Dosing and uses of Zioptan (tafluprost)
Adult dosage forms and strengths
ophthalmic solution
- 0.0015% (0.015mg/mL)
Elevated Intraocular Pressure
Indicated for reducing elevated IOP in patients with open-angle glaucoma or ocular hypertension
Instill 1 drop in affected eye(s) once daily in the evening
Administration
Instill into conjunctival sac of affected eye(s)
Do not exceed once daily dosing regimen; more frequent administration of prostaglandin analogs may lessen the IOP lowering effect
Reduction of intraocular pressure starts approximately 2 - 4 hours after first administration with maximum effect reached after 12 hr
If other topical ophthalmics are prescribed, each should be administered 5 minutes apart
Preservative free product; use immediately after opening one unit-dose for administration; sterility cannot be maintained after opening
Pediatric dosage forms and strengths
Not recommended because of potential safety concerns related to increased pigmentation following long-term chronic use
Zioptan (tafluprost) adverse (side) 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
Warnings
Contraindications
None
Cautions
Causes changes to pigmented tissues; most frequently reported changes have been of the iris, eyelid, and eyelashes; pigmentation changes of the iris is likely permanent Increases length, color, thickness, and number of eyelashes
Caution with active intraocular inflammation (may exacerbate condition)
Macular edema reported; caution in aphakic patients, in pseudophakic patients with a torn posterior lens capsule, or with known risk factors for macular edema
Pregnancy and lactation
Pregnancy category: C; teratogenic when administered IV in rats and rabbits
Lactation: Unknown whether distributed in breast milk
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Zioptan (tafluprost)
Mechanism of action
Prostaglandin analog; exact mechanism by which it reduces IOP is unknown, but it is thought to increase uveoscleral outflow
Absorption
Bioavailability: Absorbed through the cornea
Onset: 2-4 hr; peak effect at 12 hr
Peak Plasma Time: 10 minutes
Peak Plasma Concentration: 26 pg/mL
AUC: 394-432 pg•min/mL
Metabolism
Tafluprost is an ester prodrug that is metabolized by hydrolysis to the biologically active acid metabolite (tafluprost acid)
Elimination
Mean plasma concentration of tafluprost acid were below the limit of quantification (ie, 10 pg/mL) at 30 minutes following topical ocular administration
