.05 % w/v

Pharmaceutical form:

SOLUTION, STERILE

Composition:

Epinastine HCl 0.05 % w/v

Administration route:

OPHTHALMIC

Prescription type:

Prescription Only

Manufactured by:

Allergan Pharmaceuticals Ireland

Authorization status:

ACTIVE

Authorization date:

2010-06-15

Patient Information leaflet

RELESTAT
®
(EPINASTINE HCL OPHTHALMIC SOLUTION) 0.05%
STERILE
DESCRIPTION
RELESTAT
®
(epinastine HCl ophthalmic solution) 0.05% is a clear, colorless,
sterile isotonic
solution containing epinastine HCl, an antihistamine and an inhibitor
of histamine release from
the mast cell for topical administration to the eyes.
Epinastine HCl is represented by the following structural formula:
C
16
H
15
N
3
HCl Mol. Wt. 285.78
CHEMICAL
NAME:
3-Amino-9,
13b-dihydro-1H-dibenz[c,f]
imidazo[1,5-a]
azepine
hydrochloride
EACH ML CONTAINS:
Active: Epinastine HCl 0.05% (0.5 mg/mL) equivalent to epinastine
0.044% (0.44 mg/mL);
PRESERVATIVE:
Benzalkonium chloride 0.01%;
INACTIVES:
Edetate
disodium;
purified
water;
sodium
chloride;
sodium
phosphate,
monobasic;
and
sodium
hydroxide and/or hydrochloric acid (to adjust the pH).
RELESTAT
®
has a pH of approximately 7 and an osmolality range of 250 to 310
mOsm/kg.
CLINICAL PHARMACOLOGY
Epinastine is a topically active, direct H
1
-receptor antagonist and an inhibitor of the release of
histamine from the mast cell. Epinastine is selective for the
histamine H
1
-receptor and has
affinity for the histamine H
2
-receptor. Epinastine also possesses affinity for the ∂
1
-, ∂
2
-, and 5-
HT
2
-receptors. Epinastine does not penetrate the blood/brain barrier and,
therefore, is not
expected to induce side effects of the central nervous system.
Fourteen subjects, with allergic conjunctivitis, received one drop of
RELESTAT
®
ophthalmic
solution in each eye twice daily for seven days. On day seven average
maximum epinastine
plasma concentrations of 0.04 ±0.014 ng/ml were reached after about
two hours indicating low
systemic exposure. While these concentrations represented an increase
over those seen
following a single dose, the day 1 and day 7 Area Under the Curve
(AUC) values were
unchanged indicating that there is no increase in systemic absorption
with multiple dosing.
Epinastine is 64% bound to plasma proteins. The total systemic
clearance is approximately 56
L/hr and the terminal plasma e

Summary of Product characteristics

RELESTAT
®
(EPINASTINE HCL OPHTHALMIC SOLUTION) 0.05%
STERILE
DESCRIPTION
RELESTAT
®
(epinastine HCl ophthalmic solution) 0.05% is a clear, colorless,
sterile isotonic
solution containing epinastine HCl, an antihistamine and an inhibitor
of histamine release from
the mast cell for topical administration to the eyes.
Epinastine HCl is represented by the following structural formula:
C
16
H
15
N
3
HCl Mol. Wt. 285.78
CHEMICAL
NAME:
3-Amino-9,
13b-dihydro-1H-dibenz[c,f]
imidazo[1,5-a]
azepine
hydrochloride
EACH ML CONTAINS:
Active: Epinastine HCl 0.05% (0.5 mg/mL) equivalent to epinastine
0.044% (0.44 mg/mL);
PRESERVATIVE:
Benzalkonium chloride 0.01%;
INACTIVES:
Edetate
disodium;
purified
water;
sodium
chloride;
sodium
phosphate,
monobasic;
and
sodium
hydroxide and/or hydrochloric acid (to adjust the pH).
RELESTAT
®
has a pH of approximately 7 and an osmolality range of 250 to 310
mOsm/kg.
CLINICAL PHARMACOLOGY
Epinastine is a topically active, direct H
1
-receptor antagonist and an inhibitor of the release of
histamine from the mast cell. Epinastine is selective for the
histamine H
1
-receptor and has
affinity for the histamine H
2
-receptor. Epinastine also possesses affinity for the ∂
1
-, ∂
2
-, and 5-
HT
2
-receptors. Epinastine does not penetrate the blood/brain barrier and,
therefore, is not
expected to induce side effects of the central nervous system.
Fourteen subjects, with allergic conjunctivitis, received one drop of
RELESTAT
®
ophthalmic
solution in each eye twice daily for seven days. On day seven average
maximum epinastine
plasma concentrations of 0.04 ±0.014 ng/ml were reached after about
two hours indicating low
systemic exposure. While these concentrations represented an increase
over those seen
following a single dose, the day 1 and day 7 Area Under the Curve
(AUC) values were
unchanged indicating that there is no increase in systemic absorption
with multiple dosing.
Epinastine is 64% bound to plasma proteins. The total systemic
clearance is approximately 56
L/hr and the terminal plasma e