Naltrexone

• Anti-craving Agents
• Depressants
• Alcohol Antagonists
• Opiate Antagonists
• ATC:N07BB04

• Celupan
• N-Cyclopropylmethylnoroxymorphone
• Naltrexona [Inn-Spanish]
• Naltrexone Hcl
• Naltrexone [Usan:Ban:Inn]
• Naltrexonum [Inn-Latin]
• ReVia
• Vivitrex

• No information avaliable

C₂₀H₂₃NO₄

http://www.rxlist.com/cgi/generic2/naltrexone.htm

Naltrexone FDA

Naltrexone MSDS

No information avaliable

341.401 g/mol

169-170 ^oC (274-276 ^oC for hydrochloride salt)

100 mg/mL (as hydrochloride salt)

Solid

1.692 (1.92 by expt)

Tablet (scored, film-coated, 50 mg)

For use in the treatment of alcohol dependence and for the blockade of the effects of exogenously administered opioids.

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.

Although well absorbed orally, naltrexone is subject to significant first pass metabolism with oral bioavailability estimates ranging from 5 to 40%.

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.

It is recommended that the prescribing physician relate the following information to patients being treated with REVIA:

You have been prescribed REVIA as part of the comprehensive treatment for your alcoholism or drug dependence. You should carry identification to alert medical personnel to the fact that you are taking REVIA. A REVIA medication card may be obtained from your physician and can be used for this purpose. Carrying the identification card should help to ensure that you can obtain adequate treatment in an emergency. If you require medical treatment, be sure to tell the treating physician that you are receiving REVIA therapy.

You should take REVIA as directed by your physician. If you attempt to self-administer heroin or any other opiate drug, in small doses while on REVIA, you will not perceive any effect. Most important, however, if you attempt to self-administer large doses of heroin or any other opioid while on REVIA, you may die or sustain serious injury, including coma.

REVIA is well-tolerated in the recommended doses, but may cause liver injury when taken in excess or in people who develop liver disease from other causes. If you develop abdominal pain lasting more than a few days, white bowel movements, dark urine, or yellowing of your eyes, you should stop taking REVIA immediately and see your doctor as soon as possible.

Humans and other mammals