Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
An antiglaucoma agent, a fluorinated analogue of prostaglandin F 2? . The acid of tafluprost, being its biologically active metabolite, has a high activity and selectivity for the human FP-prostanoid receptor. The affinity of tafluprost acid for the FP receptor is 12 times higher than the affinity of latanoprost. Tafluprost lowers intraocular pressure, increasing the outgrowth of watery moisture. Promotes increased blood flow in the optic disc.
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 on days 1 and 8. C max in plasma was achieved 10 min after instillation and decreased to a level lower than the lower limit of detection (10 pg / ml) in less than 1 h after instillation. The average 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 the same for 1 and 8 days.
An autoradiography study in rats showed that the highest concentration of radioactivity was observed in the cornea, a lower concentration in the eyelids, sclera, and iris. There was a systematic spread of radioactivity - to the tear apparatus, the sky, the esophagus, the gastrointestinal tract, the kidneys, the liver, the bile and the bladder. The binding of tafluprost at a concentration of 500 ng / ml with human serum albumin in vitro is 99%.
The main way of metabolism of tafluprost in the human body, in vitro, is hydrolysis with the formation of a pharmacologically active metabolite, tafluprost acid, which is then masturbated by glucuronization or beta oxidation to form pharmacologically inactive 1,2-dinor and 1,2,3,4-tetranor tafluprost acids, which can be glucuronated or hydroxylated. The enzymatic system of cytochrome P450 does not participate in the metabolism of tafluprost acid. It has been established that carboxyl esterase is the main esterase responsible for ether hydrolysis of tafluprost acid. Butyrylcholinesterase, but not acetylcholinesterase, can also promote hydrolysis.
In a study in rats, after a single instillation of 3H-tafluprost in both eyes for 21 days, about 87% of the total radioactive dose was detected in feces. About 27-38% of the total dose was excreted in the urine, with feces about 44-58%.
INDICATIONS
To reduce the 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 do not tolerate first-line drugs or who have contraindications to these drugs; as an additional therapy for beta-blockers.
DOSING MODE
Bury in the lower conjunctival sac of the affected eye 1 time / day, in the evening.
SIDE EFFECT
From the side of the organ of vision: often - itchy eyes, 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, erythema eyelids, superficial dot keratitis, photophobia, increased teardrop, blurred vision, decreased visual acuity, and increased iris pigmentation; infrequent - eyelid pigmentation, eyelid edema, asthenopia, edema of the conjunctiva, the appearance of the discharge from the eyes, blepharitis, inflammation of the anterior chamber, a feeling of discomfort in the eyes, the anterior chamber of the eye, conjunctival pigmentation, conjunctival follicles, allergic conjunctivitis, atypical sensation in the eye, hypertrichosis .
From the nervous system: often - a headache.
CONTRAINDICATIONS
Hypersensitivity to tafluprost.
PREGNANCY AND LACTATION
Do not use tafluprost during pregnancy, except in cases of extreme necessity.
Women of childbearing age in the period of treatment should use reliable contraception.
Tafluprost may 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).
Pre-clinical studies in animals have shown that tafluprost has a toxic effect on the reproductive system. In female and male rats, mating ability and fertility remained unchanged with iv administration of tafluprost up to 100 mcg / kg / day. In studies on rats it was found that after topical application tafluprost is excreted in breast milk.
SPECIAL INSTRUCTIONS
Before the treatment, patients should be warned about the possibility of excessive growth of eyelashes, darkening of the skin of the eyelids 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 has been treated.
The change in iris pigmentation is slow and may not be noticeable for several months. The change in eye color is observed mainly in patients with iridescent colors of mixed colors, for example, if the eyes are brownish-blue, gray-brown, yellow-brown or green-brown. Treatment of only one eye can lead to persistent heterochromia.
There is no experience with tafluprost in cases of neovascular, occlusive, narrow-angle or congenital glaucoma. There is only limited experience in the treatment of tafluprost patients with aphakia, pigmentary or pseudoexfoliation glaucoma.
Caution should be exercised in treating tafluprost patients with aphakia, artifacts damaged by the posterior lens capsule, or lens implantation in the anterior chamber of the eye, as well as patients with established risk factors for cystoid macular edema or iritis / uveitis.
Experience with tafluprost in patients with severe bronchial asthma is not available, so this category of patients requires caution.
Impact on the ability to drive vehicles and manage mechanisms
Tafluprost does not affect the ability to drive vehicles and work with machinery. As with any other ophthalmic device, a brief blurring of vision may occur after instillation. In this case, the patient should wait until the vision is fully restored, and only then drive the vehicle or operate mechanical equipment.
