Pharmacokinetics, oral bioavailability and tissue distribution of azithromycin in cats.
Azithromycin is the first of a class of antibiotics classified as azalides. In an initial experiment four cats were given a single dose of azithromycin 5 mg/kg orally (p.o.), followed 2 weeks later by a single intravenous bolus (i.v.) dose of 5 mg/kg. Subsequently, six cats were given [14C]azithromycin p.o. in a single dose of 5.4 mg/kg for the study of tissue distribution and metabolism. In both experiments, serial blood samples were collected and the plasma assayed for unchanged azithromycin to determine various pharmacokinetic parameters. After p.o. administration, bioavailability was 58% and absorption rapid with a tmax of 0.85 +/- 0.72 h and a Cmax of 0.97 +/- 0.65 microgram/mL. The harmonic mean terminal t1/2 after i.v. administration was 35 h. Tissue half-lives varied from 13 h in fat to 72 h in cardiac muscle. Three metabolites were identified in bile. Unchanged azithromycin accounted for 100% of the total radioactivity in lung and skin tissues when assayed. In comparison with other species, the bioavailability in cats is higher than in humans but lower than in dogs. As in the dog, > 50% of the azithromycin-related material in feline bile was unchanged azithromycin.
Hunter
R P
RP
Department of Drug Metabolism, Pfizer Inc., Central Research Division, Groton, CT 06340, USA.
Lynch
M J
MJ
Ericson
J F
JF
Millas
W J
WJ
Fletcher
A M
AM
Ryan
N I
NI
Olson
J A
JA
D000042:Absorption / Q000502:physiology; D000273:Adipose Tissue / Q000378:metabolism; D000284:Administration, Oral; D000818:Animals; D017963:Azithromycin / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D001646:Bile / Q000378:metabolism; D001682:Biological Availability; D001921:Brain / Q000378:metabolism; D002247:Carbon Isotopes; D002415:Cats / Q000378:metabolism*; D002851:Chromatography, High Pressure Liquid; D005123:Eye / Q000378:metabolism; D005260:Female; D006207:Half-Life; D007275:Injections, Intravenous / Q000662:veterinary; D007553:Isotope Labeling; D007668:Kidney / Q000378:metabolism; D008099:Liver / Q000378:metabolism; D008168:Lung / Q000378:metabolism; D008297:Male; D013058:Mass Spectrometry; D009132:Muscles / Q000378:metabolism; D009206:Myocardium / Q000378:metabolism; D014018:Tissue Distribution
D002247:Carbon Isotopes; D017963:Azithromycin