title: Pharmacokinetics of imipenem in serum and skin window fluid in healthy adults after intramuscular or intravenous administration.
abstract: The pharmacokinetic profiles of imipenem after intramuscular (i.m.) and intravenous injections were examined in adult volunteers. Levels of imipenem in serum after i.m. injection of a microcrystalline suspension of imipenem-cilastatin (500 mg each) reached a peak (8.0 micrograms/ml) at 1.5 h after administration, and concentrations were maintained in excess of 1.5 micrograms/ml for 6 h. Serum elimination half-life (1.3 h), volume of distribution (14.5 liters), and area under the curve (AUC; 27.8 micrograms.h/ml) after i.m. injection did not significantly differ from those of a comparable dose given by intravenous infusion. Bioavailability after i.m. injection was 89%. Imipenem levels in skin window fluid after i.m. administration were maximal (4.3 micrograms/ml) at 4 h after injection, at which time imipenem concentrations exceeded those produced by intravenous infusion. The AUCskin window/AUCserum ratio for skin window fluid after i.m. injection was 68%, indicating good penetration of the drug into skin fluid. This study shows that i.m. injection of 500 mg of imipenem-cilastatin results in concentrations of imipenem in serum and skin fluid that are, for at least 6 h, consistent with antimicrobial activity against susceptible organisms.
authors.affiliation: Department of Pharmacology, Northeastern Ohio Universities College of Medicine, Rootstown 44272.
authors.forename: S A
authors.initials: SA
authors.lastname: Signs
authors.forename: J S
authors.initials: JS
authors.lastname: Tan
authors.forename: S J
authors.initials: SJ
authors.lastname: Salstrom
authors.forename: T M
authors.initials: TM
authors.lastname: File
mesh_terms: D000328:Adult; D001682:Biological Availability; D015377:Cilastatin / Q000008:administration & dosage / Q000493:pharmacokinetics; D006801:Humans; D015378:Imipenem / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D007262:Infusions, Intravenous; D007273:Injections, Intramuscular; D008297:Male; D008875:Middle Aged; D012867:Skin / Q000378:metabolism*
chemical_list: D015377:Cilastatin; D015378:Imipenem