Naltrexon

Strukturformel

Naltrexon är ett läkemedel bland annat använt mot alkoholberoende.

Farmakologi

Naltrexon fungerar som opioidantagonist med verkan på samtliga opioidreceptorer (μ, δ och κ).[1] Genom så kallad kompetitiv inhibition upphävs effekterna av närvarande opioider vare sig de är kroppsegna (till exempel endorfiner) eller intagna utifrån (som morfin och heroin).[2] Skillnaden mellan naltrexon och naloxon, som används mot heroinöverdoser, är framför allt att naltrexon har en avsevärt längre verkan.[2] Halveringstiden i plasma är omkring 4 timmar för naltrexon och 13 timmar för dess aktiva metabolit 6-β-naltrexol.[1]

Användning

Effekterna av naltrexon vid alkoholberoende har varierat mellan olika studier, en sammanfattande studie sammanlänkar dessa till synes tvetydiga resultat och pekar på att skillnaderna i effekt kan bero på olika polymorfismer av opioida mu-receptorer inom den studerade gruppen.[3]

Naltrexon ingår även för förstärkande effekt i ett aptitdämpande medel vid viktreduktionsbehandling.[4]

Forskning

Studier pågår av naltrexons effekter på andra typer av beroende, till exempel kokain, amfetamin och sexberoende.[5]

Användning mot autoimmuna tillstånd

Naltrexon används också i betydligt lägre doser mot vissa former av autoimmuna tillstånd, framför allt multipel skleros.[6] Tidigare teorier kring verkningsmekanismen har varit reglering av immunförsvaret genom påverkan av kroppens endorfinsystem, eller placebo. Senare studier har dock visat att naltrexon blockerar TLR-4-receptorer, som är viktiga i immunförsvaret. Denna mekanism kan även vara orsak till symtomlindrande effekten av låga doser av naltrexon vid toleranstillstånd mot opioida smärtstillande läkemedel.

Källor

  1. ^ [a b] Niciu, Mark J.; Arias, Albert J. (2013). ”Targeted Opioid Receptor Antagonists in the Treatment of Alcohol Use Disorders”. CNS drugs 27 (10): sid. 777–787. doi:10.1007/s40263-013-0096-4. ISSN 1172-7047. PMID 23881605. PMC: 4600601. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4600601/. Läst 12 september 2021. 
  2. ^ [a b] ”Naltrexone Monograph for Professionals” (på engelska). Drugs.com. 19 juli 2021. https://www.drugs.com/monograph/naltrexone.html. Läst 12 september 2021. 
  3. ^ Kimura M, Higuchi S.. ”Genetics of alcohol dependence.”. Psychiatry Clin Neurosci. http://www.ncbi.nlm.nih.gov/pubmed/21507127. Läst 17 december 2011. 
  4. ^ Mysimba (naltrexon/bupropion)[död länk] Läkemedelsverket. 21 april 2018.
  5. ^ https://www.umu.se/nyheter/lakemedel-mot-alkoholism-testat-mot-sexmissbruk_9249459/
  6. ^ Cree BA, Kornyeyeva E, Goodin DS.. ”Pilot trial of low-dose naltrexone and quality of life in multiple sclerosis.”. Annals of Neurology. http://www.ncbi.nlm.nih.gov/pubmed/20695007. Läst 17 december 2011. 
v • r
Opioider
Opiumalkaloider
Syntetiska opioider
Semisyntetiska
Fenylheptylamin
Piperanilider
Fenylpiperidiner
Petidin (meperidin) · ketobemidon · MPPP · Allylprodin · Alfameprodin · Betaprodin · PEPAP
Difenylpropylamin
Bensomorfanderivat
Oripavin
Morfinanderivat
Övriga
Opioidantagonister

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