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. |
| Molecular Weight | 350.45 |
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 | Avoid use due to potential risk of spontaneous abortion and malformations. Insufficient human data; animal studies show fetal harm. |
| 2nd trimester | Avoid use unless clearly needed; may cause uterine contractions and fetal harm. Non-teratogenic but risk of reduced fetal growth. |
| 3rd trimester | Avoid use due to risk of premature labor and fetal harm. Prostaglandin analogs can stimulate uterine contractions. |
Clinical note
Comprehensive clinical and safety monograph for TRAVOPROST (TRAVOPROST).
| Placental transfer | Prostaglandin analogs cross placenta; animal studies indicate significant transfer and fetal exposure. |
| Breastfeeding | Excretion into human milk unknown; not recommended during breastfeeding due to potential for systemic effects in infant (e.g., diarrhea, hypotension). |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to travoprost or any componentActive ocular infectionHistory of macular edema in pseudophakic patients
| 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. |
| Food/Dietary | No specific food interactions are known. Avoid excessive alcohol intake as it may impair intraocular pressure control. No dietary restrictions required. |
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| Lactation Rating |
| L4 (Possibly Hazardous) |
| 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. |
| 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. |
| Clinical Pearls |
| Travoprost is a prostaglandin F2α analogue used for reducing intraocular pressure in open-angle glaucoma or ocular hypertension. Advise patients to remove contact lenses before administration and wait 15 minutes before reinserting. To minimize systemic absorption, apply pressure to the nasolacrimal duct for 1 minute after instillation. Travoprost can cause gradual changes in iris pigmentation (may be permanent), periorbital skin darkening, and eyelash growth. Contraindicated in patients with macular edema, uveitis, or active intraocular inflammation. Caution in patients with risk factors for cystoid macular edema (e.g., aphakia, pseudophakia with torn posterior lens capsule). Monitor for conjunctival hyperemia, ocular pruritus, and blurred vision. Do not administer simultaneously with other ophthalmic agents; separate by at least 5 minutes. |
| Patient Advice | Use exactly as prescribed; do not increase frequency. · Do not touch the dropper tip to the eye or any surface to avoid contamination. · Remove contact lenses before use; wait 15 minutes before reinserting. · Apply pressure to the inner corner of the eye (nasolacrimal duct) for 1 minute after each drop to reduce side effects. · May cause gradual brownish darkening of the iris, which is likely permanent. · May cause eyelash growth, thickening, or increased pigmentation. · Inform your doctor if you experience eye pain, vision changes, or persistent redness. · Do not use if pregnant or breastfeeding unless advised by your doctor. |