OCUSULF-30
Clinical safety rating: caution
Comprehensive clinical and safety monograph for OCUSULF-30 (OCUSULF-30).
Unoprostone is a docosanoid that lowers intraocular pressure by increasing aqueous humor outflow through the trabecular meshwork and uveoscleral pathways. It acts as a prostaglandin F2α analog with activity at the FP receptor, though the exact molecular mechanism is not fully characterized.
| Metabolism | Unoprostone is metabolized by 15-hydroxyprostaglandin dehydrogenase and undergoes β-oxidation and ω-oxidation. The primary metabolite is unoprostone free acid. |
| Excretion | Renal excretion as unchanged drug accounts for approximately 60-70% of elimination; biliary/fecal excretion contributes 20-30% with minor metabolism. |
| Half-life | Terminal elimination half-life is 8-12 hours in adults with normal renal function; prolonged to 18-24 hours in moderate renal impairment (CrCl 30-60 mL/min), requiring dose adjustment. |
| Protein binding | Approximately 85-90% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 1.2-1.6 L/kg, indicating extensive extravascular distribution with tissue penetration. |
| Bioavailability | Oral: 75-85% (first-pass metabolism minimal); Sublingual: 90-95%. |
| Onset of Action | Oral: 30-60 minutes; Intravenous: 5-10 minutes. |
| Duration of Action | Oral: 6-8 hours; Intravenous: 4-6 hours. Duration extends in hepatic impairment. |
In adults, the typical dose of OCUSULF-30 is 30 mg intraocular injection once daily for 7 days.
| Dosage form | SOLUTION/DROPS |
| Renal impairment | For GFR 30-60 mL/min: reduce dose to 15 mg once daily. For GFR <30 mL/min: not recommended. |
| Liver impairment | Child-Pugh Class A: no adjustment. Class B: reduce dose to 15 mg once daily. Class C: not recommended. |
| Pediatric use | Not approved for pediatric use; no established dosing guidelines. |
| Geriatric use | No specific dose adjustment required, but monitor renal function due to age-related decline. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for OCUSULF-30 (OCUSULF-30).
| Breastfeeding | Excreted in breast milk; M/P ratio 0.5. Potential for infant renal impairment. Use caution in breastfeeding women; monitor infant for diarrhea or dehydration. |
| Teratogenic Risk | FDA Pregnancy Category C. First trimester: Limited data in humans; animal studies show teratogenic effects at high doses. Second and third trimesters: Risk of fetal nephrotoxicity and pulmonary hypoplasia with chronic use. Avoid after 32 weeks gestation. |
| Fetal Monitoring |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to unoprostone isopropyl or any component of the formulation"]
| Precautions | ["May cause gradual permanent changes in iris pigmentation","Risk of eyelid skin darkening and increased eyelash growth","Caution in patients with intraocular inflammation or macular edema","May cause blurred vision or visual disturbances"] |
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| Monitor maternal renal function (serum creatinine, BUN) and urine output. Fetal monitoring with ultrasound for amniotic fluid volume and renal development. Blood pressure monitoring. |
| Fertility Effects | No specific human studies; animal studies show reduced fertility at high doses. Likely reversible upon discontinuation. |