Label: LOTEMAX- loteprednol etabonate gel

  • NDC Code(s): 24208-503-07, 24208-503-48
  • Packager: Bausch & Lomb Incorporated
  • Category: HUMAN PRESCRIPTION DRUG LABEL
  • DEA Schedule: None
  • Marketing Status: New Drug Application

Drug Label Information

Updated 10/14

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  • HIGHLIGHTS OF PRESCRIBING INFORMATION
    These highlights do not include all the information needed to use LOTEMAX ®  (loteprednol etabonate ophthalmic gel) 0.5% safely and effectively. See full prescribing information for LOTEMAX ®.


    LOTEMAX ® (loteprednol etabonate ophthalmic gel) 0.5%
    Initial U.S. Approval: 1998

    INDICATIONS AND USAGE

    LOTEMAX is a corticosteroid indicated for the treatment of post-operative inflammation and pain following ocular surgery. (1)

    DOSAGE AND ADMINISTRATION

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

    Apply one to two drops of LOTEMAX into the conjunctival sac of the affected eye four times daily beginning the day after surgery and continuing throughout the first 2 weeks of the post-operative period. (2)

    DOSAGE FORMS AND STRENGTHS

    LOTEMAX contains 5 mg/g of loteprednol etabonate, as a sterile preserved ophthalmic gel. (3)

    CONTRAINDICATIONS

    LOTEMAX, 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. (4)

    WARNINGS AND PRECAUTIONS

    Intraocular pressure (IOP) increase - Prolonged use of corticosteroids may result in glaucoma with damage to the optic nerve, defects in visual acuity and fields of vision. If this product is used for 10 days or longer, IOP should be monitored. ( 5.1)

    Cataracts- Use of corticosteroids may result in posterior subcapsular cataract formation. ( 5.2)

    Delayed healing–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. ( 5.3)

    Bacterial infections–Prolonged use of corticosteroids may suppress the host response and thus increase the hazard of secondary ocular infection. In acute purulent conditions, steroids may mask infection or enhance existing infection. ( 5.4)

    Viral infections–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). ( 5.5)

    Fungal infections–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. ( 5.6)

    ADVERSE REACTIONS

     The most common adverse drug reactions were anterior chamber inflammation (5%), eye pain (2%), and foreign body sensation (2%). (6)

    To report SUSPECTED ADVERSE REACTIONS, contact Bausch & Lomb at 1-800-323-0000 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch

    See 17 for PATIENT COUNSELING INFORMATION.

    Revised: 10/2014

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  • FULL PRESCRIBING INFORMATION: CONTENTS*
  • 1 INDICATIONS AND USAGE

    LOTEMAX® is a corticosteroid indicated for the treatment of post-operative inflammation and pain following ocular surgery.

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  • 2 DOSAGE AND ADMINISTRATION

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

    Apply one to two drops of LOTEMAX into the conjunctival sac of the affected eye four times daily beginning the day after surgery and continuing throughout the first 2 weeks of the post-operative period.

    Close
  • 3 DOSAGE FORMS AND STRENGTHS

    LOTEMAX (loteprednol etabonate ophthalmic gel) 0.5% contains 5 mg/g of loteprednol etabonate, as a sterile preserved ophthalmic gel.

    Close
  • 4 CONTRAINDICATIONS

    LOTEMAX, 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.

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  • 5 WARNINGS AND PRECAUTIONS

    5.1 Intraocular Pressure (IOP) Increase

    Prolonged use of corticosteroids 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.

    5.2 Cataracts

    Use of corticosteroids may result in posterior subcapsular cataract formation.

    5.3 Delayed Healing

    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.

    5.4 Bacterial Infections

    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.

    5.5 Viral Infections

    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).

    5.6 Fungal Infections

    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.

    5.7 Contact Lens Wear

    Patients should not wear contact lenses during their course of therapy with LOTEMAX.

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  • 6 ADVERSE REACTIONS

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

    The most common adverse drug reactions reported were anterior chamber inflammation (5%), eye pain (2%), and foreign body sensation (2%).

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  • 8 USE IN SPECIFIC POPULATIONS

    8.1 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 resulted in teratogenicity (absent innominate artery at ≥5 mg/kg/day doses, and cleft palate and umbilical hernia at ≥50 mg/kg/day) and embryotoxicity (increased post-implantation losses at 100 mg/kg/day and decreased fetal body weight and skeletal ossification with ≥50 mg/kg/day). Treatment of rats with 0.5 mg/kg/day (6 times the maximum clinical dose) during organogenesis did not result in any reproductive toxicity. 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.

    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 (significantly decreased body weight gain), gave rise to decreased growth and survival, and retarded development in the offspring during lactation; the NOEL for these effects was 5 mg/kg/day. Loteprednol etabonate had no effect on the duration of gestation or parturition when administered orally to pregnant rats at doses up to 50 mg/kg/day during the fetal period.

    There are no adequate and well controlled studies in pregnant women. LOTEMAX® should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

    8.3 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 LOTEMAX is administered to a nursing woman.

    8.4 Pediatric Use

    Safety and effectiveness in pediatric patients have not been established.

    8.5 Geriatric Use

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

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  • 11 DESCRIPTION

    LOTEMAX (loteprednol etabonate ophthalmic gel) 0.5% contains a sterile, topical corticosteroid for ophthalmic use. Loteprednol etabonate is a white to off-white powder.

    Loteprednol etabonate is represented by the following structural formula:

    Loteprednol etabonate structural formula

    Chemical Name:

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

    Each gram contains:

    ACTIVE: Loteprednol Etabonate 5 mg (0.5%);

    INACTIVES: Boric acid, edetate disodium dihydrate, glycerin, polycarbophil, propylene glycol, sodium chloride, tyloxapol, water for injection, and sodium hydroxide to adjust to a pH of between 6 and 7.

    PRESERVATIVE: benzalkonium chloride 0.003%.

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  • 12 CLINICAL PHARMACOLOGY

    12.1 Mechanism of Action

    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.

    12.3 Pharmacokinetics

    Loteprednol 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 LOTEMAX has not been studied in humans.

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  • 13 NONCLINICAL TOXICOLOGY

    13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility

    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 male and female rats with up to 50 mg/kg/day and 25 mg/kg/day of loteprednol etabonate, respectively, (600 and 300 times the maximum clinical dose, respectively) prior to and during mating did not impair fertility in either gender.

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  • 14 CLINICAL STUDIES

    In two randomized, multicenter, double-masked, parallel-group, vehicle-controlled studies in 813 subjects with, post-operative inflammation, LOTEMAX 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, LOTEMAX had a statistically significant higher incidence of subjects with complete clearing of anterior chamber cells (31% vs. 14-16%) and were pain free at post-operative day 8 (73-76% vs. 42-46%).

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  • 16 HOW SUPPLIED/STORAGE AND HANDLING

    LOTEMAX® (loteprednol etabonate ophthalmic gel) 0.5% is a sterile ophthalmic gel supplied in a white low density polyethylene plastic bottle with a white controlled drop tip and a pink polypropylene cap in the following size:

    5 g in a 10 mL bottle (NDC 24208-503-07)

    Use only if imprinted neckband is intact.

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

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  • 17 PATIENT COUNSELING INFORMATION

    17.1 Administration

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

    17.2 Risk of Contamination

    Patients should be advised not to allow the dropper tip to touch any surface, as this may contaminate the gel.

    17.3 Contact Lens Wear

    Patients should be advised not to wear contact lenses when using LOTEMAX.

    17.4 Risk of Secondary Infection

    If pain develops, redness, itching or inflammation becomes aggravated, the patient should be advised to consult a physician.



    Bausch & Lomb Incorporated
    Tampa, Florida 33637 USA

    US Patent No. 5,800,807

    ©Bausch & Lomb Incorporated
    ®/™ are trademarks of Bausch & Lomb Incorporated or its affiliates.

    Reference ID: 3196435

    9269100 Flat

    9269200 Folded

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  • PACKAGE/LABEL PRINCIPAL DISPLAY PANEL

    LOTEMAX® (loteprednol etabonate ophthalmic gel) 0.5% label

    NDC 24208-503-07

    BAUSCH + LOMB

    LOTEMAX®

    loteprednol etabonate
    ophthalmic gel 0.5%

    Sterile

    Rx only

    5 g

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  • INGREDIENTS AND APPEARANCE
    LOTEMAX 
    loteprednol etabonate gel
    Product Information
    Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:24208-503
    Route of Administration OPHTHALMIC DEA Schedule     
    Active Ingredient/Active Moiety
    Ingredient Name Basis of Strength Strength
    LOTEPREDNOL ETABONATE (LOTEPREDNOL) LOTEPREDNOL ETABONATE 5 mg  in 1 g
    Inactive Ingredients
    Ingredient Name Strength
    BORIC ACID  
    EDETATE DISODIUM  
    GLYCERIN  
    POLYCARBOPHIL  
    PROPYLENE GLYCOL  
    SODIUM CHLORIDE  
    TYLOXAPOL  
    WATER  
    SODIUM HYDROXIDE  
    BENZALKONIUM CHLORIDE  
    Packaging
    # Item Code Package Description Marketing Start Date Marketing End Date
    1 NDC:24208-503-07 1 in 1 CARTON
    1 5 g in 1 BOTTLE
    2 NDC:24208-503-48 1 in 1 CARTON
    2 0.5 g in 1 BOTTLE
    Marketing Information
    Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
    NDA NDA202872 10/12/2012
    Labeler - Bausch & Lomb Incorporated (196603781)
    Establishment
    Name Address ID/FEI Business Operations
    Bausch & Lomb Incorporated 807927397 MANUFACTURE(24208-503)
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