| Attributes | Values |
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| rdf:type
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| http://linked.open...gbank/description
| - Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of naloxone. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence. [PubChem] (en)
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| http://linked.open...y/drugbank/dosage
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| http://linked.open...generalReferences
| - # Schmitz JM, Stotts AL, Rhoades HM, Grabowski J: Naltrexone and relapse prevention treatment for cocaine-dependent patients. Addict Behav. 2001 Mar-Apr;26(2):167-80. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/11316375 # Krystal JH, Gueorguieva R, Cramer J, Collins J, Rosenheck R: Naltrexone is associated with reduced drinking by alcohol dependent patients receiving antidepressants for mood and anxiety symptoms: results from VA Cooperative Study No. 425, "Naltrexone in the treatment of alcoholism". Alcohol Clin Exp Res. 2008 Jan;32(1):85-91. Epub 2007 Dec 7. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18070245 # Ray LA, Chin PF, Miotto K: Naltrexone for the treatment of alcoholism: clinical findings, mechanisms of action, and pharmacogenetics. CNS Neurol Disord Drug Targets. 2010 Mar;9(1):13-22. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/20201811 (en)
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| http://linked.open...gy/drugbank/group
| - approved (en)
- investigational (en)
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| http://linked.open...drugbank/halfLife
| - 4 hours for naltrexone and 13 hours for the active metabolite 6 beta-naltrexol. (en)
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| http://linked.open...ugbank/indication
| - Used as an adjunct to a medically supervised behaviour modification program in the maintenance of opiate cessation in individuals who were formerly physically dependent on opiates and who have successfully undergone detoxification. Also used for the management of alcohol dependence in conjunction with a behavioural modification program. (en)
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| http://linked.open...bank/manufacturer
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| sameAs
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| Title
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| adms:identifier
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| http://linked.open...mechanismOfAction
| - Naltrexone is a pure opiate antagonist and has little or no agonist activity. The mechanism of action of naltrexone in alcoholism is not understood; however, involvement of the endogenous opioid system is suggested by preclinical data. Naltrexone is thought to act as a competitive antagonist at mc, κ, and δ receptors in the CNS, with the highest affintiy for the μ receptor. Naltrexone competitively binds to such receptors and may block the effects of endogenous opioids. This leads to the antagonization of most of the subjective and objective effects of opiates, including respiratory depression, miosis, euphoria, and drug craving. The major metabolite of naltrexone, 6-β-naltrexol, is also an opiate antagonist and may contribute to the antagonistic activity of the drug. (en)
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| http://linked.open...drugbank/packager
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| http://linked.open...y/drugbank/patent
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| http://linked.open...outeOfElimination
| - Both parent drug and metabolites are excreted primarily by the kidney (53% to 79% of the dose), however, urinary excretion of unchanged naltrexone accounts for less than 2% of an oral dose and fecal excretion is a minor elimination pathway. The renal clearance for naltrexone ranges from 30 to 127 mL/min and suggests that renal elimination is primarily by glomerular filtration. (en)
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| http://linked.open.../drugbank/synonym
| - Naltrexone (en)
- N-Cyclopropylmethylnoroxymorphone (en)
- N-Cyclopropylmethyl-14-hydroxydihydromorphinone (en)
- Naltrexon (en)
- Naltrexona (en)
- Naltrexonum (en)
- 17-(Cyclopropylmethyl)-4,5alpha-epoxy-3,14-dihydroxymorphinan-6-one (en)
- 17-(Cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-one (en)
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| http://linked.open...drugbank/toxicity
| - In the mouse, rat and guinea pig, the oral LD<sub>50</sub>s were 1,100-1,550 mg/kg; 1,450 mg/kg; and 1,490 mg/kg; respectively. High doses of naltrexone (generally ≥1,000 mg/kg) produce salivation, depression/reduced activity, tremors, and convulsions. (en)
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| http://linked.open...umeOfDistribution
| - * 1350 L [intravenous administration] (en)
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| http://linked.open.../drug/hasAHFSCode
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| http://linked.open...k/foodInteraction
| - Take without regard to meals. (en)
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| http://linked.open.../drugbank/mixture
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| http://linked.open...nk/proteinBinding
| - 21% bound to plasma proteins over the therapeutic dose range. (en)
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| http://linked.open...ogy/drugbank/salt
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| http://linked.open...ynthesisReference
| - Bao-Shan Huang, Yansong Lu, Ben-Yi Ji, Aris P Christodoulou, "Preparation of naltrexone from codeine and 3-benzylmorphine." U.S. Patent US6013796, issued March, 1990. (en)
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| foaf:page
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| http://linked.open...ugbank/IUPAC-Name
| |
| http://linked.open...gy/drugbank/InChI
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| http://linked.open...Molecular-Formula
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| http://linked.open.../Molecular-Weight
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| http://linked.open...noisotopic-Weight
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| http://linked.open...y/drugbank/SMILES
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| http://linked.open.../Water-Solubility
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| http://linked.open...ogy/drugbank/logP
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| http://linked.open...ogy/drugbank/logS
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| http://linked.open...l/drug/hasATCCode
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| http://linked.open...nd-Acceptor-Count
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| http://linked.open...-Bond-Donor-Count
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| http://linked.open...drugbank/InChIKey
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| http://linked.open...urface-Area--PSA-
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| http://linked.open...nk/Polarizability
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| http://linked.open...bank/Refractivity
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| http://linked.open...atable-Bond-Count
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| http://linked.open...ugbank/absorption
| - Although well absorbed orally, naltrexone is subject to significant first pass metabolism with oral bioavailability estimates ranging from 5 to 40%. (en)
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| http://linked.open.../affectedOrganism
| - Humans and other mammals (en)
|
| http://linked.open...casRegistryNumber
| |
| http://linked.open...drugbank/category
| |
| http://linked.open...rugbank/clearance
| - * ~ 3.5 L/min [after IV administration] (en)
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| http://linked.open...gbank/containedIn
| |
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