How does buprenorphine work?

Buprenorphine is a partial mu-receptor agonist that attaches to receptors in the brain. More on how burprenorphine works in the central nervous system and in the body here.

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Prescribed buprenorphine is important part of pharmacological treatment for heroin or opiate addiction. We have prepared this article to describe how buprenorphine works in the brain and the body, the length if its duration of action, and how to optimize your use of buprenorphine. Save your questions at the end. We try to respond to all questions and comments with a personal and prompt reply.

How does buprenorphine affect the brain?

Buprenorphine is a natural alkaloid of the opium poppy and semi-synthetic, partial opioid agonist derived from thebaine. In general, opioids (synthetic opiates) attach to receptors in the brain. Buprenorphine, an opioid sold as brand name Suboxone or Subutex) is a partial mu-receptor agonist with a slow rate of dissociation. This means that buprenorphine has the ability to stick to the receptors and block them a lot longer than other opioids or opiates. In effect, buprenorphine binds to brain receptor but without a perfect match, which results in occupation of these receptors without all of the opioid effects – the reason why it’s used to treat heroin or opiate addition. In other words, receptor acts as if they have been affected by opiates WITHOUT stimulating a strong and disturbing euphoric effect.

How does buprenorphine affect the body?

Buprenorphine mainly causes physical effects of reduced respiration and decreased pain. Although buprenorphine can produce typical opioid agonist effects, compared to heroin and methadone, is a lot weaker. However, at low doses it justifies its medicinal use, enabling opioid addicted individuals to discontinue misuse of opioids avoiding the uncomfortable withdrawal symptoms. Still, users go through a period of withdrawal upon cessation of use after developing physical dependence on the opioid. What does withdrawal from buprenorphine feel like? Like a really severe flu.  The main routes of buprenorphine administration are intramuscular injection, intravenous infusion, transdermal patch, ethanolic liquid oral solution and sublingual tablets.

How fast or quickly does buprenorphine work?

It is difficult to determine how quickly buprenorphine begins to work. The rate of onset is determined by a number of factors such as the drug’s route of administration, its half‐life, and its lipophilicity (which determines how fast the drug reaches the brain). Buprenorphine has poor oral bioavailability and moderate sublingual bioavailability.

When taken as prescribed, buprenorphine has a “balancing effect” on the brain and should take effect in the first days after initial dosing. The formulations used in prescriptions usually take the form of sublingual tablets, pills which are put under the tongue and let them melt. The half-life of buprenorphine varies between 24 and 60 hours, depending on the drug history of the user and the dose administered.

How long does buprenorphine work?

Buprenorphine is a long-acting form of opioid addiction treatment, with the ability to stay in the brain’s opiate receptors for over 24 hours. Buprenorphine is metabolized by the liver, with an elimination half-life of 20 to 73 hours.

How does buprenorphine work better?

Tablets containing buprenorphine, such as Suboxone or Subutex, are prescribed only by a physicians who have attended a special training and received a certificate for buprenorphine prescription for opioid addiction treatment. In order to avoid fake prescriptions, each doctor is allowed to treat not more than 30 patients with prescribed buprenorphine.

So, the best way to use buprenorphine is to follow the doctor’s recommendations and not change the timeline and prescribed doses. One thing is certain, buprenorphine should not be taken with any other drugs or medications and definitely should not be mixed with alcohol. Poly-drug use and drug interactions (such as mixing buprenorphine and alcohol) may only increase adverse effects to an unknown limit.

Does buprenorphine work for everyone?

No, buprenrophine does not work for everyone. Many drugs, including buprenorphine, manifest gender-specific differences in rates of abuse, overdoses and fatalities. Sometimes weight loss, codependency, problems sleeping, and depression can occur as unwanted side effects of taking buprenorphine. Further, buprenorphine is highly not recommended for use during pregnancy, although it is well known for use in treating neonatal abstinence. Additionally, some users will develop a level of tolerance towards buprenorphine and can experience withdrawal even after low dose, short-term use.

Buprenorphine use questions

If you have any question related to how buprenorphine works in the body, the brain, or how use of burprenorphine can trigger drug abuse, please use the space in the comments section to ask your question or post your comments. We will do our best to provide you with a personal and prompt answer.

Reference Sources: NY State Department of Health: Buprenorphine: A New Drug for Treating Heroin Addiction
National Institute of Health: Buprenorphine: A Unique Drug With Complex Pharmacology
SAMSHA: The Facts About Buprenorphine
About the author
Lee Weber is a published author, medical writer, and woman in long-term recovery from addiction. Her latest book, The Definitive Guide to Addiction Interventions is set to reach university bookstores in early 2019.
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