Latanoprost eye drops
Function and Efficacy
The active ingredient, latanoprost, is an analog of prostaglandin F2α and a selective prostaglandin FP receptor agonist that can reduce intraocular pressure by increasing aqueous humor outflow. In humans, intraocular pressure reduction begins approximately 3-4 hours after administration and reaches maximum effect 8-12 hours later. The intraocular pressure-lowering effect can be maintained for at least 24 hours. Animal and human studies have shown that the main mechanism of action of the drug is to increase the outflow of aqueous humor from the uveoscleral bypass, although in humans, it has also been reported that the convenience of aqueous humor outflow (reduced drainage resistance) is increased. Pivotal clinical studies have shown that Xalatan is effective as a single-drug therapy. Although no clear clinical studies on combination therapy have been conducted, a 3-month study showed that latanoprost is effective in combination with a beta-adrenergic blocker (timolol). Short-term studies (1 or 2 weeks) have shown that the effects of latanoprost combined with adrenergic agonists (dipivalylepinephrine), oral carbonic anhydrase inhibitors (acetazolamide), and at least partially combined with cholinergic agonists (pilocarpine). Clinical studies have also shown that latanoprost has no significant effect on the production of aqueous humor and no effect on the blood-aqueous humor barrier. At clinical doses and in monkey studies, latanoprost has no or negligible effect on intraocular blood circulation. However, mild to moderate conjunctival or scleral congestion may occur with topical administration. Long-term use of latanoprost in monkeys with extracapsular lens removal has been shown to have no effect on retinal vessels as determined by fluorescein angiography. Short-term treatment with latanoprost does not cause fluorescein leakage from the posterior chamber intraocular lens. No significant pharmacological effects of latanoprost on the cardiovascular or respiratory systems have been found at clinical therapeutic doses. Ocular and systemic toxicity studies of latanoprost have been conducted in several animal species. In general, latanoprost is well tolerated with a wide safety margin, with a difference of at least 1000 times between the clinical ocular dose and the systemic toxic dose. An increase in respiratory rate was observed in unanesthetized monkeys given high doses of latanoprost intravenously (approximately 100 times the clinical dose/kg body weight), which may reflect transient bronchoconstriction. Latanoprost has not been shown to have sensitizing properties in animal studies. In rabbits and monkeys, no ocular toxicity was observed at doses up to 100 mcg/eye/day (clinical dose is 1.5 mcg/eye/day). However, latanoprost caused an increase in iris pigmentation in monkeys. The mechanism of the increase in pigmentation appears to be stimulation of melanin production in iris melanocytes, but no proliferative changes were observed. The iris pigmentation changes may be permanent. In long-term ocular toxicity studies, administration of latanoprost 6 mcg/eye/day also caused an enlargement of the palpebral fissure, an effect that was reversible and occurred only at doses above the clinical dose. This effect has not been observed in humans. Latanoprost was negative in the bacterial mutation reversal assay, the mouse lymphoma gene mutation assay, and the mouse micronucleus assay. Chromosomal abnormalities were observed in the in vitro human lymphocyte assay. Similar effects were observed with prostaglandin F2α, a normally occurring prostaglandin, suggesting that this effect is common to this class of substances. Regarding mutagenicity tests, unscheduled DNA synthesis studies in rats in vivo and in vitro were conducted, and the results were negative, indicating that latanoprost has no mutagenic effect. Carcinogenicity tests in mice and rats were also negative. 3 In animal experiments, latanoprost was not found to have any effect on male and female fertility. In rat embryotoxicity studies, no embryotoxicity was observed when latanoprost was administered intravenously at doses of 5, 50 and 250mcg/kg/day. However, in rabbits, latanoprost can cause embryonic death at doses of 5mcg/kg/day or more. A dose of 5mcg/kg/day (approximately 100 times the clinical dose) can cause significant embryofetal toxicity, manifested as an increased incidence of late resorption and abortion and a decrease in fetal weight. No teratogenic effects were found.
Ingredients
Latanoprost. Chemical name: (Z)-7-[(1R, 2R, 3R, 5S) 3,5-dihydroxy-2-[(3R)-3-hydroxy-5-phenyl-1-pentyl]cyclopentyl-5-heptanoic acid isopropyl ester.
| Name | Description | Content | CAS NO. | Manufacturer |
|---|---|---|---|---|
| LatanoprostIngredients |
The active ingredient, latanoprost, is an analog of prostaglandin F2α and a selective prostaglandin FP receptor agonist that can reduce intraocular pressure by increasing aqueous humor outflow. The main mechanism of action of the drug is to increase the outflow of aqueous humor through the uveoscleral bypass, and it has also been reported in humans to increase the convenience of aqueous humor outflow (reducing drainage resistance). No significant pharmacological effects of clinical therapeutic doses of latanoprost on the cardiovascular or respiratory systems have been found. More |
130209-82-4 | 36 |
Appearance
This product is a colorless clear liquid.
Indication
It is suitable for reducing intraocular pressure in patients with open-angle glaucoma and ocular hypertension, as well as patients who cannot tolerate or have poor efficacy in other intraocular pressure-lowering drugs (multiple measurements fail to reach the target intraocular pressure reduction standard).
Usage and Dosage
Recommended adult dose (including the elderly): one drop each time, once a day, in the affected eye. It is best to use it at night. Xalatan should not be used more than once a day, because more frequent use will weaken the effect of lowering intraocular pressure. If you forget to take the medicine, you should still take it as usual at the next time you take it. If other eye medications are needed, they should be taken at least 5 minutes apart. In humans, the reduction in intraocular pressure begins about 3-4 hours after taking the medicine, and the maximum intraocular pressure-lowering effect is achieved in 8-12 hours. The intraocular pressure-lowering effect can last for at least 24 hours.
Adverse Reactions
Xalatan eye drops can cause the brown pigmentation of the iris to darken, which is particularly obvious in patients with mixed iris colors (such as blue-brown, gray-brown, green-brown, yellow-brown), which is due to an increase in the melanin content in the melanocytes at the base of the iris. Based on evidence obtained from serial photography, this effect was observed in 16% of patients in a 12-month clinical trial. The highest incidence was in patients with mixed green-brown and yellow-brown irises, about 50%. Iris color changes occur slowly and may not be noticed for months to years. In clinical trials, iris color changes were not accompanied by any symptoms or pathological changes. The brown pigmentation of the iris will not darken further after cessation of treatment, but the color change that has occurred may be permanent. In a two-year clinical trial, color changes were rare in patients with pure blue, gray, green or brown irises (see
Precautions
1. People who are known to be allergic to any ingredient in Xalatan Eye Drops. 2. People who wear contact lenses.
Special Population Medication
Precautions for children: Safety data for children's use has not been established, and in principle, it is not recommended for children. Precautions for pregnancy and lactation: Precautions for pregnant and lactating women. Precautions for the elderly: Safety and effectiveness are no different from those for adults, and can be used according to clinical doses.
Drug Interactions
Not yet clear.
Storage
Refrigerate at 2-8°C before opening and keep away from light. After opening, store at room temperature below 25°C and use up within 4 weeks.
Packaging Specification
0.005% (2.5 ml: 125 micrograms)
Validity Period
36 months