BuprenorphineA medication that treats opioid addiction under supervision, and can become dangerous outside it

14What is buprenorphine?

It may seem strange to treat opioid addiction with an opioid medication. But buprenorphine was designed to give the brain just enough to stop withdrawal and cravings, without the surge that drives a person toward the next dose. That is why it has become one of the most important addiction treatment tools in the world.

Buprenorphine is a semi-synthetic opioid, classed by MedlinePlus as a “partial agonist-antagonist” at opioid receptors. It is used as tablets or films that dissolve under the tongue or inside the cheek to treat opioid dependence, and other forms exist for pain. According to the StatPearls review, the US Food and Drug Administration approved it in 2002 for opioid dependence, alone and combined with naloxone.

The World Health Organization’s guidelines for treating opioid dependence recommend medication combined with psychological support, and name buprenorphine and methadone as the two main options for substitution treatment. In other words, when buprenorphine is used with a prescription and a plan, it is a medication with a clear place in medicine, and calling it a “substitute drug” is inaccurate.

15How does buprenorphine work in the brain?

Buprenorphine binds to “mu” opioid receptors, the same receptors that heroin and morphine act on, but it activates them to a lesser degree. The US National Institute on Drug Abuse (NIDA) explains that it can also block other opioids from attaching to these receptors. This gives it four characteristics:

• Partial activation: enough to ease withdrawal and cravings, without the strong high in someone accustomed to opioids.
• Strong binding: it competes with other opioids for the receptor, weakening their effect if they are used on top of it.
• Ceiling effect: the StatPearls review notes that its effect on suppressing breathing has a ceiling, which makes it safer than methadone in substitution treatment, but this ceiling does not protect someone who mixes it with sedatives or alcohol.
• Long-acting: the average half-life is about 38 hours after taking it under the tongue, according to the same reference, so taking it once a day is often enough, as the doctor directs.

16What are the medical uses of buprenorphine?

17Forms of buprenorphine and its brand names

MedlinePlus notes that buprenorphine comes as sublingual tablets, and that its combination with naloxone comes as sublingual tablets under the name Zubsolv and as films placed under the tongue or in the cheek under the name Suboxone, while Subutex is the best-known brand name for buprenorphine alone. NIDA adds newer forms such as long-acting injections and implants. Available names differ from country to country.

Naloxone was added to Suboxone for a protective reason: it has almost no effect when the medication dissolves in the mouth as directed, but it causes unpleasant withdrawal if injected. For this reason, the StatPearls review notes that buprenorphine alone has a higher potential for misuse than its combination with naloxone.

18Is buprenorphine effective for treating opioid addiction?

Yes, and the evidence here is strong. A Cochrane review published in 2014 included about 31 randomized trials with more than 5,400 participants, and found, with high-quality evidence, that buprenorphine is better than placebo at keeping patients in treatment, and that at sufficient doses it reduces illicit opioid use. When the dose was adjusted to the patient’s needs, methadone was slightly better at retention, while the two medications were close in reducing use among those who stayed in treatment.

NIDA sums up the picture by saying that medications for opioid use disorder reduce the risk of death from overdose and of behaviors that spread infections, and that methadone and buprenorphine may be equally effective at reducing use. The choice between them is a medical decision that takes into account the severity of dependence, the person’s health and what is available.

19Precipitated withdrawal: why buprenorphine is not taken right away

Because buprenorphine binds tightly to the receptors, if it is taken while a full-strength opioid such as heroin or methadone is still in the body, it pushes that opioid off the receptors and replaces it with a weaker effect. The result is sudden, severe withdrawal called “precipitated withdrawal.” The StatPearls review notes that giving it too soon after a full agonist can cause this, which is why the doctor decides when to start based on the substance and the last use, usually after clear withdrawal signs appear.

20Why is buprenorphine misused?

• Trying to treat withdrawal on one’s own, without assessment or follow-up, using tablets obtained outside the medical system.
• Using it by injection or in larger amounts than prescribed in search of a stronger effect, especially in people not accustomed to opioids.
• Believing it is completely safe because it is a “treatment medication,” and so mixing it with sedatives, pregabalin or alcohol.
• Selling or sharing a prescribed medication, which MedlinePlus warns against because it may be targeted by people who misuse medications.

MedlinePlus explicitly warns against injecting the tablets or films because this can cause severe reactions, including withdrawal symptoms, and the StatPearls review links injecting it to liver damage in patients with hepatitis. A medication that protects under supervision becomes a danger when used in a way it was not designed for.

21Buprenorphine compared with methadone and naltrexone

Learn about naltrexone and the other addiction treatment medications; each suits a different patient.

22The legal status of buprenorphine in Egypt

Buprenorphine is a controlled opioid medication, dispensed only with a medical prescription and within a medical setting. Possessing, trading or using it outside this framework is an offense that exposes the person to legal liability. The availability of its forms and treatment programs varies from place to place, and the addiction physician determines the appropriate option available for each case. The Fund for Drug Control and Treatment of Addiction offers free, confidential treatment through the hotline 16023.

This is general educational information and not legal advice.

23Buprenorphine in numbers

Sources: the StatPearls review on buprenorphine, the Cochrane review (Mattick et al., 2014), and the US National Institute on Drug Abuse (NIDA). The last figure applies to the United States.

24Buprenorphine harms, withdrawal and how long it stays: in brief

Harms: the most common are constipation, headache, insomnia and drowsiness. Among the most serious are respiratory depression when mixed with sedatives, dental problems the Food and Drug Administration has warned about, and liver effects in some patients. Details are in the guide to buprenorphine harms.

Withdrawal: stopping suddenly causes symptoms similar to opioid withdrawal, though usually slower and milder, which is why stopping should be by gradual reduction decided by the doctor. After stopping, tolerance falls, so returning to heroin at the old amount becomes a deadly risk.

How long it stays: the usual opioid test does not detect it; it needs a specific test for the drug and its metabolite. Details are in the guide to how long buprenorphine stays in the body.

25Buprenorphine guide: everything you need to know

We have gathered everything about buprenorphine into 4 pages, each answering one question in detail. Choose what you are looking for:

26What should the family do if a member is taking buprenorphine?

1. If it is part of a treatment plan, support their attendance at appointments and do not pressure them to stop suddenly; the decision to reduce is made with their doctor.
2. Keep the medication locked away from children and visitors; a small amount can be dangerous to a child.
3. Tell any doctor or dentist that they are taking it before prescribing sedatives or painkillers or performing surgery.
4. If they are getting it without a prescription, treat it as opioid dependence that needs a specialist assessment. You can start with the guide to persuading a person with addiction to accept treatment.
5. Memorize the emergency signs and the ambulance number, 123.