Pharmacodynamics and pharmacokinetics
Pharmacodynamics
Antiglaucoma drug, synthetic analogue of prostaglandin F2α . On the one hand, it dilates the blood vessels of the eye, activates the outflow of aqueous humor and improves microcirculation, which normalizes intraocular pressure . On the other hand, it regulates cellular metabolism, improves tissue trophism, increasing the content of cAMP . This allows it to be used in open-angle glaucoma as a monotherapy drug.
A decrease in intraocular pressure is observed after 3-4 hours, and the overall effect lasts 24 hours.
Pharmacokinetics
Penetrates through the cornea and is hydrolyzed to its active form. Cmax in aqueous humor is achieved 2 hours after instillation. Metabolism occurs in the liver; it is almost not metabolized in the tissues of the eye. Metabolites have weak activity. Excreted by the kidneys. The half-life is 17 minutes.
pharmachologic effect
Latanoprost in the drug is a prostaglandin F2α analogue, a selective FP receptor agonist.
The decrease in intraocular pressure under the influence of the drug occurs by improving the outflow of aqueous humor along the uveoscleral pathway or trabecular meshwork. Glauprost is not able to have a significant effect on the production of aqueous humor or affect the blood-ophthalmic barrier.
The drug has a delayed effect, which begins 3-4 hours after its administration, maximum effectiveness is observed 8-12 hours after administration of the drug, the effect lasts a full day.
Side effects
- Pain in the eyes;
- burning sensation in the eyes;
- blurred vision;
- feeling of sand in the eyes;
- itching;
- swelling of the eyelids;
- blepharitis;
- lengthening eyelashes and enhancing their pigmentation;
- conjunctival hyperemia
- change in iris pigmentation;
- darkening of the skin of the eyelids;
- dyspnea;
- dizziness;
- attacks of bronchial asthma ;
- pain in muscles and joints.
Glauprost, 3 pcs., 2.5 ml, 0.005%, eye drops
Latanoprost can gradually change eye color by increasing the amount of brown pigment in the iris. Before starting treatment, patients should be informed about the possible permanent change in eye color. Using the drug in one eye may cause irreversible heterochromia.
This change in eye color was predominantly observed in patients with unevenly colored irises, namely: brown-blue, gray-brown, yellow-brown and green-brown. In studies of latanoprost, darkening usually began within the first 8 months of treatment, rarely during the second or third year, and was not observed after 4 years of treatment. The progression of iris pigmentation decreased over time and stabilized after 5 years. There is 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 iris color was minor and often not clinically detected. The incidence ranged from 7 to 85% in patients with unequally colored irises, predominant in patients with yellow-brown irises. No changes were observed in patients with uniformly colored blue irises; in rare cases, changes were observed in uniformly colored gray, green and brown irises.
The change in eye color is caused by an increase in the melanin content 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 acquire a brown color. After discontinuation of therapy, no further pigmentation was observed. According to available clinical data, the color change was not associated with any symptoms or pathological disorders.
The drug has no effect on nevi and lentigines of the iris. According to the results of 5-year clinical studies, pigment accumulation in the sclero-corneal trabecular meshwork or other parts of the anterior chamber of the eye was not noted. It has been shown that darkening of the iris does not lead to undesirable clinical consequences, so the use of latanoprost when such darkening occurs can be continued. However, such patients should be monitored regularly and, depending on the clinical situation, treatment may be discontinued.
Experience with the use of latanoprost in the treatment of angle-closure and congenital glaucoma, pigmentary glaucoma, and open-angle glaucoma in patients with pseudophakia is limited.
There is no information on the use of latanoprost in the treatment of secondary glaucoma due to inflammatory eye diseases and neovascular glaucoma.
Latanoprost has no effect on pupil size. Due to the lack of experience with the use of latanoprost in the treatment of acute attacks 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 case of acute herpetic keratitis, as well as in the case of anamnestic information about chronic recurrent herpetic keratitis, it is necessary to avoid prescribing latanoprost.
Macular edema, including cystoid edema, was observed during latanoprost therapy, mainly in patients with aphakia, pseudophakia, rupture of the posterior lens capsule, or in patients with risk factors for the development of cystoid macular edema (in particular, diabetic retinopathy and retinal vein occlusion).
Caution should be exercised when using latanoprost in patients with aphakia, pseudophakia with a posterior capsule tear or anterior chamber intraocular lens, or patients with known risk factors for cystoid macular edema.
Caution should be exercised when using latanoprost in patients with risk factors for developing iritis/uveitis.
Experience with the use of latanoprost in patients with bronchial asthma is limited, but in a number of cases, exacerbation of asthma and/or the appearance of shortness of breath were observed in the post-registration period.
Caution should be exercised when using latanoprost in this category of patients (see also section "Side effects").
There have been cases of darkening of the skin of the periorbital area, which in a number of patients was reversible with continued therapy with latanoprost.
Latanoprost can cause gradual changes in eyelashes and vellus hair, such as lengthening, thickening, increased pigmentation, increased thickness, and a change in the direction of eyelash growth. Changes in eyelashes were reversible and disappeared after cessation of therapy.
Glauprost contains benzalkonium chloride, often used as a preservative in ophthalmic medications. Benzalkonium chloride may cause eye irritation, punctate keratopathy and/or toxic ulcerative keratopathy, and may be absorbed and discolored by soft contact lenses. Careful monitoring of the condition of patients with dry eye syndrome or other corneal diseases is required during long-term use of latanoprost. Before using the drug, you must remove contact lenses and reinsert them no earlier than 15 minutes after instillation (see also section “Method of administration and dosage”).
Children
Information on the effectiveness and safety of latanoprost in children under one year of age is limited. There is no experience with the use of the drug in premature infants (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 aged 0 to 3 years, surgical intervention (goniotomy/trabeculotomy) remains the standard treatment method.
Impact on the ability to drive vehicles and operate machinery
As with other ophthalmic medications, temporary visual disturbances may occur; It is not recommended to drive vehicles or operate machinery until it is restored.
Glauprost, instructions for use (Method and dosage)
Place 1 drop in the eyes 1 time in the evening. If the procedure is missed, then the next dose is administered at the prescribed time the next day, without doubling it.
The use of the drug causes a change in eye color due to an increase in brown pigment. It is usually observed in individuals with mixed iris color. If there is an intense change in pigmentation, treatment is stopped. Patients who use drops in one eye may experience heterochromia . The doctor informs the patient about the likelihood of eye color changes. Changes in eyelashes in the form of lengthening and thickening disappear after treatment.
If other eye drops are prescribed, they should be administered at intervals of 5 minutes. Before the procedure, contact lenses are removed and reinserted after 15 minutes.
special instructions
When treated with Glauprost, a gradual change in the color of the iris occurs due to an increase in the amount of brown pigment in it. The patient must be warned about this in advance. In case of intense eye pigmentation, therapy should be stopped, as the changes that have occurred are irreversible.
Patients with damage to one eye may develop heterochromia.
Hair and eyelash growth caused by latanoprost is reversible after treatment with the drug is completed.
Benzalkonium chloride contained in the drug can be adsorbed by contact lenses. Therefore, the lenses must be removed before using it and inserted only 15 minutes after instillation.
In combination therapy with eye drops, Glauprost is administered at intervals of 5 minutes with other drugs.
If the patient experiences temporary blurred vision after administration of the drug, it is not recommended to drive or operate machinery until it is restored.
An unopened bottle of Glauprost is best stored in the refrigerator at a temperature of 2-6°C. After opening, the drug is left at room temperature in a place protected from light. The shelf life is 42 days.
Reviews of Glauprost
According to research results, Glauprost eye drops in patients with intraocular pressure of 24-25 mm Hg. Art. reduced it by 6-8 mm Hg. Art. If we compare its effectiveness with timolol , then one instillation of Glauprost is equivalent to 2 times a day of timolol. This drug has a longer and more pronounced hypotensive effect, as evidenced by patient reviews.
- “... Glauprost suits the fact that you can drip only once a day. I tolerate the treatment well, there is no eye irritation.”
- “... My husband uses these drops, they help well, but after six months we noticed a change in eye color. The doctor didn’t warn us, so we panicked.”
- “... They help well, but are a little expensive, considering that treatment for glaucoma is lifelong.”
Negative reviews note side effects such as redness and pain in the eyes, unbearable itching and conjunctivitis , due to which the drug was discontinued. Its high cost is also noted.
Contraindications
Glauprost should not be prescribed to patients under 18 years of age, or if there is hypersensitivity to the components of the drug.
Caution is required in the treatment of people with aphakia, a high risk of developing macular edema, pseudophakia (with rupture of the posterior lens capsule), and other types of glaucoma (neovascular, congenital, inflammatory).
Treatment of pregnant women is carried out only under the strict supervision of a doctor, subject to high expected benefit. Since the drug and its metabolites can pass into breast milk, it is better to avoid breastfeeding during the treatment period.
Glauprost price, where to buy
You can buy Glauprost at any pharmacy. The cost of one 2.5 ml dropper bottle is 525-842 rubles.
- Online pharmacies in RussiaRussia
ZdravCity
- Glauprost eye drops 0.005% 2.5 ml 3 pcs. K.O.Rompharm Company S.r.L.
RUB 1,749 order - Glauprost eye drops 0.005% 2.5 mlK.O.Rompharm Company S.r.L.
RUR 742 order
