Loteprednol Etabonate

Description

DESCRIPTION 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: C 24 H 31 ClO 7 Mol. Wt. 466.96 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, Water for Injection and Tyloxapol. Hydrochloric Acid and/or Sodium Hydroxide may be added to adjust the pH to 5.0 - 6.0. The suspension is essentially isotonic with a tonicity of 250 to 310 mOsmol/kg. PRESERVATIVE ADDED: Benzalkonium Chloride Solution (50%) 0.2 mg. spl-loteprednol-structure

What Is Loteprednol Etabonate Used For?

INDICATIONS AND USAGE 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 ophthalmic suspension 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 ophthalmic suspension 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 ophthalmic suspension and 6% with prednisolone acetate 1%. Loteprednol etabonate ophthalmic suspension 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.

Dosage and Administration

DOSAGE AND ADMINISTRATION SHAKE VIGOROUSLY BEFORE USING. Steroid Responsive Disease Treatment: Apply one to two drops of loteprednol etabonate ophthalmic suspension into the conjunctival sac of the affected eye(s) 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 ophthalmic suspension into the conjunctival sac of the operated eye(s) four times daily beginning 24 hours after surgery and continuing throughout the first 2 weeks of the post-operative period.

Side Effects (Adverse Reactions)

ADVERSE REACTIONS 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% to 15% of patients treated with loteprednol etabonate ophthalmic suspension (0.2% to 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 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 Sun Pharmaceutical Industries, Inc. at 1-800-818-4555 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

Contraindications

CONTRAINDICATIONS Loteprednol etabonate ophthalmic suspension, 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 ophthalmic suspension is also contraindicated in individuals with known or suspected hypersensitivity to any of the ingredients of this preparation and to other corticosteroids.

Pregnancy and Breastfeeding

Pregnancy Teratogenic Effects: Pregnancy Category C. Loteprednol etabonate has been shown to be embryotoxic (delayed ossification) and teratogenic (increased incidence of meningocele, abnormal left common carotid artery, and limb flexures) when administered orally to rabbits during organogenesis at a dose of 3 mg/kg/day (35 times the maximum daily clinical dose), a dose which caused no maternal toxicity. The no-observed-effect-level (NOEL) for these effects was 0.5 mg/kg/day (6 times the maximum daily clinical dose). Oral treatment of rats during organogenesis with 50 mg/kg/day or 100 mg/kg/day (600 and 1,200 times the maximum clinical dose) resulted in embryotoxicity (increased post-implantation losses with 100 mg/kg/day, and decreased fetal body weight and skeletal ossification with 50 mg/kg/day and 100 mg/kg/day); doses of 5 mg/kg/day (60 times the maximum daily clinical dose), 50 mg/kg/day and 100 mg/kg/day caused teratogenicity (absent innominate artery at all doses, and cleft palate and umbilical hernia at 50 mg/kg/day and 100 mg/kg/day). Loteprednol etabonate was maternally toxic (significantly reduced body weight gain during treatment) when administered to pregnant rats during organogenesis at doses of 5 mg/kg/day to 100 mg/kg/day but not at 0.5 mg/kg/day. The NOELs for the embryotoxic and teratogenic effects in rats were 5 mg/kg/day and 0.5 mg/kg/day (60 and 6 times the maximum daily clinical dose) for embryotoxicity and teratogenicity, respectively. Oral exposure of pregnant rats to 5 mg/kg/day and 50 mg/kg/day of loteprednol etabonate during the fetal period, a maternally toxic treatment regimen (significantly decreased body weight gain), resulted in teratogenicity (umbilical herniation) and embryotoxicity (decreased fetal birth weight); the NOEL for these effects was 0.5 mg/kg/day. Oral exposure of female rats to 50 mg/kg/day of loteprednol etabonate from the start of the fetal period through the end of lactation, a maternally toxic treatment regimen...

Nursing Mothers It is not known whether topical ophthalmic administration of corticosteroids could result in sufficient systemic absorption to produce detectable quantities in human milk. Systemic steroids appear in human milk and could suppress growth, interfere with endogenous corticosteroid production, or cause other untoward effects. Caution should be exercised when loteprednol etabonate ophthalmic suspension is administered to a nursing woman.

How Supplied

HOW SUPPLIED Loteprednol etabonate ophthalmic suspension is supplied in a white opaque LDPE plastic dropper bottle with LDPE white opaque plug and HDPE pilfer-proof pink cap as follows: 5 mL (NDC 62756-232-90) 10 mL (NDC 62756-232-55) 15 mL (NDC 62756-232-56) Storage: Store upright between 20°C-25°C (68°-77°F). DO NOT FREEZE. KEEP OUT OF REACH OF CHILDREN. Rx only Manufactured by: Sun Pharmaceutical Medicare Ltd. Baska Ujeti Road, Ujeti, Halol-389350, Gujarat, India. Distributed by: Sun Pharmaceutical Industries, Inc. Cranbury, NJ 08512 Version Date: ISS. 08/2020