Opioid Substances Overview - TDIN
Transcript of Opioid Substances Overview - TDIN
2016-12-20
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Opioid Substances Overview
October 2016
Opioids
Four classes of opioids
1. Naturally produced in the body (such as
endorphins)
2. Opiates derived from opium poppy (morphine,
codeine)
3. Semi-synthetic compounds (Heroin, OxyContin,
Dilaudid, and Percocet)
4. Fully synthetic opioids (Methadone, Demerol)
• Historically opiates were derived from the poppy plant;
opioids were synthetically derived
• Opioids often refers to both these days
• Both affect the same receptors in the brain
Opiates vs. Opioids?Opiates in nature
• Opiates occur naturally in
poppy plant
• Poppies are native to
Europe and East Asia
• They also grow in Mexico,
Columbia, and the Middle
East
Opiate based substances
• Substances made
using natural opiates
include
• Heroin
• Morphine
• Codeine
• Made from the milky
substance inside the
poppy plant pod
Heroin CodeineMorphine
• 30 mg Codeine, 15 mg of
caffeine and 300 mg of
acetaminophen, sold without a
prescription (T3s)
• A similar tablet called an AC&C
which contains 325 mg of
acetylsalicylic acid (Aspirin)
instead of acetaminophen
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Heroin
• Mainly administered IV; also snorted and smoked
• Dose depends greatly on the purity of the heroin and level
of tolerance• Common IV doses generally fall between 5 and 10 mg; smoked
heroin doses may range from 15 to 25 mg.
• Use small quantities of new supply to determine potency and
reduce the risk of overdose
• ± $50 a point (1/10 of a gram)
• Intense feelings of euphoria and well-being (for some)
• Sedation, analgesia, nausea are common, especially with
higher doses
• Tolerance builds and ceasing use may result in
withdrawal symptoms
• https://erowid.org/chemicals/heroin/heroin.shtml
Cough medicine
Synthetic Opioids
• Synthetically manufactured to
mimic natural opiates
• Most often prescribed for pain
relief
• Synthetic:
• Fentanyl
• Demerol
• Methadone
• Buprenorphine
• Semi-synthetic:
• Oxycodone
• Percocet
• Hydromorphone
Opioid substances*not all inclusive
• Pharmaceutical• Codeine (e.g., Tylenol 3)
• Oxycodone (e.g., Percocet)
• Oxycontin (time release oxycodone)
• Morphine
• Hydromorphone (e.g., Dilaudid)
• Hydrocodone (e.g., Hycodan)
• Meperidine (e.g., Demerol)
• Fentanyl (and analogues)• Transdermal patch;
• Illicit powder; analogues
• Substitutes • Methadone
• Bubrenorphine
• Suboxone (Bup + naloxone)
Image: cbc.ca
Image: theinfluence.org
Common generic, trade and street
names for opioids
Source: CCSA
• Oxycodone was developed in 1917
• OxyContin contains Oxycodone in
a timed-release tablet• Introduced in 1996 by Purdue
Pharma
• Designed for 12-hour pain relief
• Reduces pill-burden
• In 2012, Oxycontin was discontinued and
replaced by OxyNEO
• OxyNEO is still Oxycodone but in a
supposedly harder to tamper with pill
OxyContin / Oxycodone
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• When used illicitly could be
taken in pill form, or crushed
and then ingested, snorted, or
injected• Delivering the whole time released
dose at once
• Many users tend to trust pills
because they assume they are
of pharmaceutical quality, but
there are many counterfeit
“Oxy’s”
OxyContin
The top image is a
real 80mg OxyContin.
The bottom image is
a counterfeit 80mg
OxyContin. The
shade of green is
clearly wrong.
Counterfeit 80mg OxyContin.
The outer casing colour (green)
is extremely close, however, the
inside should be white.
Source: www.studiolonline.net
Prescription Opioids and their
Ingredients
Tylenol #2, #3 and #4
Codeine with acetaminophen
Percocet Oxycodone with acetaminophen
Oxy Neo
OxyContinOxycodone in a time-released formula
Dilaudid Hydromorphone
Prescription Opioids and their
ingredients
MS Contin, M-Eslon Morphine
Duragesic patch Fentanyl
Talwin Pentazocine
Demerol Meperidine
Fentanyl
• Medically used for pain relief
• Typically as a patch, dispensing drug for several
hours (2-3 days)
• Micrograms vs milligrams!
• Now in many opioid street drugs and
occasionally some stimulant drugs
• Illicit powder > patch diversion
• “Bootleg fentanyl” and analogues
• 0.4mg naloxone should reverse overdose
• May not be enough for some analogues
• Extremely potent pain medication
• Usually prescribed as a trans-dermal, time
release patch.• 5 strengths with 1.25, 2.5, 5.0, 7.5, 10 mg
• Delivers 12, 25, 50, 75, 100 mcg/hr for 72 hours
• When used off prescription, people may
suck, or scrape the patch and smoke or
inject the fentanyl• Uneven distribution on patch
• One patch can give about 10 injections
• People can easily inject too much and overdose
• Testing strips?
Fentanyl patch Novel Synthetic Opioids
• Counterfeit pharmaceuticals manufactured illegally
• Designed to look like legitimate pharmaceuticals
• In the US and Canada there are counterfeit pills
including OxyContin and Percocet
– Often contain a synthetic opioid different from the active
substance users believe is present
• Novel synthetic opioids that have been used include
“bootleg fentanyl” and fentanyl analogues
• Other substances that have been used, or might be
used, include W-18 (not actually an opioid), U-47700,
AH-7921 and MT-45.
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Source:
https://www.googl
e.com/patents/W
O2012062439A1?
cl=en
Carfentanil
• Carfentanil (4-carbomethoxyfentanyl) is an analog of the
synthetic opioid analgesic fentanyl
• Four orders of magnitude or 10,000 times more potent
than morphine; 100 times more potent than Fentanyl
• One of the most potent known and the most potent commercially used
opioids
• First synthesized in 1974
• Marketed under the trade name Wildnil as a general
anaesthetic agent for large animals
• As little as 20 micrograms could be fatal to the average person (one
microgram is smaller than a grain of salt)
• Canadian seizures include powders, pills and blotter tabs
• Would need more than one dose of naloxone (US report of 18mg
needed; standard dose is 0.4mg)
• W-18 is a compound in a series of 32 substances (named W-1 to W-32)
• First synthesized in research on analgesic drugs in the 1980s
• Started appearing illicit/recreationally in the 2010s
• W-18 was commonly reported to be an opioid but new understanding
shows this is not true
• W-18 was found to obtain weak activity at both sigma receptors and
the translocator protein (peripheral benzodiazepine receptor)
• http://www.forbes.com/sites/davidkroll/2016/07/28/w-18-is-not-a-
super-potent-designer-opioid-as-originally-believed
• May not respond to naloxone
• In Canada, W-18 and its analogues were made Schedule I controlled
substances effective November 2016
W-series of compounds Novel Synthetic Opioids
• CCSA bulletin:
Novel Synthetic Opioids in Counterfeit Pharmaceuticals
and Other Illicit Street Drugs
http://www.ccsa.ca/Resource%20Library/CCSA-
CCENDU-Novel-Synthetic-Opioids-Bulletin-2016-en.pdf
Concerns
• The use of many and diverse active substances
in counterfeit pharmaceuticals and other illicitly
produced powders means that people using
these products have little information about what
or how much of the substance or substances
they are taking, or their potency and toxicity
• This places them at great risk of overdose
• Information should be provided to people who
use drugs (PWUDs) about what might be
included in the tablets and powders they are
consuming
Concerns
• In their pure form substances such as fentanyl and other synthetic
opioids can be orders of magnitude more potent, and therefore
possibly more toxic, than morphine. However, rarely do those
purchasing these substances in the illicit market encounter them in
their pure form. Instead, they purchase products mixed with bulking
agents or diluents designed to increase the volume of the product
without increasing the amount of active ingredient. However,
clandestine labs or illicit pill pressing operations have difficulty
distributing the active substance evenly across an entire batch of
tablets or powders, particularly when the active dose is very small,
as when using such potent substances as fentanyl. The result is an
uneven distribution of active substance, which means that some
tablets or powders might contain a small quantity of the active
substance, while other tablets or powders might contain a lethal
dose.
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Communicating drug alerts among
people who use drugs
• Flyers, posters or other advisories should avoid
terms that might attract users, such as “potent”,
“strong”, or “more powerful”, which could
inadvertently result in an increase in people
seeking out the drug
• Better alternatives are “toxic”, “dangerous”, or
“lethal” - terms that imply harm
• Date information materials so that people know
when something is a recent concern, not an
ongoing issue
Communicating drug alerts among
people who use drugs
• Include specific calls to action. If individuals
decide to use substances regardless of the
danger, advise them to:
• Make a plan in case of overdose
• Make sure that someone with them is sober enough
to call 911 if an overdose is suspected
• Use a small amount to start
• If an overdose is suspected, perform rescue
breathing, administer naloxone and call 911
Communicating drug alerts among
people who use drugs
• Consider mentioning some of the signs of an
overdose, so people know what to look out for:
• Early signs of opioid overdose include severe
sleepiness; trouble breathing (can sound like
laboured snoring); slow, shallow breathing; cold,
clammy skin; and unresponsiveness to pain.
• Ontario Harm Reduction Distribution Program
poster
– http://www.ohrdp.ca/wp-
content/uploads/pdf/SignsSymptoms.pdf
• All are “downers”
• Primary risks are slowed breathing and heart rate
• High potential for tolerance and dependence with many
• Heroin use has become an increasingly marginal form of
drug use among illicit opioid users in Canada, particularly
outside of Vancouver and Montréal
• Most of the pharmaceuticals are prescribed for pain
management but have increasingly become the predominant
form of illicit opioid use
• “Opioid-rich" environment:
• Canada is a world per capita consumer of
pharmaceutical opioids
Opioids
Ontario, Canada - Student Data Bioavailability and half-life
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Percocet 5 mg tabs $5
Oxycocet 5 mg tabs $3
Morphine 30 mg tabs $4
Morphine 100 mg tabs $8
Oxycontin 10 mg tabs $7-8
Oxycontin 40 mg tabs $20-30 ($20 Renfrew Cty)
Oxycontin 80 mg tabs $45-60 ($40 Renfrew Cty)
Fentanyl 50 mcg patch $30
“Underground Economy”
South East LHIN – North Hastings
From presentation: “Below the Radar: Exploring Substance Use In Rural Ontario”. Kathy Hardill and Sean Lee-Popham
(North Hastings Harm Reduction Network), Canada Harm Reduction 2011 Conference , Ottawa
*In Northern Ontario, in some First Nation’s communities, 80mg pills can be sold for $200-$500.
What’s most cost effective for dealers?
Source: European Monitoring Centre for Drugs and Drug Addiction
Opioid deaths in Ontario
Depressant intoxication: What are the signs?
• Breathing is very slow, erratic or not there at all
• Finger nails & lips turn blue or purple
• Body is very limp
• Deep snoring or gurgling sounds
• Vomiting
• Loss of consciousness
• Unresponsive to stimuli
• Pinpoint pupils
• *Not all symptoms have to be present*
• A short clip explaining what an opioid overdose is and how the
emergency medicine naloxone (Peterborough Drug Strategy)
– https://youtu.be/g-9KyxMtGXg www.ohrdp.ca
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Opioid Overdose vs ‘The Nods’
Check for:• Breathing
• A good way to check someone’s breathing is by using the
back of your hand (very sensitive) or your cell phone to
see if there is ‘fog’
• Alertness
• Pulse
• Other signs?
• It’s important to not let too much time pass
before deciding whether or not to administer
naloxone and call EMS
Depressant overdose response myths
Do Not Implications
Put the person in a bath/cold waterCould drown or put
person into shock
Induce vomiting Could choke
Inject them with anything (saltwater, cocaine, milk) other than naloxone
Will not help and
could cause more
harm
Slap too hard, kick them in the testicles, burn
the bottom of their feet
Could cause serious
harm
Let them sleep it off!Could stop breathing
and die
*Toronto Public Health
Opioid overdose – calling 911
When calling 911, keep it simple: Ask for an ambulance
Let them know that a person is not
breathing/unresponsive/turning blue/unconscious
Let them know the exact location where the person is
Keep the loud noise in the background to a minimum, so that
the safety of the paramedics is not in question
When EMS/paramedics arrive: Let them know what drugs the person may have been using so
they can administer naloxone (if they have it) in a timely
manner
If naloxone has already been administered, let EMS know,
along with the outcome Toronto – Take home naloxone and training through The Works:
http://www1.toronto.ca/wps/portal/contentonly?vgnextoid=aeb94e2c82f1d410Vg
nVCM10000071d60f89RCRD
Naloxone
• Naloxone is an opioid antagonist that reverses
opioid-related respiratory depression
• Currently in Canada, naloxone is available in a
form that is to be injected intra-muscularly
• In Ontario, naloxone is used by many EMS and
emergency departments
• As of summer 2016, available for free at many
pharmacies across the province
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Opioid Overdose Prevention Resources
• There are many opioid overdose
prevention and response programs
in Ontario
• Overdose prevention and
response programs do not need to
distribute naloxone in order to
successfully work with clients to
prevent opioid overdose
• Each existing program is unique
and meets the needs of the local
community
• For resources on how to
implement a program and how to
respond to an overdose check out:
www.ohrdp.ca/opioid-overdose-prevention/
Withdrawal
• Opioid drugs can produce withdrawal symptoms just
hours after the last dose
• Symptoms can last for a week or more
• Unassisted withdrawal may not be life-threatening, but it
can lead to relapse
• Medications and therapy, accessed in medical detox,
may make relapse less likely
Withdrawal
Source: American Addiction Centers
Source: discoveryplace.info
Opiate Risk Reduction and Treatment
• Basic risk reduction strategies, particularly using new equipment when
injecting.
• Be cautious when using after periods of abstinence, as tolerance may
have dropped and risk of overdose is increased.
• naloxone may be used in cases of overdose to provide temporary
relief but person should still be taken to hospital.
• Snorting and injecting opioid painkillers can result in a quicker and
stronger effect.
• These methods can be dangerous as they release several hours
worth of opioid painkillers into your body at once.
• Mixing with other substances, particularly depressants such as alcohol
and narcotics, can be dangerous.
• Some opioid painkillers (such as codeine and hydrocodone) also
contain acetaminophen, which can cause liver toxicity with regular use
and high doses.
• Medications (Methadone; Buprenorphine) can assist with detoxification,
in combination with other therapeutic interventions.
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Some people struggling with opioid dependence are unable to
maintain a state of abstinence. Prolonged methadone
treatment can lead to:
• A decrease and often the cessation of opioid use.
• A decrease in the use of other substances.
• A substantial decrease in crime and prostitution.
• Improved health.
• An improvement in living conditions.
• Better conditions for the continuation of pregnancy.
Methadone Maintenance Programs
What is methadone?
Methadone is an effective and legal substitute for opioid drugs such as
heroin, codeine, morphine, Dilaudid® and Percodan®. Methadone is a long-
acting opioid drug. This means it acts more slowly in the body, for a longer
period of time, than most other opioids. By acting slowly it can prevent
withdrawal and eliminate or reduce drug cravings, without causing a person
to get high. People who are dependent on opioid drugs can take methadone
to help stabilize their lives and to reduce the harms related to their drug use.
It has been used in treatment programs since the early 1960s. Methadone is
available through specialized drug treatment clinics or it may be prescribed
by family physicians and dispensed by community pharmacists, in
accordance with Canadian regulations. Only physicians who have received
an exemption under Section 56 of the Controlled Drugs and Substances Act
are allowed to prescribe methadone.
Methadone Maintenance Programs
How does it work?
Methadone can be used to replace the opioid drug that a
person is dependent on. It prevents withdrawal symptoms and
cuts down on the person’s drug cravings. It does not alter
someone’s ability to work, go to school or care for their family.
Users usually need one dose every 24 hours. When
methadone is diluted in juice, it does not have a euphoric effect
or interfere with a person’s thinking, however, it does block the
euphoric effect of heroin and other opioid drugs, so it makes
the idea of using those drugs much less attractive. Methadone
works best when it is combined with drug counseling.
Methadone Maintenance Programs
Is methadone safe?
When taken as prescribed, methadone is very safe and will not cause damage to the body or
mind, even if it is taken daily for many years. On the other hand, methadone is a powerful drug
and can be extremely dangerous if not taken properly.
How is methadone taken?
Your doctor will give the pharmacy a prescription for your methadone. This prescription must be
renewed regularly by your doctor. He or she will determine how often you come for
appointments, depending on your needs and progress. Your dose of methadone is usually
mixed with orange juice. When you first start on methadone, you will be asked to go to your
pharmacy each day to drink the medication. After two months you may be able to begin to take
home some doses. These are called “carries.”
How long do people stay on methadone?
People stay on methadone as long as they need to. Some health care providers promote short-
term methadone detoxification, where the dependent person is stabilized on methadone and
then tapers off using it over the next one to six months. Others may stay on it for up to twenty
years. Whether short-term or long-term, research has shown that methadone maintenance is
the most effective treatment for opioid dependence.
Methadone Maintenance Programs
Given the costs of untreated opioid dependence, methadone maintenance treatment
offers significant benefits to society, which far outweigh the costs of providing
treatment. American researchers have found:
• The annual costs of methadone maintenance treatment are much lower than the
annual costs of either untreated heroin use, incarceration or drug-free treatment
programs;
• Criminal activities related to heroin use resulted in social costs that were four times
higher than the cost of methadone maintenance treatment;
• For every dollar spent on methadone maintenance treatment there is a savings to
the community of between US$4-$13.
Similar cost benefits are being identified in Canada. In Toronto, the average social
cost of an untreated person who is dependent on illicit opioids has recently been
estimated to be $44,600 per year. According to an estimate from the Centre for
Addiction and Mental Health in Toronto, methadone maintenance treatment can be
provided for approximately $6,000 per year. (2000)
In Canada, methadone maintenance has increased five-fold since the mid-1990s.
Methadone Maintenance Programs
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Methadone and HIV
• Some HIV meds decrease the strength of
methadone, which means you could go
into methadone withdrawal.
• Not a lot is known about how HIV meds
interact with substances - it’s a good idea
to talk with your doctor, nurse or
pharmacist about what is known so you
can stay as healthy as possible.
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Methadone Interactions
• Viramune: methadone up to 60%
• Sustiva: methadone up to 60%
• Rescriptor: Not studied
Methadone Interactions
• Crixivan: None
• Norvir: Decreases methadone levels
• Invirase/ Fortovase: Minimal effects on
methadone
• Agenerase: Decreases methadone by 13%
• Viracept: methadone 35-45%
– ( NFV 50%)
• Kaletra: methadone up to 50%
Buprenorphine/Suboxone
• Buprenorphine hydrochloride is one of the first new treatment options
for opioid dependence since methadone was introduced in Canada
over 40 years ago.
• Physicians do not have to obtain a section 56 methadone exemption1
from Health Canada in order to prescribe buprenorphine.
• While international clinical evidence indicates that buprenorphine is a
much safer drug than methadone, it is important to keep in mind that
the opioid-dependent patient population presents special risks and
challenges.
• Two formulations of buprenorphine – Subutex® and Suboxone® –
have been approved by Health Canada for use in treating opioid
dependence.
Buprenorphine
• Is efficacious as substitution therapy in the treatment of opioid dependence.
• Is an alternative to, but not a substitute for, methadone maintenance treatment.
• Is considered safer in overdose than methadone, although if combined with other CNS depressant drugs (e.g., benzodiazepines) respiratory depression can occur. If clinical symptoms of overdose occur it may require higher doses of naloxone or other measures for treatment.
• May have a lower potential for abuse and dependence than pure agonists such as morphine, although abuse does occur.
• Can be titrated to an effective dose within days, in contrast to methadone which typically may take weeks to achieve.
• May induce withdrawal in patients dependent on opioids if administered too soon after last use of full opioid agonists.
• May be easier to taper from than methadone.
• May be associated with less stigma than methadone.
• Suboxone (Buprenorphione plus naloxone) is a sub-lingual tablet, available in two different doses. The naloxone is intended to deter injection.
• Coverage for Suboxone is currently not universal in Ontario.
Source: (CAMH 2008)