Naltrexone for Alcoholism

FDA-approved medication for Alcohol Use Disorders

Brand Name:  ReVia. Vivitrol (injection).

Generic Name: Naltrexone \nal-ˈtrek-ˌsōn\

Pharmacology:  Naltrexone blocks opioid receptors, preventing opiate medications, heroin, and endorphins from having effects.  

Indications:  Alcohol dependence; Opiate dependence; Impulse control-disorders (gambling, binge-eating)

Duration:  Blockade of opioid receptors lasts 24-72 hours

Contraindications:  Liver disease.  Recent use of opiates.

Dosage Forms:  50 mg tablet.

Dosing:  25 mg for two days and then 50 mg thereafter as tolerated.

Maximum Dose:  100 mg daily.

Habit Forming:  No

Pregnancy:  Risk Category C (animal studies do not show adverse effects, but no controlled studies in humans).

Naltrexone Side Effects

  • Most common:  Nausea, vomitting, diarrhea (about 10% of users)
  • Dysphoria
  • Decreased appetite
  • Insomnia
  • Headache
  • Elevated liver enzymes

What is Naltrexone?

Naltrexone is a medication used to treat alcoholism and opiate addiction. It is sold under the brand names Vivitrol, Nalorex, Nemexin, and Revia.

Opiate is a highly addictive chemical compound derived from the plant opium poppy. Due to its pain relieving properties, it finds its use in the pain-management drugs, and for its euphoric effects, it also exists as the illicit street drugs like opium, heroin etc.

How Does Naltrexone Work?

Naltrexone is an opioid antagonist, which means naltrexone obstructs the working of alcohol and opiate substances, and thereby reduces or eliminates the associated euphoric effect.

Once the euphoria is gone, alcohol and opioid substances no more appeal to the person. Consequently, the desire to take these addictive substances also diminishes over time.

When you consume opiate substances or alcohol, their molecules rush to attach to the opioid receptors in the brain. These opioid receptors are primarily supposed to be used by the endorphin molecules (the naturally occurring opioids in your body working to relieve pain and make you happy).

Alcohol and opiate molecules, being agonists, have their structure precisely similar to the endorphin molecules. That is why they manage to bind to the opioid receptors and activate them to invoke pleasure and euphoria.

Naltrexone molecules, being opioid antagonists, also compete for the same opioid receptors and bind to them pre-emptively. Even though they bind to the opioid receptors, they never activate those receptors as the structure of naltrexone molecule is not exactly the same as endorphins.

Naltrexone molecules are supposed to just clog the opioid receptors and prevent the body from responding to alcohol and opioids.

Naltrexone for Alcohol Use Disorder

The Sinclair Method, which is devised to deal with alcoholism, entirely revolves around the opiate antagonist Naltrexone. This drug effectively decreases the alcohol drinking desire and gradually reduces and even eliminates the person’s dependence on alcohol.

A short-acting form of Naltrexone is used for alcoholism, so that the drug remains effective for only as long as the level of alcohol or opioids is high in the bloodstream. Afterward, the drug molecules are expelled by the body so that the normal functioning of endorphins is not affected.

The person needs to take Naltrexone tab about 1 hour before drinking alcohol.

Vivitrol

Low-dose Naltrexone

Naltrexone Research

The u-Opioid Receptor and Treatment Response to Naltrexone

Views about responsibility for alcohol addiction and negative evaluations of naltrexone

Internest Sex Addiction Treated with Naltrexone

Effects of Naltrexone on Smoking Cessation Outcomes and Weight Gain in Nicotine-Dependent Men and Women

Targeted Use of Naltrexone Without Prior Detoxification in the Treatment of Alcohol Dependence: A Factorial Double-Blind, Placebo-Controlled Trial

Improving clinical outcomes for naltrexone as a management of problem alcohol use