INVELTYS
Clinical safety rating: caution
Comprehensive clinical and safety monograph for INVELTYS (INVELTYS).
Corticosteroid; modulates inflammatory response by binding to glucocorticoid receptors, altering gene expression and suppressing pro-inflammatory cytokines.
| Metabolism | Primarily hepatic via CYP3A4; undergoes extensive first-pass metabolism. |
| Excretion | Primarily hepatic metabolism with minimal renal excretion (<5% unchanged in urine). Fecal elimination accounts for approximately 20% of the dose. |
| Half-life | Approximately 1.5 hours (range 1-2 hours) for the ophthalmic suspension; terminal half-life in systemic circulation is about 3 hours after topical ocular administration. |
| Protein binding | Approximately 90% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is approximately 0.5-1.0 L/kg, indicating moderate tissue distribution; largely confined to the systemic circulation and ocular tissues. |
| Bioavailability | Systemic bioavailability after topical ocular administration is minimal, estimated at <1% of the administered dose due to high first-pass metabolism in the eye and nasolacrimal drainage. |
| Onset of Action | Onset of clinical effect (reduction in ocular inflammation) occurs within 4-6 hours after topical administration to the eye. |
| Duration of Action | Duration of therapeutic effect is approximately 12-24 hours, supporting twice-daily dosing for most patients; effect may wane after 24 hours. |
Instill 1 drop into the affected eye(s) four times daily for 14 days, then taper as clinically indicated.
| Dosage form | SUSPENSION/DROPS |
| Renal impairment | No dose adjustment required for renal impairment. |
| Liver impairment | No dose adjustment required for hepatic impairment. |
| Pediatric use | Safety and effectiveness in pediatric patients have not been established. |
| Geriatric use | No specific dose adjustment recommended; use same dosing as adults. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for INVELTYS (INVELTYS).
| Breastfeeding | Systemic corticosteroids appear in human milk and could suppress growth, interfere with endogenous corticosteroid production, or cause other untoward effects. However, with ophthalmic administration, systemic absorption is minimal. It is not known whether loteprednol etabonate is excreted in human milk. Caution should be exercised when administered to a nursing woman. M/P ratio not available. |
| Teratogenic Risk | INVELTYS (loteprednol etabonate ophthalmic suspension) is a corticosteroid. Systemic exposure is low after ocular administration. No adequate and well-controlled studies in pregnant women. In animal reproduction studies, corticosteroids have been shown to be teratogenic at high systemic doses. The risk of adverse fetal outcomes (cleft palate, intrauterine growth restriction) is considered low given minimal systemic absorption. Use only if potential benefit justifies potential risk. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to any component of the formulation.","Active corneal epithelial defect (e.g., dendritic keratitis)."]
| Precautions | ["May increase intraocular pressure (IOP); monitor IOP in patients with glaucoma.","Increased risk of secondary ocular infection; use caution in patients with active infections or history of ocular herpes simplex.","Delayed wound healing; avoid use in patients with corneal or scleral thinning.","Cataract formation with prolonged use.","Not for injection into the eye."] |
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| Fetal Monitoring | No specific maternal or fetal monitoring required beyond routine pregnancy care due to low systemic absorption. Monitor for intraocular pressure, cataract formation, and secondary ocular infections during prolonged use. |
| Fertility Effects | No studies on fertility effects in humans. Animal studies with systemic corticosteroids have shown impairment of fertility at high doses. Given low systemic exposure after ocular use, significant effects on fertility are unlikely. |