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Loteprednol

产品号 DB00873 公司名称 DrugBank
CAS号 82034-46-6 公司网站 http://www.ualberta.ca/
分子式 C24H31ClO7 电 话 (780) 492-3111
分子量 466.95174 传 真
纯 度 电子邮件 david.wishart@ualberta.ca
保 存 Chembase数据库ID: 751

产品价格信息

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产品别名

标题
Loteprednol
IUPAC标准名
chloromethyl (1S,2R,10S,11S,14R,15S,17S)-14-[(ethoxycarbonyl)oxy]-17-hydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-diene-14-carboxylate
IUPAC传统名
loteprednol etabonate
商标名
Loteflam
Lotemax
Alrex
Zylet
别名
Loteprednol Etabonate

产品登记号

CAS号 82034-46-6

产品性质

疏水性(logP) 3.4
溶解度 5 mg/mL

产品详细信息

详细说明 (English)
Item Information
Drug Groups approved
Description Loteprednol (as Loteprednol Etabonate) is a topical corticoid antiinflammatory. It is used in ophthalmic solution for the treatment of steroid responsive inflammatory conditions of the eye such as allergic conjunctivitis, uveitis, acne rosacea, superficial punctate keratitis, herpes zoster keratitis, iritis, cyclitis, and selected infective conjunctivitides. As a nasal spray, is used for the treatment and management of seasonal allergic rhinitis.
Indication As an ophthalmic it is used for the treatment of steroid responsive inflammatory conditions of the eye such as allergic conjunctivitis, uveitis, acne rosacea, superficial punctate keratitis, herpes zoster keratitis, iritis, cyclitis, and selected infective conjunctivitides. As a nasal spray, used for the treatment and management of seasonal allergic rhinitis.
Pharmacology Loteprednol etabonate (LE) is a "soft" steroid belonging to a unique class of glucocorticoids. LE possesses a metabolically labile 17 beta-chloromethyl ester function which was designed in order to be hydrolyzed to an inactive carboxylic acid moiety. This inactive metabolite is more hydrophilic and is thus readily eliminated from the body. Loteprednol etabonate has good ocular permeation properties and good skin permeation properties similar to "hard" steroids. It is used as a topical agent for the treatment of steroid responsive inflammatory conditions of the eye such as allergic conjunctivitis, uveitis and iritis.
Toxicity Adverse effects include abnormal vision / blurring, burning on instillation, chemosis, discharge, dry eyes, epiphora, foreign body sensation, itching, injection, and photophobia.
Affected Organisms
Humans and other mammals
Biotransformation The drugs 17 beta-chloromethyl ester function is hydrolyzed to an inactive carboxylic acid moiety.
Absorption Very limited systemic absorption, but good absorption at the point of delivery.
References
[Pubmed]
External Links
Wikipedia
RxList
Drugs.com

参考文献