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Pharmacological properties
Pharmacodynamics. The active substance latanoprost, an analogue of prostaglandin f2α, is a selective agonist of the fp prostanoid receptor, which reduces intraocular pressure by increasing the outflow of intraocular fluid. a decrease in intraocular pressure begins approximately 3-4 hours after administration of the preparation, and the maximum effect is observed after 8-12 hours. The hypotensive effect lasts for 24 hours.
Baseline studies have shown latanoprost to be effective as monotherapy. In addition, clinical studies of the combined use of the preparation have been carried out. These included studies that showed latanoprost was effective in combination with β-adrenergic receptor blockers (timolol). Short-term (1 or 2 weeks) studies show that the effect of latanoprost is additive when used in combination with adrenergic agonists (dipivalil epinephrine), oral carbonic anhydrase inhibitors (acetazolamide) and at least partially additive when used in combination with cholinomimetics (pilocarpine) ...
Clinical studies have shown that latanoprost does not significantly affect the production of intraocular fluid. No effect of latanoprost on the blood-ophthalmic barrier was found.
Latanoprost does not cause fluorescein leakage in the posterior segment of human pseudophakic eyes during short-term treatment.
There was no significant pharmacological effect of latanoprost in clinical doses on the cardiovascular and respiratory systems.
Pharmacokinetics. Latanoprost is a prodrug isopropyl ester that is inactive by itself, but after hydrolysis to form latanoprost acid, it becomes biologically active. The prodrug penetrates well through the cornea, and all preparations that enter the intraocular fluid are hydrolyzed when passing through the cornea.
Cmax in the intraocular fluid is reached approximately 2 hours after topical application. After application of eye drops, latanoprost is distributed primarily in the anterior segment of the eye, conjunctiva and eyelids. Only a small amount of the preparation reaches the posterior segment.
In the tissues of the eye, there is practically no metabolism of latanoprost acid. The main metabolism takes place in the liver. T½ from blood plasma is 17 minutes. The main metabolites, 1, 2-dinor- and 1,2,3,4, -tetranor-metabolites have no or weak biological activity and are excreted mainly in the urine.
Indications
Decrease in increased intraocular pressure in patients with open-angle glaucoma, chronic angle-closure glaucoma and increased intraocular pressure; reduction of increased intraocular pressure in pediatric patients with increased intraocular pressure and childhood glaucoma.
Application
Recommended dose for adults, including the elderly
Recommended therapy: 1 drop into the affected eye 1 time per day. The optimal effect is achieved when using the preparation Lanotan in the evening.
Lanotan should not be used more often than 1 time per day, since it has been shown that with frequent use, the effectiveness of reducing intraocular pressure decreases.
If a dose is missed, treatment should be continued with the next dose at the usual time.
As with any eye drops, to reduce possible systemic absorption during instillation, it is recommended to squeeze the lacrimal sac in the medial corner of the eye for 1 min (occlusion of the lacrimal openings). This must be done immediately after each drop is instilled.
Before instilling eye drops, contact lenses should be removed and they can be reinstalled after 15 minutes.
When using several topical ophthalmic agents, the preparations should be used at intervals of at least 5 minutes.
Contraindications
Known hypersensitivity to any component of the preparation.
Side effects
Most of the adverse events are associated with the organ of vision. in an open five-year study of latanoprost, 33% of patients showed a change in the pigmentation of the iris (see special instructions). other ophthalmic adverse events are usually temporary and occur after preparation administration.
Infectious and parasitic diseases: herpetic keratitis.
From the nervous system: headache, dizziness.
From the side of the organ of vision: increased pigmentation of the iris, mild or moderate hyperemia of the conjunctiva, eye irritation (burning with a feeling of sand in the eyes, itching, tingling and sensation of a foreign body in the eye), changes in eyelashes and vellus hair (increase in length, thickness, pigmentation, etc. number) (most cases were observed in Japanese patients), transient punctate epithelial erosions, mostly asymptomatic, blepharitis, eye pain, photophobia, eyelid edema, dry eyes, keratitis, blurred vision, conjunctivitis, iritis / uveitis (most cases were reported in patients with associated risk factors for these diseases), macular edema; symptomatic edema and erosion of the cornea; periorbital edema, growth of eyelashes in the wrong direction, which sometimes leads to eye irritation; the appearance of an additional row of eyelashes in the excretory ducts of the meibomian glands (distichiasis), periorbital changes and changes in the eyelids, leading to a deepening of the fold of the eyelids, cyst of the iris.
From the side of the heart: unstable angina pectoris, accelerated heartbeat.
From the respiratory system, chest and mediastinal organs: asthma, exacerbation of asthma and dyspnea.
On the part of the skin and subcutaneous tissue: skin rash, local skin reaction on the eyelids; darkening of the palpebral part of the skin of the eyelids.
On the part of the musculoskeletal system and connective tissue: myalgia, arthralgia.
General disorders and reactions at the injection site: chest pain.
Cases of corneal calcification due to the use of eye drops containing phosphate have been reported very rarely in some patients with significant corneal damage.
Children. The safety profile of latanoprost in children is similar to that in adults, and no new adverse events have been identified. The short-term safety profiles in different subgroups of pediatric patients were also similar. In pediatric patients, more often than in adults, side effects such as nasopharyngitis and fever are noted.
Special instructions
Lanotan can cause gradual color changes in the eyes by increasing the amount of brown pigment in the iris. before starting treatment, patients should be informed about the possibility of permanent changes in eye color. treatment of only one eye can lead to permanent heterochromia.
Changes in eye color are observed mainly in patients with a mixed color of the iris, for example, blue-brown, gray-brown, yellow-brown, or green-brown. In studies of latanoprost, the appearance of discoloration usually occurred within the first 8 months of treatment, rarely during the second or third year, but was not observed after the fourth year of treatment. The progression of iris pigmentation decreases over time and stabilizes after 5 years. The effect of enhancing pigmentation after 5 years of preparation treatment was not evaluated. In an open five-year study of the safety of latanoprost, 33% of patients showed increased pigmentation of the iris (see SIDE EFFECTS). Changes in the color of the iris are generally minor and often clinically imperceptible. The incidence in patients with mixed iris color ranged from 7% to 85%, with those with tan iris having the highest incidence. Eye color changes were not observed in patients with uniform blue eyes and were rare in patients with uniform gray, green, or brown eyes.
The color change is due to an increase in the melanin content in the stromal melanocytes of the iris, and not due to an increase in the number of melanocytes. Typically, the brown pigmentation around the pupil spreads concentrically towards the periphery of the affected eye, but all or parts of the iris may turn brownish. No further increase in brown iris pigmentation was observed after discontinuation of treatment. Currently, clinical studies have not received data that this phenomenon is associated with any symptoms or pathological changes.
In the presence of nevi or freckles on the iris, no changes were noted under the influence of therapy. In clinical studies, no pigment accumulation was observed in the trabecular meshwork or in any other part of the anterior chamber of the eye. The results of the use of the preparation indicate that an increase in the pigmentation of the iris does not cause clinical complications and the use of latanoprost can be continued if there is a change in the pigmentation of the iris. However, patients should undergo regular examinations, and, if the clinical situation requires it, treatment with Lanotan should be discontinued.
The experience of using Lanotan is limited to chronic angle-closure glaucoma, open-angle glaucoma in patients with pseudophakia, and pigmentary glaucoma. Currently, there is no data on the use of Lanotan in inflammatory and neovascular glaucoma or in inflammatory eye diseases. Lanotan does not show or shows little effect on the pupil, however, there are no data on the use of the preparation in acute attacks of angle-closure glaucoma. In this regard, in such conditions, it is recommended to use Lanotan with caution until more data is obtained.
Research data on the use of Lanotan in the perioperative period in the surgical treatment of cataracts are limited. In this category of patients, Lanotan should be used with caution.
Lanotan should be used with caution in patients with a history of herpetic keratitis, but should be avoided in cases of active keratitis caused by the herpes simplex virus and in patients with a history of recurrent herpetic keratitis, especially associated with prostaglandin analogues.
There have been reports of cases of macular edema (see ADVERSE EFFECTS), mainly in individuals with aphakia, in patients with pseudophakia and rupture of the posterior lens capsule or anterior chamber lenses, and in patients with known risk factors for cystic macular edema (such as diabetic retinopathy and retinal vein occlusion). Lanotan should be used with caution in patients with aphakia, pseudophakia and rupture of the posterior lens capsule or anterior chamber lenses, or in persons with known risk factors for cystic macular edema.
Lanotan should be used with caution in patients with known risk factors for iritis / uveitis.
The experience of using the preparation in patients with asthma is limited, although during the post-registration period some cases of exacerbation of asthma and / or dyspnea were reported. Until sufficient clinical experience has been accumulated, the preparation should be prescribed to patients with asthma with caution (see SIDE EFFECTS).
Changes in skin color of the periorbital region were observed, with the majority of cases observed in Japanese patients. Currently available data indicate that the change in skin color of the periorbital area is not permanent, and in some cases it disappeared with continued treatment with Lanotan.
Latanoprost can gradually change eyelashes and vellus hair around the eye into which the preparation was injected, as well as in the adjacent areas; these changes include an increase in length, thickness, pigmentation and amount of hair in the eyelashes or vellus hair, as well as the growth of eyelashes in the wrong direction. Changes in eyelashes are reversible and disappear after discontinuation of the preparation.
Lanotan contains benzalkonium chloride, which is often used as a preservative in ophthalmic preparations. There have been reports that benzalkonium chloride caused punctate keratopathy and / or toxic ulcerative keratopathy. It can also cause eye irritation and discoloration of soft contact lenses. With frequent or prolonged use of the preparation Lanotan, patients with dry eyes or diseases in which the cornea is damaged, it is necessary to carefully monitor the condition. Contact lenses can absorb benzalkonium chloride, so they should be removed before using Lanotan, but can be worn after 15 minutes (see APPLICATION).
Use during pregnancy or lactation
Pregnancy. The safety of this preparation in pregnant women has not been established. Its pharmacological action has a potential risk for pregnancy, fetus or newborn. In this regard, Lanotan should not be used during pregnancy.
Lactation. Latanoprost and its metabolites are able to penetrate into breast milk, therefore, breastfeeding should discontinue treatment with Lanotan or suspend breastfeeding.
The ability to influence the reaction rate when driving or working with other mechanisms. As with other preparations, eye drops may cause temporary blurred vision. Until this effect passes, patients should not drive vehicles or operate machinery.
Interactions
Comprehensive data on interactions with other preparations are not available.
A paradoxical increase in intraocular pressure has been reported after simultaneous ocular administration of two prostaglandin analogs. Therefore, it is not recommended to simultaneously use two or more prostaglandins, prostaglandin analogs or their derivatives.
The study of preparation interactions was carried out only in adult patients.
Overdose
In addition to eye irritation and conjunctival hyperemia, there were no other side effects from the eyes with an overdose of Lanotan.
The following information may be helpful if Lanotan is accidentally swallowed. 1 bottle contains 125 mcg of latanoprost. More than 90% of the preparation is metabolized during the first passage through the liver. Intravenous infusion of the preparation at a dose of 3 μg / kg to healthy volunteers did not cause any symptoms, however, at a dose of 5.5–10 μg / kg, it caused nausea, abdominal pain, dizziness, increased fatigue, hot flashes and sweating.
However, with local administration of doses of latanoprost, 7 times higher than the clinical dose of Lanotan, bronchospasm was not observed in patients with moderate asthma.
In case of an overdose of Lanotan, symptomatic treatment should be carried out.
Storage conditions
In the dark place at a temperature of 2-8 ° c.
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