FDA Approves Lofexidine, First Non-Opioid Drug to Treat Symptoms of Opioid Withdrawal

approved with pill bottle
Benita Lee
Benita Lee, MPH, is on the Research Team at GoodRx.
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This week, the FDA approved lofexidine hydrochloride (Lucemyra), the first medication in the US developed to specifically treat the symptoms of opioid withdrawal.

Physical symptoms of withdrawal — like stomach cramps, muscle spasms, and insomnia — are a major reason why people relapse when trying to fight opioid addiction. As the first non-opioid approved to target these symptoms, lofexidine is an important milestone for the country’s fight against the current opioid crisis.

Before lofexidine, the FDA had only approved three medications to treat opioid withdrawal: methadone, buprenorphine, and naltrexone.

Methadone (Dolophine) and buprenorphine (Suboxone) are opioid drugs that patients can use as substitutes if they’re addicted to a more dangerous opioid like heroin. During addiction treatment, they help curb withdrawal symptoms as doses are tapered until the patient stops taking opioids altogether.

This process isn’t foolproof by any means. Because they’re also opioids, methadone and buprenorphine can be addictive themselves. Both drugs are also controlled substances, which means many patients have difficulty accessing them.

Then there’s naltrexone (Revia). Unlike methadone and buprenorphine, extended-release naltrexone is intended for long-term opioid addiction management, is not a controlled substance, and is not addictive.

Here’s the problem though: a patient who’s addicted to opioids can’t use naltrexone until they’ve detoxed and gone through withdrawal. But many patients are too scared or unable to cope with the symptoms of withdrawal before even getting to the point where they can take naltrexone. So, despite being a safer drug, naltrexone is often not used.

Approved for almost two decades in the UK, lofexidine is not meant to treat opioid withdrawal, but can play a role in long-term addiction management without involving other opioids. For example, lofexidine may reduce the symptoms of opioid withdrawal as patients detox and switch to long-term treatment with naltrexone or another long-term treatment modality. It also gives doctors another option to choose from when tailoring treatment plans to fit their patients’ needs.

Originally developed to treat high blood pressure, lofexidine blocks the release of norepinephrine, a brain chemical that’s believed to be the cause of many painful withdrawal symptoms. Typical dosing consists of three 0.18 mg tablets taken four times daily during the time when withdrawal symptoms are strongest (usually 5-7 days after stopping opioid use).

Currently, the FDA has approved lofexidine for use up to 14 days in adults, but safety studies for longer use and use in children (who have perhaps taken opioids while critically ill) are underway. Common side effects include low blood pressure, slow heart rate, sleepiness, sedation, and dizziness. Additional studies are looking into whether lofexidine has dangerous effects on the liver and/or blood pressure.

The US manufacturer of lofexidine, US WorldMeds, is marketing the drug under the brand name, Lucemyra, and expects it to be commercially available in August 2018 — though they have yet to release any estimates pertaining to cost.

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