Taflopress Rompharm (Drops) Instructions for Use

Marketing Authorization Holder

S.C. Rompharm Company S.R.L. (Romania)

ATC Code

S01EE05 (Tafluprost)

Active Substance

Tafluprost (Rec.INN registered by WHO)

Dosage Form

Taflopress Rompharm

Eye drops 15 mcg/ml: bottle 2.5 ml with dropper cap

Dosage Form, Packaging, and Composition

Eye drops in the form of a colorless, transparent solution.

Excipients: disodium edetate – 0.5 mg, glycerol – 18 mg, boric acid – 5 mg, tyloxapol – 1.5 mg, polyquaternium-1 – 0.01 mg, 1M hydrochloric acid solution or 1M sodium hydroxide solution – to adjust pH to 6.0±0.1, purified water – up to 1 ml.

2.5 ml – polymer bottles with a capacity of 5 ml (1) with a dropper cap – cardboard packs.

Clinical-Pharmacological Group

Antiglaucoma drug – synthetic prostaglandin F2α analogue

Pharmacotherapeutic Group

Drugs used in ophthalmology; antiglaucoma drugs and miotic agents; prostaglandin analogues

Pharmacological Action

Antiglaucoma agent, a fluorinated analogue of prostaglandin F_2α. Tafluprost acid, being its biologically active metabolite, has high activity and selectivity for the human FP prostanoid receptor. The affinity of tafluprost acid for the FP receptor is 12 times higher than that of latanoprost. Tafluprost reduces intraocular pressure by enhancing uveoscleral outflow of aqueous humor. It promotes increased blood flow in the optic nerve head.

Pharmacokinetics

After instillation of tafluprost in the appropriate dosage form once daily into both eyes for 8 days, its plasma concentrations were low and had a similar profile on days 1 and 8. C_max in plasma was reached 10 minutes after instillation and decreased to a level below the lower limit of detection (10 pg/ml) in less than 1 hour after instillation. The mean values of C_max (26.2 and 26.6 pg/ml) and AUC_0-last (394.3 and 431.9 pg/min/ml) were almost identical on days 1 and 8.

An autoradiographic study in rats showed that the highest concentration of radioactivity was observed in the cornea, with lower concentrations in the eyelids, sclera, and iris. Systemic distribution of radioactivity was observed – to the lacrimal apparatus, palate, esophagus, gastrointestinal tract, kidneys, liver, gallbladder, and urinary bladder. The binding of tafluprost at a concentration of 500 ng/ml to human serum albumin in vitro is 99%.

The main pathway of tafluprost metabolism in the human body, in vitro, is hydrolysis to form the pharmacologically active metabolite, tafluprost acid, which is then metabolized via glucuronidation or beta-oxidation to form pharmacologically inactive 1,2-dinor and 1,2,3,4-tetranor tafluprost acids, which may undergo glucuronidation or hydroxylation. The cytochrome P450 enzyme system is not involved in the metabolism of tafluprost acid. It has been established that the main esterase responsible for the ester hydrolysis of tafluprost acid is carboxylesterase. Butyrylcholinesterase, but not acetylcholinesterase, may also contribute to hydrolysis.

In a study in rats, after a single instillation of 3H-tafluprost into both eyes over 21 days, about 87% of the total radioactive dose was detected in the excreta. Approximately 27-38% of the total dose was excreted in the urine, and about 44-58% in the feces.

Indications

For the reduction of elevated intraocular pressure in patients with open-angle glaucoma and ocular hypertension; as monotherapy in patients with insufficient response to first-line therapy drugs, or who are intolerant to first-line drugs or have contraindications to these drugs; as additional therapy to beta-blockers.

ICD codes

Dosage Regimen

Instill one drop into the lower conjunctival sac of the affected eye(s) once daily, in the evening.

Administer the drops at approximately the same time each day to maintain consistent therapeutic effect.

If using more than one topical ophthalmic product, administer them at least 5 minutes apart.

To prevent contamination, avoid contact between the dropper tip and the eye, eyelids, or any other surface.

Close the bottle immediately after use.

Do not exceed the prescribed dosage; more frequent administration may decrease the intraocular pressure-lowering effect.

If a dose is missed, apply it as soon as possible on the same day; if it is the next day, skip the missed dose and resume the usual dosing schedule.

The maximum recommended dose is one drop in the affected eye(s) once every 24 hours.

Treatment is long-term; continue therapy as directed by a physician.

Regular monitoring of intraocular pressure is required to assess therapeutic response.

Adverse Reactions

Ophthalmic disorders common – eye itching, eye irritation, eye pain, conjunctival/eye hyperemia, changes in eyelashes (increased length, thickness, and number), dry eye syndrome, foreign body sensation in the eyes, eyelash discoloration, eyelid erythema, superficial punctate keratitis, photophobia, increased lacrimation, blurred vision, decreased visual acuity, and increased iris pigmentation; uncommon – eyelid pigmentation, eyelid edema, asthenopia, conjunctival edema, eye discharge, blepharitis, anterior chamber inflammation, eye discomfort, anterior chamber flare, conjunctival pigmentation, conjunctival follicles, allergic conjunctivitis, atypical eye sensation, eyelid hypertrichosis.

Nervous system disorders common – headache.

Contraindications

Hypersensitivity to tafluprost.

Use in Pregnancy and Lactation

Tafluprost should not be used during pregnancy, except in cases of extreme necessity.

Women of childbearing potential should use reliable contraceptive methods during treatment.

Tafluprost may have an adverse pharmacological effect on the course of pregnancy and/or on the fetus and newborn.

It is not known whether Tafluprost or its metabolites are excreted in human breast milk. Therefore, Tafluprost should not be used during lactation (breastfeeding).

In preclinical studies in animals, it was shown that Tafluprost has a toxic effect on the reproductive system. In female and male rats, mating ability and fertility remained unchanged with intravenous administration of tafluprost up to 100 mcg/kg/day. Studies in rats have established that after topical application, Tafluprost is excreted in breast milk.

Special Precautions

Before starting treatment, patients should be warned about the possibility of excessive eyelash growth, darkening of the eyelid skin, and increased pigmentation of the iris. Some of these changes may be permanent, and this may lead to differences in the appearance of the eyes if only one eye is treated.

Changes in iris pigmentation occur slowly and may remain unnoticeable for several months. Eye color change is observed mainly in patients with irises of mixed colors, for example, if the eyes are brown-blue, gray-brown, yellow-brown, or green-brown. Treatment of only one eye may lead to permanent heterochromia.

There is no experience with the use of tafluprost in cases of neovascular, angle-closure, narrow-angle, or congenital glaucoma. There is only limited experience in treating patients with aphakia, pigmentary, or pseudoexfoliative glaucoma with tafluprost.

Caution is recommended when treating patients with aphakia, pseudophakia, a damaged posterior lens capsule, or anterior chamber lens implantation, as well as patients with established risk factors for the development of cystoid macular edema or iritis/uveitis with tafluprost.

There is no experience with the use of tafluprost in patients with severe bronchial asthma, so caution is required in this category of patients.

Effect on the ability to drive vehicles and operate machinery

Tafluprost does not affect the ability to drive vehicles and operate machinery. As with the use of any other ophthalmic agents, temporary blurred vision may occur after instillation. In this case, the patient should wait until vision is completely restored before driving a vehicle or operating mechanical equipment.

Storage Conditions

Store at 2°C (36°F) to 8°C (46°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.