Glaumax drops 0.005%, 2.5ml

Composition

1 ml of the solution contains:

Active ingredient:

Latanoprost – 50 mcg

Auxiliary substances:

benzalkonium chloride-0.2 mg,

sodium chloride-5.69 mg,

sodium dihydrogen phosphate dihydrate-3.98 mg,

sodium hydrophosphate anhydrous-3.48 mg,

water for injection – up to 1.0 ml

Pharmacological action

Pharmacotherapy group:  anti – glaucoma agent-prostaglandin_f2a synthetic analog

ATX code:  S01EE 01 PHARMACOLOGICAL PROPERTIES

Pharmacodynamics :

Latanoprost, an analog of prostaglandin F2a, is a selective agonist of FP (prostaglandin F) receptors and reduces intraocular pressure (IOP) by increasing the outflow of aqueous humor. A decrease in IOP begins approximately 3-4 hours after use of the drug, the maximum effect is observed after 8-12 hours, and the effect persists for at least 24 hours. Animal and human studies have shown that the main mechanism of action is an increase in uveoscleral outflow, in addition, an improvement in outflow (a decrease in outflow resistance) has also been described in humans.

It was found that latanoprost has no significant effect on the production of aqueous humor and on the hematophthalmic barrier. Animal studies have shown that in clinical doses latanoprost has no (or negligible) effect on intraocular circulation.

When applied topically, conjunctival or episcleral injection of mild or moderate severity is possible.

According to fluorescence angiography, long-term treatment with latanoprost after extracapsular cataract extraction in monkeys did not affect the blood circulation of the retina. With short-term use, latanoprost did not contribute to the leakage of fluorescein in the posterior segment of the eye of patients with an artificial lens.

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

Pharmacokinetics:

Latanoprost (molecular weight 432.58) is a prodrug esterified with an isopropyl group, inactive; after hydrolysis to an acidic form, it becomes biologically active.

Suction

The prodrug is well absorbed through the cornea and is completely hydrolyzed when it gets into watery moisture.

Distribution

Studies in humans have shown that the maximum concentration in aqueous humor is reached 2 hours after instillation.

After instillation to monkeys, latanoprost is distributed mainly in the anterior chamber of the eye, conjunctiva and eyelids. Only a small amount of latanoprost reaches the posterior chamber of the eye.

Biotransformation

The active form of latanoprost is practically not metabolized in the eye, but undergoes biotransformation in the liver.

Deduction

The plasma elimination half-life is 17 minutes.

Animal studies have shown that the main metabolites (1,2-dinor – and 1,2,3,4-tetranormetabolites) do not have (or have low) biological activity and are mainly excreted in the urine.

Children

Pharmacokinetic studies of latanoprost were conducted in 22 adults and 25 children (aged 0-18 years) with ophthalmic hypertension and glaucoma. All age groups received latanoprost at a concentration of 0.005%, one drop in each eye for at least 2 weeks. Latanoprost exposure is approximately 2 times higher in children aged 3 to 12 years compared to adult patients and 6 times higher in children under 3 years of age. However, the safety profile of the drug does not differ in children and adults (see the section “Overdose”). In all age groups, the duration of maintaining the maximum concentration of latanoprost acid in blood plasma is 5 minutes. The half-life of latanoprost acid in children is the same as in adults ( No accumulation of latanoprost acid in the blood plasma occurs at the equilibrium concentration. “

Indications

Reduction of elevated intraocular pressure (IOP) in adults and children (over 1 year of age) with open-angle glaucoma or ophthalmic hypertension.

Use during pregnancy and lactation

Pregnancy The safety of using latanoprost during pregnancy in humans has not been established. Latanoprost may have toxic effects on the course of pregnancy, the fetus and the newborn. Use during pregnancy is contraindicated. Lactation Latanoprost and its metabolites can pass into breast milk. Use during the period of breastfeeding is contraindicated. If it is necessary to use the drug, breastfeeding should be discontinued. Fertility No effect of latanoprost on male and female fertility was found in animal studies.

Contraindications

* Hypersensitivity to latanoprost or other components of the drug. Age up to 1 year (efficacy and safety have not been established).

* Pregnancy and lactation (see section “Use during pregnancy and lactation”).

WITH CAUTION: Glaumax® should be used with caution in patients with aphakia, pseudoaphakia, posterior lens capsule damage, and known risk factors for macular edema (cases of macular edema, including cystic edema, have been reported with latanoprost). Currently, there are no data on the use of Glaumax® in inflammatory eye diseases, inflammatory, neovascular, angle-closure and congenital glaucoma. There is little experience with the use of the drug in open-angle glaucoma in patients with artiphakia, as well as in pigmented glaucoma. Glaumax® has no or negligible effect on the pupil, but there are no data on the effect of the drug in acute attack of angle-closure glaucoma. Glaumax® should be used with caution in these conditions.

Side effects

Most of the adverse reactions were observed on the part of the visual organ. In an open-label 5-year safety study,33% developed iris pigmentation (see section “Special Instructions”). Other adverse reactions from the visual organ are usually transient and occur immediately after instillation. The frequency of adverse reactions was graded as follows: very common (>1/10), common (≥1/100, ><1/10), infrequent (≥1/1000, <1/100), rare (≥1/10 000, <1/1000), and very rare (Infections and infestations: Frequency unknown: herpetic keratitis. From the side of the visual organ:  

• Very common: hyperpigmentation of the iris, conjunctival hyperemia, mild to moderate eye irritation (burning sensation, sand sensation in the eyes, itching, tingling and foreign body sensation), changes in the eyelashes (increase in length, thickness, quantity and pigmentation).
• Often: transient pinpoint erosion of the epithelium (mostly asymptomatic), blepharitis, eye pain.
• Infrequently: edema of the eyelids, dryness of the eye mucosa, keratitis, blurred vision, conjunctivitis.
• Rare: iritis/uveitis (mainly in predisposed patients), macular edema, eyelid edema, corneal edema, corneal erosion, periorbital edema, darkening of the skin of the eyelids, reactions from the skin of the eyelids, changing the direction of eyelash growth, thickening, darkening and lengthening of the eyelashes, distichiasis, photophobia.
• Very rare: changes in the periorbital area and in the area of the eyelashes, leading to a deepening of the furrow of the upper eyelid.
• Frequency unknown: iris cyst.
• 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.

Nervous system disorders: Frequency unknown: dizziness, headache. From the side of the heart:

• Very rare: worsening of angina in patients with concomitant angina.
• Frequency unknown: palpitation sensation.

From the respiratory system: Rarely: bronchospasm (including exacerbation of the disease in patients with a history of bronchial asthma), shortness of breath. Skin and subcutaneous tissue disorders:

• Infrequently: a rash.
• Rare: darkening of the eyelid skin and local skin reactions on the eyelids.

Musculoskeletal and connective tissue disorders: Frequency unknown: myalgia, arthralgia. General disorders and local reactions: Very rare: chest pain. According to the results of two short-term (≤12 weeks) clinical trials in 93 children, the safety profile of latanoprost in children did not differ from the safety profile in adults. The safety profile between different age groups in children is comparable. Compared to the adult population, children had the most frequent cases of nasopharyngitis and fever.

Interaction

Unambiguous data on drug interactions of latanoprost are not available.

When two prostaglandin analogs are simultaneously instilled into the eyes, a paradoxical increase in IOP is described, so the simultaneous use of two or more prostaglandins, their analogues or derivatives is not recommended.

In vitro studies have shown that when eye drops containing thiomersal are mixed with eye drops containing latanoprost, a precipitate is formed. If the simultaneous use of these drugs is necessary, a 5-minute interval between their instillation should be observed.

How to take it, course of use and dosage

Dosage regimen for adults (including the elderly)

One drop in the affected eye (s) once a day.The optimal effect is achieved when using the drug in the evening.

Do not instill the drug more often than once a day, as it has been shown that more frequent use reduces the hypotensive effect.

If one dose is missed, treatment is continued according to the usual scheme.

As with any eye drops, in order to reduce the possible systemic effect of the drug, immediately after instillation of each drop, it is recommended to press for 1 minute on the lower lacrimal point located at the inner corner of the eye on the lower eyelid. This procedure should be performed immediately after instillation.

Before instillation, remove contact lenses and install them no earlier than 15 minutes after insertion (see also the section “Special instructions”).

If several ocular dosage forms are used simultaneously, their use should be separated by a 5-minute interval.

Dosage regimen for children

Latanoprost is used in children at the same dose as in adults. Data on the use of the drug in premature children (gestational age Data for children

Overdose

In addition to irritation of the eye mucosa and hyperemia, other adverse reactions from the visual organ with an overdose of latanoprost are not described. In case of accidental ingestion of latanoprost, the following information should be taken into account: one bottle with 2.5 ml of the solution contains 125 mcg of latanoprost. More than 90% of latanoprost is metabolized during the” first pass ” through the liver. Intravenous infusion at a dose of 3 mcg / kg in healthy volunteers did not cause any symptoms, but with a dose of 5.5-10 mcg/kg, nausea, abdominal pain, dizziness, fatigue, hot flashes and sweating were observed. Intravenous use of latanoprost to monkeys at a dose of 500 mcg / kg did not cause significant effects from the cardiovascular system. Intravenous use of latanoprost to monkeys caused transient bronchospasm. In patients with moderate bronchial asthma, instillation of latanoprost into the eyes at a dose 7 times higher than the therapeutic dose did not cause bronchospasm. In case of overdose, symptomatic treatment is performed.

Description

Clear, colorless, odorless liquid

Special instructions

Latanoprost can gradually change the color of the eyes by increasing the content of brown pigment in the iris. Before starting treatment, patients should be informed about possible irreversible changes in eye color. The use of the drug in one eye can cause irreversible heterochromia. This change in eye color was mainly observed in patients with unevenly colored irises, namely: square-blue, gray-brown, yellow-brown and green-brown. In latanoprost studies, darkening usually began within the first 8 months of treatment, rarely during the second or third year, and was not observed after four years of treatment. The progression of iris pigmentation decreased over time and stabilized after 5 years. There are no data on increased pigmentation over 5 years. In an open-label 5-year safety study of latanoprost,33% of patients developed iris pigmentation (see section “Side effects”). In most cases, the change in the color of the iris was insignificant and, often, not clinically detected. The frequency of occurrence ranged from 7 to 85% in patients with different iris colors, prevailing in patients with yellow-brown irises. No changes were observed in patients with uniformly colored irises of blue color; in rare cases, changes were noted in patients with uniformly colored irises of gray, green and brown color. The change in eye color is caused by an increase in the content of melanin in the stromal melanocytes of the iris, and not by an increase in the number of melanocytes themselves. In typical cases, brown pigmentation appears around the pupil and extends concentrically to the periphery of the iris. In this case, the entire iris or parts of it turn brown. No further pigmentation was observed after discontinuation of therapy. According to available clinical data, color change was not associated with any symptoms or pathological disorders. The drug does not affect the nevi and lentigo of the iris. According to the results of 5-year clinical studies, there was no accumulation of pigment in the sclerocorneal trabecular network or other parts of the anterior chamber of the eye. It has been shown that darkening of the iris does not lead to undesirable clinical consequences, so the use of latanoprost can be continued if such darkening occurs. However, such patients should be regularly monitored and, depending on the clinical situation, treatment may be discontinued. The experience of using latanoprost in the treatment of angle-closure and congenital glaucoma, pigmented glaucoma, and open-angle glaucoma in patients with pseudoaphakia is limited. There is no information about the use of latanoprost in the treatment of secondary glaucoma due to inflammatory eye diseases and neovascular glaucoma. Latanoprost does not affect the pupil size. Due to the lack of experience with the use of latanoprost in the treatment of acute attack of angle-closure glaucoma, the drug should be used with caution in such patients. Due to the fact that information on the use of latanoprost in the postoperative period of cataract extraction is limited, caution should be exercised when using the drug in this category of patients. Caution should be exercised when using latanoprost in patients with a history of herpetic keratitis. In acute herpetic keratitis, as well as in the presence of anamnestic information about chronic recurrent herpetic keratitis, it is necessary to avoid the appointment of latanoprost. Macular edema, including cystic edema, was observed during latanoprost therapy mainly in patients with aphakia, pseudoaphakia, rupture of the posterior lens capsule, or in patients with risk factors for cystic macular edema (in particular, diabetic retinopathy and retinal vein occlusion). Caution should be exercised when using latanoprost in patients with aphakia, pseudoaphakia with posterior capsule rupture or anterior chamber intraocular lenses, as well as in patients with known risk factors for cystic macular edema. Caution should be exercised when using latanoprost in patients with risk factors for iritis/uveitis. Experience with the use of latanoprost in patients with bronchial asthma is limited, but in some cases, in the post-marketing period, there was an exacerbation of the course of asthma and / or the appearance of shortness of breath. Caution should be exercised when using latanoprost in this category of patients (see also the section “Side effects”). There were cases of darkening of the skin of the periorbital area, which in a number of patients were reversible with continued therapy with latanoprost. Latanoprost can cause gradual changes in the eyelashes and downy hair, such as lengthening, thickening, increasing pigmentation, increasing density, and changing the direction of lash growth. The changes in the eyelashes were reversible and resolved after discontinuation of therapy. Latanoprost contains benzalkonium chloride, often used as a preservative in ophthalmic medicines. Benzalkonium chloride can cause eye irritation, pinpoint keratopathy, and / or toxic ulcerative keratopathy, as well as being absorbed by soft contact lenses and discoloring them. Careful monitoring of the condition of patients with dry eye syndrome or other corneal diseases with prolonged use of latanoprost is required. Before using the drug, remove contact lenses and re-install them no earlier than 15 minutes after instillation (see also the section “Dosage and use”). Children’s information about the efficacy and safety of latanoprost in children under one year of age is limited. There is no experience of using the drug in premature children (gestational age less than 36 weeks). There is no information on the safety of long-term use of latanoprost in children. For primary congenital glaucoma in children from 0 to 3 years of age, surgical intervention (goniotomy/trabeculotomy) remains the standard treatment method. EFFECTS ON THE ABILITY TO DRIVE VEHICLES AND WORK WITH MECHANICSAS with the use of other ophthalmic medications, temporary visual impairment may occur; it is not recommended to drive vehicles or work with mechanisms until it is restored.

Form of production

Eye drops.

Storage conditions

In a dark place at a temperature of 2 to 8 °C. The opened bottle should be stored at a temperature not exceeding 25 °C. Keep out of reach of children.

Shelf

life is 2 years. After opening the bottle, the drug should be used for 4 weeks. Do not use after the expiration date indicated on the package.

Active ingredient

Latanoprost

Conditions of release from pharmacies

By prescription

Dosage form

eye drops

Purpose

Nursing mothers as prescribed by a doctor, Children as prescribed by a doctor, Adults as prescribed by a doctor, Pregnant women as prescribed by a doctor

Indications

Glaucoma