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Logo EMADINE® Eye Drops

SCHEDULING STATUS:
S2

PROPRIETARY NAME
(and dosage form):

EMADINE® Eye Drops

COMPOSITION
EMADINE
® Eye Drops contains emedastine difumarate equivalent to 0.5 mg emedastine base per mL in a sterile ophthalmic solution preserved with benzalkonium chloride 0.01% (m/v).

PHARMACOLOGICAL CLASSIFICATION
A.15.4 Ophthalmic preparations, other.

PHARMACOLOGICAL ACTION
Emedastine is a potent, selective and topically effective histamine H1-antagonist. In vitro examinations of emedastine's affinity for histamine receptors (H1, H2 and H3) demonstrate 10,000-fold selectivity for the H1 histamine receptor; Kis = 1.3 nM, 49.064 nM and 12.430 nM, respectively. In vivo topical ocular administration of emedastine produces concentration-dependant inhibition of histamine-stimulated vascular permeability. Emedastine exhibits no significant effects on adrenergic, dopaminergic or serotonergic receptors.
Emedastine is absorbed systemically, as are other topically administered drugs. In a study involving 10 normal volunteers dosed bilaterally twice daily for 15 days with EMADINE 0.05% eye drops solution, plasma concentrations of the parent compound were generally below the quantitation limit of the assay (0.3 ng/mL). Samples in which emedastine was quantifiable ranged from 0.30 to 0.49 ng/mL.
The human oral bioavailability of emedastine is approximately 50% and maximum plasma concentrations were achieved within 1-2 hours after dosing.
Emedastine is principally metabolised by the liver. The elimination half-life of topical emedastine is 10 hours. Approximately 44% of an oral dose is recovered in the urine over 24 hours, with only 3.6% of the dose excreted as parent drug. Two primary metabolites, 5- and 6-hydroxyemedastine, are excreted in the urine as both free and conjugated forms. The 5’-oxo analogues of 5- and 6-hydroxyemedastine and the N-oxide are also formed as minor metabolites.

INDICATIONS
EMADINE Eye Drops is indicated for the relief of the signs and symptoms of seasonal allergic conjunctivitis.
EMADINE has not been studied in clinical trials for more than six weeks.

CONTRA-INDICATIONS
Hypersensitivity to any component of this product.
Safety in pregnancy and lactation has not been demonstrated.

WARNINGS
As the possibility of adverse effects on the corneal permeability and the danger of disruption of the corneal epithelium with prolonged or repeated usage of benzalkonium chloride preserved preparations cannot be excluded, regular ophthalmological examination is required. Caution should be exercised in the use of benzalkonium chloride preserved topical medication over an extended period in patients with extensive ocular surface disease.

DOSAGE AND DIRECTIONS FOR USE
Instil one drop of EMADINE Eye Drops to the affected eye(s) twice daily.
Elderly and Paediatric use:
Safety and effectiveness have been established in paediatric patients between the ages of 4 and 16.
EMADINE Eye Drops has not been studied in elderly patients and therefore its use is not recommended in patients over the age of 65 years.
Hepatic and renal impairment use:
EMADINE Eye Drops has not been studied in these patients and therefore its use is not recommended in this population.

SIDE-EFFECTS AND SPECIAL PRECAUTIONS
Undesirable effects: The most common ocular adverse reaction reported with EMADINE Eye Drops was discomfort (transient burning and stinging).
Ocular adverse reactions reported commonly included dry eye, ocular hyperaemia, ocular pruritis, blurred vision, corneal staining, tearing, lid oedema, infiltrate, foreign body sensation, conjunctivitis, keratitis, hordoleum, lid margin crusting, eye fatigue, decreased visual acuity, sticky sensation, ocular discharge, conjunctival oedema, accidental injury, photophobia and ocular irritation.
Occasional nonocular adverse events were headache and rhinitis, cold syndrome, pain and back pain.
Special precautions for use
Do not instil EMADINE Eye Drops while wearing contact lenses, but wait 10 minutes after instillation before reinserting lenses.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT
A topical overdose may be flushed from the eye with warm tap water. Treatment should be supportive and symptomatic. In case of accidental ingestion of the content of a bottle of EMADINE, the potential of emedastine to increase the QT interval should be borne in mind and appropriate monitoring and management should be implemented.

IDENTIFICATION
Clear, colourless to pale yellow solution.

PRESENTATION
Opaque low density polyethylene DROP-TAINER™ bottles with a 5 mL fill, fitted with a natural dispensing tip as plug and white, linerless screw-on cap.

STORAGE INSTRUCTIONS
Store below 25°C.
DO NOT USE MORE THAN 30 DAYS AFTER OPENING.
KEEP OUT OF REACH OF CHILDREN.

REGISTRATION NUMBER
34/15.4/0037

NAME AND BUSINESS ADDRESS OF THE APPLICANT
Alcon Laboratories (SA) (Pty) Ltd
261, Surrey Avenue,
Randburg, 2194

DATE OF PUBLICATION OF THIS PACKAGE INSERT
3 April 2001

0401

Updated on this site: November 2003
Source: Pharmaceutical Industry

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