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. |
| Molecular Weight | 452.55 |
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 | Tafluprost is contraindicated in pregnancy. Based on animal studies, it may cause fetal harm. There are no adequate and well-controlled studies in pregnant women. Tafluprost can cause spontaneous abortion and fetal malformations. Use is not recommended during the first trimester. |
| 2nd trimester | Tafluprost is contraindicated in pregnancy. Animal studies have shown adverse effects on fetal development. There is no evidence of safety in the second trimester. Use only if potential benefit justifies potential risk, though generally avoided. |
| 3rd trimester | Tafluprost is contraindicated in pregnancy. Due to potential oxytocic effects and risk of preterm labor, use in the third trimester is not recommended. Prostaglandin analogues can stimulate uterine contractions. |
Clinical note
Comprehensive clinical and safety monograph for TAFLUPROST (TAFLUPROST).
| Placental transfer | Tafluprost is a lipophilic drug with molecular weight 452.55 Da, suggesting ability to cross the placenta. Animal studies demonstrate placental transfer and fetal exposure. Prostaglandin analogues are known to cross the placenta and can induce uterine contractions. |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to tafluprost or any component of the formulationPregnancy (based on animal data and potential for fetal harm and uterine stimulation)
| 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 |
| Food/Dietary | No clinically significant food interactions. Avoid excessive consumption of grapefruit juice as it may theoretically affect metabolism, though not proven with tafluprost. |
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| Breastfeeding | It is not known whether tafluprost is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when tafluprost is administered to a nursing woman. Tafluprost is a prostaglandin analogue and may affect lactation. The molecular weight is low enough for potential excretion. Due to lack of data, breastfeeding is generally not recommended during treatment. |
| Lactation Rating | L4 - Possibly Hazardous (Limited human data; potential for adverse effects in infant) |
| 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. |
| 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. |
| Clinical Pearls | Tafluprost is a prostaglandin analog used for reducing intraocular pressure (IOP) in open-angle glaucoma and ocular hypertension. It is a prodrug that is hydrolyzed to the active acid form. Systemic absorption is minimal but can cause flu-like symptoms. Advise patients to apply pressure to the nasolacrimal duct after instillation to reduce systemic absorption. Caution in patients with intraocular inflammation (e.g., iritis/uveitis) as it may exacerbate. Monitor for iris pigmentation changes, eyelash growth, and periorbital fat loss. Use with caution in patients with history of herpes simplex keratitis. |
| Patient Advice | Wash hands before use. Remove contact lenses before instillation and wait 15 minutes before reinserting. · Tilt head back, pull lower eyelid down, and instill one drop in the affected eye(s). Close eye and press on the inner corner for 1-2 minutes to minimize systemic absorption. · Do not touch the dropper tip to any surface to avoid contamination. · Use exactly as prescribed; do not skip doses. If using other eye drops, wait at least 5 minutes between medications. · May cause temporary blurred vision. Do not drive or operate machinery until vision clears. · Report any eye pain, redness, vision changes, or signs of infection (e.g., discharge) immediately. · Gradual increase in brown iris pigmentation is possible and may be permanent. Eyelash changes (longer, thicker, darker) may occur. · Store at room temperature, protected from light. Keep bottle tightly closed. |