XELPROS
Clinical safety rating: caution
Comprehensive clinical and safety monograph for XELPROS (XELPROS).
Prostaglandin F2α analogue; increases uveoscleral outflow of aqueous humor by binding to FP receptors, reducing intraocular pressure.
| Metabolism | Hydrolyzed by esterases in the cornea to the active acid; further metabolized via beta-oxidation and reduction pathways. |
| Excretion | Primarily renal excretion (60-70% as unchanged drug and metabolites), with 30-40% eliminated via biliary/fecal route. |
| Half-life | Terminal elimination half-life of 14-18 hours in adults; prolonged to 20-30 hours in renal impairment (CrCl <30 mL/min) and in elderly patients. |
| Protein binding | Approximately 55-60% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | 0.5-0.8 L/kg, indicating distribution into total body water and some peripheral tissues. |
| Bioavailability | Systemic bioavailability after ophthalmic administration is <5% due to limited absorption and extensive first-pass metabolism via the nasal mucosa and liver. |
| Onset of Action | Ocular hypotensive effect begins within 2-4 hours after topical ophthalmic administration. |
| Duration of Action | Intraocular pressure reduction is maintained for 24 hours after single dose, supporting once-daily dosing; maximal effect at 8-12 hours post-dose. |
Apply 1 drop (approximately 1.5 mcg of latanoprost) to the affected eye(s) once daily in the evening.
| Dosage form | EMULSION |
| Renal impairment | No dosage adjustment required in renal impairment. |
| Liver impairment | No dosage adjustment required in Child-Pugh Class A or B. Use with caution in severe hepatic impairment due to potential increased systemic exposure. |
| Pediatric use | Safety and effectiveness in pediatric patients have not been established. |
| Geriatric use | No specific dosage adjustment required; observational studies indicate no overall differences in safety or efficacy compared to younger adults. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for XELPROS (XELPROS).
| Breastfeeding | Unknown excretion in human milk. M/P ratio not available. Caution: potential for adverse effects in nursing infant; consider developmental and health benefits of breastfeeding along with mother's clinical need for drug. |
| Teratogenic Risk | Pregnancy Category C. No adequate studies in pregnant women. In animal studies, topical administration during organogenesis caused increased post-implantation loss and reduced fetal weight at doses >0.006 mg/kg/day (3 times the maximum human exposure). Risk cannot be ruled out; use only if potential benefit justifies potential risk to fetus. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to XELPROS or any component","Hypersensitivity to other prostaglandin analogs"]
| Precautions | ["May cause gradual darkening of iris color (melanin increase)","Possible eyelash changes (length, thickness, pigmentation)","Risk of macular edema in aphakic/pseudophakic patients with torn posterior lens capsule","May cause intraocular inflammation (uveitis)"] |
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| Fetal Monitoring |
| Monitor intraocular pressure (IOP) reduction; no specific fetal monitoring required. Advise pregnant women to contact if pregnancy occurs; no routine fetal testing recommended. |
| Fertility Effects | No human data. In animal studies, no adverse effects on male or female fertility at doses up to 0.03 mg/kg/day (15 times MRHD). |