Naltrexone
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| Non-proprietary name | Naltrexone | ||||||||||||
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| Molar mass | 341,40 g · mol -1 | ||||||||||||
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Water: 1.63 g l −1 (25 ° C) |
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Naltrexone is a prescription drug and, like naloxone, is a pure opioid antagonist that acts as a competitive antagonist on all opioid receptors .
application
Opioid addiction
Naltrexone is approved in Germany for drug support in the psychotherapeutic or psychologically guided withdrawal treatment of opioid addicts after an opioid detoxification. After systematic reviews and a. According to the Cochrane Collaboration , the data on maintenance therapy in opioid addicts are so far inadequate, while there is evidence of effectiveness in the treatment of alcohol addicts .
Occasional cannabis use appears to encourage opioid addicts to remain in a naltrexone program, as opposed to no or continuous use.
Alcohol addiction
In the USA and numerous European countries, naltrexone is already approved for preventing alcohol relapse. Under the trade name Adepend ® (50 mg), approval for reducing the risk of relapse, supporting abstinence and reducing the desire for alcohol ( craving ) as part of a comprehensive therapy was granted to the pharmaceutical company Desitin on May 17, 2010 . The market launch took place on August 1, 2010. In addition to naltrexone HCl neuraxpharm, it is one of the few naltrexone preparations in Germany with the indication of relapse prophylaxis for alcohol addiction.
The data on younger alcoholics are limited.
Other
Off-label , naltrexone is used successfully in the treatment of self-harming behavior in dissociative disorders and borderline personality disorders. A benefit of naltrexone was also seen in self-harming behavior in the context of autism and mental development disorders.
Side effects
Naltrexone can trigger an acute withdrawal syndrome if the person being treated is not opiate-free for at least seven days before starting therapy. It is therefore recommended to check that the patient is free of opiates before starting treatment with a urine sample or a test with naloxone.
Sleep disorders, anxiety and increased excitability are described as very common side effects. Abdominal pain, nausea and vomiting, joint and muscle pain and headaches are also very common. Particular caution is required in patients with impaired liver or kidney function.
Simultaneous use of opiates can lead to an overdose and thus to increased, potentially fatal respiratory depression .
No dependence or development of tolerance have been observed with naltrexone treatments.
Interactions
Opioid drugs (such as codeine or loperamide ) should not be taken while taking naltrexone . In emergency situations, opioid analgesics may not be equally effective and the dose must be increased. This can lead to complications.
Pharmacological properties
150 mg naltrexone per day blocks the effect of 25 mg heroin for about 72 hours. The half-life of opiate receptor blockade is generally between 72 and 108 hours. At a dose of 50 mg per day, taken every other day, after 48 hours 70-80% of the opiate receptors are still blocked.
Low dose naltrexone (LDN)
A pilot study on effectiveness in multiple sclerosis with 40 participants from 2008 by Gironi et al. showed a significant reduction in spasticity after 6 months, only one patient showed progressive neurological degeneration. The authors of the study came to the conclusion that LDN is safe to use and well tolerated by MS patients.
Trade names
Monopreparations : Adepend (D), Dependex (A), Ethylex (A), Naltrexin (A, CH), Nemexin (D, A), Revia (A) and generics (D, A)
Web links
- Naltrexone . In: Erowid . (English)
Individual evidence
- ↑ a b c Entry on naltrexone in the ChemIDplus database of the United States National Library of Medicine (NLM) .
- ^ The Merck Index. An Encyclopaedia of Chemicals, Drugs and Biologicals . 14th edition, 2006, pp. 1101-1102, ISBN 978-0-911910-00-1 .
- ↑ a b Data sheet Naltrexone hydrochloride from Sigma-Aldrich , accessed on April 12, 2011 ( PDF ).
- ↑ Lobmaier P, Kornør H, Kunøe N, Bjørndal A: Sustained-release naltrexone for opioid dependence . In: Cochrane Database Syst Rev . No. 2, 2008, p. CD006140. doi : 10.1002 / 14651858.CD006140.pub2 . PMID 18425938 .
- ↑ Minozzi S, Amato L, Vecchi S, Davoli M, Kirchmayer U, Verster A: Oral naltrexone maintenance treatment for opioid dependence . In: Cochrane Database Syst Rev . No. 1, 2006, p. CD001333. doi : 10.1002 / 14651858.CD001333.pub2 . PMID 16437431 .
- ↑ Adi Y, Juarez-Garcia A, Wang D, et al. : Oral naltrexone as a treatment for relapse prevention in formerly opioid-dependent drug users: a systematic review and economic evaluation Archived from the original on November 17, 2011. Info: The archive link has been inserted automatically and has not yet been checked. Please check the original and archive link according to the instructions and then remove this notice. In: Health Technol Assess . 11, No. 6, February 2007, pp. Iii-iv, 1-85. PMID 17280624 . Retrieved July 1, 2009.
- ↑ Wilfrid Noel Raby, PhD, MD, Kenneth M. Carpenter, PhD, Jami Rothenberg, PhD, Adam C. Brooks, PhD, Huiping Jiang, PhD, Maria Sullivan, MD, Adam Bisaga, MD, Sandra Comer, PhD, and Edward V. Nunes, MD: "Intermittent Marijuana Use Is Associated with Improved Retention in Naltrexone Treatment for Opiate-Dependence" Am J Addict. 2009 Jul-Aug; 18 (4): 301-308. doi : 10.1080 / 10550490902927785 ; PMC 2753886 (free full text).
- ↑ Minozzi S, Amato L, Davoli M: Detoxification treatments for opiate dependent adolescents . In: Cochrane Database Syst Rev . No. 2, 2009, p. CD006749. doi : 10.1002 / 14651858.CD006749.pub2 . PMID 19370651 .
- ↑ Gottfried Fischer, Peter Riedesser (2003): Textbook of Psychotraumatology . Ernst Reinhardt Verlag, p. 246.
- ↑ Symons FJ, Thompson A, Rodriguez MC: Self-injurious behavior and the efficacy of naltrexone treatment: a quantitative synthesis . In: Ment Retard Dev Disabil Res Rev . 10, No. 3, 2004, pp. 193-200. doi : 10.1002 / billion . 20031 . PMID 15611982 .
- ↑ Gironi M, Martinelli-Boneschi F, Sacerdote P, Solaro C, Zaffaroni M, Cavarretta R, Moiola L, Bucello S, Radaelli M, Pilato V, et al. : A pilot trial of low-dose naltrexone in primary progressive multiple sclerosis Archived from the original on March 30, 2010. Info: The archive link has been inserted automatically and has not yet been checked. Please check the original and archive link according to the instructions and then remove this notice. In: Multiple Sclerosis . 14, No. 8, 2008, pp. 1076-1083. doi : 10.1177 / 1352458508095828 . Retrieved March 18, 2010.
