title: Pharmacokinetics of ipratropium bromide after single dose inhalation and oral and intravenous administration.
abstract: Single doses of ipratropium bromide were administered intravenously, orally and by slow inhalation to ten healthy male volunteers. The plasma level after oral administration followed a low but broad plateau persisting for several hours. After i.v. administration the kinetic parameters were: Vc = 25.9 l, V alpha = 13.1 l, V beta = 3.38 l, t1/2 alpha = 3.85 min, t1/2 beta = 98.4 min, AUC = 15.0 h.ng/ml, kel = 11.8 l/h and total clearance is 2325 ml/min. The bioavailability was 3.3% (range 0.9-6.1%) on comparing the plasma AUCs following i.v. and 20 mg oral administration. The cumulative renal excretion (0-24 h) after i.v. administration was compared with that after oral administration and inhalation. Following oral administration, the apparent systemic availability was around 2%, and after inhalation it was 6.9%. In comparison with oral placebo administration, only after i.v. administration was there a significant change in heart rate (from 63.7 to 90.2 beats/min). The systolic blood pressure rose from 115.1 to 119.6 mm Hg and the diastolic blood pressure from 68.3 to 78.3 mm Hg.
authors.affiliation: Department of Toxicology, State University, Groningen, The Netherlands.
authors.forename: K
authors.initials: K
authors.lastname: Ensing
authors.forename: R A
authors.initials: RA
authors.lastname: de Zeeuw
authors.forename: G D
authors.initials: GD
authors.lastname: Nossent
authors.forename: G H
authors.initials: GH
authors.lastname: Koëter
authors.forename: P J
authors.initials: PJ
authors.lastname: Cornelissen
mesh_terms: D000280:Administration, Inhalation; D000284:Administration, Oral; D000328:Adult; D001286:Atropine Derivatives / Q000493:pharmacokinetics*; D001682:Biological Availability; D001794:Blood Pressure / Q000187:drug effects; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D007275:Injections, Intravenous; D009241:Ipratropium / Q000493:pharmacokinetics* / Q000652:urine; D008297:Male
chemical_list: D001286:Atropine Derivatives; D009241:Ipratropium