新規緑内障治療薬ラタノプロスト(キサラタン)の薬理作用

  • 野村 俊治
    ファルマシア・アップジョン株式会社研究開発部門研究統括部
  • 橋本 宗弘
    ファルマシア・アップジョン株式会社研究開発部門研究統括部

書誌事項

タイトル別名
  • Pharmacological profiles of latanoprost (Xalatan), a novel anti-glaucoma drug.
  • シンヤク ショウカイ ソウセツ シンキ リョクナイショウ チリョウヤク ラタノプロスト キサラタン ノ ヤクリ サヨウ

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説明

Latanoprost is a novel prostaglandin F (PGF) derivative. Topically applied latanoprost into the glaucomatous monkey eyes lowered intraocular pressure (IOP). Latanoprost, however, failed to produce the hypotensive effect in either rabbit or cat eyes. This species difference may be attributed to its high selectivity for the FP receptor and differences in prostaglandin receptor subtypes existed in the eye amongst these species. In ligand binding studies with bovine corpus luteum cell membranes, the Kd value for the FP receptor of latanoprost was the same as that for PGF, 2.8 nM. Latanoprost augmented uveoscleral outflow (Uv) in monkeys without affecting trabecular outflow or outflow facility like PGF. Although the precise mechanism of the increase in Uv is not fully understood, it is suggested that a decrease in extracellular matrix components in ciliary muscle may contribute to the increase in Uv. On the other hand, an increase in blood flow at the optic nerve head and neuroprotective action in addition to the IOP lowering effect may contribute to the efficacy of latanoprost in glaucoma therapy. Only tolerable conjunctival hyperemia was seen in rabbits. A phase III clinical trial revealed latanoprost (0.005%) once daily produced sustained reduction of IOP in ocular hypertension or primary open-angle glaucoma patients to a greater extent than timolol did. Furthermore, the effects of latanoprost on aqueous humor dynamics in normal human volunteers were similar to those in monkeys, indicating that latanoprost lowers IOP by the increase in Uv in humans.

収録刊行物

  • 日本薬理学雑誌

    日本薬理学雑誌 115 (5), 280-286, 2000

    公益社団法人 日本薬理学会

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