Olopatadine hydrochloride.
Each ml contains Olopatadine Hydrochloride USP equivalent to Olopatadine 1 mg.
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. 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 mono-desmethyl 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.
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.
After oral dosing of olopatadine in patients with severe renal impairment, 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.
Treatment of the signs and symptoms of allergic conjunctivitis.
The dose is one drop of OLOPAN 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: OLOPAN may be used in paediatric patients three years of age and older at the same dose as in adults. The safety and efficacy of OLOPAN 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 (OLOPAN) has not been studied in patients with renal or hepatic disease. However, no dosage adjustment is expected to be necessary in hepatic or renal impairment (see Pharmacology: Pharmacokinetics under Actions).
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.
Route of Administration: Opthalmic.
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 OLOPAN 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.
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.
OLOPAN is an antiallergic/antihistaminic agent and, although administered topically, is absorbed systemically. If signs of serious reactions or hypersensitivity occur, discontinue the use of this treatment.
OLOPAN 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.
Effects on Ability to Drive and Use Machine: OLOPAN has no or negligible influence on the ability to drive and use machines.
As with any eye drop, temporary blurred vision or other visual disturbances may affect the ability to drive or use machines. If blurred vision occurs at instillation, the patient must wait until the vision clears before driving or using machinery.
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.
OLOPAN should not be used during breast-feeding.
The following adverse reactions are classified according very common, common, uncommon, rare, very rare or not known. Within each frequency grouping, adverse reactions are presented in order of decreasing seriousness. (See table.)
Click on icon to see table/diagram/image
Cases of corneal calcification have been reported very rarely in association with the use of phosphate containing eye drops in some patients with significantly damaged corneas.
No interaction studies with other medicinal products have been performed.
Olopatadine is unlikely to result in metabolic interactions with other concomitantly administered active substances.
Keep the bottle in the outer carton in order to protect from light.
Store below 30°C.
After first opening the bottle: do not store above 25°C and use within four weeks.
S01GX09 - olopatadine ; Belongs to the class of other ophthalmologic antiallergics.
Olopan eye drops 0.1% w/v
5 mL x 1's
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