Lotemax ophthalmic suspension 0.5%

Name: Lotemax ophthalmic suspension 0.5%

Clinical Pharmacology

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.

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 vivo and in vitro preclinical 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 (DELTA) 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 LOTEMAX.

Clinical Studies:

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

Giant Papillary Conjunctivitis :   Placebo-controlled clinical studies demonstrated that LOTEMAX 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 LOTEMAX 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 LOTEMAX was less effective than prednisolone acetate 1%. Overall, 72% of patients treated with LOTEMAX 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 LOTEMAX and 6% with prednisolone acetate 1%.

Indications and Usage

LOTEMAX 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.

LOTEMAX is less effective than prednisolone acetate 1% in two 28-day controlled clinical studies in acute anterior uveitis, where 72% of patients treated with LOTEMAX 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 LOTEMAX and 6% with prednisolone acetate 1%. LOTEMAX should not be used in patients who require a more potent corticosteroid for this indication.

LOTEMAX is also indicated for the treatment of post-operative inflammation following ocular surgery.

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. LOTEMAX is also contraindicated in individuals with known or suspected hypersensitivity to any of the ingredients of this preparation and to other corticosteroids.

Warnings:

  Prolonged use of corticosteroids may result in glaucoma with damage to the optic nerve, defects in visual acuity and fields of vision, and in posterior subcapsular cataract formation. Steroids should be used with caution in the presence of glaucoma.

Prolonged use of corticosteroids may suppress the host response and thus increase the hazard of secondary ocular infections. In those diseases causing thinning of the cornea or sclera, perforations have been known to occur with the use of topical steroids. In acute purulent conditions of the eye, steroids may mask infection or enhance existing infection.

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

The use of steroids after cataract surgery may delay healing and increase the incidence of bleb formation.

Dosage and Administration

SHAKE VIGOROUSLY BEFORE USING.

Steroid Responsive Disease Treatment :  Apply one to two drops of LOTEMAX 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 LOTEMAX 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.

How Supplied

LOTEMAX (loteprednol etabonate ophthalmic suspension) is supplied in a plastic bottle with a controlled drop tip in the following sizes:

2.5 mL (NDC 24208-299-25)-AB29904

  5 mL (NDC 24208-299-05)-AB29907

10 mL (NDC 24208-299-10)-AB29909

15 mL (NDC 24208-299-15)-AB29911

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

KEEP OUT OF REACH OF CHILDREN.

Bausch & Lomb Incorporated
Tampa, Florida 33637

U.S. Patent No. 4,996,335

U.S. Patent No. 5,540,930

©Bausch & Lomb Incorporated

Lotemax are trademarks of Bausch & Lomb Incorporated.

                                                                             Rev. 11/03-83

PRODUCT PHOTO(S):

NOTE: These photos can be used only for identification by shape, color, and imprint. They do not depict actual or relative size.

The product samples shown here have been supplied by the manufacturer. While every effort has been made to assure accurate reproduction, please remember that any visual identification should be considered preliminary. In cases of poisoning or suspected overdosage, the drug's identity should be verified by chemical analysis.

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