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Sublingual Buprenorphine

Drug Interactions

Sublingual buprenorphine may react with a number of other medicines (see Drug Interactions With Sublingual Buprenorphine).
 

What If I Overdose on This Medicine?

An overdose of this medication can be quite dangerous and even fatal. It is important that you seek immediate medical attention if you or someone else may have overdosed on sublingual buprenorphine.
 
(Click Subutex Overdose for more information.)
 

How Does It Work?

Sublingual buprenorphine contains buprenorphine, an opioid narcotic medication. Buprenorphine binds to specific types of opioid receptors, called opioid mu-receptors, which are located throughout the body. While the main effects occur in the central nervous system, buprenorphine can produce effects anywhere opioid mu-receptors are found.
 
Buprenorphine does not work well when swallowed, as only a small amount of the medication is actually absorbed into the bloodstream, mainly because it is destroyed by the liver first. However, sublingual buprenorphine is dissolved under the tongue and is absorbed directly through the tissues, avoiding this "first-pass effect" of the liver.
 
Some of the effects of buprenorphine are desirable. Others are undesirable and cause the side effects associated with buprenorphine use, which may include but are not limited to:
 
  • Pain relief
  • Drowsiness
  • Changes in mood, including feelings of unease (dysphoria) or unusually pleasant feelings (euphoria)
  • Cough suppression
  • Slowed or shallow breathing
  • Slowing of the digestive tract
  • Physical dependence.

 

Interestingly, buprenorphine is a partial (not full) agonist of mu-receptors. This means that it binds to the receptors, but only partially activates them. This usually translates into less of a chance of abuse, although this is not always the case.
 
Compared to full agonists, such as morphine, partial agonists, including sublingual buprenorphine, usually have a "ceiling effect." This means that there is a certain dosage after which taking more of the drug does not cause any further effects. This might make sublingual buprenorphine less dangerous than full agonist drugs, particularly in the case of an overdose.
 
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Sublingual Buprenorphine Information

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