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The concentrations of clarithromycin and its 14-hydroxy metabolite in sputum of patients with bronchiectasis following single dose oral administration

The concentrations of clarithromycin and its 14-hydroxy metabolite in sputum of patients with bronchiectasis following single dose oral administration
The concentrations of clarithromycin and its 14-hydroxy metabolite in sputum of patients with bronchiectasis following single dose oral administration

Clarithromycin and its metabolite, 14-hydroxy-clarithromycin are active against a wide range of respiratory pathogens. Antibiotics generally penetrate poorly into respiratory secretions which may therefore continue to harbour bacteria following bronchial infection. We have studied sputum and serum concentrations of clarithromycin and 14-hydroxy-clarithromycin in eight patients with idiopathic bronchiectasis without infective exacerbations (five male, three female; mean age 53.3 years). Oral single dose administration of 250 or 500 mg clarithromycin, separated by at least 6 days, was given to each patient. Serum and sputum samples were collected (the latter by physiotherapy at 0, 1, 2, 4, 8, 24 and 0, 4, 8 and 24 h respectively after administration of each dose. Serum sol phase was obtained by high speed centrifugation and concentrations of clarithromycin and 14-hydroxy-clarithromycin were determined by high performance liquid chromatography. Serum Cmax for clarithromycin and 14-hydroxy-clarithromycin were 1.20 mg/L (3 h) and 0.37 mg/L (3.1 h) for clarithromycin (250 mg)) and were 2.78 mg/L (2.5 h) and 0.68 mg/L (2.6 h) for clarithromycin (500 mg) respectively. Sputum Cmax for clarithromycin and 14-hydroxy-clarithromycin were 0.52 mg/L (5 h) and 0.30 mg/L (5.5 h) for clarithromycin (250 mg) and were 1.59 mg/L (5 h) and 0.47 mg/L (5.5 h) for clarithromycin (500 mg) respectively. The sputum/serum percentage ratios at Cmax (sputum) for clarithromycin and 14-hydroxy-clarithromycin were 74.3% and 113.9% (250 mg) and 94.7% and 99.9% (500 mg) respectively. We conclude that oral administration of clarithromycin to patients with bronchiectasis results in rapid penetration into respiratory mucus with persistent drug concentrations that exceed its MIC for many respiratory pathogens.

Administration, Oral, Adult, Aged, Bronchiectasis, Clarithromycin, Drug Administration Schedule, Female, Humans, Male, Middle Aged, Sputum, Journal Article, Research Support, Non-U.S. Gov't
0305-7453
289-297
Tsang, K.W.
7bc32883-8dad-4c92-8ffc-074f6708c0aa
Roberts, P.
c0b2254d-e9cc-4285-82b1-a8a4594a2038
Read, R.C.
b5caca7b-0063-438a-b703-7ecbb6fc2b51
Kees, F.
22c2fbfb-b0f5-4299-b6a9-211ad237b083
Wilson, R.
94eba368-b33f-4071-beb6-dac98ef23651
Cole, P.J.
8d93f747-e6ed-4557-89ea-e12e0925bbf3
Tsang, K.W.
7bc32883-8dad-4c92-8ffc-074f6708c0aa
Roberts, P.
c0b2254d-e9cc-4285-82b1-a8a4594a2038
Read, R.C.
b5caca7b-0063-438a-b703-7ecbb6fc2b51
Kees, F.
22c2fbfb-b0f5-4299-b6a9-211ad237b083
Wilson, R.
94eba368-b33f-4071-beb6-dac98ef23651
Cole, P.J.
8d93f747-e6ed-4557-89ea-e12e0925bbf3

Tsang, K.W., Roberts, P., Read, R.C., Kees, F., Wilson, R. and Cole, P.J. (1994) The concentrations of clarithromycin and its 14-hydroxy metabolite in sputum of patients with bronchiectasis following single dose oral administration. Journal of Antimicrobial Chemotherapy, 33 (2), 289-297. (doi:10.1093/jac/33.2.289).

Record type: Article

Abstract

Clarithromycin and its metabolite, 14-hydroxy-clarithromycin are active against a wide range of respiratory pathogens. Antibiotics generally penetrate poorly into respiratory secretions which may therefore continue to harbour bacteria following bronchial infection. We have studied sputum and serum concentrations of clarithromycin and 14-hydroxy-clarithromycin in eight patients with idiopathic bronchiectasis without infective exacerbations (five male, three female; mean age 53.3 years). Oral single dose administration of 250 or 500 mg clarithromycin, separated by at least 6 days, was given to each patient. Serum and sputum samples were collected (the latter by physiotherapy at 0, 1, 2, 4, 8, 24 and 0, 4, 8 and 24 h respectively after administration of each dose. Serum sol phase was obtained by high speed centrifugation and concentrations of clarithromycin and 14-hydroxy-clarithromycin were determined by high performance liquid chromatography. Serum Cmax for clarithromycin and 14-hydroxy-clarithromycin were 1.20 mg/L (3 h) and 0.37 mg/L (3.1 h) for clarithromycin (250 mg)) and were 2.78 mg/L (2.5 h) and 0.68 mg/L (2.6 h) for clarithromycin (500 mg) respectively. Sputum Cmax for clarithromycin and 14-hydroxy-clarithromycin were 0.52 mg/L (5 h) and 0.30 mg/L (5.5 h) for clarithromycin (250 mg) and were 1.59 mg/L (5 h) and 0.47 mg/L (5.5 h) for clarithromycin (500 mg) respectively. The sputum/serum percentage ratios at Cmax (sputum) for clarithromycin and 14-hydroxy-clarithromycin were 74.3% and 113.9% (250 mg) and 94.7% and 99.9% (500 mg) respectively. We conclude that oral administration of clarithromycin to patients with bronchiectasis results in rapid penetration into respiratory mucus with persistent drug concentrations that exceed its MIC for many respiratory pathogens.

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More information

Published date: February 1994
Keywords: Administration, Oral, Adult, Aged, Bronchiectasis, Clarithromycin, Drug Administration Schedule, Female, Humans, Male, Middle Aged, Sputum, Journal Article, Research Support, Non-U.S. Gov't

Identifiers

Local EPrints ID: 416954
URI: https://eprints.soton.ac.uk/id/eprint/416954
ISSN: 0305-7453
PURE UUID: 41bae1b9-0d93-4fcb-a363-740c4670ccfb
ORCID for R.C. Read: ORCID iD orcid.org/0000-0002-4297-6728

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Date deposited: 15 Jan 2018 17:31
Last modified: 14 Mar 2019 01:36

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Contributors

Author: K.W. Tsang
Author: P. Roberts
Author: R.C. Read ORCID iD
Author: F. Kees
Author: R. Wilson
Author: P.J. Cole

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