Lotepred DS

Approved Indications:

• Ocular Inflammation:
  Treatment of steroid-responsive inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the eye.
• Postoperative Ocular Inflammation and Pain:
  Indicated to treat inflammation and pain following ocular surgery, such as cataract extraction.
• Seasonal Allergic Conjunctivitis:
  Relief of signs and symptoms, such as itching and redness, associated with seasonal allergic conjunctivitis.

Clinically Accepted Off-label Uses:

• Dry Eye Disease (inflammatory subtype):
  Used to manage inflammation in dry eye syndrome, especially in short pulses.
• Vernal and Atopic Keratoconjunctivitis:
  For moderate to severe cases when topical antihistamines are insufficient.
• Blepharitis:
  Used short-term to reduce eyelid margin inflammation in blepharitis and meibomian gland dysfunction.

Route of Administration: Ophthalmic (eye drops, gel, ointment)

General Administration Advice:
Shake suspension well before use. Do not touch the dropper tip to any surface. Contact lenses should be removed prior to instillation and reinserted after 15 minutes.

Adults and Children ≥2 Years:

• 0.2% Suspension (e.g., Alrex®):
  1 drop in the affected eye(s) 4 times daily.
• 0.5% Suspension or Gel (e.g., Lotemax®):
  1 drop in the affected eye(s) 4 times daily for the first week post-surgery, then taper as needed.
• 0.5% Ointment:
  Apply ~½ inch (1.25 cm) into the conjunctival sac(s) 3–4 times daily or as directed.

Pediatrics (<2 years):

• Safety and efficacy not established.

Elderly:

• No dosage adjustment necessary; monitor intraocular pressure.

Renal/Hepatic Impairment:

• No adjustment required due to minimal systemic absorption.

Duration:

• Typically 1–2 weeks. For postoperative use, treatment may extend to 2–4 weeks with tapering as inflammation resolves.

Loteprednol Etabonate is a synthetic corticosteroid designed as a "soft steroid" for ophthalmic use. It binds to glucocorticoid receptors, inhibiting the release of inflammatory mediators such as prostaglandins and leukotrienes. This suppresses the migration of inflammatory cells and reduces capillary permeability and edema. Unlike traditional corticosteroids, loteprednol undergoes rapid deactivation into inactive metabolites after exerting its local effect, thereby minimizing systemic exposure and reducing the risk of corticosteroid-induced intraocular pressure (IOP) elevation and cataract formation.

• Absorption: Minimal systemic absorption when used topically in the eye
• Distribution: Localized to ocular tissues (cornea, conjunctiva)
• Metabolism: Rapidly metabolized by esterases in ocular tissues to inactive metabolites
• Half-life: Short ocular half-life; systemically negligible
• Excretion: Primarily via renal excretion of inactive metabolites
• Onset of Action: Typically within 24 to 48 hours of initiation

Pregnancy:

• No assigned FDA pregnancy category.
• Animal studies show no fetal harm with ophthalmic use. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Lactation:

• Unknown if loteprednol is excreted in human breast milk after topical use.
• Systemic exposure is minimal; use is generally considered safe during breastfeeding with caution.

• Primary Class: Corticosteroid (Ophthalmic)
• Subclass: Retrometabolic “soft” steroid

• Known hypersensitivity to loteprednol or any component of the formulation
• Active ocular infections caused by:
• Herpes simplex virus (HSV) epithelial keratitis
• Varicella (chickenpox)
• Mycobacterial or fungal eye infections
• Untreated purulent eye infections

• Intraocular Pressure (IOP) Elevation:
  Prolonged use may increase IOP; monitor in patients with glaucoma or a history of steroid response.
• Cataract Formation:
  Long-term use may promote posterior subcapsular cataract development.
• Delayed Healing:
  Corticosteroids may delay wound healing, particularly post-surgery.
• Secondary Infections:
  May suppress immune response, masking or worsening existing infections.
• Use in Children:
  Safety beyond 2 weeks of use in children has not been established.
• Contact Lens Wearers:
  Soft contact lenses should not be worn during treatment due to preservative-related irritation.

Common Side Effects:

• Eye discomfort (burning, stinging)
• Conjunctival hyperemia
• Blurred vision
• Increased tear production or dryness
• Foreign body sensation

Serious or Rare Side Effects:

• Elevated intraocular pressure
• Glaucoma progression
• Posterior subcapsular cataract
• Secondary ocular infections (e.g., HSV keratitis)
• Corneal thinning or perforation (very rare)

Onset & Severity:

• Most common side effects are mild and occur within the first few days.
• IOP elevation and cataracts generally occur with prolonged use (beyond 10–14 days).

• Ophthalmic NSAIDs: Concurrent use may delay wound healing.
• Other corticosteroids: Increased risk of systemic and ocular side effects.
• No significant CYP450-related interactions due to negligible systemic absorption.
• Contact lens disinfectants or preservatives (e.g., benzalkonium chloride): May interact with lens material, causing irritation.

• AAO and ESCRS Guidelines (2023):
  Loteprednol is recommended as first-line treatment in steroid-responsive ocular inflammation due to its safety profile, particularly in patients at risk of IOP elevation.
• FDA Recommendations:
  Emphasize routine monitoring of IOP with long-term use and discourage prolonged unsupervised use.
• Preferred over prednisolone or dexamethasone in patients with glaucoma or ocular hypertension due to its lower IOP-raising potential.

• Temperature: Store between 15°C and 25°C (59°F to 77°F)
• Humidity: Protect from excessive moisture
• Light Protection: Keep container closed and protected from light
• Handling Instructions:
• Shake well before use (suspension only)
• Do not freeze
• Discard after 30 days of opening
• Do not touch the dropper tip to any surface