Pharmacodynamics and pharmacokinetics of epidural ropivacaine in humans. 1990

J A Katz, and P O Bridenbaugh, and D C Knarr, and S H Helton, and D D Denson
Department of Anesthesia, University of Cincinnati College of Medicine, OH 45267-0531.

The purpose of this study was to characterize the pharmacodynamics and pharmacokinetics of three concentrations of the new long-acting amide local anesthetic, ropivacaine, given epidurally in 15 physical status ASA I or II patients for elective lower-extremity orthopedic procedures using a nonrandomized open-label design. Three groups of five patients each received either 0.5%, 0.75%, or 1.0% ropivacaine. Upper and lower levels of analgesia to pinprick were determined at frequent intervals until normal sensation had completely returned. Motor blockade was assessed by use of a modified Bromage scale after each determination of level of analgesia. Fifteen venous blood samples were collected over 12 h after ropivacaine injection. Pharmacokinetic parameters were derived using serum concentration-time data. No significant differences were found between the three groups in terms of onset or recovery of motor and sensory blockade. Median maximum thoracic levels of analgesia achieved were 8, 6, and 5 for the 0.5%, 0.75%, and 1.0% groups, respectively, and occurred at 29 +/- 11, 37 +/- 21, and 30 +/- 9 min. Respective times to two-segment regression were 2.8 +/- 1.0, 3.0 +/- 0.5, and 2.9 +/- 0.6 h. Total durations of sensory blockade were 5.4 +/- 0.7, 6.5 +/- 0.4, and 6.8 +/- 0.8 h, respectively. No statistically significant differences were noted between the three groups in terms of clearance (CL). The mean residence time (MRT) was significantly longer for the 0.5% group when compared with the 1% group. The peak concentration (Cmax) for the 0.5% group was found to be significantly lower than for either the 0.75% or 1% groups.(ABSTRACT TRUNCATED AT 250 WORDS)

UI MeSH Term Description Entries
D008297 Male Males
D008657 Metabolic Clearance Rate Volume of biological fluid completely cleared of drug metabolites as measured in unit time. Elimination occurs as a result of metabolic processes in the kidney, liver, saliva, sweat, intestine, heart, brain, or other site. Total Body Clearance Rate,Clearance Rate, Metabolic,Clearance Rates, Metabolic,Metabolic Clearance Rates,Rate, Metabolic Clearance,Rates, Metabolic Clearance
D008875 Middle Aged An adult aged 45 - 64 years. Middle Age
D005260 Female Females
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000077212 Ropivacaine An anilide used as a long-acting local anesthetic. It has a differential blocking effect on sensory and motor neurons. 1-Propyl-2',6'-pipecoloxylidide,AL 381,AL-381,LEA 103,LEA-103,Naropeine,Naropin,Ropivacaine Hydrochloride,Ropivacaine Monohydrochloride,Ropivacaine Monohydrochloride, (S)-isomer,1 Propyl 2',6' pipecoloxylidide,AL381,LEA103
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults
D000577 Amides Organic compounds containing the -CO-NH2 radical. Amides are derived from acids by replacement of -OH by -NH2 or from ammonia by the replacement of H by an acyl group. (From Grant & Hackh's Chemical Dictionary, 5th ed) Amide
D000767 Anesthesia, Epidural Procedure in which an anesthetic is injected into the epidural space. Anesthesia, Extradural,Anesthesia, Peridural,Epidural Anesthesia,Anesthesias, Epidural,Anesthesias, Extradural,Anesthesias, Peridural,Epidural Anesthesias,Extradural Anesthesia,Extradural Anesthesias,Peridural Anesthesia,Peridural Anesthesias
D000779 Anesthetics, Local Drugs that block nerve conduction when applied locally to nerve tissue in appropriate concentrations. They act on any part of the nervous system and on every type of nerve fiber. In contact with a nerve trunk, these anesthetics can cause both sensory and motor paralysis in the innervated area. Their action is completely reversible. (From Gilman AG, et. al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed) Nearly all local anesthetics act by reducing the tendency of voltage-dependent sodium channels to activate. Anesthetics, Conduction-Blocking,Conduction-Blocking Anesthetics,Local Anesthetic,Anesthetics, Topical,Anesthetic, Local,Anesthetics, Conduction Blocking,Conduction Blocking Anesthetics,Local Anesthetics,Topical Anesthetics

Related Publications

J A Katz, and P O Bridenbaugh, and D C Knarr, and S H Helton, and D D Denson
September 2007, Anesthesia and analgesia,
J A Katz, and P O Bridenbaugh, and D C Knarr, and S H Helton, and D D Denson
May 1994, Methods and findings in experimental and clinical pharmacology,
J A Katz, and P O Bridenbaugh, and D C Knarr, and S H Helton, and D D Denson
January 1986, International anesthesiology clinics,
J A Katz, and P O Bridenbaugh, and D C Knarr, and S H Helton, and D D Denson
July 1985, Journal of pharmaceutical sciences,
J A Katz, and P O Bridenbaugh, and D C Knarr, and S H Helton, and D D Denson
October 2001, Anesthesia and analgesia,
J A Katz, and P O Bridenbaugh, and D C Knarr, and S H Helton, and D D Denson
January 1999, Tobacco control,
J A Katz, and P O Bridenbaugh, and D C Knarr, and S H Helton, and D D Denson
October 1989, Blood,
J A Katz, and P O Bridenbaugh, and D C Knarr, and S H Helton, and D D Denson
July 1985, Journal of pharmaceutical sciences,
J A Katz, and P O Bridenbaugh, and D C Knarr, and S H Helton, and D D Denson
August 2006, Annals of the New York Academy of Sciences,
J A Katz, and P O Bridenbaugh, and D C Knarr, and S H Helton, and D D Denson
April 1995, Clinical pharmacology and therapeutics,
Copied contents to your clipboard!