Version January 2024
Dry eye disease: Ophthalmic: 0.25% suspension: Instill 1 to 2 drops into each eye 4 times daily for up to 2 weeks.
Ophthalmic inflammatory conditions: Ophthalmic: 0.5% suspension: Instill 1 to 2 drops into the conjunctival sac of the affected eye(s) 4 times daily. During the initial treatment within the first week, the dosing may be increased up to 1 drop every hour. Do not discontinue therapy prematurely; withdraw therapy with gradual tapering of dose in chronic conditions. If signs and symptoms fail to improve after 2 days, re-evaluate the patient.
Postoperative ophthalmic inflammation/pain: Ophthalmic:
0.38% gel: Apply 1 drop into the conjunctival sac of the affected eye(s) 3 times daily beginning 24 hours after surgery and continuing throughout the first 2 weeks of the postoperative period.
0.5% ointment: Apply ~1/2 inch ribbon into the conjunctival sac of the affected eye(s) 4 times daily beginning 24 hours after surgery and continuing throughout the first 2 weeks of the postoperative period.
0.5% gel, 0.5% suspension: Instill 1 to 2 drops into the conjunctival sac of the affected eye(s) 4 times daily beginning 24 hours after surgery and continuing throughout the first 2 weeks of the postoperative period.
1% suspension: Instill 1 to 2 drops into the affected eye(s) twice daily beginning the day after surgery and continuing throughout the first 2 weeks of the postoperative period.
Seasonal allergic conjunctivitis: Ophthalmic: 0.2% suspension: Instill 1 drop into affected eye(s) 4 times daily.
There are no dosage adjustments provided in the manufacturer's labeling. However, dosage adjustment unlikely due to low systemic absorption.
There are no dosage adjustments provided in the manufacturer's labeling. However, dosage adjustment unlikely due to low systemic absorption.
Refer to adult dosing.
(For additional information see "Loteprednol: Pediatric drug information")
Postoperative inflammation and pain: Infants, Children, and Adolescents: Ophthalmic: 0.5% gel (Lotemax): Instill 1 to 2 drops into the conjunctival sac of the affected eye(s) 4 times daily beginning postoperative day 1 and continuing throughout the first 2 weeks of the postoperative period; trials in young pediatric patients (mean age: 3 years) were conducted following cataract surgery.
There are no dosage adjustments provided in the manufacturer's labeling; however, dosage adjustment unlikely due to low systemic absorption.
There are no dosage adjustments provided in the manufacturer's labeling; however, dosage adjustment unlikely due to low systemic absorption.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
>10%:
Endocrine & metabolic: Chemosis (5% to 15%)
Local: Application site burning (5% to 15%)
Nervous system: Headache (2% to <15%)
Ophthalmic: Anterior chamber inflammation (2% to 25%), blurred vision (5% to 15%), epiphora (5% to 15%), eye discharge (5% to 15%), eye pruritus (5% to 15%), foreign body sensation of eye (2% to 15%), injected sclera (5% to 15%), photophobia (5% to 15%), visual disturbance (5% to 15%), xerophthalmia (5% to 15%)
Respiratory: Pharyngitis (<15%), rhinitis (<15%)
1% to 10%:
Dermatologic: Erythema of eyelid (<5%)
Local: Application site pain (5%)
Ophthalmic: Conjunctival hyperemia (4% to 5%), conjunctivitis (<5%), corneal changes (<5%), corneal edema (4% to 5%), eye discomfort (<5%), eye irritation (<5%), eye pain (1% to 5%), increased intraocular pressure (2%), keratoconjunctivitis (<5%), secondary cataract (1%), uveitis (<5%)
Miscellaneous: Papilla (<5%)
Hypersensitivity to loteprednol, other corticosteroids, and any component of the formulation; viral disease of the cornea and conjunctiva (including epithelial herpes simplex keratitis, vaccinia, varicella); mycobacterial infection of the eye; fungal disease of ocular structures.
Concerns related to adverse effects:
• Cataracts: Use of corticosteroids may result in posterior subcapsular cataract formation. Use following cataract surgery may delay healing and increase the incidence of bleb formation.
• Corneal thinning: Various ophthalmic disorders, as well as prolonged use of corticosteroids, may result in corneal and scleral thinning. Continued use in a patient with thinning may result in perforation.
• Glaucoma: Prolonged use of corticosteroids may result in elevated intraocular pressure (IOP) and/or glaucoma; damage to the optic nerve; and defects in visual acuity and fields of vision. Use with caution in patients with glaucoma; monitor IOP in any patient receiving treatment for ≥10 days.
• Immunosuppression: Prolonged use of corticosteroids (including ophthalmic preparations) may increase the incidence of secondary ocular infections (including fungal infections). Acute purulent ocular infections may be masked or exacerbated with use. Fungal infection should be suspected in any patient with persistent corneal ulceration who has received corticosteroids.
• Systemic absorption: Studies have demonstrated topical ophthalmic corticosteroids are absorbed systemically and may cause endogenous corticosteroid production reduction. Caution is advised with prolonged use of topical ophthalmic corticosteroids in terms of systemic immunosuppression and additional systemic hazard of corticosteroid exposure (Burch 1968).
Disease-related concerns:
• Herpes simplex: Corticosteroids should not be used to treat ocular herpes simplex; may exacerbate the severity of the infection. Use extreme caution in patients with history of herpes simplex.
Special populations:
• Contact lens wearers: Some preparations may contain benzalkonium chloride, which may be absorbed by contact lenses. Contact lenses should not be worn when using loteprednol 0.38% gel or 0.5% ophthalmic gel, ointment, or suspension. However, contact lenses may be reinserted 15 minutes following administration of loteprednol 0.25% and 1% ophthalmic suspension or ≥10 minutes following administration of loteprednol 0.2% ophthalmic suspension.
• Pediatric: Avoid use of ointment in children following amblyopia treatment since ointment consistency may hinder ability to see out of treated eye.
Dosage form specific issues:
• Propylene glycol: Some dosage forms may contain propylene glycol; large amounts are potentially toxic and have been associated with hyperosmolality, lactic acidosis, seizures, and respiratory depression; use caution (AAP ["Inactive" 1997]; Zar 2007).
Other warnings/precautions:
• Acute anterior uveitis: More potent steroids may be required for this indication.
• Appropriate use: For ophthalmic use only; patients should be re-evaluated if symptoms fail to improve after 2 days. Initial prescription and renewal of medication after 14 days should be made by healthcare provider only after examination with the aid of magnification such as slit lamp biomicroscopy or fluorescein staining (if appropriate) and evaluation of intraocular pressure (0.25% suspension). Avoid contamination; do not touch tip of applicator or let tip of applicator touch eye.
Increased intraocular pressure (IOP) may occur especially with prolonged use of ophthalmic corticosteroids; in children on ophthalmic dexamethasone, increased IOP has been shown to be dose dependent and produce a greater IOP in children <6 years than older children (Lam 2005).
Some dosage forms may contain propylene glycol; in neonates, large amounts of propylene glycol delivered orally, intravenously (eg, >3,000 mg/day), or topically have been associated with potentially fatal toxicities which can include metabolic acidosis, seizures, renal failure, and CNS depression; toxicities have also been reported in children and adults including hyperosmolality, lactic acidosis, seizures, and respiratory depression; use caution (AAP 1997; Shehab 2009).
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Gel, Ophthalmic, as etabonate:
Lotemax: 0.5% (5 g) [contains benzalkonium chloride, edetate (edta) disodium dihydrate, propylene glycol]
Lotemax SM: 0.38% (5 g) [contains benzalkonium chloride, edetate (edta) disodium dihydrate, propylene glycol]
Generic: 0.5% (5 g)
Ointment, Ophthalmic, as etabonate:
Lotemax: 0.5% (3.5 g)
Suspension, Ophthalmic:
Eysuvis: 0.25% (8.3 mL) [contains benzalkonium chloride, edetate (edta) disodium dihydrate]
Inveltys: 1% (2.8 mL) [contains benzalkonium chloride, edetate (edta) disodium dihydrate]
Suspension, Ophthalmic, as etabonate:
Alrex: 0.2% (5 mL, 10 mL)
Lotemax: 0.5% (5 mL, 10 mL, 15 mL)
Generic: 0.5% (5 mL, 10 mL, 15 mL)
May be product dependent
Gel (Lotemax Ophthalmic)
0.5% (per gram): $57.79
Gel (Lotemax SM Ophthalmic)
0.38% (per gram): $57.79
Gel (Loteprednol Etabonate Ophthalmic)
0.5% (per gram): $46.24
Ointment (Lotemax Ophthalmic)
0.5% (per gram): $116.17
Suspension (Alrex Ophthalmic)
0.2% (per mL): $67.71
Suspension (Eysuvis Ophthalmic)
0.25% (per mL): $72.02
Suspension (Inveltys Ophthalmic)
1% (per mL): $129.29
Suspension (Lotemax Ophthalmic)
0.5% (per mL): $72.02
Suspension (Loteprednol Etabonate Ophthalmic)
0.5% (per mL): $45.07 - $51.29
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Gel, Ophthalmic, as etabonate:
Lotemax: 0.5% (5 g) [contains benzalkonium chloride, edetate (edta) disodium dihydrate, propylene glycol]
Ointment, Ophthalmic, as etabonate:
Lotemax: 0.5% (3.5 g)
Suspension, Ophthalmic, as etabonate:
Alrex: 0.2% (5 mL)
Lotemax: 0.5% (5 mL, 10 mL)
Ophthalmic: For topical ophthalmic use only; wash hands before use. To avoid contamination, do not touch dropper or tube tip to eyelids or other surfaces. Remove contacts prior to administration. Contact lenses should not be worn when using ophthalmic gel, ointment, or suspension. However, contact lenses may be reinserted 15 minutes following administration of loteprednol 0.25% and 1% ophthalmic suspension or ≥10 minutes following administration of loteprednol 0.2% ophthalmic suspension. When used for the treatment of seasonal allergic conjunctivitis, do not wear contacts if eyes are red.
Gel: While bottle is closed, invert and shake once to fill tip prior to instilling drops.
Suspension: Shake well before using. The manufacturer's labeling for the 0.25% and 1% suspension formulation recommends separating administration of other ophthalmic agents by at least 5 minutes.
Ophthalmic: For topical ophthalmic use. Avoid contamination; do not touch dropper or tube tip to eyelids or other surfaces. Remove contacts prior to administration; contact lenses should not be worn when using loteprednol gel.
Gel: While bottle is closed, invert and shake once to fill tip prior to instilling drops.
Dry eye disease (0.25% suspension): Treatment of signs and symptoms of dry eye disease.
Ophthalmic inflammatory conditions (0.5% suspension): Treatment of ocular, anterior segment inflammation that is expected to be responsive to topical corticosteroid therapy.
Postoperative inflammation/pain (0.38% gel; 0.5% suspension/ointment/gel; 1% suspension): Treatment of postoperative inflammation and pain following ocular surgery.
Seasonal allergic conjunctivitis (0.2% suspension): Temporary relief of signs and symptoms of seasonal allergic conjunctivitis.
None known.
There are no known significant interactions.
The amount of loteprednol absorbed systemically following ophthalmic administration is not known but expected to be <1 ng/mL.
If ophthalmic agents are needed during pregnancy, the minimum effective dose should be used in combination with punctal occlusion to decrease potential exposure to the fetus (Samples 1988).
It is not known if loteprednol is present in breast milk following ophthalmic administration; however, systemic absorption is expected to be limited.
According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother.
Intraocular pressure (if >10 days of treatment); signs and symptoms of infection
Corticosteroids inhibit the inflammatory response including edema, capillary dilation, leukocyte migration, and scar formation. Loteprednol is highly lipid soluble and penetrates cells readily to induce the production of lipocortins. These proteins modulate the activity of prostaglandins and leukotrienes.
Onset of action: Seasonal allergic conjunctivitis: Reduction of symptoms seen within 2 hours of instillation.
Absorption: Minimal; chronic ophthalmic administration resulted in plasma levels of loteprednol and its metabolite below the level of quantitation (1 ng/mL).
Distribution: Penetrates most readily into the cornea, followed by the iris/ciliary body and aqueous humor.
Metabolism: Metabolized to inactive carboxylic acid metabolites by corneal esterases primarily in the cornea. Once the glucocorticoid receptor is activated, loteprednol undergoes rapid metabolism and minimizing adverse effects (Sheppard 2016).
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