What is Buprenorphine?

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What is Buprenorphine?

Buprenorphine is an opiod (narcotic analgesic) derived from thebaine (codeine methyl enol ether), an opiate alkaloid. Thebaine is similar to morphine and codeine, all isolated ingredients from the opium poppy. Buprenorphine is a bit different to other opiates, however, in that it has a stimulatory rather than depressive effect.

Commercial formulations include Bunavail, Cizdol, Subutex, Suboxone, and Zubsolv. It is available as sublingual (under tongue) tablets, transdermal patches, and injections.

What is buprenorphine indicated for?

It is primarily used in medicine to treat moderate pain in lower doses, as well as opiod withdrawal, dependence, and replacement therapy in higher doses. Typical opiods targeted for replacement are heroin and oxycodone.

It is a semi-synthetic drug, meaning that is has naturally-derived components as well as components manufactured in a lab.

What is buprenorphine for withdrawal similar to in function?

Buprenorpphine is similar to methadone. Both are used for detoxification during withdrawal for opiods. They are similar in effectiveness and benefit/risk, but buprenorphine is typically less sedating. There is also another critic difference, which may help explain why buprenorphine is generally safer and less addicting that other opiates.

There are three types of drugs – agonist, antagonist, and partial agonist.

An agonist drug binds to and activates opiate receptors in the brain FULLY. An example of an agonist are the highly potent opiods heroin and oxycodone.

An antagonist drug bind to receptors, but instead of activating them, it blocks them from usage. It is a narcotic that basically reverses the effects of other narcotics. Examples of an opiate antagonist is naloxene. This is often used in case of opiod overdose.

A partial antagonist activates the receptors, but to a lesser extent, and also acts as an antagonist, blocking other opiods. Buprenophine is a partial antagonist, meaning it has the qualities of both agonists and antagonists, making it the perfect drug for withdrawal and dependence. In this sense, buprenophine is very unique drug. Methadone, on the other hand, is a straight-up agonist.

Patients dependent on very high doses of opiods generally do better on methadone. Because of the unique quality of buprenorphine, it has a ceiling effect (point where the effect does not increase) at a moderate dose. Thus, many of its effects may be similar to full agonists, but it’s maximal effect is much less, and therefore, safer.

What is buprenorphine dosage?

Buprenophine dosage depends on formulation, administration method, patient characteristics, and purpose. For example, Subotex as a subligual tablet is typically used for maintenance treatment (for dependence) and can range from 4mg to 24mg per day, often given in progressive amounts in increments of 2mg.

What are serious side effects of buprenorphine?

Although buprenorphine is a relatively safe drug, there are some possible adverse reactions of concern:

  • Confusion
  • Shortness of breath/trouble breathing or shallow breathing
  • Dizziness or light-headed feeling, especially when quickly moving from a lying or sitting position
  • Pale blue lips, nails, or skin
  • Unusual fatigue
  • Diarrhea or vomiting
  • Depressed mood
  • Abnormally fast or slow heart rate

If you suspect that you or someone you know is addicted to an opiate/opiod, please seek help immediately.

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