title: Pharmacokinetics and pharmacodynamics of edrophonium in elderly surgical patients.
abstract: The effect of age (over 70 yr) on the pharmacokinetics and pharmacodynamics of edrophonium was evaluated in seven patients aged 76-87 yr and in seven patients aged 27-57 yr. When elderly patients were compared with younger controls, the elderly exhibited a statistically significant decreased plasma clearance (5.9 +/- 2 versus 12.1 +/- 4 mL.kg-1.min-1) and a prolonged elimination half-life (84.2 +/- 17 versus 56.6 +/- 16 min). Pharmacodynamically, a higher concentration of edrophonium is required in elderly patients to produce the same effect as in the younger controls. This observation may be explained in part by changes in neuromuscular transmission that are a function of the aging process. In addition, even though plasma concentrations were significantly greater at every sampling point in the elderly than the younger group, there was no difference between either the maximum duration or the total duration of action of edrophonium in the two groups. The maximum duration of action of edrophonium in both groups was very brief (1.3-2.2 min). These results contrast with a previous study of the anticholinesterases neostigmine and pyridostigmine, in which the action of these drugs was significantly prolonged in elderly patients. Explanations for the observed differences between edrophonium and other anticholinesterases may relate to differences in chemical structure and the possibility that edrophonium produces antagonism of neuromuscular blockade by a different mechanism than neostigmine or pyridostigmine.
authors.affiliation: Department of Anesthesiology, College of Physicians and Surgeons, Columbia University, New York, NY 10032.
authors.forename: R S
authors.initials: RS
authors.lastname: Matteo
authors.forename: W L
authors.initials: WL
authors.lastname: Young
authors.forename: E
authors.initials: E
authors.lastname: Ornstein
authors.forename: A E
authors.initials: AE
authors.lastname: Schwartz
authors.forename: P A
authors.initials: PA
authors.lastname: Silverberg
authors.forename: J
authors.initials: J
authors.lastname: Diaz
mesh_terms: D000328:Adult; D000368:Aged; D000369:Aged, 80 and over; D000375:Aging / Q000187:drug effects / Q000378:metabolism; D001921:Brain / Q000601:surgery; D002986:Clinical Trials as Topic; D004491:Edrophonium / Q000097:blood / Q000493:pharmacokinetics / Q000494:pharmacology; D006801:Humans; D008875:Middle Aged; D009469:Neuromuscular Junction / Q000187:drug effects / Q000502:physiology; D009435:Synaptic Transmission / Q000187:drug effects / Q000502:physiology
chemical_list: D004491:Edrophonium