Instructions Lanotan eye drops 0.05 mg/ml bottle with dropper 2.5 ml
Composition
active ingredient: latanoprost;
1 ml of the drug contains 0.05 mg of latanoprost;
Excipients: benzalkonium chloride, sodium dihydrogen phosphate monohydrate, sodium hydrogen phosphate anhydrous, sodium chloride, water for injections.
Dosage form
Eye drops.
Main physicochemical properties: clear colorless liquid.
Pharmacotherapeutic group
Antiglaucoma drugs and miotics. Prostaglandin analogues. ATX code S01E E01.
Pharmacological properties
Pharmacodynamics.
The active substance latanoprost, a prostaglandin F2a analogue, is a selective agonist of the prostanoid FP receptor, which reduces intraocular pressure by increasing the outflow of aqueous humor. The reduction in intraocular pressure in humans begins approximately 3-4 hours after administration of the drug, and the maximum effect is observed after 8-12 hours. The hypotensive effect lasts for at least 24 hours.
Basic studies have shown that latanoprost is effective as monotherapy. In addition, clinical studies of the combination use of the drug have been conducted. These included studies that showed that latanoprost is effective in combination with beta-blockers (timolol). Short-term (1 or 2 weeks) studies show that the effect of latanoprost is additive when used in combination with adrenergic agonists (dipivalyl epinephrine), oral carbonic anhydrase inhibitors (acetazolamide) and at least partially additive when used with cholinergic agonists (pilocarpine).
Clinical studies have shown that latanoprost does not significantly affect the production of intraocular fluid. No effect of latanoprost on the blood-ophthalmic barrier was detected.
Latanoprost did not cause fluorescein leakage in the posterior segment of human pseudophakic eyes during short-term treatment.
No significant pharmacological effects of latanoprost at clinical doses on the cardiovascular and respiratory systems were detected.
Pharmacokinetics.
Latanoprost (molecular weight 432.58) is the isopropyl ester of the active substance, i.e. a prodrug that is inactive in itself, but after hydrolysis to form latanoprost acid, it becomes biologically active.
Prodrugs penetrate the cornea well, and all drugs that enter the intraocular fluid are hydrolyzed while passing through the cornea.
Studies in humans have shown that maximum concentrations in the intraocular fluid are reached approximately 2 hours after topical administration. After topical administration in monkeys, latanoprost is distributed mainly in the anterior segment, conjunctiva and eyelids. Only a small amount of the drug reaches the posterior segment.
Latanoprost acid is practically not metabolized in the eye. The main metabolism of the drug occurs in the liver. In humans, the plasma half-life is 17 minutes.
Indication
For the reduction of elevated intraocular pressure in patients with open-angle glaucoma and elevated intraocular pressure.
For the reduction of elevated intraocular pressure in pediatric patients with elevated intraocular pressure and pediatric glaucoma.
Contraindication
Known hypersensitivity to any component of the drug.
Interaction with other medicinal products and other types of interactions
There are no comprehensive data on interactions with other drugs.
Paradoxical increases in intraocular pressure have been reported following concomitant ocular administration of two prostaglandin analogues. Therefore, concomitant use of two or more prostaglandins, prostaglandin analogues or their derivatives is not recommended.
Drug interaction studies have only been conducted in adult patients.
Application features
Eye colour changes are observed mainly in patients with mixed iris colours, e.g. blue-brown, grey-brown, yellow-brown or green-brown. In studies with latanoprost, the onset of colour changes usually occurred within the first 8 months of treatment, rarely during the second or third year and was not observed after the fourth year of treatment. The progression of iris pigmentation decreases over time and stabilises after 5 years. The effect of increased pigmentation after 5 years of treatment with the drug has not been evaluated. In an open-label 5-year safety study with latanoprost, 33% of patients were reported to have increased iris pigmentation (see section 4.8). Iris colour changes are in most cases minor and often clinically unnoticeable. The incidence in patients with mixed iris colours ranged from 7% to 85%, with patients with yellow-brown irises having the highest incidence. Eye color changes were not observed in patients with uniform blue eye color and were rare in patients with uniform gray, green, or brown eye color.
The color change is due to an increase in melanin content in the stromal melanocytes of the iris, and not to an increase in the number of melanocytes. Typically, the brown pigmentation around the pupil spreads concentrically towards the periphery of the affected eye, but the entire iris or parts of it may become more brown. After discontinuation of treatment, no further increase in brown pigmentation of the iris has been observed. To date, there is no evidence in clinical studies that this phenomenon is associated with any symptoms or pathological changes.
In the presence of nevi or freckles on the iris, no changes were noted under the influence of therapy. In clinical studies, no accumulation of pigment was observed in the trabecular meshwork or in any other part of the anterior chamber of the eye. The results of the drug use indicate that increased iris pigmentation does not cause clinical complications and the use of latanoprost can be continued in the event of a change in iris pigmentation. However, patients should undergo regular examinations and, if the clinical situation requires it, treatment with Lanotan® should be discontinued.
Experience with Lanotan® is limited in chronic angle-closure glaucoma, open-angle glaucoma in patients with pseudophakia, and pigmentary glaucoma. There are currently no data on the use of Lanotan® in inflammatory and neovascular glaucoma or in inflammatory eye diseases. Lanotan® has no or negligible effect on the pupil, but there are no data on the use of the drug in acute attacks of angle-closure glaucoma. Therefore, it is recommended to use Lanotan® with caution in such conditions until more data are available.
There are limited data on the use of Lanotan® in the perioperative period for cataract surgery. Lanotan® should be used with caution in such patients.
Lanotan® should be used with caution in patients with a history of herpetic keratitis, but its use should be avoided in cases of active keratitis caused by the herpes simplex virus and in patients with a history of recurrent herpetic keratitis, especially associated with prostaglandin analogues.
Cases of macular edema have been reported (see section 4.8), mainly in aphakic patients, in pseudophakic patients with torn posterior lens capsule or anterior chamber lenses, and in patients with known risk factors for cystic macular edema (such as diabetic retinopathy and retinal vein occlusion). Lanotan® should be used with caution in aphakic patients, in pseudophakic patients with torn posterior lens capsule or anterior chamber lenses, or in patients with known risk factors for cystic macular edema.
Lanotan® should be used with caution in patients with known risk factors for the development of iritis/uveitis.
Experience in patients with bronchial asthma is limited, although some cases of exacerbation of bronchial asthma and/or dyspnea have been reported in the post-marketing period. Until sufficient clinical experience has been gained, the drug should be prescribed with caution to patients with bronchial asthma, see also section "Adverse reactions".
Periorbital skin discoloration has been observed, with the majority of cases occurring in Japanese patients. Currently available data suggest that periorbital skin discoloration is not permanent and in some cases resolves with continued treatment with Lanotan®.
Lanotan® contains benzalkonium chloride, which is often used as a preservative in ophthalmic preparations. Benzalkonium chloride has been reported to cause punctate keratopathy and/or toxic ulcerative keratopathy. It may also cause eye irritation and discolouration of soft contact lenses. Patients with dry eyes or diseases that damage the cornea should be closely monitored during frequent or prolonged use of Lanotan®. Contact lenses may absorb benzalkonium chloride and should be removed before using Lanotan® but may be reinserted 15 minutes later (see section 4.2).
Use during pregnancy or breastfeeding
Pregnancy
The safety of this medicinal product for use in pregnant women has not been established. Its pharmacological action poses a potential risk to the course of pregnancy, to the fetus or to the newborn. Therefore, Lanotan® should not be used during pregnancy.
Breast-feeding
Latanoprost and its metabolites may pass into breast milk, therefore, nursing mothers should discontinue treatment with Lanotan® or discontinue breastfeeding.
Ability to influence reaction speed when driving vehicles or other mechanisms
As with other medications, instillation of eye drops may cause temporary blurred vision. Until this effect has passed, patients should not drive or operate machinery.
Method of administration and doses
Recommended dose for adults, including the elderly
Recommended therapy: 1 drop in the affected eye once a day. The optimal effect is achieved when using Lanotan® in the evening.
Lanotan® should not be used more often than once a day, as it has been shown that more frequent use reduces the effectiveness of reducing intraocular pressure.
If a dose is missed, treatment should be continued by taking the next dose at the usual time.
As with any eye drops, to reduce possible systemic absorption during instillation, it is recommended to compress the lacrimal sac in the medial canthus of the eye for 1 minute (punctal occlusion). This should be done immediately after instillation of each drop.
Contact lenses should be removed before instilling eye drops and can be reinserted after 15 minutes.
When using multiple topical ophthalmic agents, the drugs should be applied at least 5 minutes apart.
Children
Lanotan® eye drops can be used in pediatric patients with the same dosage as for adults.
Data on the efficacy and safety of the drug in the age group up to 1 year are very limited. There are no available data on the use in premature infants (born before 36 weeks of gestation).
In children aged birth to 3 years, who suffer mainly from primary congenital glaucoma, surgical intervention (e.g., trabeculotomy/goniotomy) remains the first-line treatment.
The long-term safety of the drug in children has not been established.
Overdose
Apart from eye irritation and conjunctival hyperemia, no other ocular side effects have been reported with Lanotan® overdose.
The following information may be useful in the event of accidental ingestion of Lanotan®. One vial contains 125 mcg of latanoprost. More than 90% is metabolized during the first pass through the liver. Intravenous infusion of the drug at a dose of 3 mcg/kg to healthy volunteers did not cause any symptoms, but at a dose of 5.5-10 mcg/kg it caused nausea, abdominal pain, dizziness, increased fatigue, hot flashes and sweating.
However, when topically applied to the eyes, doses of latanoprost that are 7 times higher than the clinical dose of Lanotan® were used, bronchostenosis was not observed in patients with moderate bronchial asthma.
In case of overdose of Lanotan®, symptomatic treatment should be carried out.
Adverse reactions
The majority of adverse events are related to the visual system. In an open-label 5-year study of latanoprost, changes in iris pigmentation were reported in 33% of patients (see section 4.4). Other ophthalmic adverse events are usually transient and occur after administration of the drug.
Infectious and parasitic diseases: herpetic keratitis.
On the part of the organs of vision: increased pigmentation of the iris; mild or moderate conjunctival hyperemia, eye irritation (burning with a feeling of sand in the eyes, itching, tingling and a feeling of a foreign body in the eye); changes in eyelashes and vellus hair (increase in length, thickness, pigmentation and number) (the vast majority of cases were observed in Japanese patients), transient punctate epithelial erosions, mostly asymptomatic; blepharitis; eye pain; photophobia; eyelid edema; dry eyes; keratitis; blurred vision; conjunctivitis, iritis/uveitis (most cases were registered in patients with concomitant risk factors for these diseases); macular edema; symptomatic corneal edema and erosions; periorbital edema; growth of eyelashes in the wrong direction, which sometimes leads to eye irritation; the appearance of an extra row of eyelashes near the excretory ducts of the meibomian glands (distichiasis), periorbital and eyelid changes leading to a deepening of the eyelid fold, iris cyst.
Cardiac: unstable angina, palpitations.
Respiratory, thoracic and mediastinal disorders: bronchial asthma, exacerbation of bronchial asthma and dyspnea.
Gastrointestinal: infrequently - nausea, vomiting.
Skin and subcutaneous tissue disorders: skin rash, local skin reaction on the eyelids; darkening of the palpebral skin of the eyelids.
Musculoskeletal and connective tissue disorders: myalgia, arthralgia.
General disorders and administration site conditions: chest pain.
Cases of corneal calcification in association with the use of phosphate-containing eye drops have been reported very rarely in some patients with significantly damaged corneas.
Children
The safety profile of latanoprost was similar to that in adults and no new adverse events were identified. The short-term safety profiles in the different subgroups of paediatric patients were also similar. The following adverse events were observed more frequently in paediatric patients than in adults: nasopharyngitis and fever.
Expiration date
2 years.
The shelf life of the drug after opening the bottle is 42 days.
Do not use the drug after the expiration date indicated on the package.
Storage conditions
Store in the original packaging at a temperature of 2 ºС to 8 ºС.
Keep out of reach of children.
Packaging
2.5 ml in bottle No. 1.
Vacation category
According to the recipe.
Producer
JSC "Farmak".
Location of the manufacturer and its business address
Ukraine, 04080, Kyiv, Kyrylivska St., 74.
