Tafluprost: prostaglandin analogue for lowering intraocular pressure

Tafluprost (brand names Saflutan, Taflotan) is a prostaglandin F2 alpha analogue used to lower intraocular pressure in glaucoma and ocular hypertension. A particular feature is its preservative free formulation, which makes it especially suitable for patients with sensitive ocular surface or chronic use of multiple eye drops. Tafluprost has been licensed in the EU since 2008.

Compared with other prostaglandin analogues such as latanoprost, bimatoprost and travoprost, tafluprost lowers intraocular pressure with comparable efficacy by about 20 to 30 %. It is available as single dose units and in multidose bottles with a special preservative free system.

Mechanism of action

Tafluprost is a prodrug that is hydrolysed in the cornea to its free acid. The free acid is a selective agonist at the prostaglandin FP receptor. Activation of these receptors increases the uveoscleral outflow of aqueous humour while leaving normal trabecular outflow unchanged. This lowers intraocular pressure.

The effect begins after 2 to 4 hours, with maximum effect reached after 12 hours. Once daily evening dosing produces stable pressure values over 24 hours.

Unlike beta blockers such as timolol, tafluprost has no systemic cardiovascular or pulmonary effects and is therefore also suitable for patients with asthma or heart failure.

Indications

• Primary open angle glaucoma (POAG): standard indication
• Ocular hypertension: elevated intraocular pressure without proven glaucomatous damage
• Pseudoexfoliation syndrome with raised intraocular pressure
• Pigment dispersion glaucoma
• Off label or as reserve therapy: in other glaucoma forms

Tafluprost is not suitable for the treatment of acute glaucoma attacks; other agents (acetazolamide, mannitol, pilocarpine) are required.

Dosing and administration

Standard dose: 1 drop once daily in the evening into the conjunctival sac of the affected eye (or both eyes).

Application:

• Wash hands, remove contact lenses
• Tilt head slightly back, gently pull down the lower lid
• Drop one drop directly into the conjunctival sac without touching the eye or lashes with the tip
• Close the eye, press the tear duct at the inner corner with a finger for 1 to 2 minutes (reduces systemic absorption)
• Reinsert contact lenses no earlier than 15 minutes later

If the patient uses several eye drops, allow at least 5 minutes between different agents.

Adverse effects

Very common: conjunctival hyperaemia (eye redness), particularly pronounced in the first weeks and usually subsiding.

Common: ocular pruritus, burning, stinging, foreign body sensation, increased tearing, lid irritation, transiently blurred vision, lid pigmentation, lash changes with lengthening, thickening and darkening.

Uncommon: iris hyperpigmentation (especially in green or light brown eyes), periorbital changes with deepening of the lid sulcus, cystoid macular oedema (very rare).

Rare: asthma worsening, dyspnoea, periocular rash, iritis, uveitis (mainly in predisposed patients).

Important points:

• Iris hyperpigmentation is usually permanent and cosmetically relevant, particularly with unilateral use and a different eye colour
• Periorbital changes with deepening of the lid sulcus may be cosmetically disturbing and are often visible only after months
• Lash changes are sometimes welcomed (longer and denser) and sometimes not
• The preservative free profile makes tafluprost attractive in dry eye and under multiple ophthalmic therapies

Interactions

• Other eye drops: separate use by at least 5 minutes
• Other pressure lowering agents: additive effect, often clinically sensible
• Latanoprost and other prostaglandin analogues: do not use simultaneously, as additive effect is small and paradoxical effects have been described

Special considerations

Pregnancy: not recommended because of limited data and theoretical uterotonic potential of prostaglandins.

Breastfeeding: not recommended.

Children: experience limited, not approved in the EU for children.

Asthma and respiratory disease: theoretically safe but observe with pre existing severe asthma symptoms.

IOP control: regularly, particularly in the first weeks after start and every 3 to 6 months thereafter.

Iris hyperpigmentation: inform before therapy, particularly with unilateral use. The change is usually slowly progressive and not reversible after stopping.

Patient communication: realistic expectations about effect (pressure lowering 20 to 30 %), adverse events (lash changes, iris hyperpigmentation) and the importance of consistent daily use. Glaucoma is a chronic disease whose treatment success depends on adherence.

Related substances

• Latanoprost, classical prostaglandin analogue
• Bimatoprost, another prostaglandin analogue
• Pilocarpine, cholinomimetic in glaucoma
• Aflibercept, intravitreal in AMD and DME

Frequently asked questions

Sources

• EMA European Medicines Agency
• BfArM German Federal Institute for Drugs and Medical Devices
• AWMF guidelines glaucoma
• Gelbe Liste tafluprost monograph