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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for EYSUVIS (EYSUVIS).
| Breastfeeding | Unknown if loteprednol etabonate or its metabolites are excreted in human milk. Systemic absorption after ocular administration is minimal. Caution advised. No M/P ratio available. |
| 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. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to loteprednol etabonate or any component of the formulation","Active viral (e.g., herpes simplex keratitis), bacterial, fungal, or mycobacterial infections of the eye"]
| 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"] |
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| 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). |