Pharmacokinetics of 8-phenyltheophylline in the rat.
The pharmacokinetics of the adenosine antagonist 8-phenyltheophylline (8-PT) have been investigated in the rat. After intravenous administration to male rats with normal renal function, 8-PT was rapidly cleared from plasma with a t1/2 of about 14 min. Its apparent volume of distribution was some 76 mL/100 g and plasma clearance was 3.5 mL min-1/100 g. Injection via the carotid artery did not alter the kinetics of 8-PT, but when given through the portal vein a first-pass effect was observed. Moreover, 8-PT could not be detected in plasma following intraperitoneal injection. The kinetics of 8-PT were not altered in male rats with acute renal failure and no difference was noted between male and female animals with respect to the kinetics of 8-PT following intravenous injection. It is concluded that the pharmacokinetic properties of 8-PT are likely to complicate its use in-vivo.
Wormald
A
A
Department of Pharmacology, University of Leeds, UK.
Bowmer
C J
CJ
Yates
M S
MS
Collis
M G
MG
D058186:Acute Kidney Injury / Q000188:drug therapy / Q000378:metabolism; D000818:Animals; D002851:Chromatography, High Pressure Liquid; D005260:Female; D006207:Half-Life; D007269:Injections, Intra-Arterial; D007275:Injections, Intravenous; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013806:Theophylline / Q000031:analogs & derivatives* / Q000493:pharmacokinetics
D013806:Theophylline; C028322:8-phenyltheophylline