Instructions for use Glautan eye drops 0.04 mg/ml bottle 2.5 ml
Composition
active ingredient: travoprost;
1 ml of drops contains travoprost 0.04 mg;
Excipients: polyethoxylated hydrogenated castor oil; boric acid; propylene glycol; sorbitol (E 420); zinc chloride; concentrated hydrochloric acid; sodium hydroxide; water for injections.
Dosage form
Eye drops.
Main physicochemical properties: clear colorless liquid.
Pharmacotherapeutic group
Means for use in ophthalmology. Antiglaucoma drugs and miotics. Prostaglandin analogues. ATX code S01E E04.
Pharmacological properties
Pharmacodynamics
Travoprost, a prostaglandin F2a analogue, is a full, selective agonist of prostaglandin F2a with high affinity for prostaglandin FP receptors. It reduces intraocular pressure (IOP) by increasing the outflow of aqueous humor through the trabecular meshwork and uveoscleral pathways. IOP reduction in humans begins approximately 2 hours after administration, with a maximum effect occurring 12 hours later. Significant IOP reductions following a single dose can persist for more than 24 hours.
In clinical trials, patients with open-angle glaucoma or ocular hypertension with a baseline IOP of 25–27 mmHg who received travoprost once daily in the evening experienced a reduction in IOP of 7–8 mmHg. Subgroup analyses of these studies showed that the reduction in IOP in black patients was 1.8 mmHg greater than in non-black patients. It is currently unknown whether this difference is related to race or to highly pigmented irises.
Pharmacokinetics
Travoprost is an ester prodrug. It is absorbed through the cornea, where the isopropyl ester is hydrolyzed by corneal esterases to the active free acid. Data from 4 pharmacokinetic studies (total of 107 patients) showed that plasma free acid concentrations were below 0.01 ng/mL (limit of quantification) in two-thirds of patients. In subjects with a defined plasma concentration (N=38), the mean plasma Cmax was 0.018±0.007 ng/mL (range 0.01 to 0.052 ng/mL) and was reached within 30 minutes. According to these studies, the plasma half-life is 45 minutes. There were no differences in plasma concentrations between days 1 and 7, indicating that steady-state concentrations were achieved early and that there was no significant accumulation.
Systemically, travoprost free acid is metabolized to inactive metabolites by beta-oxidation of the (carboxylic acid) chain to form 1,2-dinor- and 1,2,3,4-tetranor-analogues through oxidation of the 15-hydroxyl moiety, as well as by cleavage of the 13,14 double bond.
Elimination of travoprost free acid from plasma was rapid, and levels were generally below the limit of quantification within 1 hour of dosing. The terminal elimination half-life of travoprost free acid was estimated in 14 patients and ranged from 17 to 86 minutes with a mean half-life of 45 minutes. Less than 2% of a topical ocular dose of travoprost is excreted in the urine within 4 hours as travoprost free acid.
Indication
Reduction of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.
Contraindication
Hypersensitivity to the active substance or to other components of the medicinal product.
Interaction with other medicinal products and other types of interactions
No studies on interactions with other drugs have been conducted.
Application features
Pigmentation
Travoprost ophthalmic solution has been reported to cause tissue pigmentation. Increased pigmentation of the iris, periorbital area (eyelids), and eyelashes has been reported most frequently. Pigmentation increases as long as travoprost is used. Pigmentation occurs by increasing melanin content in melanocytes, not by increasing the number of melanocytes. After discontinuation of travoprost, iris pigmentation is likely to be permanent, while periorbital pigmentation and changes in the eyelash area are reversible in some patients. Patients using the drug should be informed of the possibility of increased pigmentation. The long-term effects of increased pigmentation are unknown.
The change in iris color may not be noticeable for several months to several years. Usually, brown pigmentation around the pupil spreads concentrically to the periphery of the iris of the affected eye, but the entire iris or parts of it may acquire a more intense brown color. In the presence of nevi or freckles on the iris, no changes were noted under the influence of therapy. The use of the drug Glautan can be continued if a noticeable change in iris pigmentation has occurred, but patients should undergo regular examinations.
Eyelash changes
Travoprost may gradually change the structure of the eyelashes and vulva of the eye in which it is used. These changes have included an increase in the length, thickness, and number of eyelashes. Eyelash changes are usually reversible and disappear after stopping treatment with travoprost.
Glautan should be used with caution in patients with inflammatory eye diseases, such as uveitis, as inflammation may be exacerbated.
Angle-closure glaucoma, inflammatory or neovascular glaucoma
There is no experience with the use of travoprost in angle-closure, inflammatory or neovascular glaucoma.
Macular edema
Macular edema, including cystoid macular edema, has been reported during treatment with travoprost solution.
It is recommended to prescribe Glautan with caution to patients with aphakia, pseudophakia, posterior lens capsule rupture, anterior chamber lenses, or with risk factors for macular edema.
Bacterial keratitis
Bacterial keratitis has been reported to be associated with the use of reusable containers for topical ophthalmic medications. These containers were inadvertently contaminated by patients, most of whom had concomitant corneal disease or compromised epithelial surface integrity.
Use in elderly patients
Overall, no clinical difference was observed in the safety and efficacy of the drug between elderly patients and other adult patients.
Excipients
Glutan contains propylene glycol, which may cause skin irritation.
The product contains polyethoxylated hydrogenated castor oil, which may cause skin reactions.
Contact lenses
Patients should remove contact lenses before instilling Glautan and wait 15 minutes after instillation before reinserting contact lenses.
Use with other ophthalmic drugs
If more than one topical ophthalmic agent is used, the drugs should be instilled at least 5 minutes apart.
Ability to influence reaction speed when driving vehicles or other mechanisms
As with any eye drops, temporary blurred vision or other visual disturbances may affect the ability to drive or use machines. If blurred vision occurs immediately after instillation, the patient should wait until vision clears before driving or using machines.
Use during pregnancy or breastfeeding
Pregnancy
Animal studies have shown adverse effects of travoprost on the fetus, there are no adequate controlled studies in pregnant women, it should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Teratogenic effects
Travoprost was teratogenic in rats at intravenous doses up to 10 mcg/kg/day (more than 250 times the maximum recommended human ocular dose (MRD)), as evidenced by increased incidence of skeletal malformations and external and visceral malformations such as sternal fusion, domed head, and hydrocephalus. No teratogenic effects were observed in rats at intravenous doses of 3 mcg/kg/day (75 times the MRD) or in mice at subcutaneous doses up to 1 mcg/kg/day (25 times the MRD). Travoprost caused increased post-implantation losses and decreased fetal viability in rats at intravenous doses greater than 3 μg/kg/day (75 times the MRD) and in mice at subcutaneous doses greater than 0.3 μg/kg/day (7.5 times the MRD).
In the offspring of female rats treated subcutaneously with travoprost from day 7 of gestation to day 21 of lactation at a dose of 0.12 mcg/kg/day (3 times the MRD), the incidence of postnatal mortality was increased and neonatal weight gain was reduced. Neonatal development of the neonate was also impaired, as evidenced by delayed eye opening, auricular detachment and separation of the foreskin, and decreased motor activity.
Breast-feeding
It is not known whether travoprost or its metabolites from eye drops are excreted in human breast milk. Animal studies have shown that travoprost and its metabolites are able to pass into breast milk, therefore the use of Glautan during breastfeeding is not recommended.
Method of administration and doses
For ophthalmic use.
Use in the treatment of adults, including elderly patients
1 drop of Glautan into the conjunctival sac of the affected eye once daily. The optimal effect is achieved when the dose is administered in the evening. Glautan should not be administered more than once daily, as more frequent administration of prostaglandin analogues leads to a decrease in the effect of lowering elevated IOP.
Nasolacrimal occlusion or slight eyelid closure is recommended after instillation. This reduces systemic absorption of drugs administered into the eye and reduces the likelihood of systemic side effects.
Glautan can be used simultaneously with other topical ophthalmic drugs to lower IOP. If more than one topical ophthalmic drug is used, the interval between their applications should be at least 5 minutes.
If another ophthalmic antiglaucoma agent is replaced with Glautan, the use of the other drug should be discontinued and Glautan should be started the next day.
Use in liver and kidney dysfunction
Travoprost has been studied in patients with hepatic impairment and in patients with renal impairment (creatinine clearance less than 14 mL/min). No clinically significant changes in hematology, blood chemistry, or urine laboratory parameters were observed in these patients. No dose adjustment is necessary in these patients.
To prevent contamination of the dropper tip and solution, care must be taken not to touch the eyelids, surrounding areas, or other surfaces with the dropper tip.
Children
The drug is not recommended for pediatric use in children under 16 years of age due to potential safety concerns related to increased pigmentation after prolonged use.
Overdose
There have been no reports of any cases of overdose. Local overdose is unlikely to result in toxic effects. In case of local overdose with Glautan, the eye(s) should be rinsed with warm water. In case of accidental ingestion, symptomatic and supportive therapy should be administered.
Adverse reactions
Data on adverse reactions were obtained during clinical trials and during the post-marketing period of use of the drug.
On the part of the organs of vision: conjunctival hyperemia, ocular hyperemia, iris hyperpigmentation, eye pain, photophobia, ocular discomfort, foreign body sensation in the eye, decreased visual acuity, blurred vision, dry eye, eye itching, keratitis, eye inflammation, corneal discoloration, blepharitis, conjunctivitis, cataract, eyelid margin scaling, subconjunctival hemorrhages and tears, macular edema, visual impairment, iris discoloration, deepening of the sulcus around the eyelids, tearing.
Skin and subcutaneous tissue disorders: reversible hyperpigmentation of periorbital tissues and eyelashes, reversible increase in length, thickness and number of eyelashes.
On the part of the immune system: allergy.
From the nervous system: headache, anxiety, depression, insomnia.
Cardiac: angina pectoris, bradycardia, arrhythmia, tachycardia.
From the vascular system: arterial hypertension or hypotension.
Respiratory system: flu-like syndrome, chest pain, bronchitis, sinusitis, nosebleeds.
Gastrointestinal: gastrointestinal disorders, dyspepsia, vomiting.
Musculoskeletal system: arthritis, back pain.
From the genitourinary system: urinary incontinence, urinary tract infections, prostate disease.
Others: hypercholesterolemia, infection, pain.
Expiration date
2 years.
The shelf life of the drug after opening the bottle is 28 days.
Do not use the drug after the expiration date indicated on the package.
Storage conditions
Store at a temperature of 2 ° C to 8 ° C. Keep out of the reach of children.
Packaging
2.5 ml per bottle. 1 bottle per pack.
Vacation category
According to the recipe.
Producer
JSC "Farmak".
Location of the manufacturer and its business address
Ukraine, 04080, Kyiv, Kyrylivska St., 74.
