Loteprednol Etabonate

Pronunciation: LOE-te-PRED-nol ET-a-BOE-nate
Class: Ophthalmic corticosteroid

Trade Names

Alrex
- Suspension, ophthalmic 0.2%

Lotemax
- Ointment, ophthalmic 0.5%
- Suspension, ophthalmic 0.5%

Pharmacology

Corticosteroids inhibit edema, fibrin deposition, capillary dilation, leukocyte migration, capillary and fibroblast proliferation, collagen deposition, and scar formation associated with inflammation. The mechanism of ocular corticosteroids is not known.

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Pharmacokinetics

Absorption

Systemic absorption after ocular instillation of loteprednol suspension is below the limit of quantitation (less than 1 ng/mL).

Metabolism

Undergoes extensive metabolism to inactive carboxylic acid metabolites.

Indications and Usage

Treatment of steroid-responsive inflammation of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe ( Lotemax suspension); treatment of inflammation and pain associated with ocular surgery ( Lotemax suspension/ointment); relief of the signs and symptoms of seasonal allergic conjunctivitis ( Alrex ).

Contraindications

Most active viral diseases of the cornea and conjunctiva, including epithelial herpes simplex keratitis (dendritic keratitis), vaccinia, and varicella; mycobacterial infection of the eye; fungal disease of ocular structures; hypersensitivity to any component of the product.

Dosage and Administration

Ophthalmic Instill 1 to 2 drops into the conjunctival sac of the operated eye(s) 4 times daily beginning 24 h after surgery and continuing throughout the first 2 wk of the postoperative period.

Ophthalmic Apply a small amount (approximately ½-inch ribbon) into the conjunctival sac(s) 4 times daily beginning 24 h after surgery and continuing throughout the first 2 wk of the postoperative period.

Ophthalmic Instill 1 drop into the affected eye(s) 4 times daily.

Ophthalmic Instill 1 to 2 drops into the conjunctival sac of the affected eye(s) 4 times daily. During the initial treatment within the first week, the dosing may be increased up to 1 drop every hour, if necessary. Care should be taken not to discontinue therapy prematurely.

General Advice

• Shake suspension vigorously before using.

Storage/Stability

Store between 59° and 77°F. Do not freeze.

Drug Interactions

None well documented.

Adverse Reactions

CNS

Headache (2%).

Ophthalmic

Anterior chamber inflammation (25%); abnormal vision/blurring, burning on instillation, chemosis, discharge, dry eyes, epiphora, foreign body sensation, injection, itching, photophobia (5% to 15%); conjunctival hyperemia, corneal edema, eye pain (4% to 5%); conjunctivitis, corneal abnormalities, eyelid erythema, keratoconjunctivitis, ocular irritation/pain/discomfort, papillae, uveitis (less than 5%); elevated IOP, which may be associated with optic nerve damage; perforation of the globe where there is thinning of the cornea or sclera; posterior subcapsular cataract formation; secondary ocular infection from pathogens, including herpes simplex; visual acuity and field defects.

Respiratory

Pharyngitis, rhinitis (less than 15%).

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Bacterial infection

Prolonged use may suppress the host response, increasing the hazard of secondary ocular infections. In acute purulent conditions, steroids may mask infection or enhance existing infection.

Cataracts

Posterior subcapsular cataract formation may occur.

Fungal infections

Prolonged use may increase the risk of fungal infections of the cornea.

Glaucoma

Prolonged use may result in glaucoma with damage to the optic nerve and defects in visual acuity and fields of vision. Use with caution in the presence of glaucoma.

Perforations

In those diseases causing thinning of the cornea or sclera, perforations have been known to occur with the use of topical steroids.

Viral infection

Use may prolong the course and exacerbate the severity of many ocular viral infections, including herpes simplex. Use with caution in patients with a history of herpes simplex.

Wound healing

Healing may be delayed and risk of bleb formation may be increased.

Overdosage

Symptoms

Systemic absorption is minimal following ocular instillation.

Patient Information

• Instruct patients on the proper method of ophthalmic ointment application into the conjunctival sac and suspension instillation.
• Advise patients to consult their health care provider if pain develops or if redness, itching, or inflammation becomes aggravated.
• Advise patients not to wear contact lenses when using loteprednol ointment or 0.5% suspension.
• Advise patients not to wear contact lenses during therapy if their eyes are red. Instruct patients using soft contact lenses whose eyes are not red to wait at least 10 min after loteprednol 0.2% suspension instillation before inserting contact lenses.
• Instruct patients to wash hands prior to using loteprednol.
• Inform patients to tell their health care provider if symptoms do not improve within 2 days.
• Advise patients not to touch the eyelid or surrounding areas with the tip of the tube or to allow the dropper tip to touch any surface because this may contaminate the product.

Copyright © 2009 Wolters Kluwer Health.