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Definition and meaning of Naloxone

Definitions

Naloxone (n.)

1.(Cismef)N-allyl-noroxymorphine. Antagoniste de la morphine et des autres opiacés, dépourvue d'activité propre. Elle est utilisée en cas de surdosage ou d'intoxication par les opiacés.

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Wikipedia

Naloxone

                   
Naloxone
Structure de la naloxone
Structure de la naloxone
Général
Nom IUPAC 17-allyl-4,5α-époxy-
3,14-dihydroxymorphinan-6-one
No CAS 465-65-6
No EINECS 207-365-7
Code ATC V03AB15
Propriétés chimiques
Formule brute C19H21NO4  [Isomères]
Masse molaire[1] 327,3743 ± 0,0181 g·mol−1
C 69,71 %, H 6,47 %, N 4,28 %, O 19,55 %,
Données pharmacocinétiques
Biodisponibilité 2%
Métabolisme hépatique
Demi-vie d’élim. 1-1.5 heures
Excrétion urine, Bile
Considérations thérapeutiques
Voie d’administration IV, IM
Unités du SI & CNTP, sauf indication contraire.

La naloxone est le principal antagoniste des récepteurs de la morphine. Dans les cas d'intoxication aiguë aux morphiniques (notamment surdose), la naloxone est administrée afin de déplacer la morphine de ses sites récepteurs et d'arrêter son action. Elle permet de réveiller le sujet comateux, sauf en cas de poly-intoxication. Sa durée d'action est de 30 minutes.

La naloxone est un traitement pour l'analgésie congénitale quand celle-ci est due a l'enképhaline (un inhibiteur des nociceptifs) au niveau des synapses. Ayant la même conformation spatiale que l'enképhaline, elle le remplace dans les récepteurs post-synaptiques, ce qui diminue l'utilisation de l'enképhaline et augmente donc le passage des nociceptifs. (source : http://www.ac-nancy-metz.fr/enseign/SVT/eleve/bac/ES03/ES03.htm)

  Notes et références

  1. Masse molaire calculée d’après Atomic weights of the elements 2007 sur www.chem.qmul.ac.uk.
   
               

 

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