SUBOXONE AND SUBUTEX
Suboxone and Subutex are manufactured by Reckitt Benckiser Pharmaceuticals, Inc. These opioid drugs were approved by the Food and Drug Administration in 2002. Only doctors approved by the Substance Abuse and Mental Health Services Administration, a department in the United States Department of Health and Human Services, are allowed to dispense Suboxone and Subutex 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 also 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 between 24—60 hours. Opioids are generally classified as Schedule II drugs, but because they have less ability to be abused, Suboxone and Subutex are classified as Schedule III drugs.
WHY COMBINE A PARTIAL AGONIST AND AN ANTAGONIST?
When people learn that Suboxone contains an antagonist, there is a reluctance to take something that could throw them into withdrawal. The naloxone is included in the Suboxone to prevent it from being crushed and snorted or injected.
The reason is bioavailability. Bioavailability is a term used to define how effectively a drug can be absorbed and used by the body. Buprenorphine has poor bioavailability if just swallowed and moderate bioavailability if placed under the tongue (sublingual) and allowed to dissolve. What this means is that normally a person will get the effects of approximately 40-60% of the buprenorphine when taken sublingually and allowed to dissolve but this will activate, partially, the endorphin producing receptors and provide the extra stimulation needed to make the withdrawal more comfortable. If administered sublingually, naloxone has low bioavailability and the person will receive only about 10% 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 increased but only by about twice as much as if it were taken sublingually. However, the effect of the naloxone will be increased by 15 times and will dominate. The naloxone will bind to the receptors and block the buprenorphine from activating the receptors and this will precipitate the painful withdrawal which can occur if Suboxone is misused.
Subutex contains just buprenorphine. In order for it to be effective, It is 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 the person completes their medical detox using Suboxone.
HOW PARTIAL AGONISTS LIKE BUPRENORPHINE CAN TRIGGER WITHDRAWAL
Many of our patients have heard, or even experienced, taking a partial agonist like buprenorphine and immediately going into withdrawal and getting very sick. They believe that this is Suboxone withdrawal but it is not. 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 you take buprenorphine, it goes to the receptors and literally kicks out any other full agonists that were there and still activating the receptors, and then it effectively seals that receptor off and will commence to partially activate it to produce endorphins but at a much lower level and this creates the symptoms of withdrawal.
This lowering of endorphin production continues longer because Suboxone is slower-acting than many other opioids and stays on the receptor for a longer period of time.
Using our elevator analogy, if the full agonist was still stimulating some of the receptors before the introduction of the partial agonist and causing our elevator to rise to the eighth floor, buprenorphine evicts the full agonist but only produces enough endorphins for the elevator to go to the fourth floor. This is like suddenly being dropped from the eighth floor to the fourth floor. It isn’t as bad as being dropped all the way to the first floor, but the person is going to get very sick as the body reacts to the sudden lowering of the amount of endorphins available—similar to trying to withdraw at home from opioids by just not taking them.
From one of our patients:
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“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 is taking Suboxone or Subutex and needs help,
CALL Novus Medical Detox Center NOW:
We are available 7 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.