Description
Latin name
XALATAN
Release form
Xalatan. Eye drops
Packaging
2.5 ml – polyethylene dropper bottle (3) – packs of cardboard with the control of the first opening.
Pharmacological action
Pharmacodynamics
Latanoprost – an analogue of prostaglandin F2 is a selective agonist of FP receptors (prostaglandin F) and reduces intraocular pressure (IOP) by increasing the outflow of aqueous humor, mainly by the uveoscleral route, as well as through the trabecular network. The decrease in IOP begins approximately 3-4 hours after the administration of the drug, the maximum effect is observed after 8-12 hours, the effect persists for at least 24 hours. It was found that latanoprost does not significantly affect the production of aqueous humor and the blood-brain barrier.
When used in therapeutic doses, latanoprost does not have a significant pharmacological effect on the cardiovascular and respiratory systems.
Pharmacokinetics
Absorption
latanoprost, Being a prodrug, it is absorbed through the cornea, where it is hydrolyzed to a biologically active acid. Concentration in aqueous humor reaches a maximum approximately two hours after topical application.
Distribution
Distribution volume is 0.16 ± 0.02 l / kg. Latanoprost acid is determined in aqueous humor during the first 4 hours, and in plasma – only during the first hour after topical application.
Metabolism
Latanoprost, being a prodrug, undergoes hydrolysis in the cornea under the influence of esterases to form a biologically active acid. Latanoprost acid entering the systemic circulation is metabolized mainly in the liver by beta-oxidation of fatty acids with the formation of 1,2-dinor and 1,2,3,4-tetranor metabolites.
Excretion
Latanoprost acid is rapidly excreted from plasma (t1 / 2 = 17 min). Systemic clearance is approximately 7 ml / min / kg. After beta oxidation in the liver, metabolites are excreted mainly by the kidneys: after topical application, approximately 88% of the administered dose is excreted in the urine.
Children
Exposure to latanoprost is approximately 2 times higher in children aged 3 to 12 years compared with adult patients and 6 times higher in children younger than 3 years. However, the safety profile of the drug is not different in children and adults.
The time to reach the maximum concentration of latanoprost acid in plasma is 5 minutes for all age groups. The half-life of latanoprost acid in children is the same as in adults. In equilibrium concentration, cumulation of latanoprost acid in blood plasma does not occur.
Indications
Decreased increased intraocular pressure (IOP) in adults and children (over the age of 1 year) with open-angle glaucoma or increased ophthalmotonus.
Use in pregnancy and lactation
Adequate controlled studies in pregnant women have not been conducted.
The drug should be prescribed during pregnancy only in cases where the potential benefit to the mother outweighs the potential risk to the fetus.
Latanoprost and its metabolites may be excreted in breast milk, therefore, during breast-feeding, the drug should be used with caution.
Composition of
1 ml of the solution contains:
active substance:
latanoprost – 50 μg
excipients:
sodium chloride,
sodium dihydrogen phosphate (monohydrate),
sodium hydrogen phosphate (anhydrous, benzon chloride,
r, srdl).
Dosage and administration of
In adults and children older than 1 year – one drop in the affected eye (a) once a day.
The optimal effect is achieved when using the drug in the evening.
As with any eye drops, in order to reduce the possible systemic effect of the drug, immediately after installing each drop, it is recommended to press on the lower lacrimal opening located at the inner corner of the eye on the lower eyelid.
This must be done within 1 minute.
Side effects
The following adverse reactions have been recorded related to the use of the drug:
From the organ of vision: eye irritation (burning sensation, feeling of sand in the eyes, itching, tingling and sensation of a foreign body) blepharitis conjunctival hyperemia eye pain increased iris pigmentation transient point erosion of the corneal epithelium, eyelid edema, periorbital edema, conjunctivitis edema and corneal erosion lengthening, thickening, increase in the number and enhancement of eyelid pigmentation and pigmentation edema, including a cystoid change in the direction of eyelash growth, sometimes an irritation of the eye, the growth of an additional row of eyelashes above the meibomian glands, changes in the periorbital region and in the region of the eyelashes, leading to deepening of the groove of the upper eyelid, blurred vision, photophobia, dry mucous membrane of the eyes.
From the skin and subcutaneous tissues: rash, darkening of the skin of the eyelids and local skin reactions on the eyelids, toxic epidermal necrolysis.
From the nervous system: dizziness, headache.
On the part of the respiratory system: bronchospasm (including acute attacks or exacerbation of the disease in patients with a history of bronchial asthma), shortness of breath.
From the musculoskeletal system and connective tissue: muscle / joint pain.
General and local reactions: nonspecific chest pain.
Infections and infestations: herpetic keratitis.
There have also been cases of retinal artery embolism, retinal detachment, and vitreous hemorrhage in patients with diabetic retinopathy.
In some patients with significant corneal damage, very rare cases of corneal calcification have been reported due to the use of phosphate-containing eye drops.
Children
The safety profile of Xalatan ® in children did not differ from the safety profile in adults. Compared with the adult population, nasopharyngitis and fever were most commonly observed in children.
Overdose
In addition to irritation of the mucous membrane of the eye, conjunctival hyperemia or episcleras, other undesirable changes on the part of the organ of view when overdosed with latanoprost are unknown.
The following information should be taken into account when latanoprost is taken accidentally: one vial of 2.5 ml solution contains 125 μg latanoprost. More than 90% of the drug is metabolized at the first passage through the liver.
An intravenous infusion of 3 g / kg in healthy volunteers did not cause any symptoms, however, nausea, abdominal pain, dizziness, fatigue, hot flashes, and sweating were observed with a dose of 5.5-10 μg / kg.
In patients with moderate bronchial asthma, the introduction of latanoprost into the eyes at a dose 7 times the therapeutic did not cause bronchospasm.
In case of overdose, symptomatic treatment is performed.
Storage conditions
Store at + 2 – + 8 ° C in a dark place.
Store the opened bottle at a temperature not exceeding + 25 ° ¡.
The Expiration of
is 3 years.
Open vial for 4 weeks.
Deystvuyuschee substances
Latanoprost
Pharmacy terms
Prescription
Dosage form
Dosage form
eye drops
