Alrex

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 mm Hg) 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. Among the smaller group of patients who were studied with ALREX, the incidence of clinically significant increases in IOP ( ≥ 10 mm Hg) was 1% (1/133) with ALREX and 1% (1/135) with placebo.

You should not use this medicine if you are allergic to loteprednol or other steroids, or if you have any type of fungal, viral, or bacterial infection of your eye (including herpes or chickenpox).

To make sure loteprednol is safe for you, tell your doctor if you have:

• glaucoma;

• cataracts (or if you have recently had cataract surgery); or

• herpes infection of your eye.

FDA pregnancy category C. It is not known whether loteprednol will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medication.

It is not known whether loteprednol passes into breast milk or if it could harm a nursing baby. Tell your doctor if you are breast-feeding a baby.

Do not give this medication to anyone under 18 years old without medical advice.

Follow all directions on your prescription label. Do not use this medicine in larger or smaller amounts or for longer than recommended.

Do not use loteprednol for longer than 2 weeks unless your doctor tells you to.

Do not use this medication while wearing contact lenses. Loteprednol may contain a preservative that can discolor soft contact lenses. Wait at least 10 minutes after using the eye drops before putting in your contact lenses.

If you use loteprednol ophthalmic gel, do not wear contacts at all throughout your treatment with the gel.

Shake the eye drops well just before each use. If using the gel, turn the bottle upside down and shake once to fill the dropper tip with gel.

Wash your hands before using the eye drops.

To apply the eye drops or gel:

• Tilt your head back slightly and pull down your lower eyelid to create a small pocket. Hold the dropper above the eye with the tip down. Look up and away from the dropper and squeeze out a drop.

• Close your eye and gently press your finger to the inside corner of the eye for about 1 minute, to keep the liquid from draining into your tear duct.

• Use only the number of drops your doctor has prescribed. If you use more than one drop, wait about 5 minutes between drops.

• Wait at least 10 minutes before using any other eye drops your doctor has prescribed.

Do not touch the tip of the eye dropper or place it directly on your eye. A contaminated dropper can infect your eye, which could lead to serious vision problems.

Do not use the eye drops if the liquid has changed colors or has particles in it. Call your pharmacist for new medicine.

Call your doctor if your symptoms do not improve after 2 days of treatment.

To be sure loteprednol is not causing harmful effects, your eyes may need to be checked after using the medication for 10 days or longer.

Store at room temperature away from moisture and heat. Do not freeze. Keep the bottle tightly closed when not in use.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

In the U.S.

• Alrex
• Lotemax

Available Dosage Forms:

• Gel/Jelly
• Suspension
• Ointment

Therapeutic Class: Ophthalmologic Agent

Pharmacologic Class: Adrenal Glucocorticoid

Loteprednol is used to treat eye pain, redness, and swelling caused by certain eye problems or eye surgery. It is also used to temporarily treat itching of the eye caused by a condition known as seasonal allergic conjunctivitis. This medicine belongs to the group of medicines known as corticosteroids (steroids or cortisone-like medicines).

This medicine is available only with your doctor's prescription.

• If your symptoms or health problems do not get better or if they become worse, call your doctor.
• Do not share your drugs with others and do not take anyone else's drugs.
• Keep a list of all your drugs (prescription, natural products, vitamins, OTC) with you. Give this list to your doctor.
• Talk with the doctor before starting any new drug, including prescription or OTC, natural products, or vitamins.
• Some drugs may have another patient information leaflet. Check with your pharmacist. If you have any questions about this medicine, please talk with your doctor, nurse, pharmacist, or other health care provider.
• If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

This information should not be used to decide whether or not to take Alrex or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to Alrex (loteprednol eye drops 0.2%). This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.

Review Date: October 4, 2017

Alrex® (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:

C24H31ClO7
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 2 mg (0.2%);

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 ADDED: 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 A2inhibitory 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 A2. 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 Δ1 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 Alrex.

Clinical Studies

In two double-masked, placebo-controlled six-week environmental studies of 268 patients with seasonal allergic conjunctivitis, Alrex, when dosed four times per day was superior to placebo in the treatment of the signs and symptoms of seasonal allergic conjunctivitis. Alrex provided reduction in bulbar conjunctival injection and itching, beginning approximately 2 hours after instillation of the first dose and throughout the first 14 days of treatment.

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.