Tafluprost

Registered South African indications:

• Reduction of elevated intraocular pressure in open-angle glaucoma or ocular hypertension

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients

Cautions

• Pregnancy
• Women of childbearing age/potential (unless adequate contraceptive measures are in place)
• Breastfeeding
• Renal impairment
• Hepatic impairment
• Mixed coloured irises (blue-brown, grey-brown, yellow-brown and green-brown)
• Unilateral treatment (See additional prescribers points)
• Repeated contact with the skin surface (See additional prescribers points)
• Severe asthma
• Neovascular glaucoma
• Angle-closure glaucoma
• Narrow-angle glaucoma
• Congenital glaucoma
• Pigmentary glaucoma
• Pseudoexfoliative glaucoma
• Aphakia
• Pseudophakic patients with a torn posterior lens capsule or anterior chamber lenses
• Known risk factors for macular oedema (South African manufacturer recommendations)
• Known risk factors for cystoid macular oedema (International manufacturer recommendations)
• Known risk factors for iritis/uveitis
• May impair ability to drive and operate machinery (See additional prescribers points)

Forms avail. in SA and covered in this monograph: eed

Dosages below include:

• South African manufacturer recommendations
• International manufacturer recommendations

South African manufacturer recommendations

Reduction of elevated intraocular pressure in open-angle glaucoma or ocular hypertension

• Ophthalmic (eed): 1 drop in the conjunctival sac of the affected eye(s), dly in the evening

The dose should not be administered more than once daily as more frequent administration may lessen the intraocular pressure lowering effect

Tafluprost is a sterile solution that does not contain a preservative. For single use only, one container is sufficient to treat both eyes. Any unused solution should be discarded immediately after use

If more than one topical ophthalmic agent is being used, each one should be administered at least 5 minutes apart

International manufacturer recommendations

Reduction of elevated intraocular pressure in open-angle glaucoma and ocular hypertension
- As monotherapy in those who would benefit from preservative free eye drops or insufficiently responsive to first-line therapy or intolerant/ contraindicated to first-line therapy
- As adjunctive therapy to beta-blockers

• Ophthalmic (eed): 1 drop in the conjunctival sac of the affected eye(s), dly in the evening

The dose should not be administered more than once daily as more frequent administration may lessen the intraocular pressure lowering effect

If more than one topical ophthalmic medicinal agent is being used, each one should be administered at least 5 minutes apart

Not established for use in children below 18 years

Pregnancy
South African manufacturer recommendations

• Caution; positive evidence of risk in animal studies
• The safety of tafluprost in pregnant women has not been established. Embryotoxicity and teratogenic effects have been seen in animal studies
• Tafluprost should not be used in women of childbearing age/potential unless adequate contraceptive measures are in place

International manufacturer recommendations

• Caution; not recommended
• There are no adequate data from the use of tafluprost in pregnant women
• Tafluprost can have harmful pharmacologic effects on pregnancy and/or the foetus/newborn child. Studies in animals have shown reproductive toxicity. Therefore, tafluprost should not be used during pregnancy unless clearly necessary (in case no other treatment options are available)
• Tafluprost must not be used in women of childbearing age/potential unless adequate contraceptive measures are in place

Breastfeeding
South African manufacturer recommendations

• Caution; not recommended
• A study with radiolabeled tafluprost demonstrated that tafluprost and/or its metabolites were excreted in the milk of lactating rats
• It is not known whether tafluprost and/or its metabolites are excreted in human milk. Therefore, tafluprost should not be used during breastfeeding

International manufacturer recommendations

• Caution; not recommended
• It is unknown whether tafluprost and/or its metabolites are excreted in human milk. A study in rats has shown excretion of tafluprost and/or its metabolites in breast milk after topical administration. Therefore tafluprost should not be used during breastfeeding

Fertility 

• In female and male rats, mating performance and fertility was unaffected by intravenous tafluprost doses up to 100µg/kg/day

Renal Impairment

• Caution; no information available 
  Tafluprost has not been studied in patients with renal insufficiency and should therefore be used with caution in such patients

Hepatic Impairment

• Caution; no information available 
  Tafluprost has not been studied in patients with hepatic insufficiency and should therefore be used with caution in such patients

Elderly

• No dose adjustment recommended 

Porphyria Information 

• Not porphyrinogenic (NP) 

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders 

• Headache

Respiratory Disorders

• Exacerbation of asthma
• Dyspnoea

Skin and Subcutaneous Tissue Disorders 

• Hypertrichosis of eyelid

Sensory Disorders 

• Ocular hyperaemia
• Eye pruritus
• Eye irritation
• Eye pain
• Conjunctival/ocular hyperaemia
• Changes in eyelashes (increased length, thickness and number of lashes)
• Dry eye
• Foreign body sensation in eyes
• Eyelash discolouration
• Erythema of eyelid
• Superficial punctate keratitis (SPK)
• Photophobia
• Increased lacrimation
• Blurred vision
• Reduced visual acuity 
• Increased iris pigmentation
• Blepharal pigmentation
• Eyelid oedema
• Asthenopia
• Conjunctival oedema
• Eye discharge
• Blepharitis
• Anterior chamber cells
• Ocular discomfort
• Anterior chamber flare
• Conjunctival pigmentation
• Conjunctival follicles
• Allergic conjunctivitis 
• Abnormal sensation in eye
• Iritis/uveitis
• Deepened lid sulcus
• Macular oedema/cystoid macular oedema
• Corneal calcification 

No significant interactions

• Intraocular pressure

Additional observations

• Increased iris pigmentation

Unilateral treatment

• Before treatment is initiated, patients should be informed of the possibility of eyelash growth, darkening of the eyelid skin and increased iris pigmentation. Some of these changes may be permanent and may lead to differences in appearance between the eyes when only one eye is treated
• The change in iris pigmentation occurs slowly and may not be noticeable for several months. The change in eye colour has predominantly been seen in patients with mixed coloured irises, e.g. blue-brown, grey-brown, yellow-brown and green-brown. Unilateral treatment can result in permanent heterochromia

Repeated contact with the skin surface

• There is a potential for hair growth to occur in areas where tafluprost solution comes repeatedly in contact with the skin surface

Method of administration

• Patients should be informed of the correct handling of the bottle. When using for the first time, before delivering a drop to the eye, the patient should first of all practice using the bottle by squeezing it slowly to deliver one drop away from the eye. The patient should practice until being confident to deliver one drop at a time. Otherwise, the unpreserved alternative of the same medicinal product in single dose units may be more appropriate
• To prevent potential contamination of the solution, the patients should not touch their eyelids, surrounding areas or any other surfaces with the applicator tip of the bottle. The residual liquid remaining at the dropper tip after application of the eye drops should immediately be removed by shaking the bottle once downwards. The dropper tip should not be touched or wiped
• To reduce the risk of darkening of the eyelid skin the patients should wipe off any excess solution from the skin. As with any other eye drops, nasolacrimal occlusion or gently closing the eyelid after administration is recommended. This may reduce the systemic absorption of medicinal products administered via the ocular route
• There will be a residual volume of approximately 1ml, which cannot be dosed. The patient should not try to empty the bottle

Effects on ability to drive and use machines

• Tafluprost has minor influence on the ability to drive and use machines. If transient blurred vision occurs at instillation, the patient should wait until the vision clears before driving or using machinery

Tafluprost is a fluorinated analogue of prostaglandin F_2α. Tafluprost acid, the biologically active metabolite of tafluprost, is a highly potent and selective agonist of the human prostanoid prostaglandin F (FP) receptor. Tafluprost acid has a 12-fold higher affinity for the FP receptor than latanoprost. Pharmacodynamic studies in monkeys indicate that tafluprost reduces intraocular pressure by increasing the uveoscleral outflow of aqueous humour.

Ear/eye drops (per ml) 15µg

• Saflutan (Mundipharma) originator