What is Buprenorphine?
Buprenorphine is a medication approved by the Food and Drug Administration (FDA) to treat opioid use disorder (OUD) as a medication-assisted treatment (MAT). As with all medications used in MAT, buprenorphine should be prescribed as part of a comprehensive treatment plan that includes counseling and other behavioral therapies to provide patients with a whole-person approach.
Here we will discuss about:
What is Buprenorphine and What Does it Treat?
Buprenorphine is a partial opioid agonist, which means it operates in a similar way to an opioid but has less side effects than a full agonist opioid like heroin or methadone. Buprenorphine also has a "ceiling effect," which means that the opioid effects diminish as the dosage is increased. As a result, there is a lower risk of misuse, dependence, and negative effects.
Buprenorphine reduces the symptoms of opioid addiction, such as withdrawal symptoms and the desire to use opioids, without having the full intensity or effects of opioids.
Buprenorphine has also been used to treat chronic pain in rare cases. However, research on its effectiveness for this purpose is contradictory. Many doctors believe that among those who aren't addicted to opioids, buprenorphine is ineffective as a painkiller.
How Buprenorphine Works
Buprenorphine has unique pharmacological properties that help:
Reduce the likelihood of misuse
Reduce the side effects of opiate addiction, including as withdrawal symptoms and cravings.
Increase the level of safety in case of an overdose.
Buprenorphine is a partial opioid agonist. This means it has similar effects to opioids, such as euphoria and respiratory depression. However, the effects of buprenorphine are less potent than those of full-strength opiates like heroin and methadone.
The opioid effects of buprenorphine increase with each dose until they level at moderate doses, even with further dose increases. This "ceiling effect" reduces the likelihood of abuse, dependence, and negative side effects. Many people may not need to take buprenorphine every day because of its long-acting action.
Comparision of buprenorphine products
The main differences between medications containing buprenorphine are method of administration, timing of administration, and whether naloxone is present.
Suboxone is a drug that combines buprenorphine and naloxone. It's available as a tablet and a film. The film can be placed under the tongue or inside the cheek, and the tablets disintegrate under the tongue. Suboxone is an opioid addiction drug that can be administered at any stage of medication-assisted treatment.
Bunavail contains buprenorphine and naloxone, and it comes in a buccal film that is placed inside the cheek. The Bunavail film has a higher bioavailability of buprenorphine than the Suboxone film. A Bunavail buccal film containing 4.2 mg of buprenorphine and 0.7 mg of naloxone is equivalent to a Suboxone film containing 8 mg of buprenorphine and 2 mg of naloxone.
Zubsolv is similar to Suboxone. It is available in tablet form and contains both buprenorphine and naloxone. However, Zubsolv has higher buprenorphine bioavailability than Suboxone, which means that a lower dose of Zubsolv delivers the same amount of buprenorphine as a higher dose of Suboxone. Suboxone films typically contain 8 mg of buprenorphine and 2 mg of naloxone, whereas Zubsolv contains 5.7 mg of buprenorphine and 1.4 mg of naloxone.
Subutex is the brand name for a buprenorphine-containing medication. It came in the form of sublingual tablets that dissolved under the tongue and was intended for use during the early stages of opioid addiction treatment. Subutex does not contain naloxone, an ingredient that acts as a deterrent to opiate drug abuse. Subutex in sublingual form was discontinued in the United States in 2011, but it is still available in generic form.
Probuphine is a drug that is implanted into the upper arm's skin. Over the course of six months, buprenorphine is steadily released. Patients who forget to take their meds on time may benefit from this approach. The implant is only successful in persons who have been stabilized on low-to-moderate dosages of a buprenorphine-containing medication (no more than 8 mg per day).
Side Effects of Buprenorphine
Buprenorphine’s side effects are similar to those of opioids and can include:
Nausea, vomiting, and constipation.
Muscle aches and cramps.
Inability to sleep.
Distress and irritability.
Buprenorphine Misuse Potential
Because of buprenorphine’s opioid effects, it can be misused, particularly by people who do not have an opioid dependency. Naloxone is added to buprenorphine to decrease the likelihood of diversion and misuse of the combination drug product. When these products are taken as sublingual tablets, buprenorphine’s opioid effects dominate and naloxone blocks opioid withdrawals. If the sublingual tablets are crushed and injected, however, the naloxone effect dominates and can bring on opioid withdrawals.
People should use the following precautions when taking buprenorphine:
Do not take other medications without first consulting your doctor.
Do not use illegal drugs, drink alcohol, or take sedatives, tranquilizers, or other drugs that slow breathing. Mixing large amounts of other medications with buprenorphine can lead to overdose or death.
Do ensure that a physician monitors any liver-related health issues that you may have.
Pregnant or Breastfeeding Women and Buprenorphine
Limited information exists on the use of buprenorphine in women who are pregnant and have an opioid dependency. But the few case reports available have not demonstrated any significant problems resulting from use of buprenorphine during pregnancy. The FDA classifies buprenorphine products as Pregnancy Category C medications, indicating that the risk of adverse effects has not been ruled out.
Review SAMHSA’s Federal Guidelines for Opioid Treatment Programs – 2015 for more information about the use of buprenorphine in pregnancy. In the United States, methadone remains the current standard of care for the use of MAT with pregnant women who have opioid dependency.