Buprenorphine/Naloxone tablet picture

Buprenorphine Treatment for Opiate Addiction-2014

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What is Buprenorphine?

Buprenorphine Brand names:
Suboxone®1, Subutex®2, Zubsolv®3, Bunavail™4, Probuphine®5



Buprenorphine

suboxne tablets in bottle
Suboxone(bup/nx) tablets

Buprenorphine is an opioid medication used to treat opioid addiction in the privacy of a physician's office. It can be dispensed for take-home use, by prescription. This, in addition to the pharmacological and safety profile, makes it an attractive treatment for patients addicted to opioids.

At the correct dose, buprenorphine suppresses cravings and withdrawal symptoms and blocks the effects of other opioids.

Buprenorphine is not new. It was first patented in 1969 and has been used in the U.S. to treat pain and in Europe to treat pain and opioid addiction for over 20 years, and is a semi-synthetic opioid and is a partial agonist.

buprenorphine ceiling effect graph
Fig. 1. Unlike full agonist opioids, buprenorphine has a limit to its effects

Buprenorphine can act as both an agonist and antagonist. It attaches to the opioid receptors but only activates them partially, enough to suppress withdrawal and cravings, but not enough to cause extreme euphoria in opioid-tolerant patients. When all available receptors are occupied with buprenorphine, no additional opioid effect is produced by taking more. This is called the 'ceiling effect'. The antagonist property of the medication expels, replaces and blocks other opioids from the opioid receptor sites. Therefore, if the patient decides to misuse opioid drugs after taking buprenorphine, the effects can be blocked, depending on dosage. Alternately, if taken too soon after other opioids, by an opioid-physically dependent patient, the buprenorphine can precipitate withdrawal. The ceiling effect, blocking ability, and possibility of precipitating withdrawal, contribute to buprenorphine having a favorable safety profile and helps lower the risk of overdose and misuse.5

Buprenorphine (Bup) and
Buprenorphine / Naloxone (bup/nx) combination

In October 2002 the FDA approved the first two prescription bup medications for the treatment of opioid addiction; Subutex® (bup) and Suboxone® (bup/nx). Since 2009 the FDA approved generic bup and bup/nx sublingual tablets, the brand-name bup/nx sublingual tablet called Zubsolv® and a buccal film bup/nx product called Bunavail. Both Suboxone and Subutex tablets were discontinued and replaced with Suboxone Film® which is a bup/nx sublingual film.

Suboxone Film Packet 8mgs
Suboxone Film single-unit packaging
single Suboxone (bup/nx) 8mg film
 bup/nx 8/2mg.

The only reason for the addition of naloxone is to reduce the risk of misuse of full agonist opioids by injection. If the bup/nx combination is injected, the naloxone can help cause immediate withdrawal symptoms in opioid-physically dependent people. However, naloxone is poorly absorbed sublingually. Therefore, when taken as directed, very little naloxone enters the blood. Normally, patients are unaffected by the presence of it, and it is considered clinically insignificant. Buprenorphine itself can cause withdrawal in physically dependent people misusing full agonist opioids. Naloxone may only slightly attenuate the effects of buprenorphine if misused by injection.

Generic bup/nx bottles
Generic bup/nx 8/4mg 2/1mg

Isn't buprenorphine just switching one addiction for another?

No, because with successful bup or bup/nx 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. Remember, it is the uncontrollable compulsive behavior that we're looking to stop, because that's what's destructive, not taking a medication. With all the drug war propaganda we've been exposed to it's easy to mistake the problem as a drug problem when really it is the addiction that is destructive. At one time the two were the same, but with the advent of treatment medications, being anti-drug might lead someone to dismiss effective evidence-based treatment medications.

How Buprenorphine works

opioid receptors not occupied  - withdrawal

Opioid receptor is empty – As someone becomes tolerant to opioids, they become less sensitive and require more opioids to produce the same effect. Whenever there is an insufficient amount of opioid receptors activated, the patient feels discomfort. This happens in withdrawal.

receptors occupied with strong opioid - high

Opioid receptor satisfied with a full agonist opioid - The strong opioid effect of heroin and painkillers can cause euphoria and stop the withdrawal for a period of time (4-24 hours). The brain begins to crave opioids, sometimes to the point of an uncontrollable compulsion (addiction), and the cycle repeats and escalates.

receptors occupied with buprenorphine - no high, no withdrawal, no cravings

Opioids replaced and blocked by bup - Buprenorphine competes with the full agonist opioids for the receptor. Since bup has a higher affinity (stronger binding ability than other opioids) it expels existing opioids and blocks others from attaching. As a partial agonist, the bup has a limited opioid effect, enough to stop withdrawal but not enough to cause intense euphoria.

Buprenorphine leaves receptors slowly - long acting

Over time (24-72 hours) bup dissipates - but still creates a limited opioid effect (enough to prevent withdrawal) and continues to block other opioids from attaching to the opioid receptors. Since bup is long acting, patients remain out of withdrawal between doses.


References:
  1. Suboxone tablets FDA approved in Oct. 2002. Tablets discontinued in the US in 2011 in favor of a film version.
  2. Subutex (bup) brand tablets discontinued in the US in 2009. Generics available.
  3. Zubslov, brand name bup/nx tablet better bio-availability, lower dose, with better taste. - site
  4. Bunavail, Bup/Nx FDA approved 6-6-2014. buccal film, better bio-availability, lower dose, less side effects.
  5. Probuphine Bup 6 month implant, rejected by FDA. More research needed expected approval in 2016
  6. National Alliance of Advocates for Buprenorphine Treatment- www.NAABT.org

Notes:

  1. Brand names for buprenorphine/naloxone (bup/nx)

    combination products in the US:
    Suboxone Film
    ,
    Zubsolv
    ,
    Bunavail
    , and generic equivalents of the discontinued Suboxone Sublingual Tablets.
  2. Buprenorphine products in the US WITHOUT the added naloxone

    safeguard:
    1. Subutex Tablets
      (
      discontinued in 2009
      ) but the
      generic equivalents remain available
      .
    2. Buprenex®
      is an injectable,
      FDA approved for pain
      NOT addiction -
      illegal to prescribe for opioid addiction
      .
    3. Butrans®
      Patch, also
      FDA approved for pain
      and NOT addiction -
      illegal to prescribe for opioid addiction
      .
    4. Pharmacy-compounded bup or bup/nx
      preparations - NOT FDA approved for addiction -
      illegal to prescribe for opioid addiction
      .
  3. Probuphine®
    is an insertable
    buprenorphine rod
    which goes under the skin and releases bup over the course of 6 months. It is
    not FDA approved yet
    , but will be for the treatment of addiction.
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Disclaimer:

  1. Nothing on this site should be confused for medical advice. The information provided here should only serve to inspire you to find out more from credible sources. We hope to help you understand the disease better so that you know what questions to ask your doctor. Never take any online medical advice over that of a healthcare professional, assume it's all made up. Despite the links to peer reviewed studies all interpretations of said studies may be opinion, unreliable or erroneous. If some patients found something beneficial to them it's not an indication that it will be beneficial to you, on the contrary, it may be dangerous. You, not us, are responsible for what you do with the information you get from this site or any site.

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