Measurement of blood concentrations of FK506 (tacrolimus) and its metabolites in seven liver graft patients after the first dose by h.p.l.c.-MS and microparticle enzyme immunoassay (MEIA).

Abstract:

:1. Blood and urine concentrations of the macrolide immunosuppressant FK506 and its metabolites were measured in seven orthotopic liver transplant patients after the first oral dose of FK506 (0.04 +/- 0.02 mg kg-1) used as primary immunosuppressant. A specific h.p.l.c.-MS assay was used, allowing the measurement of parent drug and eight metabolites. Results were compared with those obtained using a microparticle enzyme immunoassay (MEIA). 2. Blood drug concentrations were described by an open two compartment model with first-order absorption giving the following mean data: tmax: 1.9 (h), Cmax: 17.4 (microgram l-1), AUC: 328.1 (microgram l-1 h), t1/2,1: 0.74 (h). The terminal elimination half-life was estimated at about 26 h using the h.p.l.c.-MS assay. 3. The metabolites found in blood were demethyl-FK506 and demethyl-hydroxy-FK506, while in urine FK506 and eight of its metabolites were detected.

journal_name

Br J Clin Pharmacol

authors

Gonschior AK,Christians U,Braun F,Winkler M,Linck A,Baumann J,Sewing KF

doi

10.1111/j.1365-2125.1994.tb04398.x

subject

Has Abstract

pub_date

1994-12-01 00:00:00

pages

567-71

issue

6

eissn

0306-5251

issn

1365-2125

journal_volume

38

pub_type

临床试验,杂志文章
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  • Experience with labetalol in hypertension.

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    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1111/j.1365-2125.1983.tb02114.x

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  • Hypnotic efficacy and safety of midazolam and oxazepam in hospitalized female patients.

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    pub_type: 临床试验,杂志文章

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    pub_type: 临床试验,杂志文章

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    pub_type: 杂志文章

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    pub_type: 临床试验,杂志文章,随机对照试验

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    doi:10.1111/j.1365-2125.1990.tb03692.x

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