Tafluprost

Products

Tafluprost is available in the form of eye drops (saflutane). It was approved in many countries in 2010. In 2016, a fixed combination with timolol was also registered (Taptiqom).

Structure and properties

Tafluprost (C₂₅H₃₄F₂O₅, M_r = 452.53 g/mol) is a fluorinated analog of prostaglandin F2α (Figure). It is a prodrug and is converted at the eye by esterases by cleavage of the isopropyl ester to the active tafluprostatic acid. Esterification serves to increase permeability through the cornea. Tafluprost has structural similarities to the other prostaglandin analogs.

Effects

Tafluprost (ATC S01EE05) lowers intraocular pressure by approximately 30% by increasing aqueous humor outflow. It is an agonist at the prostaglandin receptor and has a higher affinity than latanoprost.

Indications

To lower elevated intraocular pressure in open-angle glaucoma and ocular hypertension. Tafluprost can be combined with a beta-blocker such as timolol.

Dosage

According to the SmPC. 1 drop is placed in the eye or eyes once daily in the evening. Do not use more frequently or the pressure-lowering effect will be weakened. See also under the article Administering eye drops.

Contraindications

• Hypersensitivity
• Pregnancy
• For use in children and adolescents under 18 years of age or during lactation, no adequate data are available to date.

Women of childbearing age must use a safe method of contraception, as tafluprost may have adverse effects on the fetus. Patients should be made aware that eyelashes and iris pigmentation may change permanently during treatment. Full precautions can be found in the drug label.

Interactions

Not known to date. No CYPs are involved in metabolism to inactive metabolites. Latanoprost is known to cause a paradoxical increase in intraocular pressure with concomitant use of prostaglandin analogues.

Adverse effects

Adverse effects are comparable to those of other prostaglandin analogues. Very common:

• Increased blood flow to the conjunctiva or eyes, red eye.

Common:

• Changes in eyelashes (increase in length, thickness and number of eyelashes, discoloration), increased iris pigmentation, change in eye color, eyelid pigmentation, localized darkening of the skin
• Eye irritation, eye pain, dry eye, itching, foreign body sensation, eyelid redness, blurred vision, eye tearing, discharge from the eye, decrease in visual acuity, photophobia, swollen eyelids. Other less common ocular adverse effects.
• Headache