Patients with severe renal impairment do not require dose adjustment of roflumilast A. Drollmann, M. Hartmann, K. Zech, M. David, C. Weimar, T. D. Bethke (Konstanz, Germany)
Source: Annual Congress 2002 - Asthma and COPD: pharmacology
Session: Asthma and COPD: pharmacology Session type: Thematic Poster Session Number: 743
Disease area: Airway diseasesAbstract Roflumilast (ROF) is a novel, orally active, selective PDE4 inhibitor for treatment of COPD and asthma. In this study, we evaluated the impact of severe renal impairment on the pharmacokinetics of ROF and its active metabolite ROF-N-oxide. In an open label, parallel group comparison, 12 patients with severe renal impairment (10 [lte] CLCr [lte] 30 ml/min/1.73 m2 ) and 12 healthy control subjects (matched according to sex, age, weight and height) received a single oral dose of 500μg ROF. Plasma concentrations of ROF and ROF-N-oxide were measured by HPLC. No relevant changes in vital signs, ECG, or laboratory parameters were observed and no serious adverse events occurred. Geometric means of pharmacokinetic characteristics of ROF and ROF-N-oxide in patients with severe renal impairment and in healthy subjects are given in the table below.
Geometric means (68%-range)
Severe renal impairment
Healthy
ROF AUC [μg*h/l]
35.5 (23.7 - 53.0)
44.7 (33.5 - 59.7)
Cmax [μg/l]
4.3 (2.7 - 6.6)
5.1 (3.6 - 7.1)
t1/2 [h]
22.1 (14.2 - 34.4)
18.5 (11.4 - 30.0)
ROF-N-oxide AUC [μg*h/l]
428.9 (334.2 - 550.5)
461.2 (366.2 - 580.7)
Cmax [μg/l]
6.8 (5.4 - 8.7)
7.8 (6.4 - 9.5)
t1/2 [h]
37.4 (21.9 - 63.9)
28.7 (22.0 - 37.5)
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A. Drollmann, M. Hartmann, K. Zech, M. David, C. Weimar, T. D. Bethke (Konstanz, Germany). Patients with severe renal impairment do not require dose adjustment of roflumilast. Eur Respir J 2002; 20: Suppl. 38, 743
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