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Pharmacokinetics of dextromoramide in surgical patients
Pharmacological Research Communications, VoL 20, Supplement II, 1988
PHARMACOKINETICS OF DEXTROMORAMIDE N. Barzaghi, E. P e r u c c a
25
IN SURGICAL PATIENTS
I. Pagani, F. Crema, D. Ego I, V. Rovei I
and
Departments of Pharmacology and A n e s t h e s i o l o g y , U n i v e r s i t y o f Pavia, Pavia, Italy and D e l a l a n d e Research L a b o r a t o r i e s , R u e i l - g a l m a i s o n , France Key words: Dextromoramide, P h a r m a c o k i n e t i c s Although dextromoramide has been in clinical use for more than 30 years, the lack of an adequate method for determining the drug in body fluids has hampered previous attempts to characterize its pharmacokinetics
in man. In the present study, a newly
developed highly sensitive and specific GC-MS method was used to determine plasma dextromoramide levels in 9 patients aged 18-63 years who were given a single oral 7.5 mg dose of the drug as part of standard premedication for minor surgical procedures. In addition to dextromoramide,
8 patients received an anticho-
linergic agent and subarachnoidal anesthesia with lidocaine and/or bupivacaine. One patient received general anesthesia. Dextromoram[de was absorbed relatively rapidly, peak plasma concentrations ranging from 68 to 177 ng/ml being usually detected within 2-4 hours of administration.
In 5 subjects, the
decline of plasma dextromoramide concentration followed a biphasic pattern, with an apparent terminal half-life of 5 to 22 hours.
In the remaihing 4 subjects,
the half-life calculated
over the period between 4 and I0 hours after dosing ranged from 1.5 to 4.7 hours. The concentration of the drug in CSF samples collected via the subarachnoidal
line 1 hour after administra-
tion was al~$ays below the detection limit of the method (2ng/m~. Less than 0.06% of the administered dose was excreted unchanged in urine within 8 hours.
PHARMACOKINETICS OF DEXTROMORAMIDE N. Barzaghi, E. P e r u c c a
25
IN SURGICAL PATIENTS
I. Pagani, F. Crema, D. Ego I, V. Rovei I
and
Departments of Pharmacology and A n e s t h e s i o l o g y , U n i v e r s i t y o f Pavia, Pavia, Italy and D e l a l a n d e Research L a b o r a t o r i e s , R u e i l - g a l m a i s o n , France Key words: Dextromoramide, P h a r m a c o k i n e t i c s Although dextromoramide has been in clinical use for more than 30 years, the lack of an adequate method for determining the drug in body fluids has hampered previous attempts to characterize its pharmacokinetics
in man. In the present study, a newly
developed highly sensitive and specific GC-MS method was used to determine plasma dextromoramide levels in 9 patients aged 18-63 years who were given a single oral 7.5 mg dose of the drug as part of standard premedication for minor surgical procedures. In addition to dextromoramide,
8 patients received an anticho-
linergic agent and subarachnoidal anesthesia with lidocaine and/or bupivacaine. One patient received general anesthesia. Dextromoram[de was absorbed relatively rapidly, peak plasma concentrations ranging from 68 to 177 ng/ml being usually detected within 2-4 hours of administration.
In 5 subjects, the
decline of plasma dextromoramide concentration followed a biphasic pattern, with an apparent terminal half-life of 5 to 22 hours.
In the remaihing 4 subjects,
the half-life calculated
over the period between 4 and I0 hours after dosing ranged from 1.5 to 4.7 hours. The concentration of the drug in CSF samples collected via the subarachnoidal
line 1 hour after administra-
tion was al~$ays below the detection limit of the method (2ng/m~. Less than 0.06% of the administered dose was excreted unchanged in urine within 8 hours.