RESCULA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for RESCULA (RESCULA).
Unoprostone is a docosanoid that reduces intraocular pressure by increasing aqueous humor outflow through the trabecular meshwork and uveoscleral pathways. It is a prostanoid FP receptor agonist with additional effects on calcium-activated potassium channels and chloride channels.
| Metabolism | Unoprostone is metabolized by hydrolysis and beta-oxidation; the primary metabolite is unoprostone free acid. Enzymes involved include esterases and possibly cytochrome P450 isozymes. |
| Excretion | Renal: 70% unchanged; biliary/fecal: 30% as metabolites |
| Half-life | Terminal elimination half-life: 2 hours; clinical context: requires dosing every 2 hours for sustained intraocular pressure reduction |
| Protein binding | 55% bound to plasma albumin |
| Volume of Distribution | 0.3 L/kg; indicates distribution primarily into extracellular fluid |
| Bioavailability | Topical ophthalmic: ~5% systemic absorption; negligible oral bioavailability due to first-pass metabolism |
| Onset of Action | Topical ophthalmic: 1-2 hours; significant reduction in intraocular pressure within 2 hours |
| Duration of Action | 4-6 hours; clinical note: duration sufficient for dosing every 2 hours during waking hours |
One drop of 2.5% solution in the affected eye(s) three times daily.
| Dosage form | SOLUTION/DROPS |
| Renal impairment | No dose adjustment required; Rescula is not significantly excreted renally. |
| Liver impairment | No specific guidelines; caution in severe hepatic impairment (Child-Pugh C) due to lack of data. |
| Pediatric use | Safety and efficacy in pediatric patients have not been established; off-label use with caution. |
| Geriatric use | No specific dose adjustment; monitor intraocular pressure closely due to potential systemic absorption. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for RESCULA (RESCULA).
| Breastfeeding | It is not known whether unoprostone is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when rescula is administered to a nursing woman. M/P ratio unknown. |
| Teratogenic Risk | Pregnancy Category C. No adequate studies in pregnant women. In animal studies, rescula (unoprostone) did not show teratogenicity at doses up to 6.25 mg/kg/day (250 times the human exposure). However, it should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Risk cannot be ruled out in the first trimester. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to unoprostone or any component of the formulation"]
| Precautions | ["May cause gradual and permanent changes in iris pigmentation (increased brown pigmentation)","May cause eyelash changes (increase in length, thickness, pigmentation, and number)","Possible periorbital tissue pigmentation and eyelid skin darkening","Use with caution in patients with intraocular inflammation or those at risk for macular edema (e.g., aphakic patients, pseudophakic patients with torn posterior lens capsule)","May cause temporary blurred vision after instillation; patients should not drive or operate machinery until vision clears"] |
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| Fetal Monitoring |
| Monitor intraocular pressure (IOP) regularly during pregnancy. Assess for systemic effects of the drug (e.g., hypotension, bronchospasm) in the mother. No specific fetal monitoring required unless maternal systemic effects occur. |
| Fertility Effects | No studies on fertility in humans. In animal studies, unoprostone had no effect on fertility in rats at doses up to 12.5 mg/kg/day. |