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Adelaida Inger

Gustavo Ibarra

Health 1050 403

October 30, 2017

Research Paper: Buprenorphine

Addiction is a chronic, relapsing brain disease characterized by the pursuit of reward

and/or relief by substance use. Many drugs and medications carry the risk for addiction leading

many individuals to become dependent on these substances. There are many different routes

when it comes to treatment, one of the most effective forms being Buprenorphine.

Buprenorphine is an opioid medication used to treat opioid and/or heroin addiction, its unique

pharmacological characteristics make it ideal for use in a variety of settings. This medication is

secure, meaning not just anyone can get their hands on it, only so many doctors have the proper

training to prescribe buprenorphine. Its unique.

Buprenorphine is a semi synthetic opioid derived from thebaine, a naturally occurring

alkaloid of the opium poppy discovered sometime in the 1960s. Because it is an opioid, it can

produce some of the same effects as other opioids. It was originally developed as an analgesic or

pain reliever yet had been discussed for potential management of opioid dependence since the

early 1970s. n October of 2002 buprenorphine was approved by the FDA as a Schedule III

narcotic, its now used for treating opioid dependency and neonatal abstinence syndrome.

Buprenorphine comes in several different forms including pill (Suboxone/Subutex),

liquid (Buprenex), implant (Puobuphine) and even patch. Suboxone and Subutex are two of the

most commonly heard of, both are used sublingually, under the tongue. In the 1970s,

pharmaceutical companies were working hard to discover a medication that would provide a
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cure for addiction, the focus shifted from opiate agonists, such as buprenorphine, to opiate

antagonists like naloxone. Leading to the creation of Suboxone, a combination of both

buprenorphine and naloxone at a 4:1 ratio. Buprenorphine itself can be abused if injected, reports

of this very thing happening in other countries also pushed for naloxone in suboxone. Naloxone

is present in Suboxone to discourage misuse, if injected the naloxone will cause withdrawal in

patients that are already addicted to other opioids. It can not be absorbed orally, naloxone is

completely insignificant when taken properly, sublingually.

Before one can understand how Buprenorphine works in the brain, you must understand

how the brain works. The brain has three main opiate receptors called mu, kappa, and delta. The

release of endorphins onto these receptors causes pleasant sensations increasing the likelihood of

a person performing the same actions. For example, exercise, laughing and eating a favorite food

cause this release, making it more likely that we will repeat these actions in pursuit of that

feeling. Heroin and opioids on the other hand attach themselves to these receptors in the brain

with three main effects; euphoria, pain relief and reduced respiration. This makes it a whole lot

easier for people to develop a habit of continued use that will continually act on the receptors to

replicate those feelings. This is how opiate addiction and dependence is developed.

On the other hand, Buprenorphine is a partial mu-receptor agonist, meaning it binds to

the opioid receptors in the brain without a perfect match. The better the fit of opioid and receptor

the more the effects. As a result, the buprenorphine occupies the receptors without all the opioid

effects. The receptor is fooled into thinking it has been fully satisfied without the feelings of

euphoria and without causing significant respiratory depression, this prevents other opioids from

being able to bind with the receptors as well. If the patient uses heroin or painkillers, they are
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unlikely to experience additional effects. Buprenorphine tends to block the receptors a lot longer

than opioids do, its said to last up to three days.

Buprenorphine is also an antagonist of the kappa opioid receptor, this receptor plays a

vital role in producing some of the symptoms of opioid withdrawal. Some of the symptoms

include depression, anxiety, muscle aches, restlessness etc. Buprenorphine attaches to the kappa

receptor and slows the activity, inducing a positive food and feelings of well-being.

In a comparison of methadone and buprenorphine, there isnt much of a difference,

The unique pharmacological characteristics of this medication result in less overdose risk

than other opioids (morphine, heroin, methadone, etc.), less respiratory depression and lower

signs of withdrawal symptoms. In this sense, buprenorphine is more fit for many different types

of treatment settings. Buprenorphine can more effective when taken every other day or less, it is

designed for reduced potential for abuse. It has potential for better acceptance by the general

public, patients and healthcare providers.

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