EYSUVIS
Clinical safety rating: caution
Comprehensive clinical and safety monograph for EYSUVIS (EYSUVIS).
Eysuvis (loteprednol etabonate ophthalmic suspension) is a corticosteroid that works by inducing phospholipase A2 inhibitory proteins, collectively called lipocortins, which inhibit the release of arachidonic acid and subsequent synthesis of prostaglandins and leukotrienes, thereby reducing inflammation.
| Metabolism | Loteprednol etabonate is metabolized via ester hydrolysis to its inactive metabolites, primarily in the eye and systemically. |
| Excretion | Primarily renal (90-95% as unchanged drug and metabolites); minor biliary/fecal (<5%). |
| Half-life | Approximately 2-4 hours for loteprednol etabonate; clinical effect correlates with dosing interval (e.g., 4 times daily). |
| Protein binding | Approximately 55-65% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Not well characterized; due to topical ocular route, systemic Vd is small (<1 L/kg) and not clinically relevant. |
| Bioavailability | Topical ocular: low systemic bioavailability (<5%) due to first-pass metabolism and local dosing. |
| Onset of Action | Ocular: within 2 hours after topical instillation for inflammatory conditions. |
| Duration of Action | Approximately 4-6 hours; clinical efficacy maintained with QID dosing. |
| Molecular Weight | 310.39 |
1 drop in each eye twice daily (approximately 12 hours apart) for 4 weeks.
| Dosage form | SUSPENSION/DROPS |
| Renal impairment | No dose adjustment required. |
| Liver impairment | No dose adjustment required. |
| Pediatric use | Safety and efficacy not established in pediatric patients. |
| Geriatric use | No dose adjustment required; use same as adult dosing. |
| 1st trimester | Insufficient human data; animal studies show risk to fetus; avoid unless benefit outweighs risk. |
| 2nd trimester | Insufficient human data; animal studies show risk to fetus; avoid unless benefit outweighs risk. |
| 3rd trimester | Insufficient human data; animal studies show risk to fetus; avoid unless benefit outweighs risk. |
Clinical note
Comprehensive clinical and safety monograph for EYSUVIS (EYSUVIS).
| Placental transfer | Unknown; low molecular weight suggests potential crossing, but no data. |
| Breastfeeding | No human data; potential for systemic absorption; caution if used on large areas or for prolonged periods. |
| Lactation Rating |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to loteprednol etabonate or any excipient
| Precautions | Prolonged use may lead to ocular hypertension/glaucoma, Corticosteroids may increase the risk of secondary ocular infections, Use with caution in patients with history of herpes simplex keratitis, Not for injection |
| Food/Dietary | No known food interactions. Avoid concurrent use of alcohol as it may exacerbate dry eye symptoms. |
| Clinical Pearls | EYSUVIS (loteprednol etabonate ophthalmic suspension 0.25%) is a topical corticosteroid indicated for the treatment of dry eye disease (DED). Clinical pearls: 1) Use as adjunctive therapy to artificial tears, not as monotherapy for mild DED. 2) Prescribe short-term (2-4 weeks) due to risk of increased intraocular pressure (IOP); monitor IOP in patients with glaucoma or those on prolonged therapy. 3) Contraindicated in active ocular infections (viral, bacterial, fungal) and corneal epithelial defects. 4) Invert bottle and shake vigorously before each use to ensure proper suspension uniformity. 5) Advise patients to wait 5-10 minutes between instillation of other ophthalmic drugs to avoid washout. |
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| L3 |
| Teratogenic Risk | Pregnancy Category C. In animal reproduction studies, topical ocular administration of loteprednol etabonate during organogenesis produced fetal toxicity (increased fetal loss, decreased fetal weight, skeletal variations) at doses 0.31 mg/kg/day (0.37 times the human ocular dose). There are no adequate and well-controlled studies in pregnant women. Risk cannot be ruled out; use only if potential benefit justifies risk. Corticosteroids may increase risk of oral clefts when used in first trimester, but systemic exposure after ophthalmic dosing is low. |
| Fetal Monitoring | Monitor intraocular pressure (IOP) as topical corticosteroids may cause IOP elevation. Monitor for secondary ocular infections, especially fungal or viral (e.g., herpes simplex). No specific fetal monitoring required due to minimal systemic absorption. |
| Fertility Effects | No studies on fertility in humans. In animal studies, no impairment of fertility was observed at doses up to 12.5 mg/kg/day (15 times the human ocular dose). |
| Patient Advice | Shake the bottle vigorously for 10 seconds before each use. · Do not touch the dropper tip to your eye or any surface to avoid contamination. · Remove contact lenses before instillation and wait at least 15 minutes before reinserting. · Use exactly as prescribed; do not use longer than directed to avoid side effects. · Temporary blurred vision may occur; wait until clear before driving or operating machinery. · Report eye pain, vision changes, redness, or worsening symptoms to your doctor immediately. · Avoid sharing this medication with others. |