ZIOPTAN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ZIOPTAN (ZIOPTAN).
ZIOPTAN (tafluprost) is a prostaglandin analog that reduces intraocular pressure by increasing the outflow of aqueous humor through the uveoscleral pathway.
| Metabolism | Metabolized by esterases in the eye to the active acid; further metabolism via beta-oxidation and reduction. |
| Excretion | Primarily renal excretion of unchanged drug (approximately 70-80% of an administered dose recovered in urine over 48 hours); biliary/fecal excretion accounts for 13% to 20% as parent drug and metabolites. |
| Half-life | Terminal elimination half-life is approximately 2.8 to 4.5 hours in patients with normal renal function; no clinically significant accumulation occurs with twice-daily dosing. |
| Protein binding | Approximately 99% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is 0.92 ± 0.27 L/kg, indicating distribution into total body water with some tissue binding. |
| Bioavailability | Bioavailability after topical ocular administration is approximately 30% due to significant metabolism in the cornea and nasolacrimal system; systemic exposure is low. |
| Onset of Action | Onset of ocular hypotensive effect occurs within 1 to 2 hours after topical instillation; maximal effect is achieved at approximately 8 to 12 hours post-dose. |
| Duration of Action | Duration of action is at least 24 hours after a single topical dose, allowing once-daily administration; clinical effect persists for 24 hours with regular use. |
250 mg orally once daily.
| Dosage form | SOLUTION/DROPS |
| Renal impairment | For GFR 30-89 mL/min: no adjustment; GFR <30 mL/min: not recommended. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B or C: not recommended. |
| Pediatric use | Not approved for use in pediatric patients. |
| Geriatric use | No specific dose adjustment required; monitor renal function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ZIOPTAN (ZIOPTAN).
| Breastfeeding | It is unknown if tafluprost is excreted in human milk after ocular administration. Systemically absorbed drug is likely negligible due to low dose. However, caution is advised because of potential for adverse effects in the infant. M/P ratio not available. Consider benefit of breastfeeding vs risk. |
| Teratogenic Risk | ZIOPTAN (tafluprost ophthalmic solution) is a prostaglandin analog. Systemic exposure after ocular administration is minimal. However, prostaglandins can increase uterine tone and contractions. Based on animal studies and mechanism of action, there is a potential risk of abortion or preterm labor. Use in pregnancy is not recommended unless clearly necessary. In first trimester: avoid unless benefit outweighs risk; second/third trimesters: may cause uterine contractions; near term: risk of preterm labor. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to tafluprost or any component of the formulation"]
| Precautions | ["May cause changes to pigmented tissues (e.g., iris, eyelids, eyelashes); use with caution in patients with intraocular inflammation (iritis/uveitis), aphakic/pseudophakic patients with torn posterior lens capsule, or those with risk factors for macular edema.","May cause eyelash changes (increased length, thickness, pigmentation) and periorbital tissue changes.","May reactivate ocular herpes simplex."] |
Loading safety data…
| Fetal Monitoring | Monitor for signs of preterm labor, uterine contractions, or vaginal bleeding during pregnancy. In neonates exposed in utero, no specific fetal monitoring required after delivery unless maternal complications occurred. Ocular effects in mother require routine ophthalmic exams. |
| Fertility Effects | No human data on fertility effects. In animal studies, tafluprost did not impair fertility. However, prostaglandin analogs may theoretically affect reproductive function; no evidence of significant impairment in clinical use. |