Buy Taflotan eye drops 0.0015% 0.3 ml 30 pcs

Taflotan® [Tafluprost]

Brand Santen

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Available since: 2019-09-19

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Clinical Pharmacology

Tafluprost is a fluorinated prostaglandin F2α analogue. Tafluprost acid, being its biologically active metabolite, has a high activity and selectivity for human FP-prostanoid receptor. The affinity of tafluprost acid to the FP receptor is 12 times higher than the affinity of latanoprost. Pharmacodynamic studies on monkeys have shown that tafluprost reduces intraocular pressure, increasing uveoscleral outflow of aqueous humor.

Pharmacodynamic effect
Experiments on monkeys with normal and elevated intraocular pressure (IOP) have demonstrated that Tafluprost is an effective drug for reducing IOP. In a study on the IOP-lowering effect of tafluprost metabolites, it was found that only tafluprost acid significantly reduces IOP.
Studies on rabbits treated for 4 weeks with tafluprost ophthalmic solution, 0.0015%, once a day, showed that blood flow in the optic nerve head increased significantly (by 15%) compared to the initial level, when measured at 14 and 28 day using laser speckle flowgrafii.

Clinical effect
The reduction in intraocular pressure begins within 2-4 hours after the first installation of the drug, and the maximum effect is achieved in about 12 hours. The duration of the effect is maintained for at least 24 hours. Leading studies on the use of tafluprost containing the preservative benzalkonium chloride have shown that tafluprost is effective as a monotherapy, and also has an additive effect when used as an adjuvant therapy for timolol. In a 6-month study, tafluprost, at various time points during the day, demonstrated a significant IOP-lowering effect: from 6 to 8 mm Hg. Art., compared with latanoprost, reducing IOP by 7-9 mm Hg. In another 6-month clinical study, tafluprost reduced IOP by 5–7 mm Hg, and timolol by 4–6 mm Hg. Art. IOP-lowering effect of tafluprost remained the same with an increase in the duration of these studies to 12 months. In a 6-week study, the IOP-lowering effect of tafluprost was compared with the effect of its indifferent filler when used in conjunction with timolol. Compared with baseline (measured after 4 weeks of treatment with timolol), the additional IOP-lowering effect was 5-6 mm Hg. in timolol-tafluprost group and 3-4 mm Hg. in the group timolol-idifferentny filler. In a small cross-sectional study, with a 4-week treatment period, the dosage forms with and without preservative showed a similar IOP-lowering effect — more than 5 mmHg.
In addition, in a 3-month study in the United States when comparing, the composition of tafluprost without a preservative with timolol. also without preservative, it was found that tafluprost reduced IOP by 6.2-7.4 mm Hg. at different time points, whereas timolol values ranged between 5.3 and 7.5 mm Hg.

Pharmacokinetics
Absorption
After installing eye drops tafluprost, 0.0015% in a dropper tube, without a preservative, once a day one drop in both eyes for 8 days, its plasma concentrations were low and had a similar profile on day 1 and 8. Plasma concentrations reached a maximum 10 minutes after the installation, and decreased to a level lower than the lower detection limit (10 pg / ml) less than an hour after drug administration. The mean values of Cmax (26.2 and 26.6 pg / ml) and AUCo-last (394.3 and 431.9 pg / mIMl) were almost the same on days 1 and 8, which indicates that during the first week of treatment, stable drug concentration. No statistically significant differences in systemic bioavailability were found between dosage forms with preservative and without preservative.
In the study in rabbits, the absorption of tafluprost into the aqueous humor, after a single installation of the ophthalmic solution of tafluprost, 0.0015% with preservative and without preservative, was comparable.

Distribution
In a study of monkeys, there was no specific distribution of radioactively-labeled tafluprost in the iris, ciliary body or in the choroid, including the retinal pigment epithelium, which indicates a low affinity of the drug for the melanin pigment.
An autoradiographic study in rats showed that the highest concentration of radioactivity was observed in the cornea, followed by the eyelids, sclera and iris. Systematically, radioactivity extended to the lacrimal apparatus, the palate, the esophagus, the gastrointestinal tract, the kidneys, the liver, the gall bladder. In vitro binding of tafluprost acid to human serum albumin is 99% for 500 ng / ml tafluprost acid.

Biotransformation
The main metabolic pathway of tafluprost in the human body tested in vitro is hydrolysis to form a pharmacologically active metabolite, tafluprost acid, which is then metabolized by glucuronidation or beta-oxidation to form pharmacologically inactive 1,2-dinor and 1,2,3,4-tetranor tafluprost acids, which can be glucuronid or hydroxylated. The cytochrome P450 enzyme system (CYP) is not involved in the metabolism of tafluprost acid. In a study conducted on rabbit cornea with refined enzymes, it was found that carboxylesterase is the main esterase responsible for the ester hydrolysis of tafluprost acid. Butyrylcholinesterase, but not acetylcholinesterase, can also promote hydrolysis.

Removal
In a study in rats, after a single installation of 3H-tafluprost (0.005% ophthalmic solution, 5 μl / eye) 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 in the urine, and about 44-58%, with feces.

Indications

to reduce elevated intraocular pressure in patients with open-angle glaucoma and ophthalmohypertension;
as monotherapy in patients for whom eye drops that do not contain a preservative, or with insufficient response to first-line drugs, or who do not tolerate first-line drugs or have contraindications to these drugs;
as an additional therapy to beta blockers.

Composition

1 ml of eye drops contains:
active substances: tafluprost 15 mcg;
Excipients: glycerol - 22.5 mg, sodium hydrogen phosphate dihydrate - 2 mg, disodium edetate - 0.5 mg, polysorbate 80 - 0.75 mg, hydrochloric acid and / or sodium hydroxide (for pH correction), water d / and - up to 1 ml.

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Dosage and Administration

The recommended dose is one drop of Taflotan eye drops in the conjunctival sac of the affected eye (s) once a day, in the evening.
The dose should be installed strictly once a day, as more frequent use may reduce the effect of reducing intraocular pressure.
For single use only. The contents of one tube-dropper is enough for instillation in both eyes. The remaining drug should be discarded immediately after use.

Use in elderly patients
When treating elderly patients, there is no need to change the dose.

Use in children and adolescents
The safety and efficacy of tafluprost in children and adolescents under the age of 18 years has not been established. No data available.

Use in violation of the functions of the kidneys / liver
There have been no studies on the effects of tafluprost on patients with renal / hepatic disorders, so care should be taken when treating this category of patients.

Application method
To reduce the risk of darkening of the eyelid skin, patients should remove excess solution from the skin. As with the use of other eye drops, nasolacrimal occlusion is recommended - soft closing of the eyelids after the installation of the drug. This may reduce the systemic absorption of medications administered through the eyes.
When using several topical ophthalmic drugs, the intervals between their use should be at least 5 minutes.

Adverse reactions

In clinical studies, over 1400 patients were treated with tafluprost with a preservative - either as monotherapy or as an additional drug for treatment with timolol, 0.5%. The most frequently detected treatment-related side effect was eye flushing. It was observed in approximately 13% of patients who participated in clinical studies of tafluprost in Europe and the USA. In most cases, hyperemia was moderate, and led to cessation of treatment in an average of 0.4% of patients. In a 3-month phase III study, in the United States, when comparing, the composition of tafluprost 0.0015% without preservative, with timolol, also without preservative, eye hyperemia was observed in 4.1% (13/320) of patients who received Tafluprost. The following side effects associated with treatment were reported during Tafluprost clinical studies in Europe and the USA after their maximum expansion for up to 24 months:

Ophthalmic

Often found (from> 1/100 to <1/10): eye itch, eye irritation, eye pain, conjunctiva / eye hyperemia, eyelash changes (increase in length, thickness and number of eyelashes), dry eye syndrome, foreign body sensation in the eyes, change in eyelash color, eyelid erythema, superficial punctate keratitis, photophobia, increased tearing, blurred vision, reduced visual acuity, and increased pigmentation of the iris.

Infrequently occurring (from> 1/1000 to <1/100): eyelid pigmentation, eyelid edema, asthenopia, conjunctival edema, appearance of discharge from the eyes, blepharitis, inflammation of the anterior chamber, feeling of discomfort in the eyes, anterior chamber flair of the eye, conjunctival pigmentation, conjunctive fever, allergic conjunctivitis, and atypical.

Nervous system disorders

Often found (from> 1/100 to <1/10): headache

Violations of the skin and subcutaneous tissue

Infrequently occurring (from> 1/1000 to <1/100): eyelid hypertrichosis

Hypersensitivity to tafluprost or any of the inert fillers Taflotan.

Drug interactions

No cross-interactions with other drugs should be expected, because after instillation of the drug into the eyes, the system concentrations of tafluprost are extremely low. Special studies on the specific cross-interaction of tafluprost with other medical products have not been conducted.
In clinical studies, tafluprost was used simultaneously with timolol, and there were no signs of cross interactions.

Pregnancy and Lactation

Women with childbearing potential / contraception
Women with childbearing potential should not use Taflotan if they do not use adequate contraception.

Pregnancy
There is insufficient data on the use of tafluprost in pregnant women. Tafluprost may have an adverse pharmacological effect on the course of pregnancy and / or on the fetus / growth child. Animal studies have shown toxic effects on the reproductive system. In this regard, Taflotan should not be used during pregnancy, except in cases where there are no other treatment options.

Lactation
It is not known whether tafluprost or its metabolites penetrate human breast milk. In a rat study, excretion of tafluprost into breast milk was established after topical administration. Therefore, Taflotan should not be used during breastfeeding.

Fertility
In female and male rats, mating ability and fertility remained unchanged with the administration of tafluprost up to 100 mcg / kg / day intravenously.

Special instructions

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

Changes in the pigmentation of the iris occurs slowly and for several months may remain imperceptible. The color change is observed mainly in patients with iris of mixed colors, for example, if the eyes are brown-blue, gray-brown, yellow-brown or green-brown. The risk of a life-long heterochromia is likely if only one eye is treated.
There is no experience of using 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.
It is recommended that caution be taken when treating flofrost of patients with aphakia, artifakia, a damaged posterior lens capsule or anterior chamber lenses, or patients with established risk factors for developing cystic edema of the macular or iritis / uveitis.

There is no experience with the drug in patients with severe asthma. In this regard, patients in this group should be treated with composure.
It has been reported that benzalkonium chloride, which is usually used as a preservative in ophthalmic preparations, causes point keratopathy and / or toxic ulcerative keratopathy. Since Taflotan in flacons contains benzalkonium chloride, careful monitoring is required in cases of frequent or prolonged use in patients with dry eyes, as well as in cases where the cornea is at risk.
Benzalkoniya chloride can also cause eye irritation and discoloration of soft contact lenses. Contact of the drug with soft contact lenses should be avoided. Remove contact lenses before using the drugs and reinsert them no earlier than 15 minutes after instillation.

Influence on ability to drive motor transport and control mechanisms

Tafluprost does not affect the ability to drive a car and work with mechanisms. As with the use of any other ophthalmologic agents, a short-term blurred vision may occur after the installation of the drug. In this case, the patient must wait until the vision is fully restored, and only after that to drive a car or operate mechanical equipment.

Overdosage

Symptoms: there were no reports of overdose. After instillation of the drug in the eye, overdose is unlikely.
In case of overdose, treatment should be symptomatic.