Taflotan
Taflotan: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal and liver function
- 12. Drug interactions
- 13. Analogs
- 14. Terms and conditions of storage
- 15. Terms of dispensing from pharmacies
- 16. Reviews
- 17. Price in pharmacies
Latin name: Taflotan
ATX code: S01EE05
Active ingredient: tafluprost (Tafluprostum)
Manufacturer: Santen OY (Finland)
Description and photo update: 2018-08-07
Prices in pharmacies: from 711 rubles.
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Taflotan is an antiglaucoma agent, a miotic, an analogue of prostaglandin.
Release form and composition
Dosage form of Taflotan - eye drops: colorless transparent liquid (0.3 ml of solution in a dropper tube, 10 dropper tubes soldered together in an aluminum foil bag, 3 or 9 bags in a cardboard box).
Composition of 1 ml solution:
- active substance: tafluprost - 0.015 mg;
- auxiliary components: sodium hydrogen phosphate dihydrate, glycerol, polysorbate 80, disodium edetate, sodium hydroxide and (or) hydrochloric acid for pH correction, water for injection.
Pharmacological properties
Pharmacodynamics
Tafluprost is a fluorinated analogue of prostaglandin F2 a. The active metabolite of tafluprost is its acid, it is highly active and has a high selectivity in relation to the human FP-prostanoid receptor. The affinity of tafluprost acid for the FP receptor is 12 times higher than that of latanoprost. Studies carried out in monkeys have shown that tafluprost reduces intraocular pressure (IOP) by increasing the uveoscleral outflow of aqueous humor.
Experiments on monkeys with normal and increased IOP revealed the effectiveness of tafluprost in reducing IOP. Studies of the IOP-lowering effect of tafluprost metabolites have shown that only tafluprost acid significantly reduces IOP.
Studies carried out on rabbits, during which for 4 weeks they received daily (1 time per day) therapy with tafluprost 0.0015%, revealed a significant (15%) increase in blood flow in the optic nerve head in comparison with the baseline level when measured using laser speckle flowgraphy.
After the first installation of Taflotan, the IOP begins to decrease within 2–4 hours; the maximum effect is achieved after 12 hours and lasts for at least 1 day.
Studies on the use of tafluprost, containing benzalkonium chloride as a preservative, have revealed the efficacy of tafluprost both as monotherapy and when used in combination therapy with timolol. The study of tafluprost, conducted for 6 months, demonstrated a significant IOP-lowering effect (at different times of the day): 6-8 mm Hg. Art., while latanoprost reduced IOP by 7-9 mm Hg. Art.
In another clinical study, which lasted 6 months, tafluprost reduced IOP by 5–7 mm Hg. Art., and timolol - by 4-6 mm Hg. Art. The IOP-lowering effect of tafluprost persisted in studies conducted throughout the year. In a 6-week study, the therapeutic effect of tafluprost was compared to that of an indifferent filler when used in combination with timolol. In comparison with the initial values (taken after a 4-week course of timolol therapy), the additional IOP-lowering effect was 5–6 mm Hg. Art. when using tafluprost and 3-4 mm Hg. Art. when using an indifferent filler. According to the results of a 4-week cross-over study, the IOP-lowering effect of the drug with and without preservative was similar.
Also in a 3-month US study comparing preservative-free tafluprost versus timolol formulations, tafluprost was found to reduce IOP by 6.2-7.4 mm Hg. Art., and timolol - by 5.3-7.5 mm Hg. Art.
Pharmacokinetics
When using tafluprost 0.0015% 1 drop once a day in both eyes, its plasma concentration is low and similar on the 1st and 8th day. The maximum concentration of the drug in plasma is reached 10 minutes after installation, and in less than 1 hour it dropped below the detection limit (10 pg / ml). The average C max and AUCo-last values were also similar on the 1st and 8th day, which means that a stable concentration of the drug is achieved within the first week of therapy. There are no statistically significant differences in systemic bioavailability between preservative and non-preservative forms.
Studies carried out on rabbits have established the comparability of the absorption of tafluprost into aqueous humor after a single use of the drug with and without a preservative.
During the studies carried out on monkeys, the specific distribution of radioactively labeled tafluprost in the ciliary body, iris or in the choroid of the eye, including the retinal pigment epithelium, was not established, which indicates a low affinity of the drug for the melanin pigment.
An autoradiographic study in rats found that the highest level of radioactivity was observed in the cornea, then in the eyelids, sclera and iris. Radioactivity spread systemically to the lacrimal apparatus, palate, esophagus, gastrointestinal tract, kidneys, liver, gallbladder and bladder. The in vitro binding of tafluprost acid to human serum albumin is 99% for 500 ng / ml of tafluprost acid.
Tafluprost is metabolized in the body through hydrolysis, during which the pharmacologically active metabolite of tafluprost acid is formed. Then it is metabolized by beta-oxidation or glucuronidation to form inactive 1, 2-dinor- and 1, 2, 3, 4-tetranor-acids of tafluprost, which can be hydroxylated or glucuronidated. The cytochrome P450 (CYP) enzymatic system does not participate in the metabolism of tafluprost acid.
A study carried out on the tissues of the cornea of a rabbit with refined enzymes showed that the main esterase responsible for the ester hydrolysis of tafluprost acid is carboxylesterase. Butyrylcholinesterase (but not acetylcholinesterase) can also promote hydrolysis.
In a study on rats, after a single instillation of ZN-tafluprost (0.005% ophthalmic solution, 5 μl / eye) in both eyes for 21 days, about 87% of the total radioactive dose was found in excrement. Approximately 27–38% of the total dose was excreted in the urine, and about 44–58% in the feces.
Indications for use
According to the instructions, Taflotan is indicated for lowering IOP in patients over 18 years of age with ophthalmic hypertension and open-angle glaucoma.
Monotherapy with Taflotan is recommended for patients who are shown preservative-free eye drops, who have contraindications to first-line drugs, cannot tolerate these drugs, as well as those who have an insufficient response to them.
The drug is recommended in combination therapy with beta-blockers.
Contraindications
Increased sensitivity to any of the components of Taflotan.
Instructions for the use of Taflotan: method and dosage
Eye drops Taflotan are recommended to be instilled once a day in the evening, 1 drop into the conjunctival sac of the affected eye / eyes.
Do not install the drug more often than 1 time per day, as this can reduce the effect of lowering IOP.
The solution in one dropper tube is sufficient for instillation in both eyes; unused solution cannot be stored, it is recommended to throw it away after use.
Remains of the drug should be removed from the skin to reduce the risk of darkening of the eyelids. After the installation of Taflotan, as well as other eye drops, nasolacrimal occlusion is recommended - soft closing of the eyelids; this can reduce systemic absorption of ophthalmic drugs.
In cases where it is necessary to use several topical ophthalmic preparations, they should be used with an interval of at least 5 minutes.
Side effects
During clinical trials of tafluprost with a preservative (as monotherapy or as part of a combination therapy with timolol 0.5%), conducted with the participation of more than 1400 patients, the most common side effect was eye flushing. It was observed in about 13% of patients. Hyperemia in most cases was moderate, discontinuation of therapy was required only in 0.4% of patients. In a 3-month phase III study in the United States, comparing preservative-free formulations of tafluprost 0.0015% and timolol, eye flushing was observed in 4.1% of patients receiving Taflotan.
The following side effects have been identified in clinical trials of tafluprost in Europe and the United States after their maximum expansion to 2 years:
- organs of vision: often - dry eyes, irritation, pain, itching in the eyes, hyperemia of the conjunctiva / eyes, changes in eyelashes (increase in thickness, length and number of eyelashes), discoloration of eyelashes, sensation of a foreign body in the eyes, erythema of the eyelids, superficial punctate keratitis, increased tearing, photophobia, blurred vision, decreased visual acuity, increased pigmentation of the iris; infrequently - a feeling of discomfort in the eyes, the appearance of discharge from the eyes, blepharitis, pigmentation and edema of the eyelids, edema of the conjunctiva, asthenopia, inflammation or fleur of the anterior chamber of the eye, pigmentation of the conjunctiva, conjunctival folliculitis, allergic conjunctivitis and atypical sensation in the eye;
- nervous system: often - headache;
- skin and subcutaneous tissue: infrequently - eyelid hypertrichosis.
Overdose
There are no reports of overdose cases. When using Taflotan according to the instructions for use, an overdose is unlikely; if it does occur, symptomatic treatment is recommended.
special instructions
The use of Taflotan eye drops can lead to darkening of the eyelid skin, excessive eyelash growth, as well as increased pigmentation of the iris. Some of these changes may be permanent; if the drug is instilled into one eye, this may cause differences in the appearance of the eyes.
The change in the pigmentation of the iris is slow and may not be noticeable for several months. Changes in eye color are especially noticeable in patients with mixed-color irises. When treating one eye, there is a risk of developing persistent heterochromia.
There is no experience of using tafluprost in cases of angle-closure, narrow-angle, neovascular or congenital glaucoma. There is limited experience with the use of Taflotan in patients with pigmentary or pseudoexfoliative glaucoma and aphakia. It is recommended to use the drug with caution in patients with risk factors for the development of cystic macular edema, iritis / uveitis, as well as with aphakia, pseudophakia, damage to the posterior lens capsule or implantation of the lens into the anterior chamber of the eye.
There is no data on the use of tafluprost in patients with severe asthma, and therefore the use of Taflotan in this group of patients requires caution.
For women of childbearing age, it is recommended to use Taflotan only in case of reliable contraception.
In studies carried out on rats, tafluprost did not affect their ability to mate (in both males and females).
Application during pregnancy and lactation
There is no sufficient data on the use of Taflotan in pregnant women. Tafluprost can have an adverse effect on the course of pregnancy, as well as on the fetus or newborn. Animal studies have shown toxic effects on the reproductive system, so the use of Taflotan during pregnancy is contraindicated, unless there are no other treatment options.
There is no data on whether tafluprost (or its metabolites) is able to pass into human breast milk. Experiments on rats have established its excretion in breast milk after topical application. In connection with the above, Taflotan is contraindicated during lactation.
Pediatric use
There is no available data on the safety and efficacy of Taflotan in persons under the age of 18.
In case of impaired renal and liver function
The effect of Taflotan on patients with kidney and liver disorders has not been studied, therefore, patients belonging to these categories should be careful when using it.
Drug interactions
The concentration of tafluprost in the systemic circulation is low, and therefore cross-interactions with other drugs are not expected; therefore, no special studies of the interaction of the drug with other drugs have been carried out.
When using tafluprost in conjunction with timolol, there were no signs of interaction.
Analogs
There is no information about the analogues of Taflotan.
Terms and conditions of storage
Store at 2-8 ° C, keep out of the reach of children. After opening the bag with the dropper tube, it is recommended to store them in the bag at temperatures up to 25 ° C for no more than 4 weeks. After a single use, the dropper tube should be discarded along with the rest of the solution.
Shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Taflotan
There are no reviews about Taflotan.
Price for Taflotan in pharmacies
Approximate price for Taflotan (0.0015%, 0.3 ml, 30 pcs.) - 920 rubles.
Taflotan: prices in online pharmacies
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Drug name Price Pharmacy |
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Taflotan 0.0015% eye drops 0.3 ml 30 pcs. 711 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
