Interactions of fentanyl with blood platelets and plasma proteins: platelet sensitivity to prasugrel metabolite is not affected by fentanyl under in vitro conditions.
Antiplatelet therapy
Blood platelets
Drug carriers
Fentanyl
Platelet activation
Protein binding
Journal
Pharmacological reports : PR
ISSN: 2299-5684
Titre abrégé: Pharmacol Rep
Pays: Switzerland
ID NLM: 101234999
Informations de publication
Date de publication:
Apr 2023
Apr 2023
Historique:
received:
14
09
2022
accepted:
04
01
2023
revised:
03
01
2023
medline:
31
3
2023
pubmed:
17
1
2023
entrez:
16
1
2023
Statut:
ppublish
Résumé
Clinical trials indicate that fentanyl, like morphine, may impair intestinal absorption and thus decrease the efficacy of oral P2Y Blood was obtained from healthy volunteers (19 women and 12 men; mean age 40 ± 13 years). Platelet function was measured in whole blood, platelet-rich plasma and in suspensions of isolated platelets by flow cytometry, impedance and optical aggregometry. Surface plasmon resonance and molecular docking were employed to determine the binding kinetics of fentanyl to human albumin, α When applied at therapeutic and supratherapeutic concentrations under various experimental conditions, fentanyl had no potential to stimulate platelet activation and aggregation, or potentiate platelet response to ADP, nor did it affect platelet susceptibility to prasugrel metabolite in ADP-stimulated platelets. In addition, fentanyl was found to interact with all the examined carrier proteins with dissociation constants in the order of 10 It does not seem that the delayed platelet responsiveness to oral P2Y
Sections du résumé
BACKGROUND
BACKGROUND
Clinical trials indicate that fentanyl, like morphine, may impair intestinal absorption and thus decrease the efficacy of oral P2Y
METHODS
METHODS
Blood was obtained from healthy volunteers (19 women and 12 men; mean age 40 ± 13 years). Platelet function was measured in whole blood, platelet-rich plasma and in suspensions of isolated platelets by flow cytometry, impedance and optical aggregometry. Surface plasmon resonance and molecular docking were employed to determine the binding kinetics of fentanyl to human albumin, α
RESULTS
RESULTS
When applied at therapeutic and supratherapeutic concentrations under various experimental conditions, fentanyl had no potential to stimulate platelet activation and aggregation, or potentiate platelet response to ADP, nor did it affect platelet susceptibility to prasugrel metabolite in ADP-stimulated platelets. In addition, fentanyl was found to interact with all the examined carrier proteins with dissociation constants in the order of 10
CONCLUSIONS
CONCLUSIONS
It does not seem that the delayed platelet responsiveness to oral P2Y
Identifiants
pubmed: 36646965
doi: 10.1007/s43440-023-00447-7
pii: 10.1007/s43440-023-00447-7
pmc: PMC10060303
doi:
Substances chimiques
Prasugrel Hydrochloride
G89JQ59I13
Platelet Aggregation Inhibitors
0
Orosomucoid
0
Fentanyl
UF599785JZ
Purinergic P2Y Receptor Antagonists
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
423-441Subventions
Organisme : Uniwersytet Medyczny w Lodzi
ID : 502-03/6-020-01/502-64-127-18
Organisme : Uniwersytet Medyczny w Lodzi
ID : 500/9-904-05/500-43-610
Organisme : Uniwersytet Medyczny w Lodzi
ID : 502-03/6-020-01/502-64-126-18
Informations de copyright
© 2023. The Author(s).
Références
Int J Biol Macromol. 2018 Feb;107(Pt B):2701-2714
pubmed: 29111269
Clin Pharmacokinet. 1982 May-Jun;7(3):234-51
pubmed: 7047043
J Pharm Pharmacol. 1981 Aug;33(8):507-14
pubmed: 6115925
J Mol Biol. 2008 Aug 29;381(2):394-406
pubmed: 18602119
J Cheminform. 2011 Oct 07;3:33
pubmed: 21982300
Nature. 1975 Jul 3;256(5512):56-7
pubmed: 1134581
J Inorg Biochem. 2019 Sep;198:110716
pubmed: 31153112
ACS Meas Sci Au. 2022 Feb 16;2(1):4-13
pubmed: 35844953
Platelets. 2013;24(4):303-7
pubmed: 22686487
Eur J Clin Pharmacol. 1986;30(2):217-9
pubmed: 2940093
J Thromb Haemost. 2013 Apr 10;:
pubmed: 23574625
Anal Bioanal Chem. 2010 Sep;398(1):53-66
pubmed: 20454782
Anesth Analg. 1986 Jul;65(7):786-804
pubmed: 3087239
Circulation. 2020 Dec 22;142(25):2479-2481
pubmed: 33347326
J Invasive Cardiol. 2019 Sep;31(9):265-271
pubmed: 31478892
Intensive Care Med. 2004 Mar;30(3):496-501
pubmed: 14735236
Naunyn Schmiedebergs Arch Pharmacol. 2015 Jan;388(1):43-9
pubmed: 25332055
Am J Clin Pathol. 2014 Nov;142(5):647-56
pubmed: 25319980
Int J Cardiol. 2021 Jun 15;333:43-44
pubmed: 33753184
J Comput Chem. 2009 Dec;30(16):2785-91
pubmed: 19399780
Neurosci Biobehav Rev. 2019 Nov;106:49-57
pubmed: 30528374
J Photochem Photobiol B. 2016 Jul;160:229-39
pubmed: 27128364
Vascul Pharmacol. 2019 Feb;113:47-56
pubmed: 30471364
Subcell Biochem. 2010;51:183-227
pubmed: 20213545
Nat Struct Mol Biol. 2017 Feb;24(2):187-193
pubmed: 28024148
J Biol Chem. 2011 Nov 4;286(44):38570-38582
pubmed: 21914797
Eur Heart J Cardiovasc Pharmacother. 2022 Jan 5;8(1):4-12
pubmed: 32730628
Anesth Analg. 2012 Jan;114(1):122-8
pubmed: 22025496
Circ Cardiovasc Interv. 2016 Sep;9(9):
pubmed: 27586412
Handb Exp Pharmacol. 2017;239:363-378
pubmed: 28204957
Biochemistry. 2008 Oct 28;47(43):11340-7
pubmed: 18831538
Heliyon. 2019 Nov 21;5(11):e02879
pubmed: 31844752
Br J Pharmacol. 1992 Aug;106(4):917-23
pubmed: 1393289
Thromb Res. 1988 May 1;50(3):429-36
pubmed: 3394122
J Pharm Pharmacol. 1982 Feb;34(2):102-6
pubmed: 6121867
Naunyn Schmiedebergs Arch Pharmacol. 1975;288(2-3):163-77
pubmed: 240130
Anaesthesist. 1996 Apr;45(4):323-9
pubmed: 8702049
Platelets. 2020 Oct 2;31(7):845-852
pubmed: 31906818
Int J Lab Hematol. 2015 Apr;37(2):143-7
pubmed: 25055983
J Pharm Sci. 1993 May;82(5):493-7
pubmed: 8360825
J Biol Chem. 2003 Jun 27;278(26):23227-32
pubmed: 12709430
Platelets. 2015;26(8):730-5
pubmed: 25549285
Can Anaesth Soc J. 1980 Jul;27(4):319-22
pubmed: 7407667
Thromb Haemost. 2018 Aug;118(8):1409-1418
pubmed: 29972861
J Cardiovasc Pharmacol. 2020 Sep;76(3):267-275
pubmed: 32649576
Eur J Clin Pharmacol. 1984;27(1):51-6
pubmed: 6489427
Front Immunol. 2020 Mar 04;11:300
pubmed: 32194554
J Pharm Pharmacol. 1982 Mar;34(3):181-5
pubmed: 6121896
J Physiol. 1963 Aug;168:178-95
pubmed: 14056485
Biochem Pharmacol. 2020 Apr;174:113827
pubmed: 31987853
J Immunoassay Immunochem. 2005;26(4):285-93
pubmed: 16153013
Clin Immunol Immunopathol. 1983 May;27(2):240-9
pubmed: 6307570
Arch Int Pharmacodyn Ther. 1982 May;257(1):4-19
pubmed: 6214227
Anesth Analg. 1997 Feb;84(2):315-8
pubmed: 9024020
Br J Haematol. 2004 Apr;125(1):79-82
pubmed: 15015973
Xenobiotica. 2015 Mar;45(3):207-12
pubmed: 25314012
Anesth Analg. 1999 Jul;89(1):26-31
pubmed: 10389773
Thromb Res. 2020 Oct;194:183-189
pubmed: 32788114
Neurogastroenterol Motil. 2015 Apr;27(4):509-23
pubmed: 25690069
J Biomed Sci. 2003 May-Jun;10(3):292-301
pubmed: 12711856
Nature. 1992 Jul 16;358(6383):209-15
pubmed: 1630489
J Biol Chem. 2021 Dec;297(6):101392
pubmed: 34758357