Buprenorphine: 7 things you should know
Medically reviewed by Carmen Fookes, BPharm. Last updated on Nov 6, 2020.
1. How it works
- Buprenorphine is an opioid medicine that may be given in a sublingual form for the treatment of opioid addiction. Other forms may be used to treat moderate-to-severe pain.
- Buprenorphine acts on mu opioid receptors to provide pain relief. At low dosages it acts as a partial mu agonist and provides analgesic effects; however, at higher dosages buprenorphine's analgesic effects plateau and it then behaves like an antagonist. It also has weak kappa antagonist activity.
- Buprenorphine belongs to the class of medicines known as narcotic analgesics. It may also be called an opioid analgesic. An analgesic is a drug that is used to relieve pain.
- Transdermal buprenorphine (a buprenorphine patch) may be used for the treatment of moderate-to-severe chronic pain that requires around-the-clock opioid analgesia.
- The injectable form may be used postoperatively or for the relief of moderate-to-severe pain associated with conditions such as cancer, kidney stones, and nerve disorders.
- Sublingual buprenorphine (buprenorphine given under the tongue) may be used either alone or in fixed combination with naloxone for the treatment of opioid dependence under strict conditions.
- Generic buprenorphine is available.
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:
- Respiratory depression (severe difficulty with breathing) is the main toxicity associated with buprenorphine. More likely to occur in the elderly, debilitated, or in those with pre-existing breathing problems. The risk is higher with IV administration.
- May cause sleepiness or dizziness and affect a person's ability to drive or operate machinery. Avoid alcohol.
- May also cause vertigo, nausea, headache, adrenal suppression, and serious liver effects. Liver function may need monitoring.
- May cause a severe lowering of blood pressure, or a sudden drop in blood pressure when going from sitting to standing.
- Buprenorphine has a high potential for abuse, similar to other opioid analgesics. The risk may be higher in those with a personal or family history of substance or alcohol abuse or with a psychiatric disorder.
- Sublingual forms of buprenorphine have been associated with fatal overdosage when used in opioid-naive patients for analgesia. Reserve sublingual forms for the treatment of opioid addiction only.
- There is a risk of heart rhythm disorders (such as QT prolongation) associated with buprenorphine, particularly at higher dosages (for example, more than 20 mcg/hour of transdermal buprenorphine).
- Buprenorphine may be addictive and cause psychological dependence and withdrawal symptoms, particularly when used for long periods of time.
- Transdermal buprenorphine may be irritating or cause a rash at the site of application. The site where the patch is applied to the skin and the surrounding skin should not be exposed to external heat sources because this may alter how buprenorphine is released from the patch and could potentially result in overdosage or death.
- May interact with a number of other drugs including other opioids, benzodiazepines, and other central nervous system depressants resulting in profound sedation, respiratory depression, and sometimes death. May also interact with drugs metabolized through a number of CYP hepatic enzyme systems (such as CYP3A4 or CYP2D6) or drugs that also release serotonin (such as antidepressants, antipsychotics, and tramadol).
- May not be suitable for some people, or the dosage of buprenorphine may need reducing in those with liver disease, the elderly or frail, with a history of drug or alcohol abuse, with psychiatric disorders, previous head injury or raised intracranial pressure, a history of seizure disorders, with certain gastrointestinal conditions, respiratory disease, or certain other concomitant conditions. Use during pregnancy may cause withdrawal symptoms in the newborn baby.
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
- Transdermal patches should be applied to a clean, dry, rash-free, hairless, or nearly hairless area of skin on the upper chest, back, or arm, or side of the chest. Hair may need to be clipped prior to application (not shaved). Only use water to clean the area of skin prior to application because other substances (such as soaps, oils, or gels) may alter the absorption of the drug. Transdermal buprenorphine should be worn continuously for seven days and then subsequent systems applied to different sites after removal of the previous system. Discard used patches carefully and out of reach of children or pets.
- Avoid exposing the site where the patch is located to excessive heat (such as electric blankets, saunas, or prolonged direct sunlight) as this may cause a faster-than-normal release of buprenorphine, increasing the risk of overdosage and death.
- Sublingual tablets must be placed under the tongue and allowed to dissolve; swallowing the tablets reduces how much buprenorphine is actually absorbed. Drinking warm fluids prior to administration may help with the dissolution of buprenorphine. Always try to take your tablets the same way to ensure blood levels of buprenorphine remain consistent.
- Sublingual strips should be placed side-by-side on the tongue (minimize overlapping) and allowed to dissolve. Avoid talking, chewing, or swallowing while a strip is dissolving.
- Use buprenorphine strictly as directed by your doctor. Do not use on an "as needed" basis or increase or decrease the dosage without your doctor's advice.
- Some forms of buprenorphine have a REMS (Risk Evaluation and Mitigation Strategy) associated with them which means you will need to fill in a patient enrolment form with your Healthcare prescriber. Always read the medication guide prescribed with buprenorphine.
- If you are taking buprenorphine for severe pain, tell your doctor if you begin to have breakthrough pain.
- When used to treat drug addiction, it is important that you take advantage of any social support and counseling services offered to you as withdrawal from opioids is a long and often difficult process and a successful outcome is dependent upon a multi-targeted approach.
- Tell your doctor if you experience any difficulty with breathing or shortness of breath after taking buprenorphine, especially within the first 24 to 72 hours of initiating therapy.
- Avoid sudden discontinuation of buprenorphine. The dosage of buprenorphine must be tapered off slowly to minimize withdrawal symptoms which include restlessness, runny nose and eyes, muscle pain, and insomnia. When the time comes to discontinue buprenorphine, your doctor will advise you on a tapering schedule.
- Rise carefully from a sitting to a standing position to minimize blood pressure lowering effects from buprenorphine which may result in dizziness increasing your risk of falls.
- Always talk to your doctor or pharmacist before buying anything over-the-counter to check if it is compatible with buprenorphine.
6. Response and Effectiveness
- The analgesic effect after IV administration usually occurs within 10-30 minutes; peak analgesic effects occur within 60 minutes. The analgesic effect of buprenorphine usually lasts for an average of six hours but the duration may vary between individuals.
- When injected subcutaneously (under the skin), the extended-release formulation precipitates out and forms a solid depot which gradually releases buprenorphine via diffusion and biodegradation of the depot.
- It takes about three days for transdermal buprenorphine to reach a steady level.
- Sublingual preparations of buprenorphine vary in the time they take to dissolve (from just a few minutes to up to 12 minutes). People should not eat, drink, or talk during this time. Some relief from withdrawal symptoms should be expected within 30 minutes of the first dose. It may take several doses before the full effects are seen. A decrease in the response to buprenorphine may indicate that a higher dosage is needed.
Medicines that interact with buprenorphine may either decrease its effect, affect how long it works for, increase side effects, or have less of an effect when taken with buprenorphine. 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 include:
- antidepressants, such as tricyclic antidepressants (eg, amitriptyline), monoamine oxidase inhibitors (eg, isocarboxazid, phenelzine, and tranylcypromine), or SSRIs (eg, fluoxetine, sertraline)
- antipsychotics (such as butyrophenones, phenothiazines, or thioxanthenes) and atypical antipsychotics (eg, olanzapine, quetiapine, ziprasidone)
- any medication that inhibits or induces CYP3A4
- any medication that may cause drowsiness, such as amphetamines, benzodiazepines (eg, diazepam, lorazepam), first-generation antihistamines (such as doxylamine or promethazine), metoclopramide, or opioids (such as codeine, methadone, or morphine)
- HIV medications such as ritonavir
- naloxone and naltrexone
- QT-prolonging medications such as amiodarone and flecainide
- St. John's Wort.
Avoid drinking alcohol or taking illegal or recreational drugs while taking buprenorphine.
Note that this list is not all-inclusive and includes only common medications that may interact with buprenorphine. You should refer to the prescribing information for buprenorphine for a complete list of interactions.
- Buprenorphine. Revised 05/2020. Drugs.com. https://www.drugs.com/ppa/buprenorphine.html
Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use buprenorphine only for the indication prescribed.
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