Xalapa

Active material: Latanoprost
When ATH: S01EE01
CCF: Antiglaucoma drug
ICD-10 codes (testimony): H40.0, H40.1
When CSF: 26.01.01.07
Manufacturer: PFIZER MFG. BELGIUM N.V. (Belgium)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

Eye drops 0.005% clear, Colorless.

Excipients: sodium chloride, sodium dihydrogen (monohydrate), sodium hydrogen phosphate (anhydrous), benzalkonium chloride, water d / and.

2.5 ml – dropper bottle plastic (1) – packs cardboard.
2.5 ml – dropper bottle plastic (3) – packs cardboard.

Pharmacological action

Antiglaucoma drug, analogue of prostaglandin F_2a, selective FP receptor agonist. Has an antiglaucoma effect. Reduces IOP by increasing aqueous humor outflow, mainly, by uveoskleral'nym, as well as through the trabecular network. Established, that latanoprost does not have a significant effect on the production of aqueous humor and the blood-ophthalmic barrier.

When used in therapeutic doses, latanoprost does not have a significant pharmacological effect on the cardiovascular and respiratory systems and has an antiglaucoma effect..

The decrease in IOP begins approximately after 3-4 hours after injection, maximum effect is observed after 8-12 no, the effect lasts for at least 24 no.

Pharmacokinetics

Absorption

Latanoprost is a prodrug, absorbed through the cornea, where does its hydrolysis occur? (under the influence of esterases) with the formation of a biologically active compound – latanoprost acid. C_max latanoprost in aqueous humor is achieved in approximately 2 h after topical application of the drug.

Distribution

V_d is 0.16 ± 0.02 l/kg.. Acid latanoprosta is defined in the watery moisture during the first 4 no, and in plasma – only during the first hour after topical application.

Metabolism

Acid latanoprosta, coming into the bloodstream, metabolized mainly in the liver by beta-oxidation of fatty acids to form 1,2-dinor- and 1, 2, 3, 4--tetranor metabolites.

Deduction

Latanoprost acid is rapidly cleared from plasma: T_1/2 is 17 m. System clearance is approximately 7 ml / min / kg. After beta-oxidation in the liver, metabolites are excreted mainly by the kidneys: after topical application it is excreted in urine approximately 88% dose.

Testimony

Reducing elevated IOP in patients:

— with open-angle glaucoma;

- with increased ophthalmotonus.

Dosage regimen

The drug is instilled into the conjunctival sac of the affected eye according to 1 drop 1 time / day, in the evening. If a dose is missed, the next use of the drug is carried out as usual (ie. do not double the dose). More frequent use of the drug leads to a decrease in its effectiveness.

If necessary, use during therapy with Xalatan^® other eye drops, they should be used at intervals of at least 5 m.

Side effect

On the part of the organ of vision: eye irritation (burning sensation, feeling of sand in the eyes, itch, tingling and foreign body sensation), .Aloe, conjunctival hyperemia, sore eyes, increased pigmentation of the iris, transient punctate erosions of the epithelium, swelling of the eyelids, edema and corneal erosion, conjunctivitis, elongation, thickening, the upsurge and increased pigmentation of the eyelashes and downy hair, iritis/uveitis, keratit, macular edema (incl. cystoid), changing the direction of Eyelash growth, sometimes causes irritation of the eyes, blurred vision.

Dermatological reactions: rash, darkening of the skin of the eyelids and local skin reactions on the eyelids.

From the nervous system: dizziness, headache.

The respiratory system: bronchial asthma (incl. acute attacks or exacerbation of the disease in patients with a history of bronchial asthma), breathlessness.

On the part of the musculoskeletal system: muscle aches, joint pain.

Other: non-specific chest pain.

Contraindications

- Up to 18 years;

- Hypersensitivity to the drug.

FROM caution the drug should be used in patients with aphakia, pseudophakia with rupture of the posterior lens capsule, patients with known risk factors for macular edema (When treating latanoprostom myocarditis development of macular edema, incl. cistoidnogo); inflammatory, neovascular or congenital glaucoma (due to the lack of sufficient experience with the drug).

Pregnancy and lactation

There is no sufficient experience on the use of the drug during pregnancy and lactation. Application of Xalatan^® during pregnancy and lactation it is possible only under the supervision of a doctor and only if, if the expected benefit to the mother outweighs the risk of possible side effects in the fetus or infant.

If necessary, prescribe Xalatan^® during the lactation period should take into account, that latanoprost and its metabolites can be excreted in breast milk.

Cautions

Xalatan^® should not be prescribed more often 1 times / day, tk. more frequent use of latanoprost leads to a weakening of the IOP-lowering effect.

If one dose is missed, the next dose should be administered at the usual time..

Latanoprost can be used concomitantly with other classes of topical ophthalmic medications to lower IOP. If the patient is simultaneously use other eye drops, then they should be used at intervals, at least, 5 m.

The composition of the drug Xalatan^® includes benzalkonium chloride, which can be absorbed by contact lenses. Before instilling drops, contact lenses must be removed and reinserted through 15 m.

Latanoprost can cause a gradual increase of brown pigment in the IRIS. Changes in eye color are caused by an increase in melanin content in the stromal melanocytes of the iris, rather than an increase in the number of melanocytes themselves. In typical cases, the brown pigmentation appears around the pupil spreads concentrically and on the periphery of the IRIS. While the entire iris or parts thereof become Brown. In most cases, the color change is insignificant and may not be clinically. Increased pigmentation of the iris of one or both eyes is observed, mainly, in patients with mixed color Iris, contains the basis for Brown. The drug has no effect on nevi and Lentigo IRIS; no accumulation of pigment in the trabecular meshwork or in the anterior chamber of the eye was noted.

When determining the degree of pigmentation of the iris over more than 5 years revealed no adverse effects enhance pigmentation even with continued therapy latanoprostom. In patients, the degree of IOP reduction was the same, regardless of the presence or absence of increased iris pigmentation. Hence, latanoprostom treatment can be continued and in cases of enhancing pigmentation of the IRIS. Such patients should be monitored regularly and treatment may be discontinued depending on the clinical situation..

Increased pigmentation of the IRIS is usually observed during the first year after the start of treatment, rarely – during the second or third year. After the fourth year of treatment, this effect is not observed. The rate of progression of pigmentation over time is reduced and stabilized within 5 years. In the more remote periods of increased IRIS pigmentation effects have not been studied. After the end of treatment reinforce brown pigmentation of the IRIS is not mentioned, However, changing the eye color may be irreversible.

In connection with the application of latanoprosta cases of eyelid skin darkening, which may be reversible.

Latanoprost may cause gradual changes in eyelashes and vellus hairs, such as elongation, thickening, increased pigmentation, an increase in density and changing the direction of Eyelash growth. Eyelash changes are reversible and disappear after discontinuation of treatment.

Patients, using drops in only one eye, the development of heterochromia.

Effects on ability to drive vehicles and management mechanisms

Patients, who experience transient blurred vision after using eye drops, It is not recommended to drive vehicles or work with moving machinery for several minutes after instilling the drug.

Overdose

Symptoms: eye irritation, hyperemia of the conjunctiva or episclera.

IV infusion of latanoprost in dose 3 µg/kg in healthy volunteers did not caused any symptoms, However, when administered in a dose of 5.5-10 µg/kg experienced nausea, abdominal pain, dizziness, fatiguability, hot flashes and sweating.

In patients with moderate bronchial asthma, instillation of latanoprost into the eyes in a dose, in 7 times higher than therapeutic, did not cause bronchospasm.

Treatment: symptomatic therapy.

Drug Interactions

While zacapawanyi in the eyes of the two analogues of prostaglandins describes a paradoxical increase in IOP, Therefore, the simultaneous use of two or more prostaglandins, their analogs or derivatives is not recommended.

Pharmaceutical interaction

Xalatan^® incompatible with eye drops, containing thiomersal (precipitation occurs).

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children, dark place at a temperature of 2 ° to 8 ° C. Shelf life – 3 year.

After opening the bottle the drug should be used within 4 weeks, in this case, the bottle should be stored at a temperature not exceeding 25°C.