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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

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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 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.

The other forms such as patch and implant are really not that common, there

wasnt much information on these forms as they arent first choice for many people.

Some of the side effects that come with these forms include headache, depression,

constipation, nausea, vomiting, back pain, toothache, implant site pain, itching, redness,

etc. Regardless its an effective form of treatment as well, more than half of the

participants in a recent study showed no sign of opioid use after six months compared

with the 64% who used sublingual buprenorphine. It was almost completely equal which

is quite amazing.

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
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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 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, they both have the same purpose when it comes down to it. Methadone is
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more of a drug that needs to be given by a clinic everyday. The patient will have to go in

daily and receive the medication from one of those doctors or individuals there.

Buprenorphine can be given in a prescription, over a weeks time, a month or even a

couple of days. The real big difference being the price, buprenorphine is definitely more

expensive when it comes down to the price. Both again, both fight the same disease or

addiction. One is not proven to be better than the other, its all a matter of looking at the

dosing schedule, side effects, abuse and cost.

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.

Many people are coming around to the idea of buprenorphine for help with addiction. Its

taken a lot of time but people are definitely coming around to the idea.

It is hard to get your hands on this medication because only a number of doctors

have the correct training to prescribe it. Even at that rate a doctor is only able to prescribe

to thirty patients at a time, this prevents the drug from getting out of control.

In conclusion, buprenorphine is an effective form of treatment for opioid abuse. It

has a lot of benefits and can be used in any real setting including work and home. In my

opinion its a better choice than methadone because it is a take home medication that can

be hidden from the family members of an addict. The patient doesnt have to constantly
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be going into the clinic for their medication which is nice. Buprenorphine gives addicts a

better chance at living a normal life on the road to recovery as far as I am concerned. The

combination of buprenorphine and naloxone was also such a good idea, it literally cannot

be abused which gives peace of mind not only to the addict but also to their close

intermediate family, people that care about them. Buprenorphine is a great form of

treatment for addiction.

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Works Cited

Welsh, Christpoher Buprenorphine. US National Library of Medicine (2005)

Jones, Hendree. Practical Considerations for the Clinical Use of Buprenorphine. US National

Library of Medicine (2004)

Marotta, Ryan FDA Approves First-Ever Buprenorphine Implant. Pharmacy Times (2016)

Peddicord, Adam A Comparison of Suboxone and Methadone in the Treatment of Opiate

Addiction Journal of Addiction Research & Therapy (2015)

Painkiller abuse treated by sustained buprenorphine/naloxone National Institutes of Health

(2011)