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Naltrexone
drug data and news
Naltrexone drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Naltrexone | ||
| Brand Names/Synonyms | CCRIS 3506; Celupan; HSDB 6750; N-Cyclopropylmethylnoroxymorphone; Naltrexona [Inn-Spanish]; Naltrexone; Naltrexone Hcl; Naltrexone [Usan:Ban:Inn]; Naltrexonum [Inn-Latin]; Revia; UM-792; Vivitrex | ||
| Indication | For treatment of opioid type drug dependence. | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Naltrexone, a pure opioid antagonist, is a synthetic congener of oxymorphone with no opioid agonist properties. Naltrexone is indicated in the treatment of alcohol dependence and for the blockade of the effects of exogenously administered opioids. It markedly attenuates or completely blocks, reversibly, the subjective effects of intravenously administered opioids. When co-administered with morphine, on a chronic basis, Naltrexone blocks the physical dependence to morphine, heroin and other opioids. In subjects physically dependent on opioids, Naltrexone will precipitate withdrawal symptomatology. | ||
| Mechanism Of Action | Naltrexone binds to the opioid mu receptor antagonistically, thereby preventing conventional opiate (heroin, morphine) drugs from binding and inducing opioid neural responses. The mechanism of action of Naltrexone in alcoholism is not understood; however, involvement of the endogenous opioid system is suggested by preclinical data. Naltrexone competitively binds to such receptors and may block the effects of endogenous opioids. | ||
| Naltrexone News (When available) |
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| Dosage Forms | TABLET | ||
| Drug_Category | Anti-craving Agents; Depressants; Alcohol Antagonists; Opiate Antagonists; ATC:N07BB04 | ||
| Absorption | Not Available | ||
| Interactions |
Interactions for Naltrexone: Studies to evaluate possible interactions between REVIA and drugs other than opiates have not been performed. Consequently, caution is advised if the concomitant administration of REVIA and other drugs is required. The safety and efficacy of concomitant use of REVIA and disulfiram is unknown, and the concomitant use of two potentially hepatotoxic medications is not ordinarily recommended unless the probable benefits outweigh the known risks. Lethargy and somnolence have been reported following doses of REVIA and thioridazine. Patients taking REVIA may not benefit from opioid containing medicines, such as cough and cold preparations, antidiarrheal preparations, and opioid analgesics. In an emergency situation when opioid analgesia must be administered to a patient receiving REVIA, the amount of opioid required may be greater than usual, and the resulting respiratory depression may be deeper and more prolonged. | ||
| Toxicity | LD50 = 1450 mg/kg (rat) | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | Not Available | ||
| Chemical Formula | C20H23NO4 | ||
| Molecular Weight | 341.401 g/mol | ||
| Smiles String | C1CC1CN2CCC34C5C(=O)CCC3(C2CC6=C4C(=C(C=C6)O)O5)O | ||
| Melting Point | 169-170 oC (274-276 oC for hydrochloride salt) | ||
| Water Solubility | 100 mg/mL | ||
| State | Solid | ||
| LogP/Hphobicity | 1.692 (1.92 by expt) | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | When administered orally, naltrexone undergoes extensive biotransformation and is metabolized to 6 beta-naltrexol and other minor metabolites. | ||
| Half Life | 4 hours | ||
| Protein Binding [%] | 21% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Naltrexone.html http://www.rxlist.com/cgi/generic2/naltrexone.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00005 | ||
| CAS Registry Number | 16590-41-3 | ||
| KEGG Compound ID | C07253 | ||
| PubChem ID | SID:9462 | ||
| PharmGKB ID | PA450588 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2213826 |
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