NAPHCON-A* ophthalmic solution contains naphazoline hydrochloride, a decongestant, and pheniramine maleate, an antihistamine.

NAPHCON-A* ophthalmic solution is indicated for the relief of ocular irritation and/or congestion or for the treatment of allergic or inflammatory ocular conditions.

Posology
Instil 1 or 2 drops in each affected eye every 3 to 4 hours or less frequently, until symptoms clear up. Do not continue treatment beyond the symptomatic period.

Use in children
The safety and efficacy of NAPHCON-A* ophthalmic solution in children have not been established.

Use in patients with hepatic or renal impairment
The safety and efficacy of NAPHCON-A* ophthalmic solution in patients with hepatic or renal impairment have not been established.

Method of administration
For ocular use.

After cap is removed, if tamper evident snap collar is loose, remove before using 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. Keep the bottle tightly closed when not in use.

Nasolacrimal occlusion or gently closing the eyelid after administration is recommended. This may reduce the systemic absorption of medicinal products administered via the ocular route and result in a decrease in systemic adverse reactions.

If more than one topical ophthalmic product is being used, the products must be administered at least 5 minutes apart. Eye ointments should be administered last.

• Patients being treated with monoamine oxidase inhibitors (MAOIs) may experience a severe hypertensive crisis if administered a sympathomimetic drug (see section 4.5).
• Use with caution in children, elderly, in patients with cardiovascular disease, including cardiac arrhythmias, or in patients with sympathetic denervation (e.g. patients with insulin dependent diabetes, especially those with a tendency towards diabetic ketoacidosis, orthostatic hypotension, hypertension, hyperthyroidism) due to the risk for possible systemic effects.
• Prolonged and/or excessive use may lead to rebound ocular vasodilatation or congestion.
• NAPHCON-A* ophthalmic solution contains benzalkonium chloride which may cause eye irritation and is known to discolour soft contact lenses. Avoid contact with soft contact lenses.
Patients must be instructed to remove contact lenses prior to application of NAPHCON-A* ophthalmic solution and wait at least 15 minutes before reinsertion.

Patients being treated with monoamine oxidase inhibitors (MAOIs) may experience a severe hypertensive reaction if administered with a sympathomimetic drug. Although this reaction has not specifically been reported with naphazoline the possibility of such an interaction should be considered (see section 4.4).

Pregnancy
There are no or limited amount of data from the use of topical ophthalmic naphazoline or pheniramine in pregnant women. Animal studies are insufficient with respect to reproductive toxicity.

NAPHCON-A* ophthalmic solution is not recommended during pregnancy.

Breast-feeding
It is unknown whether topical naphazoline, pheniramine or their metabolites are excreted in human milk. However, a risk to the suckling child cannot be excluded.

A decision must be made whether to discontinue breast-feeding or to discontinue or abstain from NAPHCON-A opthalmic solution therapy taking into account the benefit of breast-feeding for the child and the benefit of therapy for the woman.

Fertility
Studies have not been performed to evaluate the effect of topical ocular administration of NAPHCON-A* ophthalmic solution on human fertility.

NAPHCON-A* ophthalmic solution may cause transient mydriasis, temporary blurred vision orؤother visual disturbances that may have a minor to moderate influence on the ability to drive or use machines. If there is mydriasis or if blurred vision occurs after instillation, the patient must wait until the vision clears before driving or using machinery.

Tabulated summary of adverse reactions
The following adverse reactions have been reported during clinical trials and identified from postmarketing surveillance. They are classified according to the subsequent convention: very common (≥ 1/10), common (≥ 1/100 to <1/10), uncommon (≥1/1,000 to <1/100), rare (≥1/10,000 to <1/1,000), very rare (<1/10,000), or not known (cannot be estimated from the available data; data from post-marketing surveillance). Within each frequency-grouping, adverse reactions are presented in order of decreasing seriousness.

Description of selected adverse reactions
Due to the presence of naphazoline in the formula, pupil dilation, increase in intraocular pressure and systemic side effects as a result of absorption may occur. Systemic toxicity has been reported from topical application of sympathomimetic drugs such as naphazoline: headache, blood pressure elevation, extrasystoles, tachycardia, hyperglycaemia, faintness and cerebrovascular accidents have been reported (see section 4.4).

Paediatric population
Excessive use of NAPHCON-A* ophthalmic solution in infants and young children may cause depression of the central nervous system and significant reduction in body temperature (see section 4.9).

To report any side effect(s):
       • Saudi Arabia:
- The National Pharmacovigilance and Drug Safety Centre (NPC)
O Fax: +966-11-205-7662
O Call NPC at +966-11-2038222, Exts: 2317-2356-2353-2354-2334-2340.
O Toll free phone: 8002490000
O E-mail: npc.drug@sfda.gov.sa
O Website: www.sfda.gov.sa/npc
      • Other GCC States:
- Please contact the relevant competent authority

In case of overdosage or accidental ingestion, naphazoline can cause the following, particularly in children: depression of the central nervous system with a clear fall in body temperature and symptoms of bradycardia excessive sweating, drowsiness and coma; hypertension followed by hypotension.

An ocular overdose of NAPHCON-A* ophthalmic solution may be flushed from the eye(s) with lukewarm water. Treatment of an oral overdose is symptomatic and supportive.

Pharmacotherapeutic group: decongestants and antiallergics – sympathomimetics used as decongestants ATC code: S01GA51

NAPHCON-A* ophthalmic solution combines the effects of the antihistamine pheniramine maleate, an H1-receptor antagonist, and the decongestant naphazoline hydrochloride.

H1-receptor antagonists do not prevent histamine release, but reduce or obliterate most effects on smooth muscles.

Naphazoline is a sympathomimetic with substantial alpha-adrenergic activity. It is a vasoconstrictor with a fast and long-lasting activity, reducing oedema and congestion when applied to the mucosa. Through its local adrenergic activity naphazoline has a vasoconstrictive effect on the blood vessels, thereby causing a decongestion of the conjunctiva.

Pheniramine is administered by both oral and topical (nasal/ocular) routes. After oral administration, the bioavailability is high with half-life ranging from 8-19 hours in serum. Two Ndemethylated metabolites have been identified after systemic administration, which along with parent drug are excreted into the urine.

Following topical application of naphazoline hydrochloride solutions to the conjunctiva, local vasoconstriction usually occurs within 10 minutes and may persist for 2-6 hours. Naphazoline may be absorbed systemically after prolonged or exaggerated dosing to produce systemic effects.
Information on the distribution and elimination of the drug in humans is not available. Poor ocular absorption was observed in subjects who wear soft contacts as assessed by pupil dilation.

The limited amount of non-clinical data available for eye drops containing naphazoline and/or pheniramine does not reveal special hazard for humans based on conventional studies of safety pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential and toxicity to reproduction and development.

Boric acid, sodium chloride, borax, disodium edetate, benzalkonium chloride, sodium hydroxide and/or hydrochloric acid (to adjust pH) and purified water.

Not applicable.

Store below 25 °C. Protect from light and excessive heat.
Do not use this medicine after the expiry date which is stated on the packaging.
Discard 4 weeks after opening.
Keep this medicine out of the sight and reach of children.

Plastic DROPTAINER (LDPE) bottle containing 15 ml, with a natural LDPE dispensing plug and a white tamper-evident (PP) closure.

No special requirements.