Loteprednol Etabonate

Prolonged use of corticosteroids, including loteprednol etabonate ophthalmic gel, may result in glaucoma with damage to the optic nerve, defects in visual acuity and fields of vision. Steroids should be used with caution in the presence of glaucoma. If this product is used for 10 days or longer, intraocular pressure should be monitored.

Use of corticosteroids may result in posterior subcapsular cataract formation.

The use of steroids after cataract surgery may delay healing and increase the incidence of bleb formation. In those diseases causing thinning of the cornea or sclera, perforations have been known to occur with the use of topical steroids. The initial prescription and renewal of the medication order should be made by a physician only after examination of the patient with the aid of magnification such as slit lamp biomicroscopy and, where appropriate, fluorescein staining.

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

Employment of a corticosteroid medication in the treatment of patients with a history of herpes simplex requires great caution. Use of ocular steroids may prolong the course and may exacerbate the severity of many viral infections of the eye (including herpes simplex).

Fungal infections of the cornea are particularly prone to develop coincidentally with long-term local steroid application. Fungus invasion must be considered in any persistent corneal ulceration where a steroid has been used or is in use. Fungal cultures should be taken when appropriate.

Patients should not wear contact lenses during their course of therapy with loteprednol etabonate ophthalmic gel.

There are no data on the presence of loteprednol etabonate in human milk, the effects on the breastfed infant, or the effects on milk production. The developmental and health benefits of breastfeeding should be considered, along with the mother's clinical need for loteprednol etabonate ophthalmic gel and any potential adverse effects on the breastfed infant from loteprednol etabonate ophthalmic gel.

Pediatric use information is approved for Bausch and Lomb Inc.'s LOTEMAX (loteprednol etabonate) ophthalmic gel. However, due to Bausch and Lomb Inc.'s marketing exclusivity rights, this drug product is not labeled with the pediatric information.

No overall differences in safety and effectiveness have been observed between elderly and younger patients.

Corticosteroids inhibit the inflammatory response to a variety of inciting agents and probably delay or slow healing. They inhibit the edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, fibroblast proliferation, deposition of collagen, and scar formation associated with inflammation. While glucocorticoids are known to bind to and activate the glucocorticoid receptor, the molecular mechanisms involved in glucocorticoid/glucocorticoid receptor-dependent modulation of inflammation are not clearly established. However, corticosteroids are thought to inhibit prostaglandin production through several independent mechanisms.

Loteprednol etabonate is lipid soluble and can penetrate into cells. Loteprednol etabonate is synthesized through structural modifications of prednisolone-related compounds so that it will undergo a predictable transformation to an inactive metabolite. Based upon in vivo and in vitro preclinical metabolism studies, loteprednol etabonate undergoes extensive metabolism to the inactive carboxylic acid metabolites, PJ-91 and PJ-90. The systemic exposure to loteprednol etabonate following ocular administration of loteprednol etabonate ophthalmic gel has not been studied in humans.

Long-term animal studies have not been conducted to evaluate the carcinogenic potential of loteprednol etabonate. Loteprednol etabonate was not genotoxic in vitro in the Ames test, the mouse lymphoma tk assay, or in a chromosome aberration test in human lymphocytes, or in vivo in the single dose mouse micronucleus assay.

Treatment of female and male rats with doses ≥ 25 mg/kg/day of loteprednol etabonate (152 times the RHOD based on body surface area, assuming 100% absorption) prior to and during mating caused preimplantation loss and decreased the number of live fetuses/live births. The NOAEL for fertility in rats was 5 mg/kg/day (30 times the RHOD).

Adult Studies

In two randomized, multicenter, double-masked, parallel-group, vehicle-controlled studies in 813 subjects with post-operative inflammation, loteprednol etabonate ophthalmic gel was more effective compared to its vehicle in resolving anterior chamber inflammation and pain following cataract surgery. Primary endpoints were complete resolution of anterior chamber cells (cell count of 0) and no pain at post-operative day 8.

In these studies, loteprednol etabonate ophthalmic gel had a statistically significant higher incidence of subjects with complete clearing of anterior chamber cells (31% vs. 14 to 16%) and were pain-free at post-operative day 8 (73 to 76% vs. 42 to 46%).

Pediatric Study

Pediatric use information is approved for Bausch and Lomb Inc.'s LOTEMAX (loteprednol etabonate) ophthalmic gel. However, due to Bausch and Lomb Inc.'s marketing exclusivity rights, this drug product is not labeled with the pediatric information.

Storage: Store upright at 15º to 25º C (59º to 77º F).

Administration

Invert closed bottle and shake once to fill tip before instilling drops.

Risk of Contamination

Advise patients not to allow the dropper tip to touch any surface, as this may contaminate the gel.

Contact Lens Wear

Advise patients not to wear contact lenses when using loteprednol etabonate ophthalmic gel.

Risk of Secondary Infection

Advise the patient to consult a physician if pain develops, redness, itching or inflammation becomes aggravated.

AKORN
Manufactured by: Akorn, Inc.
Lake Forest, IL 60045

Made in Switzerland

LO00N       Rev. 01/21