. In the past decade it has gained increasing popularity as a safer alternative to methadone
. Discover how this drug affects the body, its role in addiction treatment, and possible risks to be aware of.
Background & History
First developed in the 1970s, buprenorphine was approved by the FDA for use in treating opioid addiction in 2002. It is an opioid classified as a mixed agonist-antagonist. This means that the drug can variously act both as an agonist and an antagonist:
- Agonist – a substance that produces a physiological response when paired with a cellular receptor
- Antagonist – a substance that binds with a receptor but does not activate it, and blocks other agonists
Buprenorphine is available in different formulations under the brand names Cizdol, Subutex
, Temgesic, Buprenex, Norspan, and Butrans.
Similar to other opioids, when used as an agonist, buprenorphine can activate the opioid receptors in the brain and function as a painkiller. While a less common application of the drug, pain relief is an approved use of buprenorphine.Treatment with buprenorphine is typically for chronic pain, as opposed to acute pain or post-surgical discomfort. There are specific formulations for this use in both injectable and transdermal patch form.
Use in Treating Addiction
The primary use of buprenorphine is in the treatment of opioid dependence. As part of opioid replacement therapy, it can assist a patient manage cravings and withdrawal symptoms during drug detox
and ongoing treatment.
Opioid Replacement Therapy
Also called opioid maintenance therapy, opioid replacement therapy (ORT) involves replacing more dangerous opioids like heroin
with substitutes that are longer lasting and produce less euphoric highs.Along with other courses of treatment, the use of a substitute opioid allows patients to manage cravings and withdrawal symptoms. Over time they are safely and gradually weaned off the opioid substitute.
Buprenorphine vs. Methadone
For many decades, methadone was the primary opioid replacement in these treatments. However, studies suggest the pharmacology of buprenorphine allows for safer ORT treatment for a couple of reasons:
- Ceiling effect – unlike methadone, the euphoric effects of buprenorphine increase to a point and then level off, even with additional doses. Because this built-in “ceiling” produces a weaker high, there is a lower risk for abuse and dependence than methadone.
- Longer-lasting – buprenorphine typically lasts longer than methadone so many patients may not need daily administrations. This makes it easier to stay on a course of treatment.
While buprenorphine interacts with some opioid receptors in the brain, it blocks others. This has the added benefit of preventing other, more dangerous opioids from reacting with receptors if taken while buprenorphine is active.Because of its relative safety, buprenorphine does not require the heavily controlled clinical administration that methadone does. This improves patient access to treatment that might otherwise be challenging.
Buprenorphine shares similar adverse side effects as other types of opioids. Commonly reported side effects include:
- Drowsiness or insomnia
- Loss of coordination
- Shallow breathing
- Blurred vision
- Nausea, vomiting or stomach pain
- Memory loss or difficulty concentrating
- Dry mouth
- Sexual dysfunction
Even though buprenorphine is used to help mitigate withdrawal symptoms from other opioids, ceasing use of the drug can produce its own symptoms. Withdrawal symptoms may include:
- Drug cravings
- Nausea and vomiting
- Muscle aches
- Digestive distress
- Fever or chills
As with any drug treatment, be sure to follow the guidance of a doctor or clinic to manage symptoms and ensure safety.
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Buprenorphine is an opioid medication used in for pain management as well as treatment for