Suboxone and Subutex Information: Buprenorphine Withdrawal

Suboxone and Subutex Information: Buprenorphine Withdrawal

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Suboxone and Subutex

Suboxone and Subutex are drugs manufactured by Reckitt Benckiser Pharmaceuticals, Inc. These opioid drugs were approved by the Food and Drug Administration (FDA) in 2002. The only doctors allowed to dispense these drugs are ones approved by the Substance Abuse and Mental Health Services Administration, a department in the United States Department of Health and Human Services, and they can only do so in medical detox facilities or for outpatient Suboxone maintenance.

Suboxone contains buprenorphine, a partial agonist, and naloxone, an antagonist. The proportion is four parts of buprenorphine and one part naloxone. Suboxone comes in two dosage forms: two milligrams buprenorphine and 0.5 milligrams of naloxone and eight milligrams of buprenorphine and two milligrams of naloxone.

Half-Life of Suboxone and Subutex

It is important to remember that one of the reasons that buprenorphine is so effective in medical detox is that it has a half-life, the time it takes for half of a drug to leave the body, of 24 to 60 hours. Opioids are generally classified as Schedule II drugs, but because they are less likely to be abused, Suboxone and Subutex are classified as Schedule III drugs.

Why Combine a Partial Agonist and an Antagonist?

Some people, upon learning that Suboxone contains an antagonist, are reluctant to take it because of the chance that they could be thrown into withdrawal. However, this effect can be mitigated through proper use, aka by not crushing it to be snorted or injected into the bloodstream.

The naloxone included in this drug serves that purpose through what is known as bioavailability, a medical term used to define how effectively a drug can be absorbed and used by the body. Buprenorphine has poor bioavailability when swallowed, but moderate bioavailability when placed under the tongue (sublingual) and allowed to dissolve.

This means that normally, a person will get the effects of approximately 40 to 60 percent of the buprenorphine when taken sublingually and allowed to dissolve. However, this will partially activate the endorphin producing receptors and provide the extra stimulation the person taking the drug needs to make the withdrawal more comfortable. When naloxone is administered sublingually, it has low bioavailability and the person taking it will only receive about 10 percent of the drug. This means that a person taking Suboxone sublingually will receive mostly the effects of the partial agonist and very little of the antagonist.

On the other hand, if Suboxone is crushed and injected into the bloodstream, the effect of the buprenorphine will be slightly increased, but the effect of the naloxone will be increased tenfold. The naloxone will bind to the receptors and block the buprenorphine from activating the receptors, causing far more significant withdrawal symptoms.

Unlike Suboxone, Subutex only contains buprenorphine. In order for this drug to be effective, it needs to be taken sublingually like Suboxone. Subutex is often used in some of our medical protocols for a short time if someone has been taking heavy doses of opioids, then we transition our patient over to Suboxone to complete their medical detox.

How Partial Agonists Like Buprenorphine Can Trigger Withdrawal

Many of our patients have heard that taking a partial agonist like buprenorphine can lead to immediate withdrawal symptoms – some have even experienced it firsthand. While some believe that this is Suboxone withdrawal, it is not. In fact, it is withdrawal caused by taking Suboxone too soon.

The answer is simple: endorphin receptors prefer buprenorphine, the opioid in Suboxone, to other full agonist opioids. When taking buprenorphine, the drug goes to the receptors and kicks out any other full agonists that were there and still activating the receptors before effectively sealing that receptor off. It then partially activates it to produce endorphins at a much lower level, which leads to the withdrawal symptoms. This lowering of endorphin production continues longer because Suboxone is slower-acting than many other opioids, and it stays on the receptor for a longer period of time.

We like to use an elevator analogy when explaining the difference between this drug and other opiates. When the full agonist is stimulating some of the receptors in your brain, treat it like an elevator lifting up to the eighth floor of a building. When buprenorphine is introduced to the system, it kicks out the original stimulation and replaces it with only enough stimulation to lift up to the fourth floor. This will cause the figurative elevator to suddenly drop those four floors. While it isn’t as bad as being dropped all the way to the ground floor, it can still cause a significant reaction.

All of us here at Novus believe in the work that we do, and we’re not the only ones. From one of our patients:

"This place is the best place I've ever been to. I could not ask for anything more. Thank you so much. Y'all saved my life. Everyone here is the best. "This place gave me a lot more options with my pain. It gave me hope that there is a better life out there without drugs. I want a sober happy life. Thank you for everything."

If you or someone you care about needs help, call Novus Medical Detox Center now. We are available seven days a week to help. We can help you arrange a safer, more comfortable Suboxone detox or Subutex detox to help you on the way to permanently ending your opioid dependency or addiction.

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