Tafluprost (Monograph)

Brand name: Zioptan
Drug class: Prostaglandin Analogs
Chemical name: (5Z)-7-[(1R,2R,3R,5S)-2-[(1E)-3,3-Difluoro-4-phenoxy-1-buten-1-yl]-3,5-dihydroxycyclopentyl]-5-heptenoic acid, 1-methylethyl ester
Molecular formula: C₂₅H₃₄F₂O₅
CAS number: 209860-87-7

Medically reviewed by Drugs.com on Oct 23, 2023. Written by ASHP.

Introduction

Ocular hypotensive agent; fluorinated analog of prostaglandin F_2α (PGF_2α).^{1 8 9}

Uses for Tafluprost

Ocular Hypertension and Glaucoma

Reduction of elevated IOP in patients with open-angle glaucoma or ocular hypertension.^{1 7 15}

Preservative free; may be useful in patients who are allergic or have adverse events related to preservative-containing ocular hypotensives, have sensitive or dry eyes, or do not adequately respond to or cannot tolerate other therapies (e.g., topical prostaglandin analogs).^{3 7 10}

As effective as timolol 0.5% in reducing IOP in patients with open-angle glaucoma or ocular hypertension.^{3 16} Not as effective as latanoprost 0.005%^{2 16} and may be less effective than travoprost 0.004%.⁴

Addition of tafluprost 0.0015% to timolol 0.5% therapy may result in additional reduction in IOP.¹²

When selecting an initial ocular hypotensive agent, consider extent of the required IOP reduction, coexisting medical conditions, and drug characteristics (e.g., dosing frequency, adverse effects, cost).^{130 132} With single-agent regimens, the reduction in IOP is approximately 25–33% with topical prostaglandin analogs; 20–25% with topical β-adrenergic blocking agents, α-adrenergic agonists, or miotic (parasympathomimetic) agents; 20–30% with oral carbonic anhydrase inhibitors; 18% with topical rho kinase inhibitors; and 15–20% with topical carbonic anhydrase inhibitors.^{130 131}

A prostaglandin analog frequently is considered for initial therapy in the absence of other considerations (e.g., contraindications, cost considerations, intolerance, adverse effects, patient refusal) because of relatively greater activity, once-daily administration, and low frequency of systemic adverse effects; however, ocular adverse effects can occur.^{130 131 132 134}

Goal is to maintain an IOP at which visual field loss is unlikely to substantially reduce quality of life during the patient's lifetime.^{130 132}

Reduction of pretreatment IOP by ≥25% shown to slow progression of primary open-angle glaucoma.^{130 131} Set an initial target IOP (based on extent of optic nerve damage and/or visual field loss, baseline IOP at which damage occurred, rate of progression, life expectancy, and other considerations) and reduce IOP toward this goal.^{130 131 132} Adjust target IOP up or down as needed over course of disease.^{130 131 132}

Combination therapy with drugs from different therapeutic classes often required to control IOP.^{131 133}

Tafluprost Dosage and Administration

Administration

Ophthalmic Administration

Apply topically to the affected eye(s).¹

If more than one topical ophthalmic drug is used, administer the drugs at least 5 minutes apart.¹

Use solution from one single-use container immediately after opening; immediately discard unused portion after administration.¹

Dosage

Adults

Ocular Hypertension and Glaucoma

Ophthalmic

Tafluprost 0.0015% ophthalmic solution: One drop in the conjunctival sac of the affected eye(s) once daily in the evening.¹

More frequent dosing may diminish the IOP-lowering effect of the drug.¹

If target IOP not achieved, may initiate additional or alternative ocular hypotensive agents.^{130 131 133} (See Ocular Hypertension and Glaucoma under Uses.)

Special Populations

No special population dosage recommendations at this time.¹

Cautions for Tafluprost

Contraindications

• Manufacturer states none known.¹

Warnings/Precautions

Pigmentation

Increased pigmentation of the iris and periorbital tissue (eyelid) reported.¹ Pigmentation expected to increase as long as tafluprost is administered.¹ Following discontinuance of therapy, pigmentation of the iris is likely to be permanent, while pigmentation of periorbital tissue reportedly is reversible in some patients.¹ Long-term effects of increased pigmentation unknown.¹

Increased pigmentation of the iris may not be evident until after several months to years of tafluprost therapy.¹ May continue therapy in patients who develop noticeably increased iris pigmentation; however, examine these patients regularly.¹

Eyelash Changes

Possible gradual change in eyelashes and vellus hair in the treated eye, including increased length, color, thickness, shape, and number of eyelashes and/or misdirected growth of eyelashes.¹ Usually reversible upon discontinuance of therapy.¹

Intraocular Inflammation

Use with caution in patients with active intraocular inflammation (e.g., iritis/uveitis); may exacerbate inflammation.¹

Macular Edema

Macular edema, including cystoid macular edema, reported with prostaglandin F_2α analogs.¹ Use with caution in aphakic patients, in pseudophakic patients with a torn posterior lens capsule, or in patients with known risk factors for macular edema.¹

Specific Populations

Pregnancy

Category C.¹

Use only if potential benefits justify possible risk to the fetus.¹ Women of childbearing potential should use effective contraceptive methods.¹

Lactation

Tafluprost and/or its metabolites distribute into milk in animals; not known whether the drug or its metabolites distribute into milk in humans.¹ Caution if used in nursing women.¹

Pediatric Use

Use in pediatric patients not recommended because of potential safety concerns related to increased pigmentation following long-term use.¹ (See Pigmentation under Cautions.)

Geriatric Use

No overall differences in safety or efficacy relative to younger adults.¹

Common Adverse Effects

Conjunctival hyperemia,^{1 2 3} ocular stinging/irritation,^{1 2 3} headache,¹ ocular pruritus (including allergic conjunctivitis),^{1 2 3} common cold,¹ cataract,^{1 2} cough,¹ dry eye,^{1 2} ocular pain,^{1 2} eyelash darkening,^{1 2} growth of eyelashes,^{1 2} blurred vision,¹ urinary tract infection.¹

Drug Interactions

No formal drug interaction studies to date.¹³ However, no interactions expected because of limited systemic exposure.¹⁷

Tafluprost Pharmacokinetics

Absorption

Bioavailability

Prodrug; absorbed through the cornea following ocular instillation and hydrolyzed to active form (tafluprost acid).¹

Tafluprost acid: Peak plasma concentrations occur at a median of 10 minutes.¹

Onset

Reduction in IOP generally occurs approximately 2–4 hours after ocular instillation and peaks after 12 hours.^{1 6}

Distribution

Extent

Distributed into milk in animals; not known whether the drug or its metabolites distribute into milk in humans.¹

Crosses the placenta in animals.¹⁵

Elimination

Metabolism

Hydrolyzed by esterases in the cornea to biologically active form (tafluprost acid).^{1 8 9} Systemically, tafluprost acid is further metabolized via fatty acid oxidation and phase II conjugation.¹

Tafluprost acid: Rapidly eliminated from plasma; plasma concentrations are below the limit of quantitation within 30 minutes following ocular instillation.¹

Stability

Storage

Ophthalmic

Solution

May maintain at temperatures up to 40°C for ≤2 days during shipping; discard mail-order prescriptions of the drug if not received within 2 days of the dispensing date.¹ Store cartons and unopened foil pouches at 2–8°C.¹ After pouch is opened, may store single-use containers in opened pouch for up to 30 days at 20–25°C; discard any unused containers 30 days after first opening pouch.¹ Protect from moisture.¹

Actions

• Selective prostanoid FP receptor agonist.^{1 8 9}

• Mechanism of action not fully elucidated; appears to reduce IOP by increasing uveoscleral outflow.¹

• Potent prostanoid FP receptor agonist;^{8 9} negligible affinity for other prostanoid receptors (e.g., DP, EP2, IP, TP).⁸

Advice to Patients

• Importance of not exceeding once-daily dosing; more frequent administration may decrease IOP-lowering effect of tafluprost.¹

• Importance of administering tafluprost ophthalmic solution immediately after opening single-use container and discarding any unused portion immediately after administration.¹

• Risk of permanent increase in brown pigmentation of the iris; risk of darkening of the skin around the eyes (eyelid), which may be reversible after discontinuance of tafluprost.¹

• Risk of changes in eyelashes and vellus hair in the treated eye.¹ Potential for disparity between eyes in length, thickness, pigmentation, or number of eyelashes or vellus hairs and/or direction of eyelash growth.¹ Eyelash changes usually are reversible after discontinuance of tafluprost.¹

• Advise patients to immediately contact their clinician for advice regarding continued use of tafluprost ophthalmic solution if they develop a new ocular condition (e.g., trauma, infection), experience a sudden decrease in visual acuity, have ocular surgery, or experience ocular reactions (particularly conjunctivitis and eyelid reactions).¹

• If using more than one topical ophthalmic preparation, importance of administering the preparations at least 5 minutes apart.¹

• Importance of following instruction on proper storage of cartons, unopened foil pouches, and opened foil pouches.¹ (See Storage under Stability.) Importance of recording the date the foil pouch was opened in the space provided on the pouch and of discarding unused containers after 30 days.¹

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.¹ Women of childbearing potential should use effective contraceptive methods during tafluprost therapy.¹

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.¹

• Importance of informing patients of other important precautionary information.¹ (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Medical Disclaimer