INDICATIONS     CONTRA-INDICATIONS     DOSAGE     SIDE-EFFECTS     PREGNANCY     OVERDOSE     IDENTIFICATION     PATIENT INFORMATION

Logo RELESTAT (Eye drops)
SCHEDULING STATUS:
Schedule 2

PROPRIETARY NAME
(and dosage form):

RELESTAT (Eye drops)

COMPOSITION:
Epinastine hydrochloride 0,5 mg per mL.
Contains benzalkonium chloride 0,01% m/v as preservative.       

PHARMACOLOGICAL CLASSIFICATION
A.15.4 Ophthalmic preparations. Other

PHARMACOLOGICAL ACTION
Pharmacodynamics
Epinastine is a topically active, direct H1-receptor antagonist. Epinastine has a high binding affinity for the histamine H1-receptor and a 400 times lower affinity for the histamine H2-receptor. Epinastine also possesses affinity for the alpha1-, alpha2-, and the 5-HT2-receptor. It has low affinity for cholinergic, dopaminergic and a variety of other receptor sites. Epinastine does not penetrate the blood/brain barrier.
Following topical eye application in animals, epinastine showed evidence for antihistaminic activity, a modulating effect on the accumulation of inflammatory cells, and mast cell stabilising activity.
Pharmacokinetics
Following administration of one drop of RELESTAT in each eye twice daily, an average maximum plasma concentration of 0,042 ng/mL is reached after about two hours.
Epinastine has a volume distribution of 417 litres and is 64% bound to plasma proteins.
The clearance is 928 mL/min and the terminal plasma elimination half-life is about 8 hours.
Epinastine is mainly excreted unchanged. About 60% of an intravenous dose is recovered unchanged in the urine and about 30% in faeces. Less than 10% is metabolised. The renal elimination is mainly via active tubular secretion.
Preclinical studies in vitro and in vivo show that epinastine binds to melanin and accumulates in the pigmented ocular tissues of rabbits and monkeys. In vitro data indicate that the binding to melanin is moderate and reversible.

INDICATIONS
RELESTAT is indicated for the short term treatment of the symptoms of seasonal allergic conjunctivitis.

CONTRA-INDICATIONS
Hypersensitivity to RELESTAT or to any of the excipients.

WARNINGS
RELESTAT contains the preservative benzalkonium chloride, which may be absorbed by and discolour soft contact lenses. Contact lenses should therefore be removed prior to instillation of RELESTAT and may not be inserted until 15 minutes after administration.
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 ophthalmological 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.

INTERACTIONS
No drug-drug interactions are anticipated in humans since systemic concentrations of epinastine are extremely low following ocular dosing. In addition, RELESTAT is mainly excreted unchanged in humans indicating a low level of metabolism. Specific interaction studies with other medicinal products have not been performed with RELESTAT.

PREGNANCY AND LACTATION
Adequate and well controlled studies in pregnant women have not been done. RELESTAT should only be used during pregnancy if the potential benefit justifies the potential risk to the foetus.
RELESTAT is excreted in the breast milk of rats, but it is not known if RELESTAT is excreted in human milk. Caution should be exercised when prescribing to breast-feeding women.

DOSAGE AND DIRECTIONS FOR USE
The recommended dose for adults is one drop instilled in each affected eye twice daily.
If more than one topical ophthalmic medicinal product is being used, the medicinal products should be administered at least 5 minutes apart.
Elderly patients
RELESTAT has not been studied in elderly patients.
Children
RELESTAT may be used in children (9 years of age and older) at the same dosage as in adults.
Hepatic impairment
RELESTAT has not been studied in patients with hepatic impairment.
Renal impairment
RELESTAT has not been studied in patients with renal impairment.

SIDE-EFFECTS AND SPECIAL PRECAUTIONS
Side-effects
The most frequent adverse reaction was burning sensation in eye (mostly mild); all other adverse reactions were less frequent.
The following adverse drug reactions were reported during clinical trials with RELESTAT:
Eye disorders:
Common (>1/100, <1/10): burning sensation, conjunctival folliculosis and visual disturbance
Uncommon (>1/1000, <1/100): allergic conjunctivitis, blepharoptosis, conjunctival oedema, conjunctival hyperaemia, eye discharge, eye dryness, irritation, itching, increased sensitivity and photophobia
Nervous system disorders:
Uncommon (>1/1000, <1/100): headache
Respiratory, thoracic and mediastinal disorders:
Uncommon (>1/1000, <1/100): asthma, nasal irritation, rhinitis and sinusitis
Gastrointestinal disorders:
Uncommon (>1/1000, <1/100): oral dryness, taste alteration
Skin and subcutaneous tissue disorders:
Uncommon (>1/1000, <1/100): pruritus

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT
See “Side-effects and special precautions”. Treatment is symptomatic and supportive.

IDENTIFICATION
A clear colourless solution in a multidose bottle.

PRESENTATION
5 mL LDPE bottle with a white polystyrene screw cap with spike device for opening the bottle.

STORAGE INSTRUCTIONS
Store below 25ºC. Do not use more than 30 days after opening. KEEP OUT OF REACH OF CHILDREN.

REGISTRATION NUMBER
37/15.4/0691

NAME AND BUSINESS ADDRESS OF THE HOLDER OF THE CERTIFICATE OF REGISTRATION
Allergan Pharmaceuticals (Pty) Ltd.
30 New Road (entrance off Bavaria Road)
Randjespark Ext 11, Midrand, 1682
Johannesburg, Gauteng
SOUTH AFRICA

DATE OF PUBLICATION OF THIS PACKAGE INSERT
19 February 2006

Updated on this site: July 2008
Source: Pharmaceutical Industry

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