VEXOL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for VEXOL (VEXOL).
Selective glucocorticoid receptor agonist; binds to cytoplasmic receptors leading to inhibition of phospholipase A2, suppression of inflammatory mediators, and vasoconstriction.
| Metabolism | Presumed hepatic metabolism via CYP450 enzymes; systemically absorbed portion is metabolized similarly to other corticosteroids. |
| Excretion | Primarily hepatic metabolism with biliary excretion of metabolites. Renal excretion accounts for <2% of unchanged drug. Fecal elimination of metabolites is the major route (>90%). |
| Half-life | Terminal elimination half-life is approximately 2.3 hours in adults. This short half-life supports twice-daily dosing for maintenance of therapeutic effect. |
| Protein binding | ~99% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Vd is approximately 0.2 L/kg, indicating limited distribution primarily into extracellular fluid and ocular tissues. |
| Bioavailability | Ophthalmic suspension: Systemic bioavailability is low (<1% of ocular dose) due to limited absorption through the cornea and nasolacrimal drainage. Oral bioavailability is not applicable as it is not administered orally. |
| Onset of Action | Ocular administration: Onset of clinical effect (reduction of ocular inflammation) occurs within 2–4 hours after instillation. |
| Duration of Action | Duration of effect following ocular instillation is approximately 12–24 hours, supporting twice-daily dosing. Clinical efficacy persists with regular administration. |
1-2 drops of 1% ophthalmic suspension in the conjunctival sac of the affected eye(s) four times daily. In severe conditions, may increase frequency to every 2 hours during initial 24-48 hours.
| Dosage form | SUSPENSION/DROPS |
| Renal impairment | No dosage adjustment required for renal impairment. |
| Liver impairment | No dosage adjustment required for hepatic impairment. |
| Pediatric use | Not recommended for use in children under 18 years of age due to lack of safety and efficacy data. |
| Geriatric use | Use with caution in elderly patients due to potential increased risk of intraocular pressure elevation and cataract formation. Monitor intraocular pressure regularly. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for VEXOL (VEXOL).
| Breastfeeding | No data on M/P ratio. Systemic absorption after ophthalmic administration is negligible; therefore, amounts in breastmilk are likely minimal. Considered compatible with breastfeeding, but use lowest effective dose. |
| Teratogenic Risk | Corticosteroids are generally considered low risk for major malformations. However, first trimester exposure may be associated with a small increased risk of oral clefts. Second and third trimester use may cause fetal adrenal suppression. For ophthalmic use, systemic absorption is minimal, so risk is very low. |
■ FDA Black Box Warning
None (FDA boxed warning not applicable for ophthalmic corticosteroids).
| Serious Effects |
["Hypersensitivity to rimexolone or any component of the formulation","Active viral diseases of the cornea and conjunctiva (e.g., epithelial herpes simplex keratitis, vaccinia, varicella)","Fungal diseases of ocular structures","Mycobacterial infections of the eye"]
| Precautions | ["Prolonged use may lead to increased intraocular pressure, glaucoma, optic nerve damage, and cataract formation","Risk of secondary ocular infections, including fungal infections","May mask signs of infection or enhance existing infections","Use with caution in patients with herpes simplex keratitis"] |
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| Fetal Monitoring |
| No specific monitoring required for ophthalmic use. If used systemically or on large skin areas, monitor for maternal hyperglycemia, hypertension, and fetal growth restriction. |
| Fertility Effects | No known adverse effects on fertility from ophthalmic administration. |