Efemoline

Uses

Fluorometholone Acetate ophthalmic suspension is used for the treatment of-

• Acute and chronic non-infectious conjunctivitis and keratitis of allergic origin.
• Non-infectious inflammation of the anterior chamber of the eye (including anterior uveitis, episcleritis and scleritis).
• Post-operative irritative conditions after strabismus, cataract and glaucoma surgery.

Naphazoline is a sympathomimetic vasoconstrictor used for the symptomatic relief of redness and itching of the eye, and nasal congestion.

Naphazoline is indicated for use as OTC eyedrops for ocular vasoconstriction or as a nasal preparation for nasal congestion.

Efemoline is also used to associated treatment for these conditions: Anterior chamber inflammation, Conjunctivitis allergic, Corneal Inflammation, Inflammation, Ocular Inflammation, Ocular bacterial infectionsBacterial Conjunctivitis, Blepharoconjunctivitis, Conjunctivitis, Conjunctivitis allergic, Dacryocystitis, Dacryostenosis, Dermatitis, Eczematous of the Eyelid, Eye Pain, Eye redness, Iritis, Lacrimation, Nasal Allergies, Nasal Congestion, Noninfective conjunctivitis, Otitis Media (OM), Photophobia, Foreign body sensation in eye, Ocular bacterial infections, Ocular vasoconstriction

How Efemoline works

There is no generally accepted explanation for the mechanism of action of ocular corticosteroids. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor, arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2. Their primary target is the cytosolic glucocorticoid receptor. After binding the receptor the newly formed receptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements (GRE) in the promoter region of the target genes. The DNA bound receptor then interacts with basic transcription factors, causing the increase in expression of specific target genes.

Naphazoline is a vasoconstrictor that functions by stimulating alpha adrenergic receptors in arterioles leading to decreased congestion at the site of administration.

Naphazoline causes the release of norepinephrine in sympathetic nerves. Norepinephrine binds to alpha adrenergic receptors and causes vasoconstriction. Naphazoline is also a mild beta adrenergic receptor agonist, which can cause rebound vasodilation after the alpha adrenergic stimulation has ended. Naphazoline's release of norepinephrine also triggers a negative feedback loop which decreases production of norepinephrine, which can lead to rhinitis medicamentosa after long term use when naphazoline is stopped.

Dosage

Efemoline dosage

1 drop instilled into the conjunctival sac 2-4 times daily. During the initial 24 to 48 hours the dosage may be safely increased to 1 drop every hour. Care should be taken not to discontinue therapy prematurely. Shake well before use.

Side Effects

Glaucoma with optic nerve damage, visual acuity or field defects, cataract formation, secondary ocular infection following suppression of host immunity, perforation of the globe.

Toxicity

Side effects may include acute anterior uveitis and perforation of the globe. Keratitis, conjunctivitis, corneal ulcers, mydriasis, conjunctival hyperemia, loss of accommodation and ptosis have occasionally been reported following local use of corticosteroids. LD₅₀ = 234 mg/kg (rats)

In high doses or when ingested, naphazoline can lead to central nervous system depression (which can progress to coma and death), hypothermia, bradycardia, and death. This effect is especially pronounced in children under 6 years.

Long term use of naphazoline can lead to rhinitis medicamentosa once naphazoline is stopped. This condition is a result of norepinephrine release by naphazoline triggering a negative feedback loop.

Safety and effectiveness in children under 12 has not been established. Studies in elderly patients have yet to be performed. Risk in pregnancy, breast feeding, and on overall fertility have not been established, though pregnant and breast feeding patients should consider the risk and benefit before starting naphazoline treatment.

Precaution

Shake well before using. If this product is used for 10 days or longer, intraocular pressure should be monitored.

Interaction

Specific drug interaction studies have not been conducted with Fluorometholone ophthalmic suspension.

Volume of Distribution

Distribution data for naphazoline are scarce but imidazoline compounds are distributed throughout the body, and can cross the blood-brain barrier.

Elimination Route

Absorption data for naphazoline are scarce but imidazoline compounds in general are weakly basic and lipophilic, with high bioavailability from the gastrointestinal tract.

Half Life

Half life has not been determined but effects last for 4 to 8 hours. Other imidazoline compounds have half lives varying from 2 to 12 hours.

Clearance

Clearance data for naphazoline is unavailable.

Elimination Route

Imidazoline compounds undergo some hepatic metabolism but a large fraction of the dose may be excreted unchanged in the urine. Urinary excretion is higher with more acidic urine.

Pregnancy & Breastfeeding use

Safety of the use of topical steroids during pregnancy and lactation has not been established. Fluorometholone ophthalmic suspension should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Contraindication

• Hypersensitivity to any ingredient of the formulation.
• Infectious conjunctivitis or keratitis.
• Injuries and ulcerous processes of cornea, especially infections caused by virus, bacteria and fungi.
• Dry eyes, especially keratoconjunctivitis sicca.
• Glaucoma.

Storage Condition

Store in a cool, dry place and protected from light. Keep out of the reach of children. Discard the container 4 weeks after opening.

Innovators Monograph

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