Tafluprost

Approved Indications:

• Primary Open-Angle Glaucoma (POAG): To reduce elevated intraocular pressure (IOP).
• Ocular Hypertension: In patients who are intolerant to other intraocular pressure-lowering medications or in whom such medications are insufficient.

Off-label/Clinically Accepted Uses:

• May be used in normal-tension glaucoma when pressure-lowering treatment is still clinically beneficial.
• Sometimes used as adjunctive therapy in combination with beta-blockers or carbonic anhydrase inhibitors for additional IOP reduction.

Adults (including Elderly):

• Recommended Dose: One drop of 0.0015% Tafluprost ophthalmic solution in the affected eye(s) once daily in the evening.
• Important Note: Do not exceed once-daily dosing, as more frequent administration may reduce IOP-lowering efficacy.

Pediatrics:

• Safety and efficacy in children under 18 years have not been established; use not generally recommended.

Renal/Hepatic Impairment:

• No specific dose adjustment is required; however, caution is advised due to limited data.

Administration Guidelines:

• Administer the eye drop in the evening, unless instructed otherwise.
• Avoid contact between the dropper tip and any surface to prevent contamination.
• If using other topical ophthalmic drugs, allow at least 5 minutes between applications.

Tafluprost is a prostaglandin F2α analog that selectively binds to the prostaglandin F (FP) receptors in the eye. Activation of these receptors increases uveoscleral outflow of aqueous humor, which in turn reduces intraocular pressure. Tafluprost mimics the action of natural prostaglandins, enhancing fluid drainage from the eye without significantly affecting aqueous humor production, thus preserving intraocular homeostasis.

• Absorption: After topical administration, Tafluprost is rapidly absorbed by the cornea and converted to its active form, tafluprost acid.
• Bioavailability: Systemic exposure is extremely low; plasma levels of tafluprost acid are generally below quantifiable limits.
• Distribution: Highly distributed in ocular tissues; negligible systemic distribution.
• Metabolism: Metabolized primarily by esterases in the cornea to active tafluprost acid, followed by hepatic metabolism via beta-oxidation, glucuronidation, and oxidation.
• Elimination: Primarily via renal excretion of inactive metabolites.
• Half-life: Plasma half-life of tafluprost acid is approximately 30–45 minutes after ophthalmic administration.

• Pregnancy: Tafluprost is classified as Pregnancy Category C. Animal studies have shown reproductive toxicity. It should only be used during pregnancy if the potential benefit justifies the potential risk to the fetus. Avoid use in pregnant women unless clearly indicated.
• Lactation: It is unknown whether tafluprost or its metabolites are excreted in human milk. As a precaution, breastfeeding mothers should either discontinue the drug or stop nursing.

• Primary Class: Antiglaucoma Agent
• Subclass: Prostaglandin F2α Analog (Ophthalmic)
• Generation: Second-generation prostaglandin analog

• Known hypersensitivity to tafluprost or any component of the formulation
• Pregnancy, unless no safer alternative is available
• Active intraocular inflammation (e.g., uveitis)
• Aphakic or pseudophakic patients with torn posterior lens capsule (risk of macular edema)

• Iris and Eyelash Changes: May cause increased brown pigmentation of the iris, eyelid skin darkening, and eyelash growth/lengthening. These changes are often permanent.
• Macular Edema: Use with caution in patients with aphakia, pseudophakia, or risk of cystoid macular edema.
• Ocular Inflammation: Use cautiously in patients with active or history of uveitis or iritis.
• Contact Lenses: Remove contact lenses before instillation and wait at least 15 minutes before reinserting.
• Systemic Absorption: Though minimal, caution in patients with severe asthma or pulmonary disease due to rare reports of exacerbation.

Common Side Effects (≥1%):

• Ocular: Conjunctival hyperemia, eye irritation, stinging upon instillation, dry eye, eye pruritus, foreign body sensation.
• Cosmetic: Increased eyelash length and thickness, periorbital skin darkening.

Less Common/Rare:

• Iris pigmentation (permanent)
• Eyelid edema
• Eye pain or photophobia
• Blurred vision
• Headache

Serious Side Effects:

• Macular edema (particularly in susceptible eyes)
• Uveitis or iritis
• Worsening of asthma or bronchospasm (extremely rare)

• No significant systemic interactions due to low systemic exposure.
• Topical prostaglandin analogs: Concomitant use with other prostaglandins or prostaglandin analogs is not recommended as it may paradoxically increase IOP.
• No known CYP450 enzyme-related interactions.

• Tafluprost is now commonly preferred in preservative-free formulations (especially in patients with ocular surface disease or intolerance to benzalkonium chloride).
• No major changes to its indication or dosing, but clinical guidelines emphasize its use in patients requiring preservative-free options.
• EMA and FDA continue to support its use in glaucoma management where monotherapy or adjunct therapy is warranted.

• Store at 2°C to 8°C (refrigerated) before opening.
• Once opened, may be stored at room temperature (up to 25°C) for up to 28 days.
• Protect from light and moisture.
• Do not freeze.
• Keep the bottle tightly closed and discard unused solution after 28 days from opening.