1. Buprenorphine & Naloxone
Suboxone®
Buprenorphine & Naloxone

2. Comprehensive addiction treatment
Suboxone® is a newly developed drug increasingly being used in medication-assisted treatment for opioid addiction.
Addiction is a chronic, relapsing brain disease characterized by compulsive use despite harmful consequences.
For people with a severe substance use disorder medications can be very effective as part of a comprehensive treatment plan.
Medication-assisted treatment approaches include:
Medications (Biological)
Therapy, lifestyle changes (Psycho-Social)
Medications assist treatment – they are not a cure.

3. Medication-Assisted Treatment Goals
The basis of medication-assisted treatment is to replace the drug, typically an opioid with a medication that has a longer duration of action, less abuse potential, and better safety profile to prevent withdrawal and cravings.
Goals include:
Reduce symptoms and signs of withdrawal
Reduce or eliminate craving
Block effects of illicit opioids
Restore normal physiology
Promote psychosocial rehabilitation and non-drug lifestyle

4. Benefits of Medication-Assisted treatment
Medication-assisted treatment can help those in recovery:
Hold jobs
Avoid street crime and violence
Reduce their exposure to HIV by stopping or decreasing injection drug use and drug-related high-risk sexual behaviour
Engage more readily in counselling and other behavioural interventions essential to recovery.
Medications can be used to assist with:
Treatment of psychiatric symptoms or co-occurring disorders (e.g. anti- depressants)
Treatment of withdrawal (detox) (e.g. clonidine, benzodiazepines, methadone, Suboxone®)
Reduction of cravings and urges - Substitution/replacement therapy (e.g. methadone, Suboxone®)

5. Addiction vs Dependence
The two most commonly prescribed medications for opioid addiction are methadone and buprenorphine. Because methadone and buprenorphine are themselves opioids, some people view these treatments for opioid dependence as just substitutions of one addictive drug for another.
People on medication-assisted treatment are not considered to be addicted – addiction is pathologic use of a substance that may or may not include physical dependence.
Physical dependence on a medication for the treatment of a medical problem does not mean the person is engaging in pathologic use and other behaviours.
Mooney, L. (n.d.) Prescription drug abuse. UCLA Integrated Substance Abuse Programs.

6. Treatment Outcomes
Once stabilized on medication, the person can focus on returning to a healthy lifestyle.
They will still need treatment, counselling and aftercare supports.
Outcomes of opioid treatment are much better in individuals who make overall lifestyle changes and seek counselling combined with medication-assisted treatments, versus those who only use medication- assisted treatments.

7. Medication Treatment for Opioid Dependence
Opioid withdrawal symptoms and cravings can be so severe that the relapse rate is high, and for some people medication-assisted treatment is their best option for living a productive life.
Medication treatment is one of the most effective options for people with severe, chronic addiction to opioids, whether they are street drugs (e.g. heroin), or prescription medications with a high abuse potential (e.g. fentanyl).
Maintenance therapies alleviate withdrawal symptoms and reduce cravings, as well as alleviate chronic pain.

8. Medications for Opioid Abuse
Medications used to alleviate withdrawal symptoms, and prevent life- threatening withdrawal complications (such as seizures) include:
Methadone, buprenorphine (for severe opioid withdrawal)
Clonidine (Catapres) (for alcohol and milder opioid withdrawal)
Benzodiazepines (e.g. Diazepam) (for alcohol and milder opioid withdrawal)
Other supportive medication (e.g. anti-diarrheals, antiemetics [for vomiting and nausea], ibuprofen, muscle relaxants)
Medications used for maintenance/relapse prevention:
Methadone
Suboxone® (buprenorphine and naloxone)
Miller, N.S., & Gold, M.S. (1998). Management of withdrawal syndromes and relapse prevention in drug and alcohol dependence. Am Fam Physician. Jul 1:58(1):

9. Opioid Action
In order to understand how Suboxone® works, it is important to understand the action of opioids.
Opioid receptors are molecules on the surfaces of cells to which opioid compounds attach and through which they exert their effects.
Different types of opioid receptors are present in the brain. The receptor most relevant to opioid abuse and treatment is the mu receptor. It is through activation of the mu receptor that opioids exert their analgesic, euphoric, and addictive effects.
Opioids can interact with receptors in different ways. Three types of drug/receptor interactions are: agonists (or full agonists), antagonists, and partial agonists.
Substance Abuse and Mental Health Services Administration (SAHMSA). (20014). Clinical guidelines for the use of Buprenorphine in the treatment of opioid addiction. Treatment Improvement Protocol (TIP) Series, No. 40. Rockville, MD: Centre for Substance Abuse Treatment.

10. Full Agonists
Drugs that activate receptors in the brain are termed agonists.
Opioid agonists work by attaching themselves to opioid receptors which are found throughout the body, such as in the brain, spinal cord, gastrointestinal tract, and various other organs in the body. When the opioids attach themselves to the opioid receptor sites, they reduce the perception of pain, while simultaneously producing a euphoric effect.
Opioids with the greatest abuse potential are full agonists (e.g., fentanyl, morphine, heroin, methadone, oxycodone).
Substance Abuse and Mental Health Services Administration (SAHMSA). (20014). Clinical guidelines for the use of Buprenorphine in the treatment of opioid addiction. Treatment Improvement Protocol (TIP) Series, No. 40. Rockville, MD: Centre for Substance Abuse Treatment.

11. Antagonists
Opioid antagonists also bind to opioid receptors and are used to block the effects of opioids by blocking the receptor sites to prevent any action of an opioid agonist.
Antagonists do not activate receptors, and they prevent receptors from being activated by agonist compounds. An antagonist is like a key that fits in a lock but does not open it and prevents another key from being inserted to open the lock.
Naloxone is an opioid antagonist.
Substance Abuse and Mental Health Services Administration (SAHMSA). (20014). Clinical guidelines for the use of Buprenorphine in the treatment of opioid addiction. Treatment Improvement Protocol (TIP) Series, No. 40. Rockville, MD: Centre for Substance Abuse Treatment.

12. Partial Agonists
Partial agonists bind to receptors and activate them, but not to the same degree as do full agonists.
At lower doses and in individuals who are not dependent on opioids, full and partial agonists produce effects that are indistinguishable. As doses are increased, the increasing effects of partial agonists reach maximum levels and do not increase further, even if doses continue to rise—called the ceiling effect.
As higher doses are reached, partial agonists can act like antagonists— occupying receptors but not activating them (or only partially activating them), while at the same time displacing or blocking full agonists from receptors.
Buprenorphine is an example of a mu opioid partial agonist.
Substance Abuse and Mental Health Services Administration (SAHMSA). (20014). Clinical guidelines for the use of Buprenorphine in the treatment of opioid addiction. Treatment Improvement Protocol (TIP) Series, No. 40. Rockville, MD: Centre for Substance Abuse Treatment.

13. Opioid Effect for Opioid Full Agonists, Partial Agonists, and Antagonists
Substance Abuse and Mental Health Services Administration (SAHMSA). (2004). Clinical guidelines for the use of Buprenorphine in the treatment of opioid addiction. Treatment Improvement Protocol (TIP) Series, No. 40. Rockville, MD: Centre for Substance Abuse Treatment.
Source: SAHMSA TIP 40, 2004

14. Suboxone®
Suboxone® contains the partial agonist Buprenorphine and the opiate antagonist Naloxone.
Health Canada approved Suboxone® for the treatment of opioid-related disorders in 2007.
Suboxone® is dispensed by prescription.

15. Buprenorphine
Buprenorphine (pronounced bu-pre-'nôr-feen) is a semi-synthetic opioid.
It is used to treat moderate to severe pain, and is times more potent an analgesic than morphine.
Repeated administration of buprenorphine produces or maintains opioid physical dependence; however, because buprenorphine is a partial agonist, the level of physical dependence appears to be less than that produced by full agonists.
Buprenorphine is an opioid partial agonist which means that, although it can produce typical opioid effects and side effects such as euphoria and respiratory depression, its maximal effects are less than those of full agonists like heroin and methadone.
Buprenorphine is also able to reduce or eliminate withdrawal symptoms associated with opioid dependence.
It carries a low risk of overdose.

16. Buprenorphine blocks opioid receptors

17. Blocks other opiates
A major benefit of Suboxone® is that if someone on the drug tries to get high on another opioid (such as fentanyl or heroin) they will not be successful as the Suboxone® will block the effects of the other drug.
The buprenorphine and the other opioid will compete to attach to the opioid receptor. The buprenorphine will attach to the receptor and block attachment by the other opioid. This is due to buprenorphine’s stronger affinity (attraction) to the opioid receptors.
Therefore the other opioid would not reach the opioid receptor. This results in a major reduction in euphoria, or ‘high’, from the other opioid drug.
In fact, Buprenorphine can actually block the effects of full opioid agonists and can precipitate withdrawal symptoms if administered to an opioid-addicted individual while a full agonist is in the bloodstream.
Suboxone: A handbook for patients
Author: Chris A. Cavacuiti, MD

18. Lower dependency
Buprenorphine activates the opioid receptors in a less powerful way than other opioids.
This occurs because the buprenorphine has enough activity at the opioid receptor to relieve the symptoms of withdrawal (aches, sweating, pains, etc.) but not so much that the patient feels euphoric or “high”.
Also, the higher activity level of an opioid, the more dependent the user will be on the drug.
Since buprenorphine has such a low activity level, patients gradually become less and less physically dependent on opioids over time.
Suboxone: A handbook for patients
Author: Chris A. Cavacuiti, MD

19. Long-Lasting
Buprenorphine takes longer to separate from the opioid receptor than other shorter-acting opioids, and therefore stays in the body much longer than other opioids.
This means that buprenorphine can be taken just once a day, and in some cases, can eventually be taken every other day because the effects last such a long time, whereas most opioids stop working after about 4 to 6 hours.
This also means that the levels of buprenorphine in the brain stays much steadier and more consistent than other opioids, which keeps the patient from experiencing intoxication (too high of an opioid level) or withdrawal (too low of an opioid level).

20. Ceiling Effect
At a certain point, a higher dose of Suboxone® would not lead to significantly more activity at the opioid receptor.
The agonist effects of buprenorphine increase linearly with increasing doses of the drug until it reaches a plateau and no longer continues to increase with further increases in dosage.

21. Naloxone
Naloxone is added to Suboxone® to guard against intravenous abuse of buprenorphine by individuals physically dependent on other opiates.
Naloxone has no effect when Suboxone® is taken as prescribed, but if an addicted individual attempts to abuse Suboxone®, the naloxone will produce severe withdrawal symptoms.
Thus, this formulation lessens the likelihood that the drug will be abused or diverted to others.
If Suboxone® is misused by injection, the naloxone (along with the buprenorphine itself) will help cause immediate withdrawal in physically dependent people.

22. How Suboxone® is taken
Suboxone® is a pill taken by dissolving under the tongue. The drug is then absorbed into the mucous membranes.
It is available in 2 mg, 4 mg, 8 mg and 12 mg dosages.
The ratio of buprenorphine and naloxone is 4:1

23. Who should not take Suboxone®?
Suboxone® may not be recommended for people with any of the following conditions:
Allergic to buprenorphine or naloxone
Pregnant or breast-feeding (Alternative treatments would be Methadone or Subutex® which is a naloxone-free form of buprenorphine available through the Health Canada Special Access Program)
Severe liver dysfunction/disease
Paralytic ileus (type of intestinal blockage)
Cardiovascular instability
In acute respiratory distress or decreased level of consciousness
Inability to provide informed consent
CAMH (2012). Buprenhorphine/Naloxone for Opioid Dependence: Clinical Practice Guidelines.

24. Methadone vs Suboxone®
Full agonist
Limited access in non-urban areas
Long half-life from 8-59 hours
No ceiling effect and therefore can be abused so take-home doses less likely
Higher rates of taking illicit opioids during treatment
Provides more effective relief from withdrawal symptoms
Standard care for pregnant or breast- feeding women
Partial agonist
Can be prescribed by trained physicians
Long half-life from hours. Takes less time to arrive at appropriate dose.
Hard to abuse so take-home doses more likely
Creates less physical dependency
Less severe withdrawal than from methadone
Lower risk of fatal overdose
Preferred treatment for patients with higher risks of toxicity (e.g., the elderly, benzodiazepine users, adolescents and young adults)

25. Who can prescribe Suboxone®?
Physicians who wish to initiate or maintain buprenorphine treatment for opioid dependent patients in Alberta must:
Complete the CAMH Buprenorphine-Assisted Treatment of Opioid Dependence course;
Provide the College of Physicians & Surgeons of Alberta (CPSA) with confirmation of course completion.
No buprenorphine prescribing course is required to maintain the same dose for the duration of hospitalization or other healthcare settings with controlled medication dispensing processes (e.g. nursing homes) or incarceration.
Consultation with a physician experienced in the treatment of opioid dependence is required for any change in dose.
College of Physicians & Surgeons of Alberta. Buprenorphine Prescribing.

26. How are patients assessed?
Prior to prescribing Suboxone®, the doctor will:
Ensure a diagnosis of opioid dependence, a urine drug test has been interpreted and is positive for opioids.
Ensure the patient has provided informed consent and is aware of the possible long-term nature of this treatment and of other treatment options.
Ensure that there are no concurrent substance use disorders, psychiatric illnesses or medical disorders that should be stabilized first.
Inform the patient how long to remain abstinent from opioids to maximize the likelihood of beginning their induction in satisfactory withdrawal to minimize the likelihood of precipitated withdrawal during the induction.
Ensure the patient has no plans to drive a vehicle or operate heavy machinery during the early induction period.
CAMH (2012). Buprenhorphine/Naloxone for Opioid Dependence: Clinical Practice Guidelines.

27. Suboxone® Treatment
Person is assessed to establish the severity of opioid withdrawal and appropriateness for treatment.
Suboxone® prescribed dose of typically 2–8 mg of to be administered sublingually.
The ingestion of the dose is observed by a pharmacist or other health care professional to ensure the tablet has dissolved completely.
Doses will not be provided if the person appears intoxicated or sedated.
Patients will be regularly assessed. Even very stable patients will be assessed at least every 12 weeks.
Take-home doses may be gradually prescribed once the person is considered clinically stable.
CAMH (2012). Buprenhorphine/Naloxone for Opioid Dependence: Clinical Practice Guidelines.

28. Frequency of physician visits
During the induction process, the physician will likely see the patient one to two times per week.
Once the patient is at their maintenance dose the visits will likely be every one to two weeks.
Once the patient has achieved clinical stability and has started to be eligible for take-home doses, the visits may be every one to three months.
Visit frequency will be increased if a previously stable patient begins to demonstrate signs of clinical instability (e.g. decreased adherence to the treatment program, change in mental status exam, positive urine drug tests, etc.).
CAMH (2012). Buprenhorphine/Naloxone for Opioid Dependence: Clinical Practice Guidelines.

29. Clinical Stability: Take-home doses
Take-home doses would not be considered until the patient has established clinical stability.
Clinical stability is determined by certain patient characteristics, namely:
No evidence of ongoing problematic substance use, including alcohol
No evidence of acute or unstable psychiatric symptoms
Stable behaviour and social situation
Secure enough housing to safely store the medication.
CAMH (2012). Buprenhorphine/Naloxone for Opioid Dependence: Clinical Practice Guidelines.

30. References & Web Resources
Addiction Treatment Forum. Buprenorphine vs. Methadone.
Brands, B., Sproule, B., & Marshman, J. (eds) (1998). Drugs & drug abuse (3rd ed.). Canada: Centre for Addiction and Mental Health.
CAMH (2012). Buprenhorphine/Naloxone for Opioid Dependence: Clinical Practice Guidelines. content/uploads/2015/07/buprenorphine_naloxone_CAMH2012.pdf ?7ebd8d
College of Physicians & Surgeons of Alberta. Buprenorphine Prescribing. practices/buprenorphine-prescribing/
Miller, N.S., & Gold, M.S. (1998). Management of withdrawal syndromes and relapse prevention in drug and alcohol dependence. Am Fam Physician. July 1:58(1):

31. References & Web Resources
Mooney, L. (n.d.) Prescription drug abuse. UCLA Integrated Substance Abuse Programs.
National Institute on Drug Abuse (2012). Opioid addiction. Principles of drug addiction treatment: A research-based guide (3rd ed.).
SAHMSA Tip Series No. 40: Clinical Guidelines for the Use of Buprenorphine in the Treatment of Opioid Addiction.
The National Alliance of Advocates for Buprenorphine Treatment (U.S.) PDF literature:

32. Contact Info
Sue Howard
Landline: (604)
Cell: (250) ca