Get your patient on Loteprednol Etabonate - Loteprednol Etabonate suspension/ Drops (Loteprednol Etabonate)

Loteprednol etabonate ophthalmic suspension is indicated for the treatment of steroid-responsive inflammatory conditions of the palpebral and bulbar conjunctiva, cornea and anterior segment of the globe such as allergic conjunctivitis, acne rosacea, superficial punctate keratitis, herpes zoster keratitis, iritis, cyclitis, selected infective conjunctivitides, when the inherent hazard of steroid use is accepted to obtain an advisable diminution in edema and inflammation.

Loteprednol etabonate is less effective than prednisolone acetate 1% in two 28-day controlled clinical studies in acute anterior uveitis, where 72% of patients treated with loteprednol etabonate experienced resolution of anterior chamber cells, compared to 87% of patients treated with prednisolone acetate 1%. The incidence of patients with clinically significant increases in IOP (≥10 mmHg) was 1% with loteprednol etabonate and 6% with prednisolone acetate 1%. Loteprednol etabonate should not be used in patients who require a more potent corticosteroid for this indication.

Loteprednol etabonate ophthalmic suspension is also indicated for the treatment of post-operative inflammation following ocular surgery.

SHAKE VIGOROUSLY BEFORE USING.

Steroid-Responsive Disease Treatment: Apply one to two drops of loteprednol etabonate suspension into the conjunctival sac of the affected eye four 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. If signs and symptoms fail to improve after two days, the patient should be re-evaluated (see PRECAUTIONS ).

Post-Operative Inflammation: Apply one to two drops of loteprednol etabonate suspension into the conjunctival sac of the operated eye four times daily beginning 24 hours after surgery and continuing throughout the first 2 weeks of the post-operative period.

Loteprednol etabonate, as with other ophthalmic corticosteroids, is contraindicated in most viral diseases of the cornea and conjunctiva including epithelial herpes simplex keratitis (dendritic keratitis), vaccinia, and varicella, and also in mycobacterial infection of the eye and fungal diseases of ocular structures. Loteprednol etabonate is also contraindicated in individuals with known or suspected hypersensitivity to any of the ingredients of this preparation and to other corticosteroids.

Reactions associated with ophthalmic steroids include elevated intraocular pressure, which may be associated with optic nerve damage, visual acuity and field defects, posterior subcapsular cataract formation, secondary ocular infection from pathogens including herpes simplex, and perforation of the globe where there is thinning of the cornea or sclera.

Ocular adverse reactions occurring in 5%-15% of patients treated with loteprednol etabonate ophthalmic suspension (0.2%-0.5%) in clinical studies included abnormal vision/blurring, burning on instillation, chemosis, discharge, dry eyes, epiphora, foreign body sensation, itching, injection, and photophobia. Other ocular adverse reactions occurring in less than 5% of patients include conjunctivitis, corneal abnormalities, eyelid erythema, keratoconjunctivitis, ocular irritation/pain/discomfort, papillae, and uveitis. Some of these events were similar to the underlying ocular disease being studied.

Non-ocular adverse reactions occurred in less than 15% of patients. These include headache, rhinitis and pharyngitis.

In a summation of controlled, randomized studies of individuals treated for 28 days or longer with loteprednol etabonate, the incidence of significant elevation of intraocular pressure (≥10 mmHg) was 2% (15/901) among patients receiving loteprednol etabonate, 7% (11/164) among patients receiving 1% prednisolone acetate and 0.5% (3/583) among patients receiving placebo.

To report SUSPECTED ADVERSE REACTIONS, contact Bausch & Lomb Incorporated at 1-800-553-5340 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .

Loteprednol etabonate ophthalmic suspension contains a sterile, topical anti-inflammatory corticosteroid for ophthalmic use. Loteprednol etabonate is a white to off-white powder.

Loteprednol etabonate is represented by the following structural formula:

Chemical Name:

chloromethyl 17α-[(ethoxycarbonyl)oxy]-11β-hydroxy-3-oxoandrosta-1,4-diene-17β-carboxylate

Each mL contains:

Active: Loteprednol Etabonate 5 mg (0.5%)

Inactives: Edetate Disodium, Glycerin, Povidone, Purified Water and Tyloxapol. Hydrochloric Acid and/or Sodium Hydroxide may be added to adjust the pH. The suspension is essentially isotonic with a tonicity of 250 to 310 mOsmol/kg.

Preservative: Benzalkonium Chloride 0.01%

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. 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 A ₂ 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 A ₂ . Corticosteroids are capable of producing a rise in intraocular pressure (IOP).

Loteprednol etabonate is structurally similar to other corticosteroids. However, the number 20 position ketone group is absent. It is highly lipid soluble which enhances its penetration 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 vivoand in vitropreclinical metabolism studies, loteprednol etabonate undergoes extensive metabolism to inactive carboxylic acid metabolites.

Results from a bioavailability study in normal volunteers established that plasma levels of loteprednol etabonate and Δ ¹ cortienic acid etabonate (PJ 91), its primary, inactive metabolite, were below the limit of quantitation (1 ng/mL) at all sampling times. The results were obtained following the ocular administration of one drop in each eye of 0.5% loteprednol etabonate 8 times daily for 2 days or 4 times daily for 42 days. This study suggests that limited (<1 ng/mL) systemic absorption occurs with loteprednol etabonate.

Clinical Studies:

Post-Operative Inflammation : Placebo-controlled clinical studies demonstrated that loteprednol etabonate is effective for the treatment of anterior chamber inflammation as measured by cell and flare.

Giant Papillary Conjunctivitis: Placebo-controlled clinical studies demonstrated that loteprednol etabonate was effective in reducing the signs and symptoms of giant papillary conjunctivitis after 1 week of treatment and continuing for up to 6 weeks while on treatment.

Seasonal Allergic Conjunctivitis: A placebo-controlled clinical study demonstrated that loteprednol etabonate was effective in reducing the signs and symptoms of allergic conjunctivitis during peak periods of pollen exposure.

Uveitis: Controlled clinical studies of patients with uveitis demonstrated that loteprednol etabonate was less effective than prednisolone acetate 1%. Overall, 72% of patients treated with loteprednol etabonate experienced resolution of anterior chamber cell by day 28, compared to 87% of patients treated with 1% prednisolone acetate. The incidence of patients with clinically significant increases in IOP (≥10 mmHg) was 1% with loteprednol etabonate and 6% with prednisolone acetate 1%.

Loteprednol etabonate ophthalmic suspension is supplied in a plastic bottle with a controlled drop tip in the following sizes:

• NDC 82260-299-05 5 mL
  NDC 82260-299-10 10 mL
  NDC 82260-299-15 15 mL

Storage: Store upright between 15°C to 25°C (59°F to 77°F). DO NOT FREEZE

Keep out of reach of children.

Distributed by: Bausch & Lomb Americas Inc., Bridgewater, NJ 08807 USA

Manufactured by: Bausch & Lomb Incorporated, Tampa, FL 33637 USA

© 2023 Bausch & Lomb Incorporated or its affiliates

Revised: April 2023

9792100 (Folded)
9792200 (Flat)