Simultaneous determination of pethidine pharmacokinetics in rats: The impact of tramadol coadministration
The rats model has never thoroughly investigated the influence of tramadol on plasma pethidine concentration besides pethidine pharmacokinetics. Individually, analgesic ED<sub>50</sub>s for pethidine and tramadol are estimated as 3.55 and 24.21 mg/kg, i.p. Subsequently, their measures de...
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University of Mosul, College of Veterinary Medicine
2023-01-01
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Series: | Iraqi Journal of Veterinary Sciences |
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Online Access: | https://www.vetmedmosul.com/article_176550_e468ffcf6d1cd62e5c0c7fdf841e0d3b.pdf |
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author | Yaareb J. Mousa Mahmood B. Mahmood Zainab T. Mohammed |
author_facet | Yaareb J. Mousa Mahmood B. Mahmood Zainab T. Mohammed |
author_sort | Yaareb J. Mousa |
collection | DOAJ |
description | The rats model has never thoroughly investigated the influence of tramadol on plasma pethidine concentration besides pethidine pharmacokinetics. Individually, analgesic ED<sub>50</sub>s for pethidine and tramadol are estimated as 3.55 and 24.21 mg/kg, i.p. Subsequently, their measures decreased to 1.65 and 11.27 mg/kg, i.p., when both were given in combination at 1:1 from ED<sub>50</sub>s. Tramadol and pethidine have a form of synergistic analgesic interaction, which is therefore classified as a pharmacodynamic interaction. Pethidine (7.1mg/kg, i.p.) reveals the plasma concentration of 369.00, 493.33, 373.33, 305.33, 306.33 and 247.67 µg/ml that was measured over distinctive times of 0.25,0.5,1,2,4, and 24 hours. At the same time, the concentration of plasma levels of tramadol and pethidine (48.42 and 7.1mg/kg, i.p., correspondingly) declined to 229.33, 268.33, 233.00, 198.33, 195.67 and 180.33 µg/ml by 38, 46, 38, 35, 36 and 27%, respectively. Tramadol affected the pethidine pharmacokinetics through an elevation in the area-under-curve (AUC<sub>0-∞</sub>) 49%, area-under-moment-curve (AUMC<sub>0-∞</sub>) 343%, mean-residence-time (MRT) 137%, half-life (t<sub>1/2β</sub>) 136%, and the distribution volume (V<sub>ss</sub>) 64%. Other estimated pharmacokinetic measures were reduced which included maximal concentration (C<sub>max</sub>) 47% and elimination rate constant (K<sub>el</sub>) 60%. In general, the findings revealed a synergism as a mode of pharmacological interaction between pethidine and tramadol, in addition to a change in pethidine pharmacokinetics, which could improve pethidine effectiveness in the rat’s model. |
first_indexed | 2024-04-11T04:40:05Z |
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issn | 1607-3894 2071-1255 |
language | Arabic |
last_indexed | 2024-04-11T04:40:05Z |
publishDate | 2023-01-01 |
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series | Iraqi Journal of Veterinary Sciences |
spelling | doaj.art-46e826d7f5d84f6484e2187f9a9cc0fd2022-12-28T06:28:35ZaraUniversity of Mosul, College of Veterinary MedicineIraqi Journal of Veterinary Sciences1607-38942071-12552023-01-0137126126710.33899/ijvs.2022.133824.2307176550Simultaneous determination of pethidine pharmacokinetics in rats: The impact of tramadol coadministrationYaareb J. Mousa0Mahmood B. Mahmood1Zainab T. Mohammed2Department of Physiology, Biochemistry, and Pharmacology, College of Veterinary Medicine, University of Mosul, Mosul, IraqDepartment of Internal Medicine, Surgery and Pharmacology, College of Veterinary Medicine, University of Dohuk, Dohuk, IraqDepartment of Internal Medicine, Surgery and Pharmacology, College of Veterinary Medicine, University of Dohuk, Dohuk, IraqThe rats model has never thoroughly investigated the influence of tramadol on plasma pethidine concentration besides pethidine pharmacokinetics. Individually, analgesic ED<sub>50</sub>s for pethidine and tramadol are estimated as 3.55 and 24.21 mg/kg, i.p. Subsequently, their measures decreased to 1.65 and 11.27 mg/kg, i.p., when both were given in combination at 1:1 from ED<sub>50</sub>s. Tramadol and pethidine have a form of synergistic analgesic interaction, which is therefore classified as a pharmacodynamic interaction. Pethidine (7.1mg/kg, i.p.) reveals the plasma concentration of 369.00, 493.33, 373.33, 305.33, 306.33 and 247.67 µg/ml that was measured over distinctive times of 0.25,0.5,1,2,4, and 24 hours. At the same time, the concentration of plasma levels of tramadol and pethidine (48.42 and 7.1mg/kg, i.p., correspondingly) declined to 229.33, 268.33, 233.00, 198.33, 195.67 and 180.33 µg/ml by 38, 46, 38, 35, 36 and 27%, respectively. Tramadol affected the pethidine pharmacokinetics through an elevation in the area-under-curve (AUC<sub>0-∞</sub>) 49%, area-under-moment-curve (AUMC<sub>0-∞</sub>) 343%, mean-residence-time (MRT) 137%, half-life (t<sub>1/2β</sub>) 136%, and the distribution volume (V<sub>ss</sub>) 64%. Other estimated pharmacokinetic measures were reduced which included maximal concentration (C<sub>max</sub>) 47% and elimination rate constant (K<sub>el</sub>) 60%. In general, the findings revealed a synergism as a mode of pharmacological interaction between pethidine and tramadol, in addition to a change in pethidine pharmacokinetics, which could improve pethidine effectiveness in the rat’s model.https://www.vetmedmosul.com/article_176550_e468ffcf6d1cd62e5c0c7fdf841e0d3b.pdfpethidinepharmacokineticsplasmaratstramadol |
spellingShingle | Yaareb J. Mousa Mahmood B. Mahmood Zainab T. Mohammed Simultaneous determination of pethidine pharmacokinetics in rats: The impact of tramadol coadministration Iraqi Journal of Veterinary Sciences pethidine pharmacokinetics plasma rats tramadol |
title | Simultaneous determination of pethidine pharmacokinetics in rats: The impact of tramadol coadministration |
title_full | Simultaneous determination of pethidine pharmacokinetics in rats: The impact of tramadol coadministration |
title_fullStr | Simultaneous determination of pethidine pharmacokinetics in rats: The impact of tramadol coadministration |
title_full_unstemmed | Simultaneous determination of pethidine pharmacokinetics in rats: The impact of tramadol coadministration |
title_short | Simultaneous determination of pethidine pharmacokinetics in rats: The impact of tramadol coadministration |
title_sort | simultaneous determination of pethidine pharmacokinetics in rats the impact of tramadol coadministration |
topic | pethidine pharmacokinetics plasma rats tramadol |
url | https://www.vetmedmosul.com/article_176550_e468ffcf6d1cd62e5c0c7fdf841e0d3b.pdf |
work_keys_str_mv | AT yaarebjmousa simultaneousdeterminationofpethidinepharmacokineticsinratstheimpactoftramadolcoadministration AT mahmoodbmahmood simultaneousdeterminationofpethidinepharmacokineticsinratstheimpactoftramadolcoadministration AT zainabtmohammed simultaneousdeterminationofpethidinepharmacokineticsinratstheimpactoftramadolcoadministration |