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. |
| Molecular Weight | 432.58 |
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 | Studies in animals have shown teratogenic effects at clinically relevant doses. No adequate human studies. Avoid use during first trimester unless absolutely necessary. |
| 2nd trimester | Use only if potential benefit justifies potential risk to the fetus. Data limited; consider alternative agents. |
| 3rd trimester | May cause premature closure of the ductus arteriosus in third trimester. Avoid use after 34 weeks gestation. |
Clinical note
Comprehensive clinical and safety monograph for XELPROS (XELPROS).
| Placental transfer | Latanoprost crosses the placenta in animal studies. Data in humans are not available, but low systemic concentrations after topical ocular use suggest minimal transfer. |
| Breastfeeding | Xelpros (latanoprost) is excreted in breast milk in small amounts. Systemic absorption after topical ocular administration is minimal. However, due to potential for ocular effects in the infant, use with caution. Monitor infant for eye irritation. |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to latanoprost or any component of the formulationActive herpes simplex keratitisIntraocular inflammation (e.g., iritis, uveitis) due to risk of exacerbation
| 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) |
| Food/Dietary | No clinically significant food interactions. However, alcohol may impair vision or increase fall risk; advise caution. |
| Clinical Pearls |
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| Lactation Rating | L3 (Moderately Safe) - Use with caution; minimal systemic absorption but limited data. |
| 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. |
| 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). |
| XELPROS (latanoprost) is a prostaglandin analog used for reducing intraocular pressure in open-angle glaucoma and ocular hypertension. Monitor for gradual iris pigmentation changes, particularly in patients with mixed-colored irides. May cause eyelash changes (increased length, thickness, pigmentation). Administer in the evening for maximal efficacy. Separate administration of other ophthalmic drops by at least 5 minutes to prevent washout. |
| Patient Advice | Apply one drop in the affected eye(s) once daily in the evening. · Do not touch the dropper tip to your eye or any surface. · Remove contact lenses before administration and wait 15 minutes before reinserting. · May cause temporary blurred vision or stinging immediately after use. · Report any eye pain, redness, or vision changes to your doctor. · Iris color may darken gradually; this is usually permanent but harmless. · Eyelashes may grow longer, thicker, and darker; report any eyelid skin darkening. · Store the bottle upright at room temperature, protected from light. |