Difference Between Naloxone and Naltrexone


Two of the most frequent opioid antagonists used to treat substance abuse are naloxone and naltrexone. Although it has certain long-term uses, Narcan (Naloxone) is mostly employed as a short-term opiate drug blocker. Opioid overdose antidote that works similarly to Naltrexone (ReVia and Vivitrol) but has a shorter treatment time.

Naloxone and naltrexone are both effective and potentially lifesaving treatments for opioid addiction. Talk to your doctor first, though, because many of these drugs might have dangerous interactions with others.

What is Naloxone?

This medication aids in preventing the ill effects of opioids (substances that act on opioid receptors to produce morphine-like effects). As an opioid antagonist, it can be used to reverse the effects of an overdose on opiates, such as breathing difficulties.

Opiate replacement medications like Suboxone, which includes both naloxone and buprenorphine, also make use of naloxone (sold under the brand name Subutex). This serves as a protection against the substance being abused.

What is Naltrexone?

It's a drug prescribed for people with substance abuse disorders, particularly those who are dependent on opioids or alcohol. For those who have developed a tolerance to opioids and are trying to break that tolerance, this drug is useful because it prevents them from relapsing. The "need" for opioid is lessened as a side effect. Addiction to drugs or alcohol cannot be cured in this way.

Differences: Naloxone and Naltrexone

The following table highlights the major differences between Naloxone and Naltrexone −

Characteristics

Naloxone

Naltrexone

Definition

It saves lives by reversing the effects in case there is some drug overdose. This has very strong affinity for Mu receptor. It is a repetitive competitive antagonist. The effect lasts about 45 minutes.

It aids in recovery and prevents drug and alcohol dependence. It binds more slowly.

Uses

  • Injected into a patient suffering from an opioid overdose

  • Works rapidly to take the effect of the drug away

  • It is also used for for blood pressure support in septic shock

  • It has been in use for over 30 years

  • It is injected and slowly released into the body

  • It works in the brain to block opiate effects (for example pain relief and feelings of well-being)

Candidates

  • Opioid dose > 50 MME/day

  • Concomitant benzodiazepine and opioid use

  • History of opioid dose

  • History of substance overuse disorder

  • Respiratory conditions (e.g., Sleep Apnea and COPD)

  • Excessive alcohol use

  • Mental health condition(s)

Multiple guidance’s/guidelines also suggest prescribing naloxone to individuals who were earlier on chronic opium like substances and have lost forbearance to an earlier dose and are at a risk of resuming that dose using prescriptions of illicit drugs (e.g., opioid taper underway, recent release from prison or detoxification facility)

Anyone beginning Naltrexone must be opioid (category of drugs that include the illegal substance like heroin) free. Though there is no proper information and evidence to decide which patients with Opioid Use Disorder are the best fit for this medication called naltrexone, the eligible candidates to consider include;

  • Able to be opioid free for > 7 days before therapy

  • Highly motivated (e.g. want to live)

  • Desire a non-opioid option for OUD treatment

  • Short term opioid use (e.g. younger patients)

  • Poor response to other OUD patients

  • In a mandated monitoring program (e.g., pilots)

  • Co-morbid OUD and AUD

Patients who are not candidates for naltrexone include patients who use opioid in the last 7 days, have liverfailure, acute hepatitis or are pregnant. Patients without supervised administration are not good candidates for oral therapy. Patients with low muscle mass are not good candidates for the injection.

Length of effects

Often wears off within 30 minutes and completely gone within 90 minutes

The pill form may last all day; the injectable form may last for up to 30 days.

Precautions

This medication should not be taken during pregnancy as it may cause may cause opioid withdrawal in the foetus

Using this medicine with any of the following medicines is usually not recommended; Morphine, Naloxegol, Morphine Sulfate Liposome, Oxycodone, Naldemedine, Oxymorphone

Some products that may interact with this medication include: disulfiram, diarrhoea drug (such as diphenoxylate) dextromethorphan, opioid pain or cough relievers (for example hydrocodone, codeine), thioridazine.

Oral bioavailability

2 per cent (high absorption but extensive first-pass metabolism)

Up to 40 percent

Conclusion

Naloxone and Naltrexone are two medications that are used to treat opioid addiction, but they have different uses and mechanisms of action. Naloxone is used to reverse the effects of an opioid overdose, while Naltrexone is used to prevent relapse in people who are trying to stop using opioids.

Both medications are important tools in the fight against opioid addiction, and they can be used together to provide a comprehensive treatment plan.

Updated on: 06-Apr-2023

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