Tafluprost, a fluorinated analog of naturally occurring prostaglandin F2α (PGF2α), is an ocular hypotensive agent.1, 8, 9
Ocular Hypertension and Glaucoma
Tafluprost ophthalmic solution is used topically to reduce elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension.1, 7, 15 Elevated IOP presents a major risk factor for glaucoma progression; reduction of IOP may reduce the risk of visual field loss.131
Elevated IOP in patients with glaucoma can be reduced by medical treatment, laser therapy, and/or incisional glaucoma surgery; treatment with a topical ocular hypotensive agent frequently is the initial intervention for primary open-angle glaucoma.130 Selection of an initial ocular hypotensive agent is influenced by the extent of the required reduction in IOP, coexisting medical conditions, and the characteristics of the individual drugs (e.g., dosing frequency, adverse effect profile, 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 In the absence of other considerations (e.g., contraindications, cost considerations, intolerance, adverse effects, patient refusal), a prostaglandin analog frequently is considered for initial therapy because of the relatively greater activity, once-daily administration, and low frequency of systemic adverse effects with this drug class; however, ocular adverse effects can occur.130, 131, 132, 134
IOP should be reduced toward a target level that the clinician believes will slow disease progression and avoid visual field losses that would substantially reduce quality of life during the patient's lifetime.130, 132 The target level is an estimate and should be individualized based on such factors as the extent of optic nerve damage and/or visual field loss, the baseline IOP at which damage occurred, rate of progression, life expectancy, and other considerations.130, 132 Reducing the pretreatment IOP by 25% or more has been shown to slow progression of primary open-angle glaucoma.130, 131 The target IOP should be adjusted up or down as needed over the course of the disease.130, 131, 132 If the target IOP is not achieved with single-agent therapy, alternative or additional ocular hypotensive agents may be selected depending on the patient's response to the initial drug.130 Combination therapy with drugs from different therapeutic classes often is required to achieve adequate control of IOP.131, 133
Safety and efficacy of preservative-containing and preservative-free tafluprost have been evaluated in several multicenter, randomized, double-blind studies in patients with open-angle glaucoma or ocular hypertension.1, 2, 3, 12, 16 In these studies, which included patients with a baseline IOP of 23-26 mm Hg, ocular instillation of tafluprost 0.0015% once daily in the evening reduced IOP at 3 and 6 months by 6-8 and 5-8 mm Hg, respectively.1
Tafluprost is commercially available in the US as a preservative-free preparation;1 the drug is available in other countries as preservative-containing and/or preservative-free preparations.15 Data from a 4-week randomized, crossover phase 3 study in a limited number of patients 18 years of age and older with open-angle glaucoma or ocular hypertension indicate that preservative-containing and preservative-free tafluprost produce similar reductions in IOP (4.56-6.18 and 4.8-6.17 mm Hg, respectively, at 4 weeks).8, 16 It is not known whether preservative-free tafluprost provides any advantages (e.g., improved adherence or safety) over preservative-containing preparations;15 however, some clinicians suggest that preservative-free tafluprost 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
Tafluprost is noninferior to timolol in reducing IOP in patients with open-angle glaucoma or ocular hypertension.3, 16 In a 12-month randomized, double-blind, phase 3 study in 458 patients 18 years of age and older with open-angle glaucoma or ocular hypertension, treatment with preservative-containing tafluprost 0.0015% once daily or preservative-containing timolol 0.5% twice daily reduced IOP by 4.84-6.53 or 4.21-6.57 mm Hg, respectively, at 12 months.16 In a 12-week randomized, double-blind, phase 3 study in 643 patients 18 years of age and older with primary open-angle glaucoma, pigmentary glaucoma, capsular glaucoma/pseudoexfoliation, or ocular hypertension, treatment with preservative-free tafluprost 0.0015% once daily or preservative-free timolol 0.5% twice daily reduced IOP by 6.2-7.4 or 5.7-7.5 mm Hg, respectively, at 12 weeks.3 In this study, substantial IOP lowering was apparent after 2 weeks of treatment with tafluprost or timolol and was sustained throughout the 12-week assessment period; the IOP-lowering effect of tafluprost was noninferior to that of timolol at all visits and time points over 12 weeks.3 Results of these studies demonstrated that preservative-containing and preservative-free tafluprost are noninferior to preservative-containing and preservative-free timolol, respectively.16
Noninferiority of tafluprost to latanoprost has not been established,2, 16 and tafluprost may be inferior to travoprost4 in reducing IOP in patients with open-angle glaucoma or ocular hypertension. In a 24-month randomized, double-blind, phase 3 study in 533 patients 18 years of age and older with open-angle glaucoma, capsular glaucoma, pigmentary glaucoma, or ocular hypertension, treatment with preservative-containing tafluprost 0.0015% once daily or preservative-containing latanoprost 0.005% once daily reduced IOP by 7.1 or 7.7 mm Hg, respectively, at 24 months.2, 16 Although the difference in IOP-lowering effects was clinically small,2 this study failed to demonstrate noninferiority of tafluprost compared with latanoprost.16 In another study designed to compare efficacy and safety of tafluprost with travoprost, patients receiving tafluprost 0.0015% had slightly (but statistically significantly) higher 12-hour mean IOP compared with those receiving travoprost 0.004% (17.5 versus 16.9 mm Hg) following 6 weeks of therapy.4 Because of study limitations (e.g., small sample size [51 patients], short duration), the clinical significance of this difference in IOP-lowering effect is unclear, and whether such difference exists following long-term therapy remains to be established.4
The addition of tafluprost to existing timolol therapy further reduces IOP in patients with open-angle glaucoma or ocular hypertension.12 In a 12-week double-blind, phase 3 study, 185 patients 18 years of age and older with a mean baseline IOP of 22-30 mm Hg following timolol therapy were randomized to receive either timolol 0.5% twice daily and preservative-free tafluprost 0.0015% once daily or timolol 0.5% twice daily with vehicle once daily for 6 weeks, after which, all patients received open-label timolol with tafluprost for an additional 6 weeks.12, 16 At 6 weeks, greater reductions in diurnal IOP were achieved in patients receiving timolol and tafluprost (5.49-5.82 mm Hg) compared with patients receiving timolol and vehicle (3.99-4.15 mm Hg).12 During the extension period (weeks 6-12), patients previously randomized to receive timolol with tafluprost achieved further reduction in IOP; IOP was reduced by 6.22-6.79 mm Hg at week 12.12 These results indicate that tafluprost may be used in patients with glaucoma or ocular hypertension that is not controlled with timolol alone.12
Tafluprost is applied topically to the eye(s) as an ophthalmic solution.1
If the patient is receiving more than one topical ophthalmic drug, the drugs should be administered at least 5 minutes apart.1
Tafluprost is available as a preservative-free 0.015-mg/mL (0.0015%) solution packaged in single-use containers; each single-use container has 0.3 mL of solution, corresponding to 0.0045 mg of tafluprost.1 Because tafluprost ophthalmic solution contains no preservatives, the drug should be used immediately after opening the single-use container; any unused portion should be discarded immediately after administration since sterility cannot be maintained after the container is opened.1
The recommended adult dosage of tafluprost for the treatment of open-angle glaucoma or ocular hypertension is 1 drop of a 0.0015% ophthalmic solution in the conjunctival sac of the affected eye(s) once daily in the evening.1 Tafluprost should not be administered more frequently than once daily since more frequent dosing may diminish the intraocular pressure (IOP)-lowering effect of the drug.1
If the target IOP is not achieved, alternative or additional ocular hypotensive agents may be required.130, 131, 133 (See Uses: Ocular Hypertension and Glaucoma.)
The manufacturer makes no special population dosage recommendations at this time.1
The manufacturer states there are no known contraindications to the use of tafluprost.1
Changes in pigmented tissues, including increased pigmentation of the iris and periorbital tissue (eyelid), have been reported with tafluprost ophthalmic solution.1 Changes in pigmentation result from increased melanin content in the melanocytes rather than from an increase in the number of melanocytes.1 Pigmentation is 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 has been reported to be reversible in some patients.1 Long-term effects of increased pigmentation are unknown.1
Increased pigmentation of the iris may not be evident until after several months to years of tafluprost therapy.1 Typically, the brown pigmentation around the pupil spreads concentrically toward the periphery of the iris, and the entire iris or parts of the iris become more brownish.1 Neither nevi nor freckles of the iris appear to be affected by treatment.1 Tafluprost may be continued in patients who develop noticeably increased iris pigmentation; however, these patients should be examined regularly.1
Tafluprost may gradually change 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 These changes usually are reversible upon discontinuance of therapy.1
Tafluprost should be used with caution in patients with active intraocular inflammation (e.g., iritis/uveitis) because the inflammation may be exacerbated.1
Macular edema, including cystoid macular edema, has been reported during therapy with prostaglandin F2α analogs.1 Tafluprost should be used 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
Category C.1 (See Users Guide.)
Teratogenicity, embryolethality, and decreased fetal weight have been demonstrated in animals receiving IV tafluprost.1 There are no adequate and well-controlled studies using tafluprost in pregnant women.1 Tafluprost should not be used during pregnancy unless the potential benefits justify the potential risk to the fetus.1 Women of childbearing potential should use effective contraceptive methods during tafluprost therapy.1
Tafluprost and/or its metabolites are distributed into milk in rats; it is not known whether tafluprost and/or its metabolites are distributed into human milk.1 Because many drugs are distributed into human milk, caution should be exercised when tafluprost ophthalmic solution is administered to a nursing woman.1
Use of tafluprost ophthalmic solution in pediatric patients is not recommended because of potential safety concerns related to increased pigmentation following long-term use.1 (See Pigmentation under Cautions: Warnings/Precautions.)
No overall differences in safety or efficacy have been observed between geriatric patients and younger adults.1
Adverse ocular effects reported in 2% or more of patients receiving tafluprost ophthalmic solution include conjunctival hyperemia,1, 2, 3 ocular stinging/irritation,1, 2, 3 ocular pruritus (including allergic conjunctivitis),1, 2, 3 cataract,1, 2 dry eye,1, 2 ocular pain,1, 2, 3 eyelash darkening,1, 2 growth of eyelashes,1, 2 and blurred vision.1
Adverse nonocular effects reported in 2% or more of patients receiving tafluprost ophthalmic solution include headache,1 common cold,1 cough,1 and urinary tract infection.1
No formal drug interaction studies have been performed.13 However, no interactions are expected because of limited systemic exposure.17
Tafluprost, a fluorinated analog of prostaglandin F2α (PGF2α), is an ocular hypotensive agent that is structurally and pharmacologically related to other agents in this class (e.g., latanoprost, travoprost).1, 8, 9 Like latanoprost and travoprost, tafluprost acts as a selective prostanoid FP receptor agonist.1, 8 Although the mechanism of action of tafluprost has not been fully elucidated, the drug appears to reduce intraocular pressure (IOP) by increasing uveoscleral outflow.1
Tafluprost is an ester prodrug; the drug is rapidly hydrolyzed to its active form (tafluprost acid) by corneal esterases.1, 8, 9 Tafluprost is a potent FP receptor agonist, with affinity for the receptor that is 12 times that of latanoprost.8, 9 Tafluprost has negligible affinity for other prostanoid receptors (e.g., DP, EP2, IP, TP).8 A reduction in IOP generally occurs approximately 2-4 hours after ocular instillation and reaches maximum effect after 12 hours.1, 6
Importance of not exceeding once-daily dosing; more frequent administration may decrease the intraocular pressure (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.1 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 instructions on proper storage of cartons, unopened foil pouches, and opened foil pouches.1 Prescriptions of tafluprost ophthalmic solution obtained by mail order should not be used if the drug is received more than 2 days after the dispensing date.1 Cartons and unopened foil pouches should be stored in a refrigerator (2-8°C) and protected from moisture.1 After the pouch is opened, single-use containers may be stored in the opened foil pouch for up to 30 days at room temperature (20-25°C).1 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.)
Additional Information
Overview® (see Users Guide). For additional information on this drug until a more detailed monograph is developed and published, the manufacturer's labeling should be consulted. It is essential that the manufacturer's labeling be consulted for more detailed information on usual cautions, precautions, contraindications, potential drug interactions, laboratory test interferences, and acute toxicity.
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.
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
Ophthalmic | Solution | 0.0015% | Zioptan® | Akorn |
AHFS® Drug Information. © Copyright, 1959-2025, Selected Revisions November 2, 2020. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, MD 20814.
1. Akorn, Inc. Zioptan® (tafluprost) ophthalmic solution 0.0015% prescribing information. Lake Forest, IL; 2018 Nov.
2. Uusitalo H, Pillunat LE, Ropo A et al. Efficacy and safety of tafluprost 0.0015% versus latanoprost 0.005% eye drops in open-angle glaucoma and ocular hypertension: 24-month results of a randomized, double-masked phase III study. Acta Ophthalmol . 2010; 88:12-9. [PubMed 20420586]
3. Chabi A, Varma R, Tsai JC et al. Randomized Clinical Trial of the Efficacy and Safety of Preservative-free Tafluprost and Timolol in Patients With Open-Angle Glaucoma or Ocular Hypertension. Am J Ophthalmol . 2012; 153:1187-96. [PubMed 22310086]
4. Schnober D, Hofmann G, Maier H et al. Diurnal IOP-lowering efficacy and safety of travoprost 0.004% compared with tafluprost 0.0015% in patients with primary open-angle glaucoma or ocular hypertension. Clin Ophthalmol . 2010; 4:1459-63. [PubMedCentral][PubMed 21191441]
6. Sutton A, Gouws P, Ropo A. Tafluprost, a new potent prostanoid receptor agonist: a dose-response study on pharmacodynamics and tolerability in healthy volunteers. Int J Clin Pharmacol Ther . 2008; 46:400-6. [PubMed 18793581]
7. . Tafluprost (Zioptan) - a new topical prostaglandin for glaucoma. Med Lett Drugs Ther . 2012; 54:31-2. [PubMed 22499235]
8. Pozarowska D. Safety and tolerability of tafluprost in treatment of elevated intraocular pressure in open-angle glaucoma and ocular hypertension. Clin Ophthalmol . 2010; 4:1229-36. [PubMedCentral][PubMed 21060677]
9. Aihara M. Clinical appraisal of tafluprost in the reduction of elevated intraocular pressure (IOP) in open-angle glaucoma and ocular hypertension. Clin Ophthalmol . 2010; 4:163-70. [PubMedCentral][PubMed 20390038]
10. Erb C, Lanzl I, Seidova SF et al. Preservative-free tafluprost 0.0015% in the treatment of patients with glaucoma and ocular hypertension. Adv Ther . 2011; 28:575-85. [PubMed 21725844]
12. Egorov E, Ropo A, Investigators. Adjunctive use of tafluprost with timolol provides additive effects for reduction of intraocular pressure in patients with glaucoma. Eur J Ophthalmol . 2009 Mar-Apr; 19:214-22.
13. US Food and Drug Administration. Center for Drug Evaluation and Research. Application number 202514: Clinical pharmacology and biopharmaceutics review(s). From FDA website. [Web]
15. US Food and Drug Administration. Center for Drug Evaluation and Research. Application number 202514: Summary review. From FDA website. [Web]
16. US Food and Drug Administration. Center for Drug Evaluation and Research. Application number 202514: Statistical review(s). From FDA website. [Web]
17. US Food and Drug Administration. Center for Drug Evaluation and Research. Application number 202514: Medical review(s). From FDA website. [Web]
130. Prum BE Jr, Rosenberg LF, Gedde SJ et al. Primary open-angle glaucoma preferred practice pattern® guideline [published corrigendum appears in Ophthalmology . 2018; 125: 949]. San Francisco, CA: American Academy of Ophthalmology; 2015. From the American Academy of Ophthalmology website. [Web]
131. Liebmann JM, Lee JK. Current therapeutic options and treatments in development for the management of primary open-angle glaucoma. Am J Manag Care . 2017; 23(15 Suppl):S279-S292. [PubMed 29164845]
132. Weinreb RN, Aung T, Medeiros FA. The pathophysiology and treatment of glaucoma: a review. JAMA . 2014; 311:1901-11. [PubMed 24825645]
133. Gupta D, Chen PP. Glaucoma. Am Fam Physician . 2016; 93:668-74. [PubMed 27175839]
134. Inoue K. Managing adverse effects of glaucoma medications. Clin Ophthalmol . 2014; 8:903-13. [PubMed 24872675]