ZIOPTAN

Ophthalmic Prostaglandins including Analogs and Receptor Agonists

Tafluprost is for ophthalmic use only.
Tilt the head back slightly and pull the lower eyelid down with the index finger to form a pouch. Squeeze one drop into the pouch and gently close the eyes for 1—2 minutes. Do not blink.
To avoid contamination, do not touch the tip of the dropper to the eye, fingertips, or other surface. Tafluprost does not contain a preservative. Instruct patients to use immediately after opening and discard remaining contents from individual unit immediately after administration.
The solution may be used concomitantly with other topical ophthalmic drug products to lower intraocular pressure. If more than one topical ophthalmic drug is being used, the drugs should be administered at least 5 minutes apart.

macular edema / Delayed / Incidence not known
uveitis / Delayed / Incidence not known

conjunctival hyperemia / Early / 4.0-20.0
cataracts / Delayed / 3.0-3.0
blurred vision / Early / 2.0-2.0
iritis / Delayed / Incidence not known
conjunctivitis / Delayed / Incidence not known
dyspnea / Early / Incidence not known

ocular irritation / Rapid / 7.0-7.0
headache / Early / 6.0-6.0
ocular pruritus / Rapid / 5.0-5.0
infection / Delayed / 2.0-4.0
xerophthalmia / Early / 3.0-3.0
ocular pain / Early / 3.0-3.0
cough / Delayed / 3.0-3.0
skin hyperpigmentation / Delayed / Incidence not known
iridal discoloration / Delayed / Incidence not known

ZIOPTAN

Rx

Prostaglandin analog
Used for reducing elevated IOP in patients with open-angle glaucoma or ocular hypertension
May increase pigmentation of eyelashes, iris, and/or eyelid skin

Instill 1 drop in the conjunctival sac of the affected eye(s) once daily in the evening. More frequent administration may decrease the IOP-lowering effect.

Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.

Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.

There are no drug interactions associated with Tafluprost products.

Tafluprost/ZIOPTAN Ophthalmic Drops: 0.0015%

1 drop/day in each affected eye.

1 drop/day in each affected eye.

Safety and efficacy have not been established.

Safety and efficacy have not been established.

Safety and efficacy have not been established.

Safety and efficacy have not been established.

Tafluprost acid, a prostaglandin analog that acts as a selective agonist at the fluoroprostaglandin (FP) prostanoid receptor, is believed to reduce intraocular pressure by increasing uveoscleral outflow. The exact mechanism of action of tafluprost is unknown.

Tafluprost is administered topically to the eye.

Ophthalmic Route
After ocular administration, tafluprost is absorbed through the cornea. After administration of one drop of tafluprost 0.0015%, peak plasma concentrations of tafluprost acid are achieved within 10 minutes. In healthy volunteers, the mean plasma Cmax of tafluprost acid were 26 pg/ml and 27 pg/ml on day 1 and day 8, respectively. Reduction of intraocular pressure begins approximately 2—4 hours after the first dose with the maximum effect occurring in about 12 hours. Tafluprost is an ester prodrug that is hydrolyzed to tafluprost acid in the eye. Tafluprost acid is then further metabolized via fatty acid beta-oxidation and phase II conjugation. Tafluprost concentrations were undetectable in plasma 30 minutes after ocular administration (limit of quantification, 10 pg/ml).

Tafluprost is classified as pregnancy risk category C. Although there are no adequate and well-controlled studies of tafluprost in pregnant women, limited experience with latanoprost, another ophthalmic prostaglandin analog, in human pregnancy has not resulted in clinically significant risk to the fetus. In addition, the mean plasma concentrations of tafluprost after ophthalmic administration were below the limit of quantification suggesting exposure to the fetus is low. According to the manufacturer, tafluprost should not be administered during pregnancy unless the potential benefit justifies the potential risk to the fetus; the manufacturer also recommends that females of childbearing age or potential have adequate contraceptive measures in place.

It is not known whether tafluprost is excreted in human milk. There is minimal systemic absorption of tafluprost after ophthalmic administration ; therefore, clinically significant amounts of the drug are not expected to be bioavailable to a nursing infant via breast-milk. To further minimize the amount of drug that reaches the systemic circulation and breast milk, apply pressure over the tear duct by the corner of the eye for 1 minute after ophthalmic administration. According to the manufacturer, caution should be exercised when it is administered to a breast-feeding woman. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally administered drug, healthcare providers are encouraged to report the adverse effect to the FDA.