Taflotan eye drops 0.0015% 0.3 ml N30
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Active ingredients
Tafluprost
Release form
Drops
Composition
1 ml of eye drops contains: active substances: tafluprost 15 μg; 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;
Pharmacological effect
Antiglaucoma drug, fluorinated prostaglandin F2 analog. ;Mechanism of action. 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 (IOP), increasing the uveoscleral outflow of aqueous humor.; Pharmacodynamic effect. Experiments on monkeys with normal and elevated IOP have shown that tafluprost is an effective drug to reduce 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 ophthalmologic tafluprost solution 0.0015% 1 time / day. nerve significantly (15%) increased compared with baseline, when measured on days 14 and 28 using laser speckle-fluography; Clinical effect. IOP reduction begins within 2-4 hours after the first installation of the drug, and the maximum effect is reached in about 12 hours. The effect lasts for at least 24 hours. Leading studies on the use of tafluprost containing the preservative benzalkonium chloride showed that tafluprost is effective as monotherapy, and also has an additive effect when used as an adjuvant therapy to timolol. The 6-month study showed a significant IOP-lowering effect of tafluprost at various time points during the day: from 6 to 8 mm Hg. Art., compared with latanoprost, reducing IOP by 7-9 mm Hg. st. In another 6-month clinical study, tafluprost reduced IOP by 5–7 mm Hg.Art., and timolol at 4-6 mm Hg. st. The IOP-lowering effect of tafluprost also persisted 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. st. in timolol-tafluprost group and 3-4 mm of mercury. st. - in the group of timolol-indifferent filler.; In a small cross-sectional study, with a 4-week treatment period, a similar IOP-lowering effect of the dosage forms with a preservative and without a preservative — more than 5 mm Hg was demonstrated. In a 3-month study in the United States, when comparing, the composition of tafluprost without preservative with timolol, also without preservative, it was found that tafluprost reduced IOP by 6.2-7.4 mm Hg. at different time points, while the values for timolol varied between 5.3 and 7.5 mm Hg;
Pharmacokinetics
Absorption; After installing eye drops tafluprost, 0.0015% in a tube-dropper, without 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 / min / ml) 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 a study in rabbits, absorption of tafluprost into aqueous humor, after a single installation of ophthalmic tafluprost, 0.0015% with preservative and without preservative was comparable .; Distribution; In the study of monkeys, no specific distribution of radioactively-labeled tafluprost was observed in the iris, ciliary body, or in the choroid,including the retinal pigment epithelium, indicating 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 glucuronide. 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 enzyme system cytochrome P450 (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.; Excretion; 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 doses were detected in feces. 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 ophthalmic hypertension as monotherapy in patients: - which are indicated with eye drops that do not contain a preservative; - with insufficient response to first-line drugs; - not carrying first-line drugs or having contraindications to these drugs.; As an additional therapy to beta-blockers. ; Tafluprost is intended for patients over 18 years old .;
Contraindications
Hypersensitivity to tafluprost or any of the inert fillers Taflotan;
Use during pregnancy and lactation
Data on the use of tafluprost in pregnant women is not enough. Tafluprost may have an adverse pharmacological effect on the course of pregnancy and / or on the fetus / newborn baby. In this regard, Taflotan should not be used during pregnancy, unless there are no other treatment options.; Women of childbearing age should not be prescribed Taflotan if they do not use adequate contraceptives.; It is not known whether tafluprost or its metabolites are excreted in breast milk in person. Taflotan should not be used during breastfeeding.; In experimental animal studies, the toxic effects of tafluprost on the reproductive system have been demonstrated. In a study on rats, it was found that after topical administration, tafluprost is excreted in breast milk. Fertility of female and male rats, mating ability and fertility remained unchanged with the introduction of tafluprost to 100 mcg / kg / day / v
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.; Only for single use . 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; In the treatment of elderly patients there is no need to change the dose.; Use in children and adolescents; Safety and efficacy of tafluprost in children and adolescents under the age of 18 years has not been established. No data available; Use in renal / liver dysfunctional; 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. Method of application; To reduce the risk of darkening of the eyelid skin, patients should remove excess solution from the skin. As with the application of other eye drops, nasolacrimal occlusion is recommended - a soft closing of the eyelids after the installation of the drug.This can reduce the systemic absorption of drugs administered through the eyes.; When using several local ophthalmic drugs, the intervals between their use should be at least 5 minutes;
Side effects
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 resulted in cessation of treatment in an average of 0.4% of patients. In a 3-month phase III study, in the USA, 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 United States after their maximum expansion for up to 24 months: Ophthalmic; Common (from> 1/100 to <1/10): eye itching, eye irritation, pain conjunctival / 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 not seeing, reduced visual acuity, and increased pigmentation of the iris.; Infrequently encountered (from> 1/1000 to <1/100): eyelid pigmentation, eyelid edema, asthenopia, conjunctival edema, appearance of discharge from the eyes, blepharitis, anterior chamber inflammation , discomfort in the eyes, anterior ocular chamber veins, conjunctival pigmentation, conjunctival follicles, allergic conjunctivitis, and an atypical sensation in the eye; Disturbances of the nervous system; Frequently occurring (from> 1/100 to <1/10): headache; Disorders skin and subcutaneous tissue; Infrequently meeting Esja (from> 1/1000 to <1/100): hypertrichosis century;
Overdose
Symptoms: There were no reports of overdose cases. After instillation of the drug in the eye overdose; unlikely. In case of overdose, treatment should be symptomatic;
Interaction with other drugs
No cross-interactions with other drugs should be expected, because after instillation of the drug in the eyes, the systemic concentrations of tafluprost are extremely low. No special studies have been carried out on the study of specific cross-interactions of tafluprost with other medical products. In clinical studies, tafluprost was applied simultaneously with timolol, and no signs of cross-interaction were observed;
special instructions
Before treatment, patients should be warned about 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 was treated. The change in the pigmentation of the iris occurs slowly and may remain imperceptible over several months. The change in eye color 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 life-long heterochromia is likely if only one eye is treated. There is no experience with tafluprost in cases of neovascular, angle-closure, narrow-angle or congenital glaucoma. There is only limited experience treatment tafluprost patient with aphakia, pigment or pseudoexfoliation glaucoma;. Recommended caution in the treatment tafluprost patient with aphakia, pseudophakia, damaged posterior capsule of the lens or lens anterior chamber or patients with established risk factors for cystoid macular edema 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 caution.; It has been reported that benzalkonium chloride, which is usually used as a preservative in ophthalmic preparations, causes pinpoint keratopathy and / or toxic ulcerative keratopathy. Since Taflotan contains benzalkonium chloride in vials, careful monitoring is necessary in cases of frequent or prolonged use in patients with dry eyes, as well as in cases where the cornea is at risk. Benzalkonium 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 drug and insert them again no earlier than 15 minutes after instillation.; Influence on the ability to drive vehicles 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;