File - Spirit of Healing: Alberta First Nations Conquering

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Suboxone®
BUPRENORPHINE & NALOXONE
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.
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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:
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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
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Benefits of MedicationAssisted 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. antidepressants)
◦ Treatment of withdrawal (detox) (e.g. clonidine, benzodiazepines,
methadone, Suboxone®)
◦ Reduction of cravings and urges - Substitution/replacement therapy (e.g.
methadone, Suboxone®)
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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.
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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 medicationassisted treatments.
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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.
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Medications for Opioid Abuse
Medications used to alleviate withdrawal symptoms, and prevent lifethreatening withdrawal complications (such as seizures) include:
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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)
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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.
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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).
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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.
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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.
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Opioid Effect for Opioid Full Agonists, Partial Agonists,
and Antagonists
Source: SAHMSA TIP 40, 2004
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®
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.
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Buprenorphine
Buprenorphine (pronounced bu-pre-'nôr-feen) is a semi-synthetic opioid.
It is used to treat moderate to severe pain, and is 25-50 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.
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Buprenorphine blocks opioid
receptors
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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.
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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.
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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).
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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.
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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.
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®
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
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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
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Methadone vs Suboxone®
METHADONE
SUBOXONE®
Full agonist
Partial agonist
Limited access in non-urban areas
Can be prescribed by trained physicians
Long half-life from 8-59 hours
Long half-life from 24-60 hours. Takes less
time to arrive at appropriate dose.
No ceiling effect and therefore can be
abused so take-home doses less likely
Hard to abuse so take-home doses more likely
Higher rates of taking illicit opioids
during treatment
Provides more effective relief from
withdrawal symptoms
Standard care for pregnant or breastfeeding women
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)
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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.
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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.
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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.
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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.).
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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:
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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.
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References & Web Resources
• Addiction Treatment Forum. Buprenorphine vs. Methadone.
http://atforum.com/2013/02/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. http://cpsa.ca/wpcontent/uploads/2015/07/buprenorphine_naloxone_CAMH2012.pdf
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• College of Physicians & Surgeons of Alberta. Buprenorphine
Prescribing. http://www.cpsa.ca/physician-prescribingpractices/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): 139-146.
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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.
http://www.ncbi.nlm.nih.gov/books/NBK64236/
• The National Alliance of Advocates for Buprenorphine
Treatment (U.S.) PDF literature:
http://www.naabt.org/education/literature.cfm
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Contact Info
Sue Howard
Landline: (604) 535-2124
Cell: (250) 809-1066
Email:
sue@suehowardconsulting.
ca
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