Glaumax, eye drops 0.005% 2.5ml

Pharmacotherapeutic group: prostaglandin F_2αanalog synthetic

ATC code: S01EE01

PHARMACOLOGICAL PROPERTIES

Pharmacodynamics:

Latanoprost, a prostaglandin F2a analog, is a selective FP (prostaglandin F) receptor agonist and reduces intraocular pressure (IOP) by increasing aqueous humor outflow. Decrease of IOP starts approximately 3-4 hours after the drug administration, the maximum effect is observed after 8-12 hours, the action lasts for at least 24 hours.
Studies in animals and humans have shown that the main mechanism of action is the increase of uveoscleral outflow, besides, in humans the outflow is also described as improved (decrease of outflow resistance).

Latanoprost was found to have no significant effect on aqueous humor production or on the blood-ophthalmic barrier. Animal studies have shown that in clinical doses latanoprost has no effect (or insignificant effect) on intraocular blood flow.

Mild to moderate conjunctival or episcleral injection is possible when used topically.

According to fluorescence angiography data, long-term treatment with latanoprost after extracapsular cataract extraction in monkeys had no effect on retinal blood flow.
With short-term use, latanoprost did not promote fluorescein infiltration in the posterior segment of the eyes of patients with an artificial lens.

Latanoprost has no significant pharmacological effects on the cardiovascular and respiratory systems when used at therapeutic doses.

Pharmacokinetics:

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

Absorption

The prodrug is well absorbed through the cornea and is fully hydrolyzed when exposed to aqueous moisture.

Distribution

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

After instillation in monkeys, latanoprost is distributed predominantly 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 virtually unmetabolized in the eye, but is biotransformed in the liver.

Elimination

The plasma elimination half-life is 17 minutes.

The animal studies have shown that the major metabolites (1,2-dinor- and 1,2,3,4-tetranormetabolites) have no (or low) biological activity and are excreted mainly in the urine.

Children

Pharmacokinetic studies of latanoprost were performed in 22 adults and 25 children (ages 0-18 years) with ophthalmohypertension and glaucoma. All age groups received latanoprost at a concentration of 0.005%, one drop in each eye for at least 2 weeks. Exposure to latanoprost was approximately 2-fold higher in children aged 3 to 12 years compared to adult patients and 6-fold higher in children younger than 3 years. However, the safety profile of the drug does not differ between children and adults (see section “Overdose”). In all age groups, the duration of maintenance of the maximum plasma concentration of latanoprost acid is 5 min. The half-life of latanoprost acid in children is the same as in adults (<20 min). In equilibrium concentration there is no cumulation of lathanoprost acid in blood plasma.

Indications

Active ingredient

Composition

1 ml of the solution contains:

The active ingredient:

Latanoprost – 50 mcg

Excipients:

benzalkonium chloride – 0.2 mg,

sodium chloride – 5.69 mg,

sodium dihydrophosphate dihydrate – 3.98 mg,

How to take, the dosage

Dosing regimen in adults (including elderly)

Please put one drop in the affected eye(s) once a day. The optimal effect is achieved when the drug is used in the evening.

The drug should not be instilled more frequently than once a day because it has been shown that more frequent instillation reduces the hypotensive effect.

If a dose is missed, treatment continues as usual.

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 that pressure be applied for 1 minute to the lower lacrimal point located at the inner corner of the eye on the lower eyelid. This procedure should be done immediately after instillation.

Please remove contact lenses before the instillation and do not insert them until 15 minutes after the instillation (see also the section on “Special considerations”).

If several eye dosage forms are used at the same time, they should be separated by 5 minute intervals.

Dosing regimen in children

Latanoprost is used in children in the same dose as in adults. There are no data on the use of the drug in preterm infants (gestational age <36 weeks). Data in children <1 year old are very limited.

Interaction

Unambiguous data on drug interactions of latanoprost are not available.

The simultaneous instillation of two prostaglandin analogues into the eyes has described a paradoxical increase in IOP, so the simultaneous use of two or more prostaglandins, their analogues or derivatives is not recommended.

In in vitro studies, it has been shown that precipitate is formed when eye drops containing thiomersal are mixed with eye drops containing latanoprost. A 5-minute interval between instillations should be observed if simultaneous use of these medications is necessary.

Special Instructions

Synopsis

Contraindications

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

– Pregnancy and breastfeeding (see section “Use in pregnancy and breastfeeding”).

Side effects

Overdose

Pregnancy use

Similarities