Vivitrol vs Suboxone - A Side-By-Side Comparison

Vivitrol vs Suboxone

Opioids are drugs that bind opioid receptors in the central and peripheral nervous systems, gastrointestinal tract, and other organs.

Opioids elicit various psychoactive and somatic effects such as:

  • drowsiness
  • nausea
  • constipation
  • pain relief
  • and even respiration depression Opioids create feelings of euphoria since some opioid receptors are located in the brain region associated with reward and pleasure.

How do opioids elicit euphoria? They induce these effects by binding one or more of 5 receptors: delta, kappa, mu, zeta, and nociception opioid receptors. 1

What Kinds of Opioids Exist?

  • opiates
    • opiates are drugs derived from opium. Opioid is the broader term that encompasses the entire family of opiates including natural, synthetic and semi-syntheticsemi-synthetic.
  • synthetic opioids
  • endogenous opioids produced by the body

Opiates are drugs derived from opium poppy plants such as morphine (Brand names: Kadian and Avinza) and codeine.

Semi-synthetic and synthetic opioids, like some opiates such as morphine, are typically used as medications to alleviate pain. These medications include:

  • hydrocodone (Brand name: Vicodin)
  • oxycodone (Brand names: OxyContin, Percocet)

Lastly, there are endogenous opioids such as endorphins, and dynorphins that interact with opioid receptors to mediate various processes in the body. 2

Endogenous opioids, for example, may contribute the "runner's high" or the sense of mild euphoria that some people feel after strenuous exercise.

Opioid Withdrawal and Dependence

Short-term, appropriate use of opioids prescribed for pain management is usually not problematic. But long-term opioid use can change the chemistry of the brain leading to addiction or physical dependence, meaning that withdrawal symptoms will emerge if opioid use is abruptly stopped or significantly reduced.

Withdrawal symptoms run the gambit, from irritability and anxiety, to physical symptoms like hot and cold sweats, muscle pains, nausea and vomiting. Thus, when treating opioid dependence, pharmacological agents are often used in combination with behavioral therapy to reverse opioid effects of the brain, and reduce withdrawal symptoms, and cravings. 3

Suboxone

One such substance, Suboxone, was approved by the United States Federal Drug Administration (FDA) in 2002 to treat opiate dependence. Suboxone is an orange film labeled with white ink consisting of two substances: naloxone HCl dihydrate—a substance that blocks kappa opioid receptor activity and buprenorphine HCl—a chemical that partially activates mu opioid receptors (the only opioid receptors associated with physical dependence). 4

Routes of Administration

Suboxone is administered under the tongue (sublingual) or along the cheek (buccal).

It is available in four different doses with a 4:1 ratio of buprenorphine to naloxone (2, 4, 8 and 12mg of buprenorphine with 0.5, 1, 2 and 3mg of naloxone, respectively).

Concentrations typically peak 100 minutes after administration, and can be detected up to 48 hours later. Because Suboxone can induce withdrawal symptoms, it is only administered once signs of withdrawal emerge.

On the first day of treatment, a lower dose of sublingual film is administered. It is then increased on the next day. In the following days, it can be administered buccally or sublingually.

Dosage is adjusted according to the patient’s response, the type of opioid used, the level of dependence and the time since the patient’s last opioid use. Administration is initially supervised, but may progress to unsupervised treatments depending on the patient’s stability. When discontinuing treatment is deemed appropriate, patients are tapered off of Suboxone to prevent withdrawal symptoms. 5

Side Effects

Like any other pharmaceutical, Suboxone is associated with some side effects. The most common side effect is loss of sensation in the mouth. Others included

  • constipation vomiting
  • intoxication
  • insomnia
  • and withdrawal syndrome.

Despite its therapeutic effects, Suboxone has major drawbacks. It induces severe withdrawal symptoms similar or even worse than that caused by the original opiate.

It also needs to be taken daily for an indefinite amount of time to avoid the emergence of withdrawal symptoms in the future. Thus, a therapy with less severe withdrawal effects, and that can be taken less often was needed. This led to the development of Vivitrol. 6

Vivitrol Enters the Scence

Vivitrol is an extended-release, injectable that contains the mu-opioid receptor inhibitor naltrexone. It's indicated for treatment of alcohol dependence and prevention of opioid dependence relapse. Vivitrol was approved by the FDA to treat opioid dependence on October 12, 2010.

Naltrexone aids in preventing opioid dependence by binding of opioid receptor mu. It competes with other opioids to bind to the receptor. Since naltrexone has a strong attraction to the receptor, it prevents binding by both opioid drugs as well as opioids originating from the body. Although it binds to the receptor, it does not activate it and thus blocks opioid activation of the receptors. Therefore, the effects of a recreational opioid would not be experienced during administration of Vivitrol. 7

Dosage

Vivitrol is administered as a 380mg intramuscular gluteal injection dose once a month by a healthcare provider with a specialized needle also included with the medication. It is prepared by diluting the substance in a diluent provided with the medication, and it is only administered to patients that have abstained from opioid use for at least 7 to 10 days to reduce the severity of opioid withdrawal symptoms.

Half-Life

Plasma concentrations of Vivitrol peaks 2 hours after injection and again 2 to 3 days later. Unlike Suboxone, the effects of Vivitrol are experienced for an extended period of time. Concentrations don’t start to decline until 2 weeks after injection, and Vivitrol can be detected over a month after injection. 8

Side Effects

Vivitrol to treat opioid dependence is associated with some side effects. These include:

  • liver enzyme abnormalities
  • pain at the injection site
  • insomnia
  • and tooth ache However, these effects are much less severe than the withdrawal symptoms experienced with Suboxone

Another drawback to Vivitrol is that it needs to be administered by a medical provider 9.

Last Words

  • Chronic opioid use and abuse can lead to opioid dependence
  • Use of pharmacological therapies can treat opioid dependence by reducing the withdrawal symptoms during recovery.
  • Suboxone is an opioid receptor blocker and a partial activator that aids in the discontinuation of more addictive opioids.
  • Suboxone left much to be desired. However, since Vivitrol is associated with less severe withdrawal symptoms and only needs to be administered once a month, it has advantages over Suboxone as an alternative treatment for opioid dependence. 10

References

  1. Volkow ND. Opioid-dopamine interactions: implications for substance use disorders and their treatment. Biol Psychiatry. 2010;68(8):685-6.

  2. Rosenblum A, Marsch LA, Joseph H, Portenoy RK. Opioids and the treatment of chronic pain: controversies, current status, and future directions. Exp Clin Psychopharmacol. 2008;16(5):405-16.

  3. Rosenblum A, Marsch LA, Joseph H, Portenoy RK. Opioids and the treatment of chronic pain: controversies, current status, and future directions. Exp Clin Psychopharmacol. 2008;16(5):405-16.

  4. Yokell MA, Zaller ND, Green TC, Mckenzie M, Rich JD. Intravenous use of illicit buprenorphine/naloxone to reverse an acute heroin overdose. J Opioid Manag. 2012;8(1):63-6.

  5. Bell J, Byron G, Gibson A, Morris A. A pilot study of buprenorphine-naloxone combination tablet (Suboxone) in treatment of opioid dependence. Drug Alcohol Rev. 2004;23(3):311-7.

  6. Syed YY, Keating GM. Extended-release intramuscular naltrexone (VIVITROL®): a review of its use in the prevention of relapse to opioid dependence in detoxified patients. CNS Drugs. 2013;27(10):851-61.

  7. Johnson BA. Naltrexone long-acting formulation in the treatment of alcohol dependence. Ther Clin Risk Manag. 2007;3(5):741-9.

  8. Kjome KL, Moeller FG. Long-acting injectable naltrexone for the management of patients with opioid dependence. Subst Abuse. 2011;5:1-9.

  9. Whelan PJ, Remski K. Buprenorphine vs methadone treatment: A review of evidence in both developed and developing worlds. J Neurosci Rural Pract. 2012;3(1):45-50.

  10. Ekström M. What can we learn about breathlessness from population-based and administrative health data?. Curr Opin Support Palliat Care. 2016;10(3):223-7.