Usage
Loteprednol etabonate is prescribed 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, and selected infective conjunctivitides. It is also used to treat postoperative inflammation and pain following ocular surgery and for the short-term treatment of the signs and symptoms of dry eye disease. It is a corticosteroid, specifically a “soft” steroid with a unique chemical structure designed to minimize some of the side effects associated with traditional corticosteroids.
It works by inhibiting the inflammatory response to a variety of stimuli by suppressing the migration of polymorphonuclear leukocytes and reversing capillary permeability. Loteprednol etabonate also inhibits the release of various inflammatory mediators.
Alternate Names
While “Loteprednol etabonate” is the generic name, it is marketed under various brand names, including Lotemax, Alrex, Inveltys, and Eysuvis. There are no widely recognized international or regional variations of the generic name.
How It Works
Pharmacodynamics: Loteprednol etabonate exerts its anti-inflammatory effect by binding to glucocorticoid receptors in the eye. This binding leads to the suppression of inflammatory mediators, including prostaglandins, cytokines, and leukotrienes, thereby reducing inflammation, pain, and other associated symptoms.
Pharmacokinetics: Loteprednol etabonate, when administered as an ophthalmic preparation, demonstrates limited systemic absorption. It is metabolized extensively in the eye to inactive metabolites, primarily PJ-91 and PJ-90. These metabolites are then eliminated, mainly through hepatic excretion. Some may be excreted renally as well.
Mode of Action: Loteprednol etabonate acts by binding to glucocorticoid receptors, which then translocate to the cell nucleus and modulate gene expression. This action results in the decreased production of inflammatory mediators.
Receptor Binding, Enzyme Inhibition, or Neurotransmitter Modulation: Loteprednol etabonate’s primary mechanism involves binding to glucocorticoid receptors. It does not significantly inhibit enzymes or modulate neurotransmitters.
Elimination Pathways: Loteprednol etabonate is primarily metabolized within the eye to inactive carboxylic acid metabolites (PJ-91, PJ-90), which are then eliminated predominantly through hepatic excretion.
Dosage
Standard Dosage
Adults:
- Alrex (0.2% suspension): 1 drop in the affected eye(s) four times daily.
- Eysuvis (0.25% suspension): 1-2 drops in each eye four times daily for up to 2 weeks.
- Lotemax (0.5% suspension, 0.5% ointment, 0.5% gel): 1-2 drops (suspension/gel) or a ½-inch ribbon (ointment) in the affected eye(s) four times daily. During the initial week, the dose may be increased to 1 drop every hour if needed.
- Inveltys (1% suspension): 1-2 drops in the affected eye(s) twice daily.
- Lotemax SM (0.38% gel): 1 drop in the affected eye(s) three times daily.
Children:
- Lotemax (0.5% gel): 1-2 drops in the affected eye(s) four times daily. Pediatric use is generally limited to post-operative inflammation after cataract surgery in children with a mean age of 3 years.
Special Cases:
- Elderly Patients: No dosage adjustments are typically necessary.
- Patients with Renal Impairment: No dosage adjustments are typically necessary due to limited systemic absorption.
- Patients with Hepatic Dysfunction: No dosage adjustments are typically necessary as hepatic metabolism pertains to the inactive metabolites.
- Patients with Comorbid Conditions: Use with caution in patients with glaucoma or a history of herpes simplex keratitis.
Clinical Use Cases
Dosing for post-operative inflammation following ocular surgery is outlined in the adult and pediatric sections above. Dosage adjustments may be required based on the type of surgical procedure. No specific dosage recommendations are available for intubation, mechanical ventilation, ICU use, or emergency situations as loteprednol etabonate is exclusively for ophthalmic use.
Dosage Adjustments
Dose adjustments may be necessary in patients with severe inflammation, where more frequent administration may be indicated during the initial phase of treatment.
Side Effects
Common Side Effects:
Blurred vision, eye irritation, burning or stinging upon instillation, foreign body sensation, increased eye pressure, headache, dry eye, photophobia.
Rare but Serious Side Effects:
Allergic reactions (e.g., rash, itching, swelling), glaucoma, cataracts, corneal thinning or ulceration, secondary eye infections.
Long-Term Effects:
Prolonged use of loteprednol etabonate can increase the risk of developing glaucoma, cataracts, and other eye problems.
Adverse Drug Reactions (ADR):
Severe allergic reactions, significant increase in intraocular pressure.
Contraindications
Absolute contraindications include hypersensitivity to loteprednol etabonate or any component of the formulation, most viral diseases of the cornea and conjunctiva (including herpes simplex keratitis, vaccinia, and varicella), mycobacterial infection of the eye, and fungal diseases of ocular structures.
Drug Interactions
No clinically significant drug interactions have been reported with topical ophthalmic loteprednol etabonate due to its minimal systemic absorption. However, concomitant use of other ophthalmic medications should be discussed with a physician.
Pregnancy and Breastfeeding
Pregnancy Category C. Loteprednol etabonate should be used during pregnancy only if the potential benefit outweighs the potential risk to the fetus. It is unknown 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 have adverse effects on the nursing infant. Caution should be exercised when loteprednol etabonate is administered to a nursing woman.
Drug Profile Summary
- Mechanism of Action: Inhibits inflammatory response by suppressing migration of polymorphonuclear leukocytes and reversing capillary permeability.
- Side Effects: Blurred vision, eye irritation, burning/stinging, foreign body sensation, increased eye pressure, headache, dry eye, photophobia. Rare but serious: allergic reactions, glaucoma, cataracts, corneal thinning.
- Contraindications: Hypersensitivity, viral/fungal/mycobacterial eye infections.
- Drug Interactions: No clinically significant interactions reported.
- Pregnancy & Breastfeeding: Category C; use with caution.
- Dosage: Varies by formulation and indication; typically 1-2 drops four times daily.
- Monitoring Parameters: Intraocular pressure, visual acuity, signs of infection.
Popular Combinations
Loteprednol etabonate is sometimes combined with tobramycin (an antibiotic) for the treatment of bacterial infections with concomitant inflammation.
Precautions
- Monitor intraocular pressure.
- Avoid contact lens wear during treatment.
- Do not discontinue therapy prematurely.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Loteprednol etabonate?
A: The dosage varies depending on the specific formulation and indication. See the detailed dosage section above.
Q2: What are the most common side effects?
A: Common side effects include blurred vision, eye irritation, burning/stinging, foreign body sensation, dry eye, and headache.
Q3: Is Loteprednol etabonate safe during pregnancy?
A: It is Pregnancy Category C and should be used only if the potential benefit justifies the potential risk to the fetus.
A: Generally, contact lens wear should be avoided during treatment.
Q5: How does Loteprednol etabonate differ from other corticosteroids?
A: It’s a “soft” steroid designed to minimize some of the systemic side effects associated with other corticosteroids due to its unique chemical structure and metabolism within the eye to inactive compounds.
Q6: What should I do if my symptoms don’t improve?
A: Consult your ophthalmologist if your symptoms don’t improve after two days or if they worsen.
Q7: Are there any long-term risks associated with using this medication?
A: Prolonged use can increase the risk of glaucoma, cataracts, and other eye problems. Regular eye exams are important during long-term therapy.
Q8: Can Loteprednol etabonate be used in children?
A: Lotemax gel is approved for pediatric use, primarily for post-operative inflammation after cataract surgery in children.
Q9: How should I administer the eye drops?
A: Wash your hands thoroughly, tilt your head back, gently pull down your lower eyelid to create a pouch, instill the prescribed number of drops into the pouch, close your eye gently for a few minutes, and apply pressure to the tear duct to minimize systemic absorption.
