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Medications That Prevent Opiate Effects

Written by The Recovery Village

& Medically Reviewed by Dr. Kevin Wandler, MD

Medically Reviewed

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Last Updated - 07/07/2024

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Updated 07/07/2024

Key Takeaways

  • Opiates affect the brain’s opioid receptors, leading to euphoria and pain reduction, but also addiction and altered brain chemistry.
  • Opiate blockers, such as naloxone and naltrexone, are used to counteract the effects of opioids and are crucial in treating addiction and overdose.
  • Medications like naltrexone, methadone and buprenorphine are key in opioid addiction treatment, with each offering different benefits.
  • Medication-assisted treatment (MAT) combines opiate blockers with counseling and behavioral therapies, proven to improve patient outcomes.
  • Policy changes aim to expand access to addiction treatments, but challenges like stigma and care barriers for marginalized groups remain.
  • Research into new opiate blockers and treatments, such as non-opioid pain medications, is ongoing to address the opioid crisis.

What are Opiate Blockers?: Their Role and Function

Opiate blockers, also known as opioid antagonists, are medications designed to prevent opiates from exerting their effects on the brain and body. These drugs are crucial in the treatment of opioid addiction and overdose, providing a way to counteract the potentially life-threatening consequences of opioid misuse. 

Why Opiate Blockers Are Used

The use of opiate blockers is a key strategy in addressing the opioid epidemic, which has seen a rise in opioid-involved overdose deaths. While these medications are a vital tool in addiction treatment, they are also part of a broader approach that includes updated prescribing guidelines, monitoring and the exploration of non-opioid therapies for pain management. The goal is to reduce the risk of opioid dependence while ensuring that patients with legitimate pain needs continue to receive appropriate care.

How Opiate Blockers Work

Opiate blockers work by binding to the same receptors in the brain that opiates target, but instead of activating these receptors, they block them. This action prevents opiates from producing their typical euphoric and pain-relieving effects, which can help individuals avoid the cycle of addiction.

Common Opiate Blockers Used in Addiction Treatment

Three of the most commonly used opiate blockers are naltrexone, methadone and buprenorphine. Each has unique properties and mechanisms of action that contribute to their effectiveness in managing addiction.

  • Naloxone: It is primarily used in emergencies to reverse opioid overdose, rapidly displacing opioids from the receptors due to its strong affinity. Naloxone is considered a pure mu-opioid receptor competitive antagonist, which means it competes directly with opioids for receptor sites without activating them.
  • Methadone: With the longest history of use in OUD treatment since 1947, methadone is a full opioid agonist. It has been effective in reducing opioid use and associated risks such as infectious disease transmission and criminal behavior. Patients on methadone have shown better long-term outcomes and are more likely to stay in treatment compared to those not receiving it.
  • Buprenorphine: Approved in 2002, buprenorphine is a partial opioid agonist available alone or in combination with naloxone. It has shown similar effectiveness to methadone in reducing opioid-positive drug tests and heroin use, especially at medium-to-high doses. However, lower doses of buprenorphine may be less effective than methadone in retaining patients in treatment.
  • Naltrexone: Originally approved in pill form, Naltrexone is used for longer-term management in opioid addiction treatment. By blocking the euphoric and sedative effects of opioids, naltrexone reduces cravings and helps individuals in recovery maintain their sobriety. Extended-release formulations have demonstrated higher treatment retention and reduced drug craving and relapse.

These medications not only mitigate withdrawal symptoms and cravings but also improve the likelihood of individuals remaining in treatment. Successful treatment with these medications is linked to a lower risk of overdose, reduced transmission of HIV and hepatitis C, decreased criminal activity and an increased chance of employment. 

Opiate Blockers in Addiction Recovery Strategies

Opiate blockers  are integral to Medication-Assisted Treatment (MAT) protocols, which combine pharmacological interventions with counseling and behavioral therapies to treat substance use disorders. MAT has been recognized for its effectiveness in increasing patient survival, retaining people in treatment and improving the ability to gain and maintain employment.

Recent policy changes, such as those implemented by the Biden-Harris Administration, have aimed to expand access to these life-saving treatments. These include updating federal regulations to facilitate treatment access and amending criteria for opioid treatment program admission. 

Despite advancements in treatment options and policies, challenges remain, such as the stigma surrounding addiction, barriers to care for marginalized populations and the need for more comprehensive insurance coverage. 

Guidelines for Opiate Blocker Use in Addiction Treatment

Effective dosage and treatment duration vary depending on the specific medication and patient needs. For example, Buprenorphine typically has a maximum dose of 24 mg daily, which could be increased to 32 mg to manage withdrawal symptoms or cravings. Treatment protocols must also consider the transition from full opioid agonists to opiate blockers, where gradual tapering is often necessary.

Extended-release formulations of Naltrexone and Buprenorphine offer alternatives for those requiring long-term maintenance or struggling with adherence. These treatments, including monthly injections of Naltrexone, have the advantage of reducing the risk of diversion or misuse.

Adherence to the CDC’s Clinical Practice Guideline is crucial, with recommendations focusing on the initial opioid prescription duration, follow-up assessments and addressing potential harms of opioid use. The guideline encourages shared decision-making between clinicians and patients, ensuring tailored treatment plans that suit individual patient circumstances and promote recovery.

Benefits and Challenges of Opiate Blocker Treatments

Studies have shown that buprenorphine depot formulations can significantly increase abstinence rates compared to placebo, with some studies reporting abstinence rates as high as 41.3% and 42.7% in buprenorphine groups versus 5.0% in the placebo group. Moreover, the use of long-term buprenorphine implants has shown promising results in maintaining abstinence, with rates of 85.7% compared to 71.9% for sublingual buprenorphine over six months.

Despite these successes, the treatment landscape faces several challenges. Access to opioid treatment programs (OTPs) is uneven across the United States, with certain communities, particularly those of color, experiencing more stringent treatment requirements. These ‘liquid handcuffs’ — daily observed dosing and regular drug screens — can disrupt daily life and work schedules. Furthermore, some states have regulations that hinder the establishment of new OTPs, limiting patient access to these vital services. 

The Future of Opiate Blocker Research

The future of opiate blocker research and development is poised to address the ongoing opioid crisis with innovative biotechnological solutions. Recent studies, such as those applying infectious disease frameworks to predict opioid overdose trends, suggest that the opioid epidemic may reach its peak and subsequently decline.

Biotechnological advancements are at the forefront of new treatment modalities. Promising developments include depot injections, agonist/antagonist implants, deep brain stimulation and hapten conjugate vaccines. These technologies aim to minimize illicit opioid use, reduce the risk of overdose and painful withdrawal symptoms and prevent the diversion of medications to illicit markets. 

As the crisis evolves, the scientific community is also exploring the potential of targeting specific neurochemical receptors, such as corticotropin-releasing factor-1 and κ-opioid receptors, to mitigate heroin escalation and withdrawal-induced hyperalgesia. 

Emerging Opiate Blockers and Their Impact on Addiction Treatment

The advent of new opiate blockers is a significant development in the field of addiction treatment. One such promising drug is VX-548, an experimental pain medication that has recently met its primary goal in a late-stage clinical trial. As reported by CNN, VX-548 is poised to seek approval from the US Food and Drug Administration and could become the first new class of acute pain medicine in over twenty years.

Unlike opioids, VX-548 operates by blocking pain in the peripheral nervous system instead of acting in the brain, potentially reducing the safety risks and addictive potential associated with opioid use. Despite failing to demonstrate superior efficacy to hydrocodone/acetaminophen in a trial, the development of VX-548 represents a shift towards safer pain management alternatives. 

Evolving Opiate Blocker Policies and Regulations

The evolution of policies and regulations surrounding opiate blockers is a critical aspect of the ongoing efforts to combat the opioid epidemic. The US Drug Enforcement Administration (DEA) has consistently reduced the aggregate production quotas (APQs) for prescription opioids, with an 8.3% cut in codeine and a 7.6% cut in fentanyl, among others, proposed for 2024.

These measures aim to curtail the risk of diversion, misuse and overdose despite concerns about the impact on patients with legitimate medical needs and potential supply interruptions for inpatient care. DEA’s policy reflects an ongoing commitment to balance patient access against the imperative to limit opioid misuse.

As the landscape of opioid addiction treatment shifts, the American Medical Association (AMA) emphasizes the importance of addressing racial inequities and ensuring that marginalized communities receive equitable care. The AMA’s national policy roadmap and legislative actions, like the Comprehensive Addiction and Recovery Act (CARA) and the 21st Century Cures Act, highlight the multifaceted approach needed to end the drug overdose epidemic. 

End Opioid Addiction and Dependence Today

If you are struggling with a drug or alcohol addiction, it might be time for professional treatment. The experts at The Recovery Village Palm Beach at Baptist Health are able to identify and treat substance use disorders as well as other co-occurring mental health conditions. Contact us today to learn more about treatment programs that can work well for you.

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