Xalatan, eye drops 0.005% 2.5ml 3 pcs.

Pharmacodynamics

Latanoprost, an analogue of prostaglandin F2α, is a selective FP (prostaglandin F) receptor agonist and reduces intraocular pressure (IOP) by increasing aqueous outflow, mainly via uveoscleral and trabecular network. IOP reduction starts approximately 3-4 hours after the drug is injected, the maximum effect is observed after 8-12 hours, the action lasts for at least 24 hours. It is established that latanoprost has no significant effect on aqueous humor production and hemato-ophthalmic barrier.

When used in therapeutic doses latanoprost has no significant pharmacological effect on cardiovascular and respiratory systems.

Pharmacokinetics

Absorption

Latanoprost, being a prodrug, is absorbed through the cornea, where its hydrolysis to bioactive acid occurs. Its concentration in aqueous humor reaches a maximum about two hours after topical application.

Distribution

The volume of distribution is 0.16 ± 0.02 L/kg. Latanoprost acid is detected in aqueous humor during the first 4 hours and in plasma only during the first hour after topical administration.

Metabolism

Latanoprost, being a prodrug, undergoes hydrolysis in the cornea by esterases to form bioactive acid. Latanoprost acid entering the systemic blood flow 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 quickly eliminated from the 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 administration approximately 88% of the administered dose is excreted with the urine.

Children

Latanoprost exposure is approximately 2 times higher in children aged 3 to 12 years compared to adult patients and 6 times higher in children younger than 3 years. However, the safety profile of the drug does not differ between children and adults.

The time to reach the maximum plasma concentration of latanoprost acid is 5 minutes for all age groups. The elimination half-life of latanoprost acid in children is the same as in adults. No cumulation of latanoprost acid in plasma occurs at equilibrium concentration.

Indications

Active ingredient

How to take, the dosage

Interaction

Paradoxical elevation of IOP has been described when two prostaglandin analogues are put into the eyes at the same time, so the simultaneous use of two or more prostaglandins, their analogues or derivatives is not recommended.

Pharmaceutical interactions

Xalatan is incompatible with eye drops containing thiomersal (precipitation).

Special Instructions

Xalatan® should not be administered more than once daily because more frequent use of latanoprost will weaken the IOP-lowering effect.

If a dose is missed, the next dose should be given at the usual time.

Latanoprost can be used concomitantly with other classes of ophthalmic drugs for topical use to reduce IOP. If the patient uses other eye drops at the same time, they should be used at least 5 minutes apart.

The product Xalatan® contains benzalkonium chloride which can be absorbed by contact lenses. Contact lenses should be removed and reinserted after 15 minutes before the drops are applied.

Latanoprost may cause a gradual increase in the brown pigment in the iris. The change in eye color is due to an increase in melanin in the stromal melanocytes of the iris, not an increase in the number of melanocytes themselves. In typical cases, brown pigmentation appears around the pupil and spreads concentrically to the periphery of the iris. In this case the entire iris or its parts take on a brown color. In most cases, the color change is subtle and may not be detected clinically. Increased iris pigmentation of one or both eyes is seen mostly in patients with mixed iris color, containing brown at the core. The drug has no effect on iris nevi and lentigos; no accumulation of pigment in the trabecular network or in the anterior chamber of the eye.

In determining the degree of iris pigmentation over 5 years, there were no adverse effects of increased pigmentation even with continued latanoprost therapy. The degree of IOP reduction was similar in patients regardless of the presence or absence of iris pigmentation enhancement. Therefore, treatment with latanoprost may be continued in cases of increased iris pigmentation. These patients should be monitored regularly, and treatment may be discontinued depending on the clinical situation.

Augmentation of iris pigmentation is usually seen within the first year of treatment, rarely in the second or third year. This effect is not seen after the fourth year of treatment. The rate of progression of pigmentation decreases with time and stabilizes after 5 years. The effects of increased iris pigmentation have not been studied in the longer term. No increase in brown iris pigmentation has been observed after discontinuation of treatment, but the change in eye color may be irreversible.

Latanoprost has been associated with cases of darkening of the eyelid skin, which may be reversible.

Latanoprost can cause gradual changes to eyelashes and downy hair, such as lengthening, thickening, increasing pigmentation, increasing density, and changing the direction of eyelash growth. Eyelash changes are reversible and go away after treatment is discontinued.

In patients using drops in only one eye, heterochromia may develop.

Impact on driving and operating machinery

The use of eye drops may cause transient blurring of vision. Caution should be exercised while using the drug to drive a vehicle or operate complex machinery.

Contraindications

With caution, the drug should be used in patients with aphakia, pseudoaphakia with rupture of the posterior lens capsule, in patients with risk factors of macular edema (there have been cases of macular edema development during treatment with latanoprost, including cystic edema.including cystoid); in patients with inflammatory, neovascular glaucoma (due to insufficient experience in using the drug); with bronchial asthma, herpetic keratitis in the anamnesis.

The use of Xalatan should be avoided in patients with active herpetic keratitis and recurrent herpetic keratitis, especially those associated with the use of prostaglandin F2α analogues.

Xalatan should be used with caution in patients with risk factors for iritis/veitis.

There are limited data on the use of Xalatan in patients scheduled for cataract surgery. Therefore Xalatan should be used with caution in this group of patients.

Side effects

Overdose

Pregnancy use

Similarities