Lotemax® Ointment

Loteprednol 0.5% · ophthalmic ointment

Steroid

Approved uses

Post-operative inflammation and pain after cataract surgery

Approximately a 1/2 inch ribbon into the conjunctival sac(s) QID beginning 24 hours after surgery, continuing through the first 2 post-operative weeks

By day 8, 76% are pain free and 28% have complete resolution of anterior chamber inflammation.

Contraindications

Most viral diseases of the cornea and conjunctiva, including epithelial herpes simplex keratitis (dendritic keratitis), vaccinia, and varicella.
Mycobacterial infection of the eye.
Fungal diseases of ocular structures.

Available Forms

0.5% ointment (loteprednol etabonate 5 mg/g), 3.5 g tube

Mechanism of Action

Corticosteroid: binds and activates the glucocorticoid receptor and is thought to inhibit prostaglandin production through several independent mechanisms, suppressing the edema, fibrin deposition, capillary dilation, leukocyte migration, fibroblast proliferation, and collagen deposition of post-operative inflammation, while probably delaying healing. Systemic exposure from this ointment has not been studied in humans; the label states that QID dosing is not expected to exceed exposures attained with the 0.5% suspension dosed up to 2 drops QID, and in the suspension bioavailability study (1 drop OU 8 times daily for 2 days, or QID for 42 days) plasma drug and primary metabolite stayed below the 1 ng/mL limit of quantitation.

Warnings & Precautions

IOP elevation and glaucoma: Prolonged corticosteroid use may result in glaucoma with optic nerve damage and defects in visual acuity and visual fields; use with caution in the presence of glaucoma, and monitor IOP if this product is used 10 days or longer.
Posterior subcapsular cataract: Corticosteroid use may produce it.
Delayed healing after cataract surgery: Steroids used after cataract surgery may delay healing and increase the incidence of bleb formation.
Corneal or scleral perforation: In diseases causing thinning of the cornea or sclera, perforations have occurred with topical steroids.
Renewal beyond 14 days: Initial prescription and renewal past 14 days only after examination with magnification such as slit lamp biomicroscopy and, where appropriate, fluorescein staining.
Secondary ocular infection: Prolonged use may suppress host response and increase the hazard of secondary ocular infection; in acute purulent conditions steroids may mask infection or enhance existing infection, and the patient should be re-evaluated if signs and symptoms fail to improve after 2 days.
Viral infection exacerbation: Ocular steroids may prolong the course and worsen the severity of many ocular viral infections including herpes simplex; a history of herpes simplex requires great caution.
Fungal keratitis: Fungal corneal infection is particularly prone to develop coincidentally with long-term local steroid use; consider fungal invasion in any persistent corneal ulceration where a steroid has been used or is in use, and culture when appropriate.
Tube contamination: Do not touch the eyelid or surrounding areas with the tip of the tube, and keep the cap on the tube when not in use.
Contact lens wear: Lenses should not be worn during the course of therapy.
Route of administration: Topical ophthalmic use only; not indicated for intraocular administration.

Common Side Effects

Ocular, approximately 25%: Anterior chamber inflammation, the most common ocular adverse event in the clinical studies; the label notes many of these events may have been consequences of the surgical procedure.
Ocular, 4% to 5%: Conjunctival hyperemia, corneal edema, eye pain.
Systemic, 1.5%: Headache, the only non-ocular adverse event occurring at 1% or more.
Corticosteroid class effects: Elevated IOP with optic nerve damage and visual acuity and field defects, posterior subcapsular cataract formation, secondary ocular infection from pathogens including herpes simplex, and perforation of the globe where the cornea or sclera is thinned.

Pregnancy & Lactation

Pregnancy: No adequate and well controlled studies in pregnant women. Oral dosing produced teratogenicity at clinically relevant doses, with malformations in rabbits from 1.6 times the recommended human ophthalmic dose (spina bifida including meningocele at 0.1 mg/kg, exencephaly and craniofacial malformations from 6.5 times, abortion and resorption from 97 times) and in rats from 41 times, with reduced offspring survival in rats from 4 times. Background risk in the U.S. general population is 2% to 4% for major birth defects and 15% to 20% for miscarriage.

Lactation: No data on the presence of drug in human milk, on effects in the breastfed infant, or on milk production; weigh the developmental and health benefits of breastfeeding against the clinical need and potential adverse effects.

Pediatric Use

Safety and effectiveness in pediatric patients have not been established.