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Buprenorphine is a medication that has gained significant attention in recent years due to its potential for long-term use in treating opioid addiction and managing chronic pain.

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Buprenorphine is a partial opioid agonist medication that acts on the brain’s opioid receptors. It is commonly used to manage moderate to severe pain and as an essential component of medication-assisted treatment (MAT) for opioid addiction.

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Buprenorphine is a weak partial mu-opioid receptor agonist and a weak kappa-opioid receptor antagonist used for the treatment of severe pain.

It is also commonly used as an alternative to methadone for the treatment of severe opioid addiction.

Buprenorphine is commercially available as the brand name product Suboxone which is formulated in a fixed-dose combination product along with naloxone, a non-selective competitive opioid receptor antagonist.

Combination with naloxone is intended to reduce the abuse potential of Suboxone, as naloxone is poorly absorbed by the oral route (and has no effect when taken orally), but would reverse the opioid agonist effects of buprenorphine if injected intravenously.

Buprenorphine has poor gastrointestinal absorption and is therefore formulated as a sublingual tablet.

Buprenorphine has a number of unique pharmacokinetic and pharmacodynamic properties that make it a preferred agent for the treatment of conditions requiring high doses of strong opioids.

For example, buprenorphine dissociates from opioid receptors very slowly, resulting in a long duration of action and relief from pain or withdrawal symptoms for upwards of 24-36 hours.

Use of once-daily buprenorphine may benefit individuals who have developed tolerance to other potent opioids and who require larger and more frequent doses.

Buprenorphine may also be a preferred agent over methadone (which is also commonly used to treat severe pain and opioid use disorder), as it has less effect on Qtc interval prolongation, fewer drug interactions, reduced risk of sexual side effects, and an improved safety profile with a lower risk of overdose and respiratory depression.

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Buprenorphine acts as a partial mu-opioid receptor agonist with a high affinity for the receptor, but lower intrinsic activity compared to other full mu-opioid agonists such as heroin, oxycodone, or methadone.

This means that buprenorphine preferentially binds the opioid receptor and displaces lower affinity opioids without activating the receptor to a comparable degree.

Clinically, this results in a slow onset of action and a clinical phenomenon known as the “ceiling effect” where once a certain dose is reached, buprenorphine’s effects plateau.

This effect can be beneficial, however, as dose-related side effects such as respiratory depression, sedation, and intoxication also plateau at around 32mg, resulting in a lower risk of overdose compared to methadone and other full agonist opioids.

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It also means that opioid-dependent patients do not experience sedation or euphoria at the same rate that they might experience with more potent opioids, improving quality of life for patients with severe pain and reducing the reinforcing effects of opioids which can lead to drug-seeking behaviours.

Treatment of opioid addiction with buprenorphine, methadone, or slow-release oral morphine (SROM) is termed Opioid Agonist Treatment (OAT) or Opioid Substitution Therapy (OST).

The intention of substitution of illicit opioids with the long-acting opioids used in OAT is to prevent withdrawal symptom’s for 24-36 hours following dosing to ultimately reduce cravings and drug-seeking behaviors.

Use of OAT is also intended to improved social stabilization including a reduction in crime rates, marginalization, incarceration, and use of illicit substances such as heroin or fentanyl.

Illegally purchased opioids can often be injected and may be laced with other substances that increase the risk of harm or overdose.

Provision of OAT is often combined with education about harm reduction including use of clean needles and injection supplies in an effort to reduce the risks associated with injection drug use which includes contraction of HIV and Hepatitis C and other complications including skin infections, abscesses, or endocarditis.

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Buprenorphine patches can be habit forming, especially with prolonged use. Use buprenorphine patches exactly as directed.

Do not apply more patches, apply the patches more often, or use the patches in a different way than prescribed by your doctor. While using buprenorphine patches, discuss with your health care provider your pain treatment goals, length of treatment, and other ways to manage your pain.

Tell your doctor if you or anyone in your family drinks or has ever drunk large amounts of alcohol, uses or has ever used street drugs, or has overused prescription medications, or has had an overdose, or if you have or have ever had depression or another mental illness. There is a greater risk that you will overuse buprenorphine if you have or have ever had any of these conditions.

Talk to your health care provider immediately and ask for guidance if you think that you have an opioid addiction or call the U.S. Substance Abuse and Mental Health Services Administration (SAMHSA) National Helpline at 1-800-662-HELP.

Buprenorphine patches may cause serious or life-threatening breathing problems, especially during the first 24 to 72 hours of your treatment and any time that your dose is increased.

Your doctor will monitor you carefully during your treatment. Tell your doctor if you have or have ever had breathing difficulties, asthma, chronic obstructive pulmonary disease (COPD; a group of diseases that affect the lungs and airways), or other lung disease. Your doctor may tell you not to use buprenorphine patches.

Taking certain medications with buprenorphine patches may increase the risk of serious or life-threatening breathing problems, sedation, or coma.

Tell your doctor and pharmacist if you are taking atazanavir (Reyataz); benzodiazepines such as such as alprazolam (Xanax), chlordiazepoxide (Librium), clonazepam (Klonopin), diazepam (Diastat, Valium), estazolam, flurazepam, lorazepam (Ativan), oxazepam, temazepam (Restoril), triazolam (Halcion); medications for mental illness and nausea; other medications for pain; muscle relaxants; sedatives; sleeping pills; and tranquilizers.

Your doctor may need to change the dosages of your medications and will monitor you carefully. If you use buprenorphine transdermal with any of these medications and you develop any of the following symptoms, call your doctor immediately or seek emergency medical care: unusual dizziness, lightheadedness, extreme sleepiness, slowed or difficult breathing, or unresponsiveness.

Be sure that your caregiver or family members know which symptoms may be serious so they can call the doctor or emergency medical care if you are unable to seek treatment on your own.

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Drinking alcohol or using street drugs during your treatment with buprenorphine transdermal also increases the risk that you will experience these serious, life-threatening side effects. Do not drink alcohol, take prescription or nonprescription medications that contain alcohol, or use street drugs during your treatment.