TAFLUPROST
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TAFLUPROST (TAFLUPROST).
Selective prostaglandin FP receptor agonist that increases aqueous humor outflow via uveoscleral pathway.
| Metabolism | Hydrolyzed by esterases in the cornea and plasma to active acid form; further metabolized via beta-oxidation and phase II conjugation. |
| Excretion | Following topical ocular administration, approximately 40% of the dose is excreted renally as unchanged drug, and 60% via biliary/fecal routes as metabolites. |
| Half-life | Terminal elimination half-life is approximately 45 minutes in plasma, but due to corneal binding and slow release, the intraocular concentration declines with a half-life of about 3 hours. |
| Protein binding | Approximately 99% bound to plasma albumin. |
| Volume of Distribution | Volume of distribution is not well-characterized for topical ocular use; systemic Vd after IV administration in animals is 0.5 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Topical ocular: Systemic bioavailability is approximately 1% due to extensive first-pass metabolism in the cornea and drainage into nasolacrimal system. |
| Onset of Action | Topical: Reduction in intraocular pressure begins within 2 hours, with peak effect at 8-12 hours. |
| Duration of Action | Duration of intraocular pressure reduction is at least 24 hours with once-daily dosing. |
One drop of 0.0015% ophthalmic solution in the conjunctival sac of the affected eye(s) once daily in the evening.
| Dosage form | SOLUTION/DROPS |
| Renal impairment | No dosage adjustment required for any degree of renal impairment. |
| Liver impairment | No dosage adjustment required for mild to severe hepatic impairment (Child-Pugh A, B, or C). |
| Pediatric use | Safety and efficacy not established in pediatric patients; no dosing recommendations available. |
| Geriatric use | No dosage adjustment required; dosing is the same as for younger adults, but monitor for increased intraocular inflammation risk. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TAFLUPROST (TAFLUPROST).
| Breastfeeding | Not recommended during breastfeeding. Excretion in human milk unknown. No M/P ratio available. Tafluprost is a prostaglandin analog; systemic absorption after ocular use is minimal, but caution advised due to potential for adverse effects in nursing infants. |
| Teratogenic Risk | Pregnancy Category C. In animal studies, tafluprost caused embryofetal lethality, malformations (including skeletal abnormalities) and decreased fetal weight at systemic exposures below human therapeutic levels. No adequate human studies exist. Risk cannot be ruled out; use only if potential benefit justifies potential risk. First trimester: potential for teratogenicity based on animal data. Second and third trimesters: continued risk of fetal harm, including possible premature labor due to prostaglandin analog effects. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to tafluprost or any component of the formulation"]
| Precautions | ["May cause changes to pigmented tissues (iris, periorbital tissue, eyelashes) which are likely permanent","May cause macular edema in aphakic patients, pseudophakic patients with torn posterior lens capsule, or patients with known risk factors for macular edema","Use with caution in patients with active intraocular inflammation (iritis/uveitis)","May increase recurrence of herpetic keratitis"] |
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| Fetal Monitoring | Monitor intraocular pressure regularly. Assess pregnancy status before initiating therapy. No specific fetal monitoring required beyond standard obstetric care; however, consider ultrasound for fetal development if exposed during pregnancy. |
| Fertility Effects | No human data on fertility effects. In animal studies, no adverse effects on fertility were observed at systemic exposures greater than human therapeutic levels. |