Lotemax® Gel
Loteprednol 0.5% · ophthalmic gel
Steroid
Approved uses
Post-operative inflammation and pain after cataract surgery
1 to 2 drops into the conjunctival sac of the affected eye QID beginning the day after surgery, continuing through the first 2 post-operative weeks
By day 8, 74% are pain free and 31% have complete anterior chamber cell clearance.
Post-cataract-surgery inflammation in children 11 years and younger
Labeled regimen applies: 1 to 2 drops QID beginning the day after surgery through the first 2 post-operative weeks. The supporting pediatric trial instead used twice on the day of surgery, then QID for 2 weeks, BID for 1 week, and QD for 1 week
Matches prednisolone acetate 1% for day-14 inflammation in children 11 and under.
OFF-LABELNot in the FDA label for this product
Corticosteroid prophylaxis after photorefractive keratectomy
QID for 1 week, then TID for 3 weeks, then BID for 1 month, then QD for 1 month
Comparative trial · n=132
Single-center prospective, randomized, partially masked trial, 261 eyes of 132 patients, comparing this 3-month gel taper with prednisolone acetate 1% tapered to fluorometholone 0.1%; examiners were masked for IOP and haze grading. Corneal haze in the first 3 months occurred in 3 of 114 eyes on gel versus 7 of 147 on the comparator, and an IOP rise of 10 mmHg or more above baseline or any IOP above 21 mmHg in 2 of 114 versus 6 of 147; neither difference reached statistical significance. Visual and refractive results were equivalent, and the authors concluded only that the gel taper is clinically noninferior, not superior.
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 Forms0.5% gel (loteprednol etabonate 5 mg/g), 5 g in a 10 mL bottle
Mechanism of ActionCorticosteroid: 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. Lipid soluble and structurally engineered from prednisolone-related compounds for predictable breakdown to the inactive carboxylic acid metabolites PJ-90 and PJ-91; systemic exposure after ocular dosing of this gel has not been studied in humans.
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.
- Prescription renewal: Initial prescription and renewal only after examination with magnification such as slit lamp biomicroscopy and, where appropriate, fluorescein staining. This label sets no day count for the gate.
- Secondary ocular infection: Prolonged use may suppress host response and increase the hazard of secondary ocular infection; in acute purulent conditions of the eye steroids may mask infection or enhance existing infection.
- 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.
- Contact lens wear: Lenses should not be worn during the course of therapy.
Common Side Effects
- Ocular, 2% to 5%: Anterior chamber inflammation, eye pain, foreign body sensation, the most common adverse drug reactions in the clinical trials and the only ones the label quantifies.
- Corticosteroid class effects: Elevated IOP with infrequent optic nerve damage and visual acuity and field defects, posterior subcapsular cataract formation, delayed wound healing, secondary ocular infection from pathogens including herpes simplex, and perforation of the globe where the cornea or sclera is thinned.
Pregnancy & LactationPregnancy: No adequate and well controlled studies in pregnant women. Oral dosing produced teratogenicity at clinically relevant doses, with malformations in rabbits from 1.2 times the recommended human ophthalmic dose (spina bifida including meningocele at 0.1 mg/kg, exencephaly and craniofacial malformations from 4.9 times, abortion and resorption from 73 times) and in rats from 30 times, with reduced offspring survival in rats from 3 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 UseSafety and effectiveness established in pediatric patients, supported by a trial in patients from birth to 11 years of age.