Zioptan

Tafluprost · Solution/ Drops · Ophthalmic

Uses

1 INDICATIONS AND USAGE ZIOPTAN® is indicated for reducing elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. ZIOPTAN is a prostaglandin analog indicated for reducing elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. ( 1 )

Dosage and administration

Apply one drop in the affected eye(s) once daily in the evening. ( 2 ) 2.1 Recommended Dosage The recommended dosage is one drop in the conjunctival sac of the affected eye(s) once daily in the evening. 2.2 Administration Instructions ZIOPTAN should not be administered more than once daily since it has been shown that more frequent administration of prostaglandin analogs may lessen the intraocular pressure (IOP) lowering effect. Reduction of the intraocular pressure starts approximately 2 to 4 hours after the first administration with the maximum effect reached after 12 hours. ZIOPTAN may be used concomitantly with other topical ophthalmic drug products to lower IOP. If more than one topical ophthalmic product is being used, each one should be administered at least 5 minutes apart. The solution from one single-dose container is to be used immediately after opening for administration to one or both eyes. Since sterility cannot be maintained after the single-dose container is opened, discard the open single-dose container and the remaining contents immediately after administration.

Dosage forms and strengths

Ophthalmic solution: 0.0015% tafluprost in a single-dose container. Ophthalmic solution: 0.0015% tafluprost in a single-dose container. ( 3 )

Contraindications

None. None. ( 4 )

Side effects

6 ADVERSE REACTIONS . Most common ocular adverse reaction is conjunctival hyperemia (4% to 20%). ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Thea Pharma Inc. at 1-833-838-4028 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Studies Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Preservative-containing or nonpreserved tafluprost 0.0015% was evaluated in 905 patients in five controlled clinical studies of up to 24-months duration. The most common adverse reaction observed in patients treated with tafluprost was conjunctival hyperemia which was reported in a range of 4% to 20% of patients. Approximately 1% of patients discontinued therapy due to ocular adverse reactions. Ocular adverse reactions reported at an incidence of ≥ 2% in these clinical studies included ocular stinging/irritation (7%), ocular pruritus including allergic conjunctivitis (5%), cataract (3%), dry eye (3%), ocular pain (3%), eyelash darkening (2%), growth of eyelashes (2%) and vision blurred (2%). Nonocular adverse reactions reported at an incidence of 2% to 6% in these clinical studies in patients treated with tafluprost 0.0015% were headache (6%), common cold (4%), cough (3%) and urinary tract infection (2%). 6.2 Postmarketing Experience The following adverse reactions have been identified during postapproval use of tafluprost. Because postapproval adverse reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Respiratory disorders: exacerbation of asthma, dyspnea Eye disorders: iritis/uveitis In postmarketing use with prostaglandin analogs, periorbital and lid changes including deepening of the eyelid sulcus have been observed.

Use in specific populations

8 USE IN SPECIFIC POPULATIONS . Use in pediatric patients is not recommended because of potential safety concerns related to increased pigmentation following long-term chronic use. ( 8.4 ) 8.1 Pregnancy Risk Summary There are no adequate and well-controlled studies of ZIOPTAN administration in pregnant women to inform of drug-associated risks. In animal reproduction studies, intravenous administration of tafluprost to pregnant rabbits and rats throughout organogenesis resulted in embryofetal toxicities at exposures ≥5-times the human dose in rabbit and ≥2362-times the human dose in rat. (see Data). The estimated background risk of major birth defects and miscarriage for the indicated population(s) is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Data Animal Data In embryo-fetal development studies, intravenous administration of tafluprost to pregnant rats and rabbits during organogenesis caused increases in post-implantation losses in both species and reductions in fetal body weights in rats (≥0.03 mcg/kg/day in rabbits, 5-times the maximum clinical exposure based on Cmax; ≥10 mcg/kg/day in rats, 2362-times the maximum clinical exposure based on Cmax). Tafluprost also increased the incidence of vertebral skeletal abnormalities in rats and the incidence of skull, brain and spine malformations in rabbits at these same doses. In rats, there were no adverse effects on embryo-fetal development at a dose of 3 mcg/kg/day corresponding to maternal plasma levels of tafluprost acid that were 343 times the maximum clinical exposure based on Cmax. At the no-effect dose in rabbits (0.01 mcg/kg/day), maternal plasma levels of tafluprost acid were below the lower level of quantification (20 pg/mL). In a pre- and postnatal development study, intravenous administration of tafluprost to pregnant rats during organogenesis and through birth and lactation, caused increased mortality of newborns, decreased body weights and delayed pinna unfolding in offsprings. The no observed adverse effect level was at a tafluprost intravenous dose of 0.3 mcg/kg/day which is greater than 3 times the maximum recommended clinical dose based on body surface area comparison. 8.2 Lactation Risk Summary There are no data on the presence of tafluprost or its metabolites in human milk, the effects on the breastfed infant, or the effects on milk production following topical ocular administration. Tafluprost and/or its metabolites are present in rat milk following ocular administration. When a drug is present in animal milk, it is likely that the drug will be present in human milk. 8.4 Pediatric Use Use in pediatric patients is not recommended because of potential safety concerns related to increased pigmentation following long-term chronic use. 8.5 Geriatric Use No overall clinical differences in safety or effectiveness have been observed between elderly and other adult patients.

Pregnancy

8.1 Pregnancy Risk Summary There are no adequate and well-controlled studies of ZIOPTAN administration in pregnant women to inform of drug-associated risks. In animal reproduction studies, intravenous administration of tafluprost to pregnant rabbits and rats throughout organogenesis resulted in embryofetal toxicities at exposures ≥5-times the human dose in rabbit and ≥2362-times the human dose in rat. (see Data). The estimated background risk of major birth defects and miscarriage for the indicated population(s) is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Data Animal Data In embryo-fetal development studies, intravenous administration of tafluprost to pregnant rats and rabbits during organogenesis caused increases in post-implantation losses in both species and reductions in fetal body weights in rats (≥0.03 mcg/kg/day in rabbits, 5-times the maximum clinical exposure based on Cmax; ≥10 mcg/kg/day in rats, 2362-times the maximum clinical exposure based on Cmax). Tafluprost also increased the incidence of vertebral skeletal abnormalities in rats and the incidence of skull, brain and spine malformations in rabbits at these same doses. In rats, there were no adverse effects on embryo-fetal development at a dose of 3 mcg/kg/day corresponding to maternal plasma levels of tafluprost acid that were 343 times the maximum clinical exposure based on Cmax. At the no-effect dose in rabbits (0.01 mcg/kg/day), maternal plasma levels of tafluprost acid were below the lower level of quantification (20 pg/mL). In a pre- and postnatal development study, intravenous administration of tafluprost to pregnant rats during organogenesis and through birth and lactation, caused increased mortality of newborns, decreased body weights and delayed pinna unfolding in offsprings. The no observed adverse effect level was at a tafluprost intravenous dose of 0.3 mcg/kg/day which is greater than 3 times the maximum recommended clinical dose based on body surface area comparison.

Pediatric use

8.4 Pediatric Use Use in pediatric patients is not recommended because of potential safety concerns related to increased pigmentation following long-term chronic use.

Geriatric use

8.5 Geriatric Use No overall clinical differences in safety or effectiveness have been observed between elderly and other adult patients.

Description

(tafluprost ophthalmic solution) 0.0015% contains tafluprost, a fluorinated analog of prostaglandin F2α, for topical ophthalmic use. The chemical name for tafluprost is 1-methylethyl (5Z)-7-{(1R,2R,3R,5S)-2-[(1E)-3,3-difluoro-4-phenoxy-1-butenyl}-3,5-dihydroxycyclopentyl]-5-heptenoate. The molecular formula of tafluprost is C25H34F2O5 and its molecular weight is 452.53. Its structural formula is: Tafluprost is a colorless to light yellow viscous liquid that is practically insoluble in water. ZIOPTAN is supplied as a sterile solution with a pH range of 5.5 to 6.7 and an Osmolality range of 260 to 300 mOsmo/kg. ZIOPTAN contains Active: tafluprost 0.015 mg/mL; Inactives: disodium edetate, hydrochloric acid and/or sodium hydroxide (to adjust pH), glycerol, polysorbate 80, sodium dihydrogen phosphate dihydrate, and Water for Injection. ZIOPTAN does not contain a preservative. Chemical Structure

Mechanism of action

12.1 Mechanism of Action Tafluprost acid, a prostaglandin analog is a selective FP prostanoid receptor agonist which is believed to reduce intraocular pressure by increasing uveoscleral outflow. The exact mechanism of action is unknown at this time.

How supplied

(tafluprost ophthalmic solution) 0.0015% is supplied as a sterile solution in translucent low density polyethylene single-dose containers packaged in foil pouches (10 single-dose containers per pouch). Each single-dose container has 0.3 mL solution corresponding to 0.0045 mg tafluprost. NDC 82584-609-30; Unit-of-Use Carton of 30. Storage: Store refrigerated at 2° to 8°C (36° to 46°F). During shipment ZIOPTAN may be maintained at temperatures up to 40°C (104°F) for a period not exceeding 2 days. Mail-order prescriptions received after two days of the dispensing date noted in the prescribing label should not be used. Store in the original pouch. After the pouch is opened, unopened single-dose containers may be stored in the opened foil pouch for up to 30 days at room temperature 20° to 25°C (68° to 77°F). Protect from moisture. Write down the date you open the foil pouch in the space provided on the pouch. Discard any unopened containers 30 days after first opening the pouch.

Storage

Storage: Store refrigerated at 2° to 8°C (36° to 46°F). During shipment ZIOPTAN may be maintained at temperatures up to 40°C (104°F) for a period not exceeding 2 days. Mail-order prescriptions received after two days of the dispensing date noted in the prescribing label should not be used. Store in the original pouch. After the pouch is opened, unopened single-dose containers may be stored in the opened foil pouch for up to 30 days at room temperature 20° to 25°C (68° to 77°F). Protect from moisture. Write down the date you open the foil pouch in the space provided on the pouch. Discard any unopened containers 30 days after first opening the pouch.

Patient information

Advise patients to read the FDA-approved patient labeling (Patient Information and Instructions for Use). Potential for Pigmentation Advise patients about the potential for increased brown pigmentation of the iris, which may be permanent. Also inform patients about the possibility of eyelid skin darkening, which may be reversible after discontinuation of ZIOPTAN. Potential for Eyelash Changes Inform patients of the possibility of eyelash and vellus hair changes in the treated eye during treatment with ZIOPTAN. These changes may result in a disparity between eyes in length, thickness, pigmentation, number of eyelashes or vellus hairs, and/or direction of eyelash growth. Eyelash changes are usually reversible upon discontinuation of treatment. Once Nightly Application Advise patients to not exceed once daily dosing since more frequent administration may decrease the intraocular pressure lowering effect of ZIOPTAN. Handling the Single-Dose Container Advise patients that ZIOPTAN is a sterile solution that does not contain a preservative. The solution from one single-dose container is to be used immediately after opening for administration to one or both eyes. Since sterility cannot be maintained after the single-dose container is opened, discard the open container and remaining contents immediately after administration. Open a new single-dose container every time you use ZIOPTAN. When to Seek Physician Advice Advise patients that if they develop a new ocular condition (e.g., trauma or infection), experience a sudden decrease in visual acuity, have ocular surgery, or develop any ocular reactions, particularly conjunctivitis and eyelid reactions, they should immediately seek their physician's advice concerning the continued use of ZIOPTAN. Use with Other Ophthalmic Drugs Advise patients if more than one topical ophthalmic drug is being used, the drugs should be administered at least five (5) minutes between applications. Storage Information Instruct patients on proper storage of cartons, unopened foil pouches, and opened foil pouches [see How Supplied/Storage and Handling (16) ]. ecommended storage for cartons and unopened foil pouches is to store refrigerated at 2° to 8°C (36° to 46°F). After the pouch is opened, the single-dose containers may be stored in the opened foil pouch for up to 30 days at room temperature 20° to 25°C (68° to 77°F). Protect from moisture.

Label text from the FDA structured product label by Thea Pharma Inc. (revised Apr 23, 2026). Long sections are shortened; the complete label is on DailyMed.

Active ingredients

Tafluprost in 1 product

Zioptan NDC products (1)

NDC	Strength & form	Labeler	Type
82584-609	Tafluprost .015 mg/mL Solution/ Drops	Thea Pharma Inc.	NDA

Frequently asked questions

What is Zioptan used for?

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Who makes Zioptan?

Zioptan is listed by 1 labeler in the FDA NDC directory, including Thea Pharma Inc..