Zioptan®
Tafluprost 0.0015% · preservative-free ophthalmic solution
Antiglaucoma
Approved uses
Open-angle glaucoma or ocular hypertension
One drop in the conjunctival sac of the affected eye(s) once daily in the evening; not to exceed once daily.
Lowers IOP from about 25 mmHg to about 18 mmHg, matching timolol at every time point.
Open-angle glaucoma or ocular hypertension in patients with ocular surface signs or symptoms on preserved latanoprost
One drop once daily in the evening, substituted directly for the preserved prostaglandin with no washout in the study.
IOP holds steady after switching from preserved latanoprost while surface signs and symptoms roughly halve.
Contraindications
None.
Available Forms0.0015% (0.015 mg/mL) preservative-free ophthalmic solution, 0.3 mL single-use containers, cartons of 30 and 90, 10 containers per foil pouch
Mechanism of ActionFluorinated prostaglandin F2alpha analog given as an ester prodrug that is hydrolyzed in the eye to tafluprost acid, a selective FP prostanoid receptor agonist believed to lower IOP by increasing uveoscleral outflow; the exact mechanism is unknown. IOP begins to fall 2 to 4 hours after the first dose, with maximum effect at 12 hours.
Warnings & Precautions
- Iris pigmentation: Brown pigmentation spreads concentrically from the pupil and increases as long as dosing continues, from increased melanin content in melanocytes rather than more melanocytes; it is likely permanent after discontinuation, so examine these patients regularly. Nevi and freckles of the iris appear unaffected, and the long-term effects of increased pigmentation are not known.
- Periorbital and lash changes: Eyelid skin darkening plus increased eyelash length, color, thickness, shape, and number in the treated eye; reported reversible in some patients after discontinuation.
- Intraocular inflammation: Caution with active intraocular inflammation such as iritis or uveitis, which may be exacerbated.
- Macular edema: Macular edema including cystoid macular edema has been reported with prostaglandin F2alpha analogs; caution in aphakia, in pseudophakia with a torn posterior lens capsule, and with other known risk factors.
- Single-use container sterility: Sterility cannot be maintained once a unit is opened; use it immediately for one or both eyes and discard the remaining contents.
Common Side Effects
- Ocular, most common: conjunctival hyperemia, range 4% to 20% (905 patients across five controlled studies of up to 24 months, pooling preservative-containing and preservative-free tafluprost; about 1% discontinued for ocular reactions).
- Ocular, 2% or more: ocular stinging or irritation 7%, ocular pruritus including allergic conjunctivitis 5%, cataract 3%, dry eye 3%, ocular pain 3%, eyelash darkening 2%, growth of eyelashes 2%, blurred vision 2%.
- Ocular, postmarketing: iritis and uveitis; periorbital and lid changes including deepening of the eyelid sulcus, observed with prostaglandin analogs as a class.
- Systemic, 2% to 6%: headache 6%, common cold 4%, cough 3%, urinary tract infection 2%.
- Systemic, postmarketing: exacerbation of asthma, dyspnea.
Pregnancy & LactationPregnancy: Category C. IV tafluprost was teratogenic in rats and rabbits, increasing post-implantation loss in both, reducing fetal body weight and increasing vertebral anomalies in rats, and causing skull, brain, and spine malformations in rabbits; rabbit effects occurred at about 5 times the maximum clinical exposure by Cmax, while rats showed no embryo-fetal effects at 343 times. No adequate and well-controlled studies in pregnant women, so use only if the potential benefit justifies the potential fetal risk, with adequate contraception in women of childbearing potential.
Lactation: Radiolabeled tafluprost and its metabolites were excreted in the milk of lactating rats; excretion in human milk is unknown, so use caution in a nursing woman.
Pediatric UseNot recommended in pediatric patients because of pigmentation risk with long-term chronic use.