他克莫司软膏说明书(英文PDR).pdf

PDR - Protopic Ointment ((Fujisawa)) 页码,1/12
PDR? Electronic Library(TM)
This report is based solely on product labeling as published by Physicians?Desk Reference ? Copyright ?2003 Thomson Medical
Economics. All rights reserved.

Report generated 09-06-2004 at 08:02 pm

Protopic Ointment(Fujisawa)

FOR DERMATOLOGIC USE ONLY
NOT FOR OPHTHALMIC USE
DESCRIPTION
PROTOPIC (tacrolimus) Ointment contains tacrolimus, a macrolide immunosuppressant produced by Streptomyces tsukubaensis . It is
for topical dermatologic use only. Chemically, tacrolimus is designated as [3 S -[3 R *[ E (1 S *,3 S *,4 S *)],4 S *,5 R *,8 S *,9 E ,12
R *,14 R *, 15 S *, 16 R *,18 S *,19 S *,26a R *]] - 5,6,8,11,12,13,14,15,16,17,18, 19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-3-
[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylethenyl]-14,16-dimethoxy-4,10,12,18-tetramethyl-8-(2-propenyl)-15, 19-epoxy-3H-
pyrido[2,1- c ][1,4]oxaazacyclotricosine-1,7,20,21(4H,23H)-tetrone, monohydrate. It has the following structural formula:
·
Tacrolimus has an empirical formula of C 44 H 69 NO 12 H 2 O and a formula weight of . Each gram of PROTOPIC Ointment
contains (w/w) either % or % of tacrolimus in a base of mineral oil, paraffin, propylene carbonate, white petrolatum and white
wax.
CLINICAL PHARMACOLOGY
Mechanism of Action
Copyright ?2003 Thomson Medical Economics. All rights reserved.
PDR - Protopic Ointment ((Fujisawa)) 页码,2/12
The mechanism of action of tacrolimus in atopic dermatitis is not known. While the following have been observed, the clinical
significance of these observations in atopic dermatitis is not known. It has been demonstrated that tacrolimus inhibits T-lymphocyte
activation by first binding to an intracellular protein, FKBP-12. plex of tacrolimus-FKBP-12, calcium, calmodulin, and
calcineurin is then formed and the phosphatase activity of calcineurin is inhibited. This effect has been shown to prevent the
dephosphorylation a