A Guide to Suboxone Therapy
Introduction
Ontario, like much of the world, faces a significant challenge with opioid addiction, a crisis affecting people of all ages and backgrounds. Suboxone therapy has emerged as a vital treatment option, offering a new hope for recovery. At Keele Drug Mart and Clinic, we provide compassionate and effective care for those seeking freedom from addiction.
Suboxone Therapy and Its Pharmacology:
Suboxone, along with its generic counterparts available in Canada, combines two critical medications: buprenorphine, a partial opioid agonist, and naloxone, an opioid antagonist.
Naloxone is widely recognized for its life-saving capabilities in opioid overdose situations. It is readily accessible to anyone in Ontario—whether they use substances or not—through health units and pharmacies without a prescription. Naloxone is effective in emergencies because it binds to opioid receptors in the brain without activating them, allowing it to counteract overdoses when administered by bystanders equipped with naloxone kits.
The inclusion of naloxone in Suboxone, primarily used for treating opioid use disorder (OUD), might seem counterintuitive since antagonists can trigger withdrawal. However, naloxone’s impact is minimal when taken orally or sublingually (under the tongue) due to its poor bioavailability in these forms, meaning it doesn’t enter the bloodstream effectively to cause withdrawal unless injected or taken intranasally.
Buprenorphine’s role in Suboxone is pivotal. Unlike full agonists like oxycodone, morphine, and fentanyl, which fully stimulate opioid receptors, buprenorphine is a partial agonist. This means it only partially activates these receptors. A key benefit of this partial activation is safety; increasing the dose beyond a certain point does not enhance its effect significantly. This is especially important regarding respiratory depression—a serious risk with many opioids. Suboxone saturates 92% of opioid receptors at a dose of 16mg daily, and further doses do not significantly increase the risk of respiratory depression, making it less likely to cause a fatal overdose compared to full agonists.
Furthermore, Suboxone's high affinity for opioid receptors makes it a double-edged sword. Its strong binding prevents other opioids from activating these receptors, thus reducing the euphoria associated with opioid use and aiding in quicker cessation of drug use. However, this same characteristic complicates its use. Patients must be in moderate withdrawal before starting Suboxone. If not, Suboxone's displacement of other opioids in the brain—due to its high affinity and partial agonist action—can lead to rapid onset of withdrawal symptoms, a condition known as precipitated withdrawal. Therefore, correct timing in the administration of Suboxone is crucial for effective treatment and patient comfort.
This information is vital for understanding how Suboxone works and why careful consideration is needed when starting therapy, particularly concerning the induction phase, which will be discussed further.
How is Suboxone administered?
Suboxone should be taken sublingually, meaning it is placed under the tongue to dissolve. This method is used because swallowing the pill renders it ineffective. The reason lies in its bioavailability; when swallowed, the medication enters the portal circulation system through the small intestine, where it is then processed by the liver and largely inactivated. However, when Suboxone is absorbed directly through the oral mucosa—the lining inside the mouth—it bypasses the liver, allowing approximately 60% of the drug to enter the systemic circulation effectively, with the remaining 40% being swallowed due to salivation.
Besides the sublingual tablets, Suboxone is also available in a film form, which can be placed inside the cheek for absorption. This form dissolves more quickly, although as of spring 2021, it is not covered by the Ontario Drug Benefit (ODB) or the Non-Insured Health Benefits (NIHB) programs. Additionally, a depot form of Suboxone, known as Sublocade, is available and discussed further on this site.
Suboxone Costs and Coverage
Suboxone is covered under Ontario’s provincial drug plan (ODB) and is also eligible for coverage by NIHB (Indian Affairs) and most third-party insurance plans. If you do not have coverage, it is important to discuss your options with your pharmacist. The doctors at can provide guidance on the likely range of doses you may need.
Effects & Side Effects of Suboxone
Taking too high a dose of buprenorphine can lead to euphoria, sedation, nausea, or decreased appetite. Typically, the only effect patients notice is a reduced need for opiates. Most patients achieve a stable dose within 24 hours to a few days, unlike the weeks it may take with methadone. Once stabilized, patients do not experience a "high," nor do they suffer from withdrawal or cravings. Buprenorphine effectively blocks the euphoric effects of other opiates by occupying opioid receptors, which helps decrease the desire to use opioids.
Buprenorphine's long action duration is especially beneficial in preventing withdrawal, with most people finding that a single dose can prevent withdrawal symptoms for over 24 hours. Patients can taper off opioids slowly over weeks or months without experiencing withdrawal symptoms. It is a voluntary program; some choose to remain on it as a long-term treatment to reduce the risk of relapse.
While some side effects occur, buprenorphine is generally well-tolerated. The most common side effects include constipation (common with all opiates), dizziness, drowsiness, or headaches, which usually resolve within a week. Less common are weight gain, sweating, and sexual side effects compared to methadone. Initial withdrawal symptoms during the induction phase, such as abdominal cramps, nausea, and insomnia, typically resolve quickly once stabilized.
Buprenorphine is safe for long-term use and does not cause organ damage. Some patients may experience temporary elevations in liver enzymes, which typically reverse once the medication is discontinued.
Suboxone in Pregnancy
Suboxone is increasingly used during pregnancy. It is considered to cause a less severe Neonatal Abstinence Syndrome compared to methadone, requiring less treatment for babies born to mothers on buprenorphine. Please refer to our pregnancy-related FAQs for more information.
Treating Acute Pain with Buprenorphine
Historically, there was concern that buprenorphine might block the effects of other opioids needed to treat acute pain. However, it is now understood that patients on any opioid therapy, including methadone or buprenorphine, simply require higher doses of opioids to manage acute pain effectively. If you are scheduled for surgery or a procedure, please discuss this with your BMC physician. We are prepared to coordinate with your surgeon, dentist, or anesthesiologist.
Suboxone is an effective pain management medication but requires dosing 3-4 times per day. Currently, this specific use is not covered by ODB, NIHB, or third-party drug plans.
Will I Become Addicted to Buprenorphine?
Patients on buprenorphine are typically already physically dependent on opioids. Discontinuing buprenorphine will likely result in withdrawal symptoms. For more detailed information, refer to the section on key concepts.
Buprenorphine Maintenance
Patients in Ontario on Suboxone generally follow similar protocols to those on methadone, including clinic visits, urine testing, and restrictions on take-home doses. However, there are some differences. Suboxone maintenance is often easier to manage over the long term than methadone, particularly for those who travel. CRISM guidelines recommend trying Suboxone before methadone due to its safety profile and fewer side effects for most people.
A Guide to Suboxone Therapy
Introduction
Ontario, like much of the world, faces a significant challenge with opioid addiction, a crisis affecting people of all ages and backgrounds. Suboxone therapy has emerged as a vital treatment option, offering a new hope for recovery. At Keele Drug Mart and Clinic, we provide compassionate and effective care for those seeking freedom from addiction.
Suboxone Therapy and Its Pharmacology:
Suboxone, along with its generic counterparts available in Canada, combines two critical medications: buprenorphine, a partial opioid agonist, and naloxone, an opioid antagonist.
Naloxone is widely recognized for its life-saving capabilities in opioid overdose situations. It is readily accessible to anyone in Ontario—whether they use substances or not—through health units and pharmacies without a prescription. Naloxone is effective in emergencies because it binds to opioid receptors in the brain without activating them, allowing it to counteract overdoses when administered by bystanders equipped with naloxone kits.
The inclusion of naloxone in Suboxone, primarily used for treating opioid use disorder (OUD), might seem counterintuitive since antagonists can trigger withdrawal. However, naloxone’s impact is minimal when taken orally or sublingually (under the tongue) due to its poor bioavailability in these forms, meaning it doesn’t enter the bloodstream effectively to cause withdrawal unless injected or taken intranasally.
Buprenorphine’s role in Suboxone is pivotal. Unlike full agonists like oxycodone, morphine, and fentanyl, which fully stimulate opioid receptors, buprenorphine is a partial agonist. This means it only partially activates these receptors. A key benefit of this partial activation is safety; increasing the dose beyond a certain point does not enhance its effect significantly. This is especially important regarding respiratory depression—a serious risk with many opioids. Suboxone saturates 92% of opioid receptors at a dose of 16mg daily, and further doses do not significantly increase the risk of respiratory depression, making it less likely to cause a fatal overdose compared to full agonists.
Furthermore, Suboxone's high affinity for opioid receptors makes it a double-edged sword. Its strong binding prevents other opioids from activating these receptors, thus reducing the euphoria associated with opioid use and aiding in quicker cessation of drug use. However, this same characteristic complicates its use. Patients must be in moderate withdrawal before starting Suboxone. If not, Suboxone's displacement of other opioids in the brain—due to its high affinity and partial agonist action—can lead to rapid onset of withdrawal symptoms, a condition known as precipitated withdrawal. Therefore, correct timing in the administration of Suboxone is crucial for effective treatment and patient comfort.
This information is vital for understanding how Suboxone works and why careful consideration is needed when starting therapy, particularly concerning the induction phase, which will be discussed further.
How is Suboxone administered?
Suboxone should be taken sublingually, meaning it is placed under the tongue to dissolve. This method is used because swallowing the pill renders it ineffective. The reason lies in its bioavailability; when swallowed, the medication enters the portal circulation system through the small intestine, where it is then processed by the liver and largely inactivated. However, when Suboxone is absorbed directly through the oral mucosa—the lining inside the mouth—it bypasses the liver, allowing approximately 60% of the drug to enter the systemic circulation effectively, with the remaining 40% being swallowed due to salivation.
Besides the sublingual tablets, Suboxone is also available in a film form, which can be placed inside the cheek for absorption. This form dissolves more quickly, although as of spring 2021, it is not covered by the Ontario Drug Benefit (ODB) or the Non-Insured Health Benefits (NIHB) programs. Additionally, a depot form of Suboxone, known as Sublocade, is available and discussed further on this site.
Suboxone Costs and Coverage
Suboxone is covered under Ontario’s provincial drug plan (ODB) and is also eligible for coverage by NIHB (Indian Affairs) and most third-party insurance plans. If you do not have coverage, it is important to discuss your options with your pharmacist. The doctors at can provide guidance on the likely range of doses you may need.
Effects & Side Effects of Suboxone
Taking too high a dose of buprenorphine can lead to euphoria, sedation, nausea, or decreased appetite. Typically, the only effect patients notice is a reduced need for opiates. Most patients achieve a stable dose within 24 hours to a few days, unlike the weeks it may take with methadone. Once stabilized, patients do not experience a "high," nor do they suffer from withdrawal or cravings. Buprenorphine effectively blocks the euphoric effects of other opiates by occupying opioid receptors, which helps decrease the desire to use opioids.
Buprenorphine's long action duration is especially beneficial in preventing withdrawal, with most people finding that a single dose can prevent withdrawal symptoms for over 24 hours. Patients can taper off opioids slowly over weeks or months without experiencing withdrawal symptoms. It is a voluntary program; some choose to remain on it as a long-term treatment to reduce the risk of relapse.
While some side effects occur, buprenorphine is generally well-tolerated. The most common side effects include constipation (common with all opiates), dizziness, drowsiness, or headaches, which usually resolve within a week. Less common are weight gain, sweating, and sexual side effects compared to methadone. Initial withdrawal symptoms during the induction phase, such as abdominal cramps, nausea, and insomnia, typically resolve quickly once stabilized.
Buprenorphine is safe for long-term use and does not cause organ damage. Some patients may experience temporary elevations in liver enzymes, which typically reverse once the medication is discontinued.
Suboxone in Pregnancy
Suboxone is increasingly used during pregnancy. It is considered to cause a less severe Neonatal Abstinence Syndrome compared to methadone, requiring less treatment for babies born to mothers on buprenorphine. Please refer to our pregnancy-related FAQs for more information.
Treating Acute Pain with Buprenorphine
Historically, there was concern that buprenorphine might block the effects of other opioids needed to treat acute pain. However, it is now understood that patients on any opioid therapy, including methadone or buprenorphine, simply require higher doses of opioids to manage acute pain effectively. If you are scheduled for surgery or a procedure, please discuss this with your BMC physician. We are prepared to coordinate with your surgeon, dentist, or anesthesiologist.
Suboxone is an effective pain management medication but requires dosing 3-4 times per day. Currently, this specific use is not covered by ODB, NIHB, or third-party drug plans.
Will I Become Addicted to Buprenorphine?
Patients on buprenorphine are typically already physically dependent on opioids. Discontinuing buprenorphine will likely result in withdrawal symptoms. For more detailed information, refer to the section on key concepts.
Buprenorphine Maintenance
Patients in Ontario on Suboxone generally follow similar protocols to those on methadone, including clinic visits, urine testing, and restrictions on take-home doses. However, there are some differences. Suboxone maintenance is often easier to manage over the long term than methadone, particularly for those who travel. CRISM guidelines recommend trying Suboxone before methadone due to its safety profile and fewer side effects for most people.