TRAVOPROST
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TRAVOPROST (TRAVOPROST).
Travoprost is a synthetic prostaglandin F2α analog that acts as a selective FP receptor agonist. By binding to FP prostanoid receptors, it increases uveoscleral outflow of aqueous humor, reducing intraocular pressure.
| Metabolism | Metabolized by esterases in the eye; systemic metabolism via oxidation and reduction; not significantly metabolized by CYP450 enzymes. |
| Excretion | Renal (approximately 20% as unchanged drug and free acid metabolites); biliary/fecal (about 60% as metabolites) |
| Half-life | Terminal elimination half-life is approximately 45 minutes (range 17–86 minutes) for travoprost free acid in plasma; clinical effect (IOP reduction) persists longer due to prolonged receptor binding. |
| Protein binding | Travoprost free acid is approximately 99% bound to plasma proteins (primarily albumin). |
| Volume of Distribution | 0.9 ± 0.3 L/kg (plasma volume of distribution for travoprost free acid); clinical meaning: distributes into total body water, with extensive tissue penetration. |
| Bioavailability | Ophthalmic: Low systemic bioavailability due to hydrolysis in the cornea and ocular tissues; plasma concentration of travoprost free acid is typically below 0.005 ng/mL after topical administration. |
| Onset of Action | Ophthalmic: IOP reduction begins within 2–4 hours after topical administration. |
| Duration of Action | Ophthalmic: IOP reduction is maintained for up to 24 hours after a single dose, supporting once-daily dosing. |
One drop of 0.004% ophthalmic solution in the affected eye(s) once daily in the evening.
| Dosage form | SOLUTION/DROPS |
| Renal impairment | No dosage adjustment required for renal impairment, including hemodialysis. |
| Liver impairment | No dosage adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B). Use caution in severe hepatic impairment (Child-Pugh C) due to potential increased systemic exposure; monitor for adverse effects. |
| Pediatric use | Safety and efficacy not established; no specific dosing guidelines available. |
| Geriatric use | No specific dosage adjustment required; use same as adult dosing. Monitor for ocular adverse effects, as elderly patients may have increased sensitivity. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TRAVOPROST (TRAVOPROST).
| Breastfeeding | Travoprost is not recommended during breastfeeding. It is excreted in rat milk following systemic administration; human excretion is unknown. The M/P ratio is not established. Potential for adverse effects in infants (e.g., ocular or systemic effects) due to drug accumulation. |
| Teratogenic Risk | Travoprost is contraindicated in pregnancy (Pregnancy Category C). Animal studies have shown embryotoxicity, teratogenicity (including skeletal malformations and increased postimplantation loss), and maternotoxicity at systemic exposures significantly higher than clinical ocular doses. First trimester exposure carries potential risk of fetal harm; second and third trimester risks are unknown due to limited human data. Use only if potential benefit justifies risk. |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to travoprost or any component of the formulation; concurrent use of latanoprost (additive effect).
| Precautions | May cause gradual permanent changes in iris color, periorbital tissue pigmentation, and eyelash changes. Use with caution in patients with intraocular inflammation, aphakic/pseudophakic patients with torn posterior lens capsule, or risk of macular edema. Contains benzalkonium chloride (preservative), which may be absorbed by soft contact lenses. |
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| Fetal Monitoring | Monitor pregnancy status; obtain pregnancy test before initiation in women of childbearing potential. Advise effective contraception. If used during pregnancy, consider fetal ultrasound for skeletal development. Monitor intraocular pressure regularly; assess for systemic adverse effects (e.g., bradycardia, hypotension) during maternal use. |
| Fertility Effects | In animal studies, travoprost did not impair fertility at systemic doses up to 250 times the clinical ocular exposure. Human fertility effects are unknown; no specific studies are available. Use in women of childbearing potential should be with appropriate contraception. |