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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
Brands: Zioptan

Medically reviewed by Drugs.com. Last updated on Nov 2, 2020.

Introduction

Ocular hypotensive agent; fluorinated analog of prostaglandin F (PGF).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 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

Interactions for Tafluprost

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.

Tafluprost

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Ophthalmic

Solution

0.0015%

Zioptan

Akorn

AHFS DI Essentials™. © Copyright 2021, Selected Revisions November 2, 2020. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

References

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. http://www.ncbi.nlm.nih.gov/pubmed/20420586?dopt=AbstractPlus

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. http://www.ncbi.nlm.nih.gov/pubmed/22310086?dopt=AbstractPlus

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. http://www.ncbi.nlm.nih.gov/pubmed/21191441?dopt=AbstractPlus http://www.pubmedcentral.nih.gov/picrender.fcgi?tool=pmcentrez&artid=3009992&blobtype=pdf

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. http://www.ncbi.nlm.nih.gov/pubmed/18793581?dopt=AbstractPlus

7. . Tafluprost (Zioptan) - a new topical prostaglandin for glaucoma. Med Lett Drugs Ther. 2012; 54:31-2. http://www.ncbi.nlm.nih.gov/pubmed/22499235?dopt=AbstractPlus

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. http://www.ncbi.nlm.nih.gov/pubmed/21060677?dopt=AbstractPlus http://www.pubmedcentral.nih.gov/picrender.fcgi?tool=pmcentrez&artid=2964963&blobtype=pdf

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. http://www.ncbi.nlm.nih.gov/pubmed/20390038?dopt=AbstractPlus http://www.pubmedcentral.nih.gov/picrender.fcgi?tool=pmcentrez&artid=2850830&blobtype=pdf

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. http://www.ncbi.nlm.nih.gov/pubmed/21725844?dopt=AbstractPlus

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. http://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202514Orig1s000ClinPharmR.pdf

15. US Food and Drug Administration. Center for Drug Evaluation and Research. Application number 202514: Summary review. From FDA website. http://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202514Orig1s000SumR.pdf

16. US Food and Drug Administration. Center for Drug Evaluation and Research. Application number 202514: Statistical review(s). From FDA website. http://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202514Orig1s000StatR.pdf

17. US Food and Drug Administration. Center for Drug Evaluation and Research. Application number 202514: Medical review(s). From FDA website. http://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202514Orig1s000MedR.pdf

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. https://www.aao.org/preferred-practice-pattern/primary-open-angle-glaucoma-ppp-2015

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. http://www.ncbi.nlm.nih.gov/pubmed/29164845?dopt=AbstractPlus

132. Weinreb RN, Aung T, Medeiros FA. The pathophysiology and treatment of glaucoma: a review. JAMA. 2014; 311:1901-11. http://www.ncbi.nlm.nih.gov/pubmed/24825645?dopt=AbstractPlus

133. Gupta D, Chen PP. Glaucoma. Am Fam Physician. 2016; 93:668-74. http://www.ncbi.nlm.nih.gov/pubmed/27175839?dopt=AbstractPlus

134. Inoue K. Managing adverse effects of glaucoma medications. Clin Ophthalmol. 2014; 8:903-13. http://www.ncbi.nlm.nih.gov/pubmed/24872675?dopt=AbstractPlus