Generic Name: Tafluprost
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
Uses for Zioptan
Ocular Hypertension and Glaucoma
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
Zioptan Dosage and 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
Ocular Hypertension and Glaucoma
One drop of a 0.0015% solution 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
No special population dosage recommendations at this time.1
Cautions for Zioptan
Manufacturer states none known.1
Increased pigmentation of the iris, periorbital tissue (eyelid), and eyelashes 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 the periorbital tissue and eyelash changes reportedly are reversible in some patients.1 Long-term effects of increased pigmentation unknown.1
Increased pigmentation of the iris develops slowly; 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; examine these patients regularly.1
Possible gradual change in eyelashes and vellus hair in the treated eye, including increased length, color, thickness, shape, and number of eyelashes.1 Usually reversible upon discontinuance of therapy.1
Use with caution in patients with active intraocular inflammation (e.g., iritis/uveitis); may exacerbate inflammation.1
Macular edema, including cystoid macular edema, reported with prostaglandin F2α 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
Use in pediatric patients not recommended because of potential safety concerns related to increased pigmentation following long-term use.1
No overall clinical 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
Interactions for Zioptan
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
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
Tafluprost acid: Rapidly eliminated from plasma; plasma levels are below the limit of quantitation within 30 minutes following ocular instillation.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 28 days at 20–25°C; discard any unused containers 28 days after first opening pouch.1 Protect from moisture.1
Mechanism of action not fully elucidated; appears to reduce IOP by increasing uveoscleral outflow.1
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 increased 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.1 Potential for disparity between eyes in length, thickness, pigmentation, number of eyelashes or vellus hairs, and/or direction of eyelash growth if only one eye is treated.1 Eyelash changes are usually reversible after discontinuance of tafluprost.1
Importance of patients informing a clinician 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
Importance of administering different topical ophthalmic 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 noting the date the foil pouch was opened in the space provided on the pouch and of discarding unused containers after 28 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.)
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.
AHFS DI Essentials. © Copyright 2016, Selected Revisions September 1, 2012. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.
1. Merck & Co., Inc. Zioptan (tafluprost) ophthalmic solution 0.0015% prescribing information. Whitehouse Station, NJ; 2012 Mar.
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. [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. [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. [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.
15. US Food and Drug Administration. Center for Drug Evaluation and Research. Application number 202514: Summary review. From FDA website.
16. US Food and Drug Administration. Center for Drug Evaluation and Research. Application number 202514: Statistical review(s). From FDA website.
17. US Food and Drug Administration. Center for Drug Evaluation and Research. Application number 202514: Medical review(s). From FDA website.