Buprenorphine/naloxone: 7 things you should know
Medically reviewed by Carmen Fookes, BPharm. Last updated on April 16, 2020.
1. How it works
- Buprenorphine/naloxone tablets are a combination tablet containing buprenorphine and naloxone.
- Buprenorphine is an opioid (narcotic) that has a unique and complex mechanism of action, which includes incomplete binding to mu opioid receptors and complete binding to kappa opioid receptors. Opioid receptors have three main effects: reducing breathing (respiratory depression), producing euphoria (feelings of intense happiness or excitement), and decreasing pain. The way buprenorphine binds means it can satisfy opioid cravings without producing strong feelings of euphoria or causing significant respiratory depression. In addition, while it is bound to opioid receptors, other opioids (such as heroin, oxycodone) cannot bind. It also stays on the receptors for longer - about three days; which makes it a good choice for use in opioid addiction treatment programs.
- Naloxone is present in this combination tablet to discourage misuse. Naloxone is a very strong blocker of mu opioid receptors and will precipitate people into opioid withdrawal if drug misusers attempt to convert the tablet into an injectable form. Naloxone has virtually no other effect when taken sublingually.
- Buprenorphine/naloxone belongs to the class of medicines known as combination opioid/opioid antagonists.
- Used in the treatment of opiate dependence (under strict conditions), usually after an initial induction with buprenorphine sublingual tablets.
- Can be given as a single daily dose.
- Dosage can be progressively adjusted until the correct dosage is found that holds the patient in treatment and suppresses opioid withdrawal symptoms.
- Buprenorphine/naloxone is available in generic versions and as a branded version (Suboxone).
If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:
- Constipation, diarrhea, difficulty sleeping, flushing or redness of the skin, headache, nausea or vomiting, pain, and sweating are some of the more common side effects.
- Oral numbness has also been reported with the buccal film.
- Has the potential to cause serious, life-threatening breathing problems. This is more likely in people who misuse buprenorphine/naloxone, or when it is used in combination with other medications that also affect breathing.The elderly or debilitated, and those with pre-existing breathing problems are also at higher risk.
- May be habit-forming, even at the dosage prescribed by your doctor.
- May cause sleepiness or dizziness and affect a person's ability to drive or operate machinery. Alcohol should be avoided
- Abnormal liver function tests have also been reported; ongoing tests that monitor liver function may be needed.
- May cause a severe lowering of blood pressure, or a sudden drop in blood pressure when going from sitting to standing.
- Risk of heart rhythm disorders (such as QT prolongation), particularly at higher dosages.
- Brands of buprenorphine/naloxone are not interchangeable (for example, Suboxone sublingual tablets require a different dose than Bunavail buccal film). Monitor for signs of over-medication as well as withdrawal or under-dosing when switching brands.
- Misuse of buprenorphine/naloxone can cause addiction, overdose or death.
Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects
- Never share buprenorphine/naloxone with another person, particularly those with a history of drug abuse or addiction.
- Sublingual tablets must be placed under the tongue and allowed to dissolve; swallowing the tablets reduces how much buprenorphine is actually absorbed
- If using Bunavail buccal film, rinse the mouth with water or wet the inside of the cheek before placing the film inside the mouth. Hold the film in place for 5 seconds; the film should stay in place after this. Avoid manipulating the film with your tongue or fingers or eating or drinking until the film has dissolved. Never cut or tear the film.
- Do not eat or drink anything until buprenorphine/naloxone has completely dissolved.
- Brands of buprenorphine/naloxone are not interchangeable. When switching between brands, dosage adjustments may be necessary. Talk with your doctor.
- Buprenorphine/naloxone can cause sedation and affect your ability to drive or operate machinery.
- Do not drink alcohol while you are taking buprenorphine/naloxone.
- Talk to your doctor or pharmacist before taking any other medications or natural products with buprenorphine/naloxone because it may not be compatible with some products.
- Keep out of reach of children and pets because even one dose can be fatal.
- Tell other health providers including dentists that you are being treated with buprenorphine/naloxone.
6. Response and Effectiveness
- The time it takes to absorb buprenorphine/naloxone varies significantly from person to person; however, in most people, the peak effect is reached within 100 minutes.
- Buprenorphine has a ceiling effect, which means that once a certain dose is reached, further doses produce no further effect.
- Coadministration with liquids reduced the absorption of buprenorphine by 59% and naloxone, by up to 76%, which is why the film should be allowed to dissolve in the mouth without water or food.
Medicines that interact with buprenorphine/naloxone may either decrease its effect, affect how long it works for, increase side effects, or have less of an effect when taken with buprenorphine/naloxone. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.
Common medications that may interact with buprenorphine/naloxone include:
- antibiotics, such as azithromycin, clarithromycin, erythromycin, and norfloxacin
- antidepressants, such as tricyclic antidepressants (eg, amitriptyline), monoamine oxidase inhibitors (eg, isocarboxazid, phenelzine, and tranylcypromine), or SSRIs (eg, fluoxetine, sertraline)
- antifungal agents, such as itraconazole and ketoconazole
- anticonvulsants, such as brivaracetam, carbamazepine, divalproex, lamotrigine, phenytoin, phenobarbital, or primidone
- antipsychotics (such as butyrophenones, phenothiazines, or thioxanthenes) and atypical antipsychotics (eg, aripiprazole, olanzapine, quetiapine, ziprasidone)
- any medication that may cause drowsiness, such as benzodiazepines (eg, alprazolam, diazepam, lorazepam), sleeping pills (such as zolpidem or ziprasidone) or first-generation antihistamines (such as doxylamine or promethazine)
- heart medications such as amlodipine, atenolol, or candesartan
- HIV medications, such as delavirdine or ritonavir
- muscle relaxants, such as baclofen or cyclobenzaprine
- opioids such as codeine, fentanyl, or morphine
- sodium oxybate
- other medications that affect serotonin, such as amphetamines, lithium, tramadol, or triptans (eg, almotriptan, eletriptan, or sumatriptan).
Avoid grapefruit products and drinking alcohol or taking illegal or recreational drugs while taking buprenorphine/naloxone.
Note that this list is not all-inclusive and includes only common medications that may interact with buprenorphine/naloxone. You should refer to the prescribing information for buprenorphine/naloxone for a complete list of interactions.
Buprenorphine/naloxone. Revised 03/2020. Drugs.com https://www.drugs.com/ppa/buprenorphine-and-naloxone.html
Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use buprenorphine/naloxone only for the indication prescribed.
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