What exactly is Buprenorphine?

 

Buprenorphine (BYOO-pre-NOR-feen) ('bū-pre-'nôr-fēn) is an opioid medication used to treat opioid addiction in the privacy of your own home. Buprenorphine can be dispensed for take home use, by prescription. This in addition to buprenorphine’s pharmacological and safety profile makes it an attractive treatment for patients addicted to opioids.

Buprenorphine is different from other opioids in that it is a partial opioid agonist. This property of buprenorphine may allow for;

 

  1. less euphoria and physical dependence

  2. lower potential for misuse

  3. a ceiling on opioid effects

  4. relatively mild withdrawal profile

 

At the appropriate dose buprenorphine treatment may:

  1. Suppress symptoms of opioid withdrawal

  2. Decrease cravings for opioids

  3. Reduce illicit opioid use

  4. Block the effects of other opioids

  5. Help patients stay in treatment

 

Buprenorphine ('bū-pre-'nôr-fēn) (C29H41NO4) is a semi-synthetic opioid derived from thebaine,

an alkaloid of the poppy Papaver somniferum. Buprenorphine is an opioid partial agonist. This

means that, although Buprenorphine is an opioid, and thus can produce typical opioid effects and

side effects such as euphoria and respiratory depression, its maximal effects are less than those of

full agonists like heroin and methadone. At low doses Buprenorphine produces sufficient agonist

effect to enable opioid-addicted individuals to discontinue the misuse of opioids without

experiencing withdrawal symptoms. The agonist effects of Buprenorphine increase linearly with

increasing doses of the drug until it reaches a plateau and no longer continues to increase with

further increases in dosage. This is called the "ceiling effect." Thus, Buprenorphine carries a lower

risk of abuse, addiction, and side effects compared to full opioid agonists. In fact, Buprenorphine can

actually block the effects of full opioid agonists and can precipitate withdrawal symptoms if

administered to an opioid-addicted individual while a full agonist is in the bloodstream. This is the

result of the high affinity Buprenorphine has to the opioid receptors. The affinity refers to the

strength of attraction and likelihood of a substance to bind with the opioid receptors. Buprenorphine

has a higher affinity than other opioids and as such will compete for the receptor and win. It will

"knock off" other opioids and occupy that receptor blocking other opioids from attaching to it. If

there is enough Buprenorphine to knock the opioids off the receptors but not enough to occupy and

satisfy the receptors, withdrawal symptoms can occur; in which case the treatment is more

Buprenorphine until withdrawal symptoms disappear.

Suboxone, contains both buprenorphine and the opiate antagonist naloxone. Naloxone has

been added to Suboxone to guard against intravenous abuse of buprenorphine by individuals

physically dependent on opiates. If misused by injection, the naloxone will help cause immediate

withdrawal in opioid dependent people, however when taken sublingually, as indicated, the naloxone

is clinically insignificant.


Is buprenorphine treatment just trading one addiction for another?

No- with successful buprenorphine treatment, the compulsive behavior, the loss of control of drug use, the constant cravings, and all of the other hallmarks of addiction vanish. When all signs and symptoms of the disease of addiction vanish, we call that remission, not switching addictions.

The key to understanding this is knowing the difference between physical dependence and addiction.

Buprenorphine will maintain some of the preexisting physical dependence, but that is easily managed medically. Physical dependence, unlike addiction, is not a dangerous medical condition that requires treatment. Addiction is damaging and life-threatening, while physical dependence is an inconvenience, and is normal physiology for anyone taking large doses of opioids for an extended period of time.

It is essential to understand the definition of addiction and know how it differs from physical dependence or tolerance.

The American Academy of Pain Medicine (AAPM), American Pain Society (APS), American Society of Addiction Medicine (ASAM), and (NAABT) National Alliance of Advocates of Buprenorphine Treatment, have recognizes these definitions below.

  1. I.Addiction:
    Addiction is a primary, chronic, neurobiologic disease, with genetic, psychosocial, and environmental factors influencing its development and manifestations. It is characterized by behaviors that include one or more of the following: impaired control over drug use, compulsive use, continued use despite harm, and craving.

 

  1. I.Physical Dependence:
    Physical dependence is a state of adaptation that is manifested by a drug class specific withdrawal syndrome that can be produced by abrupt cessation, rapid dose reduction, decreasing blood level of the drug, and/or administration of an antagonist.

 

  1. I.Tolerance:
    Tolerance is a state of adaptation in which exposure to a drug induces changes that result in a diminution of one or more of the drug's effects over time.

 

Physical dependence and tolerance are normal physiology. Addiction is a disorder that is damaging and requires treatment.

When a patient switches from an addictive opioid to successful buprenorphine treatment, the addictive behavior often stops. In part due to buprenorphine's long duration of action, patients do not have physical cravings prior to taking their daily dose. The drug seeking behavior ends. Patients regain control over drug use, compulsive use ends, they are no longer using despite harm, and many patients report no cravings. Thus all of the hallmarks of addiction disappear with successful buprenorphine treatment.

Therefore, one is not trading one addiction for another addiction. They have traded a life-threatening situation (addiction) for a daily inconvenience of needing to take a medication (physical dependence), as some would a vitamin. Yes the physical dependence to opioids still remains, but that is vast improvement over addiction, is not life threatening, and it can easily be managed medically. It's also important to note that the physical dependence pre-existed the buprenorphine treatment and was not caused by it.

Addiction is a brain disease that affects behavior. This addictive behavior can be devastating to the patient and their loved ones. It's not the need to take a medication that is the problem, many people need to take a medication, but rather it is the compulsive addictive behavior to keep taking it despite doing harm to one's self or loved ones that needs to stop. Whether or not the person takes a medication to help achieve this shouldn't matter to anyone. If a medication helps stop the damaging addictive behavior, then that is successful treatment and not switching one addiction for another.