Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:dateCreated
1991-6-4
pubmed:abstractText
Clarithromycin is metabolised in man mainly to the 14-hydroxy derivative, which is also biologically active. As this metabolite is not produced in rodents, we used a murine model of Haemophilus influenzae pulmonary infection to compare the in-vivo activity of clarithromycin and 14-hydroxy clarithromycin, alone and in combination, and erythromycin. In terms of bacterial killing, clarithromycin's 14-hydroxy metabolite was much more active than clarithromycin and erythromycin at doses of 100 mg/kg. For the combination tests, low doses of 14-hydroxy clarithromycin (12, 16 and 24 mg/kg) were ineffective alone but potentiated the bactericidal activity of clarithromycin (100 mg/kg) (P less than 0.01-0.001). The in-vivo results can be explained by in-vitro and pharmacokinetic data: the MIC and MBC of 14-hydroxy clarithromycin are half those of clarithromycin and erythromycin, while the combination of clarithromycin and its metabolite was synergistic in terms of bacteriostatic and bactericidal activities. Potentially useful levels of 14-hydroxy clarithromycin were found after oral administration of low doses, with a prolonged half-life compared with that of the parent compound. On the basis of these results it appears that the 14-hydroxy metabolite may have an important role to play in the treatment of bronchopulmonary infections in man due to H. influenzae.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Feb
pubmed:issn
0305-7453
pubmed:author
pubmed:issnType
Print
pubmed:volume
27 Suppl A
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
31-41
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1991
pubmed:articleTitle
Individual and combined activities of clarithromycin and its 14-hydroxy metabolite in a murine model of Haemophilus influenzae infection.
pubmed:affiliation
Department of Microbiology, C.H.U. Xavier Bichat, Paris, France.
pubmed:publicationType
Journal Article, Comparative Study