What is Buprenorphine?

Buprenorphine is an FDA approved opioid addiction treatment. Currently Subutex® & Suboxone® are the only Buprenorphine medications approved by the FDA.

Buprenorphine itself is opioid itself, but the maximal effects are less than other more dangerous opioid agonist like methadone and herion. By producing enough agonist, individuals taking Buprenophine that have become addicted to other opioids are able to discontinue abuse with minimized withdrawl side-effects.

In 1965, K.W. Bentley discovered the class of compounds synthesized from an alkaloid of thebaine, the opium poppy plant, known as Papaver somniferum. Among these semi-synthetic compounds is Buprenorphine – the first in a series of opioid agonists. Many were more than 1000 times more effective than the analgesic, morphine.

In the 1980s, Reckitt & Colman, today known as Reckitt Benckiser, introduced Buprenorphine hydrochloride for sale. Buprenorphine, an analgesic, was first made in sublingual tablets of 0.2 mg (Temgesic). It was also made as an injectable of 0.3 mg/ml (Buprenex).



Buprenorphine Successfully Treats Opioid Addiction

Opioids are narcotics used in pain management and to induce sleep.

Physiologic reactions, similar to those caused by a substance found in nature, are produced by a drug known as an opioid agonist, that merges with a cell’s opioid receptor. Opiate receptors are scattered abundantly throughout the digestive tract, spinal cord and the brain. Morphine is an opioid agonist.

On the other hand, a drug known as an opioid antagonist will combine with and block nerve receptors, thwarting the physiological actions of a substance found in nature. Thus, it may reverse and even block the actions of an opioid agonist. Naloxone is a typical opioid antagonist.

Buprenorphine is a partial agonist opioid; It can generate the usual opioid agonist effects but, not as greatly as those produced by full agonists, such as heroin and methadone. Full agonist opioids have the risk of side effects, abuse, and addiction. Not only does Buprenorphine have fewer risks, but it can negate all the effects of opioid agonists, and even lessen withdrawal symptoms in an addict whose bloodstream is currently carrying a full agonist.

Low doses of Buprenorphine enable patients to stop misusing drugs without suffering intense withdrawal symptoms. A “ceiling effect” is reached when the agonist effects no longer increase in concurrence with dosage and stops at a moderate dose. A Buprenorphine overdose is less likely than an overdose of a full opioid agonist.

Laws, Limitation, and Lack of treatment

Although Buprenorphine promised great results, due to outdated guidelines, it was unavailable to most addicts; Doctors were limited to treating only thirty addict patients at any given time, and only in specific addiction treatment centers. The numbers of addicts seeking medical help had been sharply increasing and countless addicts had died for lack of medical treatment needed to overcome their addiction. A cacophony of concerns was heard in both the medical community and in buprenorphine treatment centers. The few addicts successfully treated with Buprenorphine brought about changes in the laws that enabled even greater numbers of addicts to also successfully beat their habit.



DATA 2000

The Drug Addiction Treatment Act (DATA) went into effect in the year of 2000. Qualified physicians may now prescribe narcotics that are specifically approved for use in settings other than methadone clinics.

DATA 2000 also decreases the regulations that burden physicians and allows them to attain waivers described in the Controlled Substances Act (CSA). The qualifying credentials of the physician must be noted in the Intent Notification. Other papers validating the physician’s capacity to send in-therapy addiction patients to non-pharmacologic therapy must be included. The physician must also note that, regardless of the number of office-based practices the physician may have, a limit of 30 or fewer patients will be in addiction therapy and counseling during the first year.

One year from the date of the primary Letter of Intent, the physician can present a second notice stating necessity and intention of treating up to, but not more than 100 patients.

Detoxification, Medically Assisted Withdrawl

Jacqueline H. Kostick, PhamD in the article “Buprenorphine Offers Alternative to Methadone for Opioid Dependence”, observes that Methadone has its limitations in the treatment of opioid dependency. Since it is classified as a controlled substance, Methadone must be used only in hospitals or at a Methadone addiction clinic.

Buprenorphine, as a Methadone replacement in the treatment of opioid dependency, was found to be just as effective. Because Buprenorphine, as a partial agonistic opioid, contains properties that aid in the prevention of drug abuse, it has become the chosen drug in treating addicts during the maintenance period.

Buprenorphine’s sublingual tablet formulations, Suboxone and Subutex, was approved by the (FDA) Food and Drug Administration in October 2002, for detoxifying and for the longtime therapy substitute for methadone in the treatment and therapy of opioid dependency. Buprenorphine currently predominates as the drug of choice to aid patients while they are in heroin and opium withdrawal.



Side Effects of Buprenorphine

Like other opioids, Buprenorphine can have withdrawl side effects:

  • Unable to Sleep
  • Cramps & Muscle Aching
  • Diarrhea, Nausea, & Vomiting
  • Cravings
  • Fever
  • Irritability

Addiction Therapy

There are 3 phases of Buprenorphine treatment therapy

  1. Induction Phase – 12 to 24 hours after last opioid use, where Buprenorphine is medically administered.
  2. Stabilization Phase – patient no longer craves opioid, useage has stopped or decreased significantly, and no longer experiencing side effects.
  3. Maintenance Phase – the detox phase where patient usage of opioid has stopped and Buprenorphine dosage is steady or ended completely.



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