Each mL of eye drop solution contains Latanoprost 50 mcg.
Excipients/Inactive Ingredients: Benzalkonium chloride, Sodium chloride, Sodium dihydrogen phosphate monohydrate, Disodium phosphate anhydrous, Sodium hydroxide solution, Hydrochloric acid solution and water for injection.
Pharmacology: Pharmacodynamics: Latanoprost is a prostanoid selective FP receptor agonist which is believed to reduce the intraocular pressure by increasing the outflow of aqueous humor. Studies in animals and man suggest that the main mechanism of action is increased uveoscleral outflow.
Elevated IOP represents a major risk factor for glaucomatous field loss. The higher the level of IOP, the greater the likelihood of optic nerve damage and visual field loss.
Pharmacokinetics: Absorption: Latanoprost is absorbed through the cornea where the isopropyl ester prodrug is hydrolyzed to the acid form to become biologically active. Studies in man indicate that the peak concentration in the aqueous humor is reached about 2 hours after topical administration.
Distribution: The distribution volume in humans is 0.16±0.02 L/kg. The acid of latanoprost could be measured in aqueous humor during the first 4 hours, and in plasma only during the first hour after local administration.
Metabolism: Latanoprost, an isopropyl ester prodrug, is hydrolyzed by esterase in the cornea to the biologically active acid. The active acid of latanoprost reaching the systemic circulation is primarily metabolized by the liver to the 1,2-dinor and 1,2,3,4-tetranor metabolites via fatty acid β-oxidation.
Excretion: The elimination of the acid of latanoprost from human plasma was rapid (t1/2=17 minutes) after both intravenous and topical administration. Systemic clearance is approximately 7 mL/min/kg. Following hepatic β-oxidation, the metabolites are mainly eliminated via the kidneys. Approximately 88% and 98% of the administered dose is recovered in the urine after topical and intravenous dosing, respectively.
Toxicology: Preclinical Safety Data: Mutagenicity and carcinogenicity: Latanoprost was not mutagenic in microbial (Ames), mouse lymphoma, or in mouse micronucleus tests; however, chromosome aberrations were observed in vitro with human lymphocytes.
No evidence of carcinogenic potential was observed in mice or rats given latanoprost by oral gavage in dosage up to 170 mcg/kg daily (approximately 2800 times the recommended maximum human dose) for 20 or 24 months, respectively. In vitro and in vivo studies evaluating unscheduled DNA synthesis in rats receiving latanoprost were negative.
Reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension.
Adults: 1 drop into affected eye(s) once daily in the evening; do not exceed the once daily dosage because it has been shown that more frequent administration may decrease the IOP lowering effect.
Method of Administration: Latanoprost ophthalmic solution contains benzalkonium chloride, which may be absorbed by some contact lenses. The manufacturer states that contact lenses should be removed prior to administration of each dose of latanoprost ophthalmic solution but may be reinserted 15 minutes after the dose.
If the patient is receiving more than one topical ophthalmic drug, the drugs should be administered at least 5 minutes apart.
Apart from ocular irritation and conjunctival or episcleral hyperemia, the ocular effects of latanoprost administered at high doses are not known. If overdosage with latanoprost sterile ophthalmic solution occurs, treatment should be symptomatic.
Latanoprost ophthalmic solution is contraindicated in patients with known hypersensitivity to latanoprost, benzalkonium chloride, or any ingredient in the formulation.
Ocular pigment changes: Latanoprost has been reported to cause changes to pigmented tissues. The most frequently reported changes have been increased pigmentation of the iris and periorbital tissue (eyelid) and increased pigmentation and growth of eyelashes. These changes may be permanent. Pigmentation is expected to increase as long as latanoprost is administered. After discontinuation of latanoprost, pigmentation of the iris is likely to be permanent while pigmentation of the periorbital tissue and eyelash changes have been reported to be reversible in some patients. Patients who receive treatment should be informed of the possibility of increased pigmentation. The effects of increased pigmentation beyond 5 years are not known.
Latanoprost sterile ophthalmic solution may gradually change eye color, increasing the amount of brown pigment in the iris by increasing the number of melanosomes (pigment granules) in melanocytes. The long-term effects on the melanocytes and the consequences of potential injury to the melanocytes or deposition of pigment granules to other areas of the eye are currently unknown. The change in iris color occurs slowly and may not be noticeable for several months to years. Patients should be informed of the possibility of iris color change.
Eyelid skin darkening has also been reported in association with the use of latanoprost.
Latanoprost may gradually change eyelashes and vellus hair; these changes include increased length, thickness, pigmentation, and number of lashes or hairs, and misdirected growth of eyelashes. Eyelash changes are usually reversible upon discontinuation treatment.
Patients who are expected to receive treatment in only 1 eye should be informed about the potential for increased brown pigmentation of the iris, periorbital tissue, and eyelashes in the treated eye and thus, heterochromia between the eyes. They should also be advised of the potential for a disparity between the eyes in length, thickness, or number of eyelashes. These changes in pigmentation and lash growth may be permanent.
Other forms of glaucoma: There is limited experience with latanoprost in the treatment of angle closure, inflammatory or neovascular glaucoma.
Infections: There have been reports of bacterial keratitis associated with the use of multiple-dose containers of topical ophthalmic products. These container has been inadvertently contaminated by patients who, in most cases, had a concurrent corneal disease or a disruption of the ocular epithelial surface.
Contact lenses: Contact lenses should be removed prior to the administration of latanoprost, and may be reinserted 15 minutes after administration.
Active intraocular inflammation (iris/uveitis): Latanoprost should be used with caution in patients with a history of intraocular inflammation (iris/uveitis) and should generally not be used in patients with active intraocular inflammation.
Macular edema, including cystoid macular edema: Macular edema, including cystoid macular edema, has been reported during treatment with latanoprost. These reports have mainly occurred in aphakic patients, in pseudophakic patients with a torn posterior lens capsule, or in patients with known risk factors for macular edema. Latanoprost should be used with caution in patients who do not have an intact posterior capsule or who have known risk factors for macular edema.
Use in Children: Safety and efficacy in children have not been established.
Use in Elderly: No overall differences in safety or efficacy have been observed between geriatric and younger patients. Results from phase III clinical studies indicate that age does not appear to affect IOP response to latanoprost.
Effects on ability to drive and use machine: Instillation of eye drops may cause transient blurring of vision. Until this has resolved, patients should not drive or use machine No information.
Use in Pregnancy: Category C.
Reproduction studies have been performed in rats and rabbits an incidence of 4 of 16 dams had no viable fetuses at a dose that was approximately 80 times the maximum human dose, and the highest nonembryocidal dose in rabbits was approximately 15 times the maximum human dose.
There are no adequate and well-controlled studies in pregnant women. Latanoprost should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Use in Lactation: It is not known whether this drug or its metabolites are excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when latanoprost is administered to a nursing woman.
The ocular adverse reaction and ocular signs and symptoms reported in 5% to 15% of the patients on latanoprost sterile ophthalmic solution in the 6-month, multicenter, double-masked, active-controlled trials were blurred vision, burning and stinging, conjunctival hyperemia, foreign body sensation, itching, increased pigmentation of the iris, and punctate epithelial keratopathy.
In addition to the above listed ocular reactions/signs and symptoms, the following were reported in 1% to 4% of the patients: Dry eye, excessive tearing, eye pain, lid crusting, lid discomfort/pain, lid edema, lid erythema, and photophobia.
The following events were reported in less than 1% of the patients: Conjunctivitis, diplopia and discharge from the eye. During clinical studies, there were extremely rare reports of the following: Retinal artery embolus, retinal detachment, and vitreous hemorrhage from diabetic retinopathy.
Incompatibilities: No information.
Store below 2-8°C in refrigerator.
S01EE01 - latanoprost ; Belongs to the class of prostaglandin analogues. Used in the treatment of glaucoma.
Eye drops 0.05 mg/mL x 2.5 mL.