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QuickView for naltrexone (compound)
PubChem
| Name: | Naltrexone |
|---|---|
| PubChem Compound ID: | 11957643 |
| 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. |
| Molecular formula: | C20H24ClNO4 |
| Molecular weight: | 377.862 g/mol |
| Synonyms: |
EU-0100846
|
DrugBank
Identification
| Name: | Naltrexone |
|---|---|
| Name (isomeric): | DB00704 |
| Drug Type: | small molecule |
| 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. |
| Synonyms: |
PTI-555
|
| Brand: | Naltrexone Hcl, N-Cyclopropylmethylnoroxymorphone, Naltrexone [Usan:Ban:Inn], Naltrexona [INN-Spanish], ReVia, Naltrexonum [INN-Latin], MorViva, Celupan, Vivitrex |
| Category: | Anti-craving Agents, Alcohol Antagonists, Depressants, Narcotic Antagonists, Opiate Antagonists |
| CAS number: | 16590-41-3 |
Pharmacology
| 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. |
|---|---|
| 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 admin...
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| Mechanism of Action: |
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 af...
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| Absorption: | Although well absorbed orally, naltrexone is subject to significant first pass metabolism with oral bioavailability estimates ranging from 5 to 40%. |
| Protein binding: | 21% bound to plasma proteins over the therapeutic dose range. |
| Biotransformation: | Hepatic. When administered orally, naltrexone undergoes extensive biotransformation and is metabolized to 6 beta-naltrexol (which may contribute to the therapeutic effect) and other minor metabolites. |
| Route of elimination: | 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. |
| Half Life: | 4 hours for naltrexone and 13 hours for the active metabolite 6 beta-naltrexol. |
| Clearance: | ~ 3.5 L/min [after IV administration] |
| Toxicity: | In the mouse, rat and guinea pig, the oral LD50s 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. |
| Affected organisms: | Humans and other mammals |
Interactions
| Food interaction: |
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Targets
Transporters
