Taflopress drops 0.015mg / ml, 2.5ml

• To reduce increased intraocular pressure in patients with open-angle glaucoma and ophthalmic hypertension;

• as monotherapy in patients with insufficient response to first-line drugs, or who cannot tolerate first-line drugs or have contraindications to these drugs;

• as an adjunct therapy to beta-blockers.

Buried in the lower conjunctival sac of the affected eye 1 time / day, in the evening.

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

1 ml tafluprost 15 mcg

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

Hypersensitivity to tafluprost.

pharmachologic effect

Antiglaucoma agent, fluorinated analogue of prostaglandin F2 ?. The acid of tafluprost, 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 increasing the uveoscleral outflow of aqueous humor. Promotes increased blood flow in the optic nerve head.

Pharmacokinetics

After instillation of tafluprost in the appropriate dosage form 1 time / day in both eyes for 8 days, its plasma concentrations were low and had a similar profile at 1 and 8 days. Cmax in plasma was reached 10 min after instillation and decreased to a level lower than the lower detection limit (10 pg / ml) in less than 1 hour after instillation. The average values ??of Cmax (26.2 and 26.6 pg / ml) and AUC0-last (394.3 and 431.9 pg / min / ml) were almost the same at 1 and 8 days. An autoradiographic study in rats showed that the highest concentration of radioactivity was observed in the cornea, less high in the eyelids, sclera and iris. There was a systemic spread of radioactivity - to the lacrimal apparatus, palate, esophagus, gastrointestinal tract, kidneys, liver, gallbladder and bladder.The binding of tafluprost at a concentration of 500 ng / ml with human serum albumin in vitro is 99%. The main metabolic pathway of tafluprost in the human body, n in vitro is hydrolysis with the formation of a pharmacologically active metabolite, tafluprost acid, which is then stabolized by glucuronization or beta-oxidation with the formation of pharmacologically inactive 1,2-dinor and 1,2,3,4-tetranor tafluprost acids, which can be glucuronidated or hydroxylated. The enzymatic system of cytochrome P450 is not involved in the metabolism of tafluprost acid. It was found that the main esterase responsible for the ester hydrolysis of tafluprost acid is carboxylesterase. Butyrylcholinesterase, but not acetylcholinesterase, can also promote hydrolysis. In a rat study,after a single instillation of 3H-tafluprost in both eyes for 21 days, about 87% of the total radioactive dose was detected in excrement. About 27-38% of the total dose was excreted with urine, with feces - about 44-58%.

Side effect

From the side of the organ of vision: often - itching of the eyes, eye irritation, eye pain, hyperemia of the conjunctiva / eyes, changes in eyelashes (increase in length, thickness and number of eyelashes), dry eye syndrome, sensation of a foreign body in the eyes, discoloration of eyelashes, erythema of the eyelids, superficial punctate keratitis, photophobia, increased lacrimation, blurred vision, decreased visual acuity, and increased pigmentation of the iris; infrequently - eyelid pigmentation, eyelid edema, asthenopia, conjunctival edema, discharge from the eyes, blepharitis, anterior chamber inflammation, discomfort in the eyes, anterior chamber flare, conjunctival pigmentation, conjunctival follicles, allergic conjunctivitis, atypical sensation in the eyelid ... From the nervous system: often - headache.

Application during pregnancy and lactation

Tafluprost should not be used during pregnancy unless absolutely necessary. Women of childbearing age should use reliable contraception during treatment. Tafluprost can have an adverse pharmacological effect on the course of pregnancy and / or on the fetus and newborn baby. It is not known whether tafluprost or its metabolites are excreted in human milk. Therefore, tafluprost should not be used during lactation (breastfeeding). In preclinical studies in animals, it has been shown that tafluprost has a toxic effect on the reproductive system. In female and male rats, the ability to mate and fertility remained unchanged with intravenous administration of tafluprost up to 100 ?g / kg / day. In studies on rats, it has been foundthat after topical application, tafluprost is excreted in breast milk.

special instructions

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 can be permanent and can lead to differences in the appearance of the eyes if only one eye has been treated. The change in the pigmentation of the iris is slow and may not be noticeable for several months. Eye discoloration occurs predominantly in patients with mixed-colored irises, for example, if the eyes are blue-brown, gray-brown, tan, or green-brown. Treatment of only one eye can lead to persistent heterochromia. There is no experience of using tafluprost in cases of neovascular, closed-angle, narrow-angle or congenital glaucoma.There is only limited experience in the treatment of patients with aphakia, pigmentary or pseudoexfoliative glaucoma with tafluprost. Caution is advised when treating tafluprost in patients with aphakia, pseudophakia, damaged posterior lens capsule or lens implantation into the anterior chamber of the eye, as well as in patients with established risk factors for developing cystic macular edema or iritis / uveitis. There is no experience of using tafluprost in patients with severe bronchial asthma, therefore, this category of patients requires caution.as well as patients with established risk factors for developing cystic macular edema or iritis / uveitis. There is no experience with the use of tafluprost in patients with severe bronchial asthma, therefore, caution is required in this category of patients.as well as patients with established risk factors for developing cystic macular edema or iritis / uveitis. There is no experience with the use of tafluprost in patients with severe bronchial asthma, therefore, caution is required in this category of patients.

Influence on the ability to drive vehicles and use mechanisms

Tafluprost does not affect the ability to drive vehicles and work with mechanisms. As with any other ophthalmic agent, short-term blurred vision may occur after instillation. In this case, the patient must wait until vision is fully restored, and only then drive a vehicle or operate mechanical equipment.