Buprenorphine/Naloxone (Suboxone®)

What is Buprenorphine/Naloxone?

Buprenorphine is a medication that was approved for the treatment of Opioid Use Disorder in 2002. It is often used on its own to alleviate the symptoms of opioid withdrawal, but is more commonly combined with Naloxone in a product most widely known as Suboxone®.

As a partial opioid agonist, Buprenorphine does not activate the opioid receptors fully, and physicians recommend that patients be in mild withdrawal before starting Buprenorphine treatment. In addition, the medication has a ceiling effect meaning that the effects will not continually increase with the dosage.

Why is the Buprenorphine mixed with Naloxone?

Naloxone is an opioid antagonist, which means that it does not cause any opioid effects, and if taken improperly causes immediate withdrawal symptoms. These can include nausea, vomiting, diarrhea, muscle cramps, etc. To be considered improper use, the Naloxone must enter the bloodstream, usually by injection. The combination of Naloxone and Buprenorphine is simply intended as a deterrent to misuse.

How is it taken?

Buprenorphine/Naloxone is a tablet that is taken “sublingually,” meaning it is placed under the tongue or in the cheek to dissolve. It is helpful to drink water before taking to moisten the inside of the mouth.

Does Buprenorphine/Naloxone have any side effects?

Most people experience few, if any, side effects. Some of the most common, and generally mild, side effects include:

  • Constipation
  • Sweating
  • Cold or flu-like symptoms
  • Headache
  • Sleep disturbances
  • Upset stomach or vomiting

Suboxone®, or any Buprenorphine medication, should not be taken with benzodiazepines or alcohol as there is danger of significant respiratory depression. If a patient takes benzodiazepines, or other medications, they should speak to their medical provider before starting a Buprenorphine/Naloxone treatment program.

What is Precipitated Withdrawal?

Precipitated withdrawal is a condition where the patient may experience severe withdrawal symptoms when taking their first dose of Buprenorphine/Naloxone if they have other opioids still in their system. There are two reasons why this might occur.

  1. Buprenorphine/Naloxone has “low intrinsic activity” because it is a partial opioid agonist. This means when the molecule attaches to a receptor site in the brain, it does not activate or light up that receptor to the same extent most other opioids do, including methadone. You can think of it like a light switch. Where methadone and other opioids turn the light on, Buprenorphine/Naloxone acts like a dimmer switch.
  2. Buprenorphine/Naloxone also has “high affinity” meaning it is a very “sticky” molecule. Once attached to the receptor, it does not like to come off. This is one of the reasons it so long acting.

So what does this have to do with precipitating withdrawal? If an individual who takes Buprenorphine/Naloxone for the first time also has other opioids in their system, the Buprenorphine/Naloxone will compete with that other opioid for the receptor. Because of its “high affinity,” it wins the battle, throwing the other opioid off the receptor site and taking its place.

Once Buprenorphine/Naloxone is in the receptor its “lower intrinsic activity” does not activate the receptor to the same extent as the opioid that was just removed. This is what causes the withdrawal. It is precipitated, meaning it comes on suddenly, and the severe symptoms are difficult to overcome for hours.

It is very important that patients present for the first dose of Buprenorphine/Naloxone in a state of mild to moderate withdrawal to eliminate the possibility of unnecessary discomfort.

How long should I wait after my last opioid use before starting Suboxone®?

In order to start Suboxone treatment, you have to be in active withdrawal. Initial withdrawal symptoms generally include yawning, sneezing, sweating, nausea, and muscle cramping. Our treatment center staff can help you determine if you are in withdrawal or not. In general, most short acting opioids (like heroin, fentanyl, morphine, and oxycodone) result in withdrawal symptoms starting about 6 hours after consumption, but this varies by individual. If you have used a long-acting opioid (like Methadone), you will need to wait much longer to enter withdrawal.

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