Zioptan

Name: Zioptan

Adverse Effects

>10%

Conjunctival hyperemia (4-20%)

1-10%

Ocular stinging (7%)

Ocular pruritus/allergic conjunctivitis (5%)

Cataract (3%)

Growth of eyelashes (2%)

Blurred vision (2%)

Postmarketing Reports

Periorbital and lid changes including deepening of the eyelid sulcus observed with prostaglandin analogs

Eye disorders: Iritis/uveitis

Respiratory disorders: Exacerbation of asthma, dyspnea

Tafluprost ophthalmic Interactions

Do not use other eye medications unless your doctor tells you to.

It is not likely that other drugs you take orally or inject will have an effect on tafluprost used in the eyes. But many drugs can interact with each other. Tell each of your healthcare providers about all medicines you use, including prescription and over-the-counter medicines, vitamins, and herbal products.

Side effects

Clinical Studies Experience

Because clinical studies 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 studies of another drug and may not reflect the rates observed in practice.

Preservative-containing or preservative-free 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%).

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.

Warnings

Included as part of the PRECAUTIONS section.

Other Requirements

  • Store the opened foil pouch at room temperature, between 68°F to 77°F (20°C to 25°C), for up to 28 days.
  • Throw away all unused Zioptan single-use containers in the opened foil pouch after 28 days.
  • Keep the Zioptan single-use containers in their original foil pouch.
  • After opening the foil pouch, refrigeration is not required.
  • Keep Zioptan and all medicines out of the reach of children.
 

What is the most important information I should know about tafluprost ophthalmic?

Tafluprost ophthalmic may cause a gradual change in the color of your eyes or eyelids and lashes. Color changes may be permanent even after your treatment ends, and may occur only in the eye being treated.

Tell your doctor right away if you have any eye injury or infection, sudden vision changes, or if you need to have any type of surgery, especially eye surgery.

Call your doctor at once if you have eye pain or redness, itchy or watery eyes, or increased sensitivity to light.

Uses for Zioptan

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

Precautions While Using Zioptan

Your eye doctor will want to examine your eyes at regular visits to make sure that the medicine is working properly and is not causing unwanted effects.

This medicine may cause a brown color in the iris (colored part), eyelid, or eyelashes of your treated eye. Your eyelashes may also become longer, thicker, and darker. Some of these changes may be permanent even if you stop using tafluprost. Check with your doctor if you have any questions about this.

Check with your doctor right away if you have an eye injury, eye infection, or plan to have eye surgery.

What do I need to tell my doctor BEFORE I take Zioptan?

  • If you have an allergy to tafluprost or any other part of Zioptan (tafluprost).
  • If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.

This medicine may interact with other drugs or health problems.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take this medicine with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

Contraindications

None.

Zioptan - Clinical Pharmacology

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.

Pharmacokinetics

Absorption

Following instillation, tafluprost is absorbed through the cornea and is hydrolyzed to the biologically active acid metabolite, tafluprost acid. Following instillation of one drop of the 0.0015% solution once daily into each eye of healthy volunteers, the plasma concentrations of tafluprost acid peaked at a median time of 10 minutes on both Days 1 and 8. The mean plasma Cmax of tafluprost acid were 26 pg/mL and 27 pg/mL on Day 1, and Day 8, respectively. The mean plasma AUC estimates of tafluprost acid were 394 pg*min/mL and 432 pg*min/mL on Day 1 and 8, respectively.

Metabolism

Tafluprost, an ester prodrug, is hydrolyzed to its biologically active acid metabolite in the eye. The acid metabolite is further metabolized via fatty acid β-oxidation and phase II conjugation.

Elimination

Mean plasma tafluprost acid concentrations were below the limit of quantification of the bioanalytical assay (10 pg/mL) at 30 minutes following topical ocular administration of tafluprost 0.0015% ophthalmic solution.

How Supplied/Storage and Handling

Zioptan (tafluprost ophthalmic solution) 0.0015% is supplied as a sterile solution in translucent low density polyethylene single-use containers packaged in foil pouches (10 single-use containers per pouch). Each single-use container has 0.3 mL solution corresponding to 0.0045 mg tafluprost.

NDC 17478-609-30; Unit-of-Use Carton of 30.
NDC 17478-609-90; Unit-of-Use Carton of 90.

Storage:

Store refrigerated at 28°C (3646°F). Store in the original pouch. After the pouch is opened, the single-use containers may be stored in the opened foil pouch for up to 28 days at room temperature: 2025°C (6877°F). Protect from moisture. Write down the date you open the foil pouch in the space provided on the pouch. Discard any unused containers 28 days after first opening the pouch.

Before using Zioptan

You should not use Zioptan if you are allergic to tafluprost.

Zioptan may cause a gradual change in the color of your eyes or eyelids and lashes, as well as increased growth or thickness of your eyelashes. These color changes, usually an increase in brown pigment, occur slowly and you may not notice them for months or years. Color changes may be permanent even after your treatment ends, and may occur only in the eye being treated. This could result in a cosmetic difference in eye or eyelash color from one eye to the other.

To make sure Zioptan is safe for you, tell your doctor if you have:

  • uveitis;

  • any swelling or infection in or around your eye; or

  • a torn or missing natural lens from inside your eye.

FDA pregnancy category C. It is not known whether Zioptan will harm an unborn baby. Use effective birth control, and tell your doctor if you become pregnant during treatment.

It is not known whether tafluprost passes into breast milk or if it could harm a nursing baby. Tell your doctor if you are breast-feeding a baby.

Do not give Zioptan to anyone under 18 years old without medical advice.

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