What medications can ease the side effects of tapering off high-dose opioids (narcotic analgesics)?

From the Guidelines

Medications such as clonidine, lofexidine, and gabapentin can effectively ease the side effects of tapering off high-dose opioids. When considering the management of opioid tapering side effects, it's crucial to prioritize medications that directly attenuate opioid withdrawal symptoms. According to the consensus panel recommendations published in the Mayo Clinic Proceedings in 2020 1, α2-Agonists like clonidine can suppress withdrawal symptoms, although careful titration is necessary due to potential hypotension. Lofexidine, which is FDA-approved for controlling opioid withdrawal symptoms, is another viable option.

For managing anxiety, insomnia, and irritability associated with opioid tapering, medications such as trazodone, gabapentin, and mirtazapine have been reported to be beneficial for short-term use 1. It's essential to note that while these medications do not specifically counteract the physiologic changes of opioid withdrawal, they can mitigate the psychological and physical discomfort. Gastrointestinal discomfort, a common side effect, may respond to loperamide, but clinicians should be aware of its potential for abuse and dangerous arrhythmias at high doses 1.

Key considerations for medication selection include:

• The potential for hypotension with clonidine and the need for careful titration
• The FDA approval of lofexidine for opioid withdrawal symptom control
• The short-term benefits of trazodone, gabapentin, and mirtazapine for anxiety, insomnia, and irritability
• The risk of abuse and arrhythmias associated with loperamide

In clinical practice, a tailored approach using these medications, alongside a gradual taper schedule, can provide the best chance for successful opioid discontinuation while minimizing discomfort. The choice of medication should be guided by the specific symptoms experienced by the patient and careful consideration of the potential benefits and risks.

From the FDA Drug Label

Inform patients seeking to discontinue treatment with buprenorphine for opioid dependence to work closely with their healthcare providers on a tapering schedule and inform them of the potential to relapse to illicit drug use associated with discontinuation of opioid agonist/partial agonist medication-assisted treatment

• Buprenorphine can be used to ease the side effects of tapering off high-dose opioids.
• Patients should work closely with their healthcare providers on a tapering schedule to minimize side effects.
• The goal is to reduce the risk of relapse to illicit drug use associated with discontinuation of opioid agonist/partial agonist medication-assisted treatment 2

From the Research

Medications for Easing Side Effects of Opioid Tapering

• Gabapentin has been shown to be effective in alleviating hyperexcitatory painful states in opiate dependence and can be used as an add-on therapy to methadone, leading to relief of withdrawal symptoms and lower methadone consumption 3
• Clonidine is an alternative agent that can be used off-label to treat opioid use disorder, although its toxic effects should be considered 4
• Loperamide, an over-the-counter medication, can be used in supratherapeutic doses to treat opioid withdrawal symptoms, but its toxic effects should also be considered 4
• Cannabinoids, such as cannabidiol (CBD) and tetrahydrocannabinol (THC), may be considered for patients experiencing opioid-related complications, and can be initiated and titrated in conjunction with opioid tapering 5
• Methadone and buprenorphine are effective pharmacologic treatments for opioid use disorder, and can be used to retain people in treatment programs and decrease illicit opioid use 4

Opioid Tapering Methods

• A two-stage method of opioid tapering may be more effective in preventing withdrawal symptoms than a monotonous tapering method, especially in patients receiving higher-dose opioids with longer administration duration 6
• Opioid tapering should be initiated when the patient reports a minor or major improvement in function, seeks less as-needed medication to control pain, and/or the cannabis dose has been optimized 5
• The opioid tapering schedule may be 5%-10% of the morphine equivalent dose (MED) every 1 to 4 weeks 5

Monitoring and Evaluation

• Patients should be monitored for withdrawal symptoms, pain intensity, and opioid-related adverse events during opioid tapering 6, 5
• Clinical success can be defined by an improvement in function/quality of life, a ≥30% reduction in pain intensity, a ≥25% reduction in opioid dose, a reduction in opioid dose to <90 mg MED, and/or reduction in opioid-related adverse events 5