Travoprost

Pharmacological properties

Travoprost, an analogue of prostaglandin f2α, is its complete selective agonist, with a high degree of affinity for prostaglandin fp receptors, reduces intraocular pressure (IOP), increasing the outflow of intraocular fluid along the trabecular meshwork and the uveoscleral pathway. a decrease in IOP in a person begins about 2 hours after the use of the drug, and the maximum effect is achieved after 12 hours. A significant decrease in IOP with a single dose can be maintained for 24 hours.

Pharmacokinetics Travoprost refers to essential prodrugs. It is absorbed through the cornea, where isopropyl ether is hydrolyzed to the active free acid.

WITH_max in blood plasma is achieved 30 minutes after topical application and is ≤25 pg / ml. Rapidly excreted from blood plasma, within 1 h, the concentration decreases below the detection threshold (10 pg / ml).

Metabolism is the main pathway for eliminating travoprost and travoprost free acid. The pathways of systemic metabolism are parallel to the pathways of metabolism of endogenous prostaglandin F_2α and are characterized by the reduction of the 13–14 double bond, the oxidation of the 15-hydrogen group and the P-oxidative cleavage of the upper side chain link. Travoprost free acid and its metabolites are mainly excreted by the kidneys.

Dose adjustment for patients with impaired liver function (from mild to severe), as well as for persons with impaired renal function from mild to severe (creatinine clearance of 14 ml / min) is not required.

Indications

Decreased IOP in patients with ocular hypertension or open-angle glaucoma.

Application

For topical use.

Use in adults, including elderly patients. 1 drop of r. Daveris in the conjunctival sac of the affected eye 1 r / day. The optimal effect is achieved with a dose in the evening.

After instillation, nasolacrimal occlusion or eyelid cover is recommended. This reduces the systemic absorption of drugs injected into the eyes, which can reduce the likelihood of systemic side effects.

When using more than one local ophthalmic agent, the interval between their use should be ≥5 min (see INTERACTIONS).

If you miss an appointment, you must continue treatment from the next scheduled appointment. The daily dose should not exceed 1 drop in the affected eye 1 time per day.

When replacing another ophthalmic anti-glaucoma agent with Daveris, it is recommended to discontinue the use of the displaced drug with the subsequent use of Daveris the next day.

Use for impaired liver and kidney function. There is no need for dose adjustment.

To prevent contamination of the dropper tip and the solution, you must be careful not to touch the eyelid, adjacent areas or other surfaces with the tip of the dropper bottle.

Children. The safety and effectiveness of the drug in patients aged 18 years have not been established, therefore, the drug should not be used in this category of patients.

Contraindications

Hypersensitivity to the active substance or other components of the drug.

Side effects

The frequency of adverse reactions: very often (≥1 / 10), often (≥1 / 100 to 1/10), infrequently (from ≥1 / 1000 to 1/100) and rarely (from ≥1 / 10,000 to 1/1000 )

Infections and infestations. Infrequently: herpes simplex, herpetic keratitis.

From the immune system. Infrequently: hypersensitivity, hypersensitivity to the drug, seasonal allergies.

From the nervous system. Infrequently: visual field disturbances, headache. Rarely: dizziness, dysgeusia.

Ophthalmic disorders. Very often: conjunctival hyperemia, hyperemia of the eye.Often: eye pain, itchy eyes, dryness, eye irritation, iris hyperpigmentation, discomfort in the eye, precipitates in the anterior chamber of the eye, opalescence in the anterior chamber of the eye, abnormal eye sensitivity, foreign body sensation in the eye, swelling of the eyelids. Infrequently: corneal erosion, punctate keratitis, keratitis, iritis, decreased visual acuity, conjunctivitis, inflammation in the anterior chamber of the eye, blepharitis, blurred vision, photophobia, cataracts, periorbital edema, itching of the eyelids, discharge from the eye, the formation of scales along the edges of the eyelids, increased lacrimation, erythema of the eyelids, eyelash growth, macular degeneration, swelling of the eyes, staining of the cornea, photopsia, defect in the corneal epithelium, the appearance of a halo around the light source, corneal pigmentation, allergic conjunctivitis, conjunctival disorders, meibomeitis, ectropion, dry keratoconjunctivitis, dry eye syndrome, pigment dispersion syndrome, eyelid pain, dark circles under the eyes, disorders of the eyelids, hyperemia of the sclera. Rarely: uveitis, iridocyclitis, the occurrence of conjunctival follicles, conjunctival edema, eye hypesthesia, eye inflammation, eyelid eczema, anterior chamber pigmentation, asthenopia, eye allergy, eyelid irritation, eyelid discoloration, eyelash thickening.

From the cardiovascular system. Infrequently: irregular heart rate, decreased blood pressure, increased blood pressure, hypotension. Rarely: decreased heart rate, heart rate, hypertension.

From the respiratory system, thoracic and mediastinal disorders. Infrequently: respiratory disorders, dysphonia, nasal congestion, sore throat. Rarely: asthma, shortness of breath, cough, sore throat, discomfort in the nose, dry nose.

From the digestive system. Infrequently: exacerbation of peptic ulcer, gastrointestinal upset. Rarely: dry mouth, constipation.

On the part of the skin and subcutaneous tissues. Infrequently: hyperpigmentation of the skin (around the eye), allergic dermatitis, contact dermatitis, erythema, rash, impaired hair structure. Rarely: skin discoloration, hypertrichosis, madarosis, hair color changes.

From the musculoskeletal system, connective tissue, bones. Infrequently: musculoskeletal pain.

Violations of the general condition and violations associated with the method of use of the drug. Infrequently: malaise. Rarely: asthenia.

There are also reports of additional adverse reactions, but according to existing data it is impossible to assess the frequency of their occurrence. Within each organ system, adverse reactions are presented in decreasing order of severity.

Mental disorders: depression, feeling of anxiety.

Ophthalmic disorders: macular edema, retraction of the eyes.

From the side of the organ of hearing and balance: tinnitus.

From the side of the heart: chest pain.

From the digestive system: diarrhea, pain in the stomach, nausea.

On the part of the skin and subcutaneous tissue: itching.

From the musculoskeletal system and connective tissue: arthralgia.

From the kidneys and urinary tract: dysuria, urinary incontinence.

Laboratory studies: increased prostate-specific antigen.

General disturbance: bradycardia, tachycardia, increased severity of asthma, vertigo, abnormal hair growth.

special instructions

The drug can gradually change eye color due to an increase in the number of melanosomes (pigment granules) in melanocytes. Before starting treatment, patients should be informed about the possibility of irreversible changes in eye color. treatment of one eye can cause irreversible heterochromia. The long-term effects and effects of prolonged exposure to melanocytes are currently unknown. discoloration of the iris occurs slowly and may not be noticeable for several months or even years.this effect is manifested mainly in patients with a mixed color of the iris (for example, blue-brown, gray-brown, green-brown or yellow-brown), but this phenomenon was also observed in patients with brown eyes. usually brown pigmentation around the pupil concentrically spreads to the periphery of the iris of the affected eye, however, the entire iris or parts of it can acquire a more intense brown color. after cessation of treatment, no further increase in the amount of brown pigment in the iris was observed.

Darkening of the skin of the eyelids and / or periorbital area was reported in 0.4% of patients due to the use of travoprost.

The drug can gradually change the structure of the eyelashes of the eye into which it is instilled (increase in length, thickness, pigmentation and / or the number of eyelashes). The mechanism for changing the structure of eyelashes and the long-term consequences of this action are unknown today.

There is no experience with the use of the drug in inflammatory diseases of the eye, with neovascular glaucoma, angle-closure glaucoma, narrow-angle or congenital glaucoma. The experience with eye diseases caused by disorders of the thyroid gland, with glaucoma in patients with pseudophakia, with pigmented or pseudoexfoliation glaucoma is limited.

During treatment with prostaglandin F analogues_2α Macular edema has been reported.

It is recommended to prescribe the drug with caution to patients with aphakia, pseudophakia and with a rupture of the posterior lens capsule or anterior chamber lenses, as well as for the treatment of patients with risk factors for the development of cystoid macular edema.

Skin contact should be avoided since a rabbit study demonstrated transdermal absorption of travoprost.

It is required to prescribe the drug with caution to patients with risk factors for the development of iritis / uveitis.

Prostaglandins and their analogues are biologically active material and can be absorbed through the skin. Therefore, pregnant women and women planning a pregnancy should follow appropriate warnings to avoid direct exposure to the contents of the vial. In case of accidental contact with a significant amount of r-ra on the skin, immediately wash the affected area thoroughly.

When using analogues of prostaglandins, changes were observed from the periorbital site and skin of the eyelids, including deepening of the furrow of the eyelid.

Contact lenses should be removed before instillation of the drug and put on no earlier than 15 minutes after application of the drug.

Use during pregnancy or lactation. Travoprost has a harmful pharmacological effect on pregnant women and / or the fetus / newborn, so it should not be used during pregnancy unless absolutely necessary.

There is no data on the effect of grass growth on human reproductive function. A study was reported on animals in which the use of herbage in a dose 250 times higher than the maximum recommended in ophthalmic practice did not adversely affect reproductive function.

Travoprost should not be used in women of reproductive age who do not use contraceptives.

It is not known whether travoprost passes from eye drops into breast milk. There are results of a study on animals, indicating the ability of travoprost and its metabolites to penetrate into breast milk. The use of the drug during lactation is not recommended.

The ability to influence the reaction rate when driving vehicles or other mechanisms. As with any eye drops, temporary blurred vision or other visual disturbances may affect your ability to drive a vehicle or work with other mechanisms.If blurred vision occurs immediately after instillation, before starting driving or working with other mechanisms, you must wait until the vision clears up.

Interactions

There were no reports of a study of the interaction of the drug with other drugs, however, clinically significant interactions are not expected.

An in vitro study of the specific interaction of travoprost and preparations containing thiomersal has been reported. No evidence of precipitation was found.

Overdose

There are no reports of overdose cases. overdose with topical application is unlikely to cause a toxic effect or be associated with it. in case of drug overdose during eye (eye) instillation, rinse with warm water. if the drug is accidentally swallowed, symptomatic and supportive therapy is performed.

Storage conditions

Store at temperatures up to 25 ˚s.