Everything You Need to Know About Buprenorphine

Buprenorphine is a prescription medication used to help patients withdraw from opioids. Ironically, buprenorphine is itself an opioid often prescribed by physicians and was the first drug of its kind to be approved by the FDA to treat opioid addiction.

If you suffer from opioid addiction or have a loved one struggling with opioid addictions, you should research buprenorphine. By understanding the characteristics of buprenorphine, how it’s used, the buprenorphine ceiling effect, and the risks involved, you can minimize associated risks and prevent overdose.

When administered properly, buprenorphine is not used by itself but in tandem with other addiction therapies such as individual psychotherapy, relapse prevention, behavior modification, or the 12 step program. Buprenorphine can be administered in an inpatient setting or taken in a patient’s home environment.

How Buprenorphine works

Buprenorphine is a Schedule III substance. By definition, a Schedule III substance means that it has less potential for being abused than drugs in Schedules I and II. It can still lead to moderate physical dependence if abused, despite acting as legitimate medical treatment. Though buprenorphine has been around since 1965 and has been legal to use in the United States since 1981, it’s only come to the general public’s attention in recent years.

Buprenorphine blocks the effects of other opioids such as heroin or hydrocodone. When it locks into a mu-opioid receptor in the central nervous system, it acts as a partial agonist. Even if the buprenorphine does bind to the receptor, the receptor is only partially activated. An opioid such as heroin would fully activate the receptor.

Buprenorphine not only blocks other drugs that would bind with the receptor, but the patient doesn’t feel the intense high that they would with an opioid such as heroin. At the same time, the patient escapes these severe withdrawal symptoms. With the assistance of buprenorphine, these substance-use sufferers are more likely to survive an overdose of buprenorphine than they would an overdose of another opioid. Because the euphoric effects of buprenorphine are much less intense, there’s less risk of it being abused or used recreationally.

How do you administer the buprenorphine

Medical personnel administer buprenorphine in a variety of ways. Physicians prescribe tablets that patients place under the tongue. In some cases, buprenorphine is a film applied under the tongue, an implant, or an extended-release injection. Often, physicians combine buprenorphine with naloxone, another opioid, for optimal results. Naloxone comes in both film and tablet forms.

Patients who begin a buprenorphine course need to abstain from their opioid use for 12 to 24 hours. Once they’ve hit this 24-hour mark, they will enter the withdrawal phase—a necessary evil. If they still have opioids in their system and haven’t gone into withdrawal, their withdrawal symptoms can be severe.

The dosage of buprenorphine and how long the patient stays on it depends on the individual patient. Some patients need to take buprenorphine for years to prevent relapsing.

Side effects of buprenorphine

Because buprenorphine is an opioid, it slows down the workings of the central nervous system. With this in mind, the common side effects include:

• constipation
• dry mouth
• insomnia
• heart palpitations
• sweating
• nausea and vomiting
• dizziness
• muscle cramps
• fever
• dilated pupils

More serious side effects include severe respiratory depression, dependence, itching skin, and potential overdose. Though physicians can prescribe pregnant women with buprenorphine, there’s a risk that it can lead to neonatal abstinence syndrome. NAS is a condition where the baby exposed to an opioid during pregnancy undergoes withdrawal shortly after birth.

To ensure that taking buprenorphine is as safe as possible, the patient shouldn’t discontinue or take other drugs with this opioid without consulting with their doctor. Any patient taking buprenorphine should have their liver monitored and tell the doctor if they’re pregnant or planning to become pregnant. A patient’s buprenorphine prescription should never be shared, even with another patient experiencing opioid addiction.

Buprenorphine ceiling effect

As previously discussed, respiratory depression is one of the side effects of buprenorphine. However, scientists believe that because buprenorphine is only a partial agonist at the opioid receptors, the respiratory depression has a ceiling and will not progress to the point where the patient’s breathing shuts down completely. With heroin and other opioids, the patient is at risk of death. Taking buprenorphine makes it less likely that the patient will die of an overdose.

This is a guest blog entry.