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外観
無色～うすい黄色透明液体
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用途
PGF2α 誘導体です。プロス
ラグンジン作用を示します。
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効能
抗緑内障薬, プロスタグランジンF受容体作動薬
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商品名
キサラタン (ファイザー)
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説明
Xalatan was launched in Sweden, Switzerland and the US for the treatment
of glaucoma. It can be synthesized, from the Corey lactone, using standard
prostaglandin chemistry. Latanoprost is a PGF2α, analog that is more lipophilic thus
is better able to penetrate the cornea. The (15R)-diastereomer has only 10% of the
activity compared to the (15S)-diastereomer. It is a selective FP receptor agonist
with little or no effect on the other prostanoid receptors. The antiglaucoma effects
are the result of reduced intraocular pressure arising by increasing uveoscleral
outflow with little or no effect on trabeculo-canalicular aqueous outflow and no effect
on retinal vasculation or permeability of the blood-aqueous barrier. The topical
application is sufficient for a single daily dosage and is well tolerated with no
detectible conjunctival hyperaemia.
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化学的特性
Light Yellow Thick Oil
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使用
Latanoprost is the isopropyl ester of 17-phenyl-13,14-dihydro prostaglandin F2α (17-phenyl-13,14-dihydro PGF2α). It is a prodrug form of the free acid, which is a potent agonist of the FP receptor in the eye. Latanoprost reduces intraocular pressure in glaucoma patients with few side effects. The EC50 value of latanoprost (tested as the free acid) for FP receptors is 3.6 nM.
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定義
ChEBI: A prostaglandin Falpha that is the isopropyl ester prodrug of latanoprost free acid. Used in the treatment of open-angle glaucoma and ocular hypertension.
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一般的な説明
Latanoprost (Xalatan) is available as a 0.005% sterileophthalmic solution in a 2.5-mL dispenser bottle.Latanoprost is also marketed as a combination ophthalmicproduct with the β-adrenergic blocking agent, timolol,which apparently enhances IOP-lowering by decreasing theproduction of aqueous humor. Cautions and side effects aresimilar to those for other ophthalmic prostanoids.
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安全性プロファイル
A poison by ingestion
and intravenous route. Human systemic
effects. When heated to decomposition it
emits acrid smoke and irritating vapors.
