Avicon

Clear, colorless liquid filled in white ophthalmic polypropylene container, free from any visible contamination.
Each mL contains: Olopatadine (as hydrochloride) 1 mg.
Preservative: Benzalkonium chloride 0.01% w/v.

Antihistamine.
Pharmacology: Pharmacodynamics: Olopatadine is a potent selective antiallergic/antihistaminic agent that exerts its effects through multiple distinct mechanisms of action. It antagonises histamine (the primary mediator of allergic response in humans) and prevents histamine-induced inflammatory cytokine production by human conjunctival epithelial cells. Data from in vitro studies suggest that it may act on human conjunctival mast cells to inhibit the release of pro-inflammatory mediators. In patients with patent nasolacrimal ducts, topical ocular administration of Olopatadine was suggested to reduce the nasal signs and symptoms that frequently accompany seasonal allergic conjunctivitis. It does not produce a clinically significant change in pupil diameter.
Pharmacokinetics: Absorption: Olopatadine is absorbed systemically, as are other topically administered medicinal products. However, systemic absorption of topically applied olopatadine is minimal with plasma concentrations ranging from below the assay quantitation limit (<0.5 ng/mL) up to 1.3 ng/mL. These concentrations are 50- to 200-fold lower than those following well-tolerated oral doses.
Elimination: From oral pharmacokinetic studies, the half-life of olopatadine in plasma was approximately eight to 12 hours, and elimination was predominantly through renal excretion. Approximately 60-70% of the dose was recovered in the urine as active substance. Two metabolites, the monodesmethyl and the N-oxide, were detected at low concentrations in the urine.
Since olopatadine is excreted in urine primarily as unchanged active substance, impairment of renal function alters the pharmacokinetics of olopatadine with peak plasma concentrations 2.3-fold greater in patients with severe renal impairment (mean creatinine clearance of 13.0 mL/min) compared to healthy adults. Following a 10 mg oral dose in patients undergoing haemodialysis (with no urinary output), plasma olopatadine concentrations were significantly lower on the haemodialysis day than on the non-haemodialysis day suggesting olopatadine can be removed by haemodialysis.
Studies comparing the pharmacokinetics of 10 mg oral doses of olopatadine in young (mean age 21 years) and elderly (mean age 74 years) showed no significant differences in the plasma concentrations (AUC), protein binding or urinary excretion of unchanged parent drug and metabolites.
A renal impairment study after oral dosing of olopatadine has been performed in patients with severe renal impairment. The results indicate that a somewhat higher plasma concentration can be expected with olopatadine in this population. Since plasma concentrations following topical ocular dosing of olopatadine are 50- to 200-fold lower than after well tolerated oral doses, dose adjustment is not expected to be necessary in the elderly or in the renally impaired population. Liver metabolism is a minor route of elimination. Dose adjustment is not expected to be necessary with hepatic impairment.

Olopatadine Ophthalmic Solution (Avicon) is indicated for the treatment of ocular signs and symptoms of seasonal allergic conjunctivitis.

Posology: The dose is one drop of Olopatadine in the conjunctival sac of the affected eye(s) twice daily (8 hourly). Treatment may be maintained for up to four months, if considered necessary.
Use in elderly: No dosage adjustment in elderly patients is necessary.
Paediatric patients: Olopatadine may be used in paediatric patients three years of age and older at the same dose as in adults. The safety and efficacy of Olopatadine in children aged under 3 years has not been established. No data are available.
Use in hepatic and renal impairment: Olopatadine in the form of eye drops has not yet been studied in patients with renal or hepatic disease. However, no dosage adjustment is expected to be necessary in hepatic or renal impairment.
Method of administration: For ocular use only.
After the bottle cap is removed, if the tamper evident snap collar is loose, remove before using the product. To prevent contamination of the dropper tip and solution, care must be taken not to touch the eyelids, surrounding areas, or other surfaces with the dropper tip of the bottle. Keep the bottle tightly closed when not in use.
In case of concomitant therapy with other topical ocular medicines, an interval of five minutes should be allowed between successive applications. Eye ointments should be administered last.

No data are available in humans regarding overdose by accidental or deliberate ingestion. Olopatadine has a low order of acute toxicity in animals. Accidental ingestion of the entire contents of a bottle of Olopatadine would deliver a maximum systemic exposure of 5 mg olopatadine. This exposure would result in a final dose of 0.5 mg/kg in a 10 kg infant, assuming 100% absorption.
Prolongation of the QTc interval in dogs was observed only at exposures considered sufficiently in excess of the maximum human exposure indicating little relevance to clinical use. A 5 mg oral dose was administered twice-daily for 2.5 days to 102 young and elderly male and female healthy volunteers with no significant prolongation of QTc interval compared to placebo. The range of peak steady-state olopatadine plasma concentrations (35 to 127 ng/mL) seen in this study represents at least a 70-fold safety margin for topical olopatadine with respect to effects on cardiac repolarisation.
In the case of overdose, appropriate monitoring and management of the patient should be implemented.

Hypersensitivity to the active substance or to any of the excipients.

Olopatadine is an antiallergic/antihistamine agent and, although administered topically, is absorbed systematically. If signs of serious reactions or hypersensitivity occur, discontinue the use of this treatment.
Olopatadine contains Benzalkonium chloride which may cause eye irritation.
Benzalkonium chloride has also been reported to cause punctate keratopathy and/or toxic ulcerative keratopathy.
Close monitoring is required with frequent or prolonged use in dry eye patients, or in conditions where the cornea is compromised.
Contact lenses: Benzalkonium is known to discolour soft contact lenses. Avoid contact with soft contact lenses.
Patients should be instructed to remove contact lenses prior to administration of the eye drop and wait at least 15 minutes after instillation before re-inserting contact lenses.

Pregnancy: There are no or limited amount of data from the use of ophthalmic olopatadine in pregnant women.
Olopatadine is not recommended during pregnancy and in women of childbearing potential not using contraception.
Breast-feeding: Available data in animals have shown excretion of olopatadine in milk following oral administration.
A risk to the newborn/infants cannot be excluded.
Olopatadine should not be used during breast-feeding.
Fertility: Studies have not been performed to evaluate the effect of topical ocular administration of olopatadine on human fertility.

Infections and infestations: rhinitis.
Immune system disorders: hypersensitivity, swelling face.
Nervous system disorders: headache, dysgeusia, dizziness, hypoaesthesia, somnolence.
Eye disorders: eye pain, eye irritation, dry eye, abnormal sensation in eyes, corneal erosion, corneal epithelium defect, corneal epithelium disorder, punctate keratitis, keratitis, corneal staining, eye discharge, photophobia, vision blurred, visual acuity reduced, blepharospasm, ocular discomfort, eye pruritus, conjunctival follicles, conjunctival disorder, foreign body sensation in eyes, lacrimation increased, erythema of eyelid, eyelid oedema, eyelid disorder, ocular hyperaemia, corneal oedema, eye oedema, eye swelling, conjunctivitis, mydriasis, visual disturbance, eyelid margin crusting.
Respiratory, thoracic, and mediastinal disorders: nasal dryness, dyspnea, sinusitis.
Gastrointestinal disorders: nausea, vomiting.
Skin and subcutaneous tissue disorders: dermatitis contact, skin burning sensation, dry skin erythema.
General disorders and administration site conditions: fatigue, asthenia, malaise.

No interaction studies with other medicinal products have been performed.
In vitro studies have shown that olopatadine did not inhibit metabolic reactions which involve cytochrome P-450 isozymes 1A2, 2C8, 2C9, 2C19, 2D6, 2E1 and 3A4. These results indicate that olopatadine is unlikely to result in metabolic interactions with other concomitantly administered active substances.

For external use only.

Store at temperatures not exceeding 30°C.

Ophthalmic Decongestants, Anesthetics, Anti-Inflammatories

S01GX09 - olopatadine ; Belongs to the class of other ophthalmologic antiallergics.

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