EMADINE - emedastine difumarate solution/ drops

País: Estados Unidos

Língua: inglês

Origem: NLM (National Library of Medicine)

Ingredientes ativos:

EMEDASTINE DIFUMARATE (UNII: 42MB94QOSM) (EMEDASTINE - UNII:9J1H7Y9OJV)

Disponível em:

Alcon Laboratories, Inc.

DCI (Denominação Comum Internacional):

EMEDASTINE DIFUMARATE

Composição:

EMEDASTINE 0.5 mg in 1 mL

Via de administração:

OPHTHALMIC

Tipo de prescrição:

PRESCRIPTION DRUG

Indicações terapêuticas:

EMADINE® (emedastine difumarate ophthalmic solution) 0.05% is indicated for the temporary relief of the signs and symptoms of allergic conjunctivitis. EMADINE® (emedastine difumarate ophthalmic solution) 0.05% is contraindicated in persons with a known hypersensitivity to emedastine difumarate or any of its components.

Resumo do produto:

EMADINE® (emedastine difumarate ophthalmic solution) 0.05% is supplied as follows: 5 mL in opaque, plastic DROP-TAINER® dispenser. 5 mL: NDC 0065-0325-05 STORAGE : Store at 4°C to 30°C (39°F-86°F). Rx Only ©2002, 2003, 2009, 2018 Novartis Distributed by: ALCON LABORATORIES, INC. Fort Worth, Texas 76134 USA Alcon® a Novartis company Revised: April 2018 T2018-34

Status de autorização:

New Drug Application

Características técnicas

EMADINE - EMEDASTINE DIFUMARATE SOLUTION/ DROPS
ALCON LABORATORIES, INC.
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EMADINE
(EMEDASTINE DIFUMARATE OPHTHALMIC SOLUTION) 0.05%
DESCRIPTION
EMADINE (emedastine difumarate ophthalmic solution) 0.05% is a sterile
ophthalmic solution
containing emedastine, a relatively selective, H1-receptor antagonist
for topical administration to the
eyes. Emedastine difumarate is a white, crystalline, water-soluble
fine powder with a molecular weight
of 534.57. The chemical structure is presented below:
STRUCTURAL FORMULA:
CHEMICAL NAME:
1H-benzimidazole,1-(2-ethoxyethyl)-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl),(E)-2-butenedioate
(1:2)
EACH ML OF EMADINE (EMEDASTINE DIFUMARATE OPHTHALMIC SOLUTION) 0.05%
CONTAINS: ACTIVE:
0.884 mg emedastine difumarate equivalent to 0.5 mg emedastine.
PRESERVATIVE: benzalkonium chloride
0.01%. INACTIVES: tromethamine; sodium chloride; hypromellose;
hydrochloric acid/sodium hydroxide
(adjust pH); and purified water. It has a pH of approximately 7.4 and
an osmolality of approximately
300 mOsm/kg.
CLINICAL PHARMACOLOGY
Emedastine is a relatively selective, histamine H1 antagonist. _In
vitro_ examinations of emedastine's
affinity for histamine receptors (H1: Ki = 1.3 nM, H2: Ki = 49,067 nM,
and H3: Ki = 12,430 nM)
demonstrate relative selectivity for the H1-histamine receptor. _In
vivo studies_ have shown concentration-
dependent inhibition of histamine-stimulated vascular permeability in
the conjunctiva following topical
ocular administration.
Emedastine appears to be devoid of effects on adrenergic, dopaminergic
and serotonin receptors.
Following topical administration in man, emedastine was shown to have
low systemic exposure. In a
study involving 10 normal volunteers dosed bilaterally twice daily for
15 days with emedastine
ophthalmic solution 0.05%, plasma concentrations of the parent
compound were generally below the
quantitation limit of the assay (less than 0.3 ng/mL).
Samples in which emedastine was quantifiable, ranged from 0.30 to 0.49
ng/mL. The elimination half-
life of