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Naloxone
NARCAN®
What is Naloxone (Narcan®)?
Naloxone is an opioid antagonist derived from an opiate alkaloid called
thebaine. It is also known by the brand name Narcan®.
Naloxone blocks the pharmacological effects of opioid analgesics, and
instantly brings on withdrawal.
It returns a person who has taken an opioid to a state where opioid
effects are not present.
Naloxone rapidly reverses opioid overdose effects, including respiratory
depression.
Naloxone does not work for non-opioid related overdose.
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Opioid Antagonists
Opioid antagonists 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.
Physical Appearance
Naloxone is a slightly off-white,
odorless crystalline substance
soluble in water and slightly
soluble in alcohol.
It is dispensed in liquid form in
ampules for purposes of injection.
A typical adult dosage is between
0.1 and 2.0 mg, repeated if
necessary.
Forms of Naloxone
There are two forms of Naloxone:
◦ Injectable Naloxone, which is
injected directly into the muscle,
skin or veins.
◦ Nasal Naloxone, is administered
through the nasal cavity (not
currently available in Canada)
Medical Uses
The primary medical use is to reverse respiratory depression and other
effects of opioid analgesics such as fentanyl, heroin, morphine, codeine.
Naloxone is also used when treating asphyxia in newborn infants whose
mothers were treated with opioid analgesics during labour.
Naloxone does not lead to overdose.
Effects of Short-Term Use: Low Doses
Naloxone takes action within 1-2 minutes when given intravenously, and
in 2-5 minutes if given subcutaneously or intramuscularly.
The duration of its effect depends on the size of dose and route of
administration – typically 30-60 minutes.
Opioid-dependent individuals will immediately experience withdrawal
symptoms very similar to following abrupt cessation of opioid use –
except the symptoms appear within minutes and last about two hours.
Naloxone Blocks Effects of Opioids
If an opioid is taken shortly after naloxone has been taken, the effects of
the opioid will be partially or totally blocked.
For example, 1 mg of naloxone has been demonstrated to completely
block the effects of 25 mg of heroin.
Tolerance & Dependence
Physical tolerance to Naloxone’s antagonist actions does not develop.
However, long-term administration of opioid antagonists such as
naloxone increase the density of opioid receptors in the brain and cause
temporary exaggeration of responses to subsequent administration of
opioid analgesics.
Extended use of naloxone will not cause harmful physical or
psychological dependence.
Can Naloxone be Abused?
Naloxone does nothing to a person who has not taken opioids, all it
does is block the effects of opioids in the brain and causes individuals
that are dependent on opioids to go into instant withdrawal.
Naloxone cannot get a person high, and does not promote opioid use.
Naloxone is used under medical supervision and is not a drug of abuse.
Opioid Overdose Antidote
Opioid overdose cause respiratory depression (breathing slows or
completely stops), which is reversed by naloxone.
For a brief period the patient’s breathing may become more rapid than
prior to the overdose.
Death, severe brain damage and other harms due to oxygen deprivation
during an opioid overdose has been shown to be reduced through
overdose education and community-based naloxone programs.
Opioid Overdose
Opioid overdose is common and one of the major causes of death in
addicts.
The highest risk time for overdose is in the period after drug use has
been discontinued because tolerance to opioid medication is quickly
lost.
Respiratory depression can also occur from drug overdose.
Abusing pain relievers along with other substances such as alcohol,
antihistamines, and general anesthetics can increase the chances of
respiratory depression.
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Why Does Overdose Happen?
Opioid overdose happens when an opioid user takes more than their
body can handle. Opioid overdose can occur for numerous reasons,
such as:
◦ When someone takes an opioid drug (e.g. Fentanyl) with a higher
concentration might be expected.
◦ When someone misuses or abuses opioids and combines the drug with
alcohol or another depressant drug.
◦ When someone returns to opioid use after a period of abstinence and
previously acquired tolerance has been lost.
Signs of Opioid Overdose
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Person cannot stay awake
Can’t talk or walk
Slow or no pulse
Slow or no breathing, gurgling
Skin looks pale or blue, feels cold
Pupils are pinned or eyes rolled back
Vomiting
Body is limp
No response to noise or knuckles being rubbed hard on the breast bone
Step 1: Rescue Breathing
Attempt to stimulate the overdose victim by calling their name or lightly
rubbing the sternum.
If the overdosing person is unresponsive call 911.
If the person is not breathing effectively, perform rescue breathing.
Step 2: Prepare Naloxone injection
Use a long needle (1 to 1 ½ inches) called an intramuscular needle (IM).
These needles can be located at either needle exchange programs or
pharmacies.
Now, pop off the orange top vial of naloxone.
From the vial, draw up to 1cc of naloxone into the syringe.
1cc=1 mL=100 u
Step 3: Administer Naloxone
Inject the needle straight into a muscle.
Thick muscle works best, such as:
◦ Thigh muscle
◦ Upper, outer quadrant of the rear
◦ Shoulder muscle
Be sure to inject straight to make sure the muscle is hit.
Step 4: Continue rescue efforts
After injection of naloxone, continue rescue breathing for 2 to 3
minutes.
If there is no change in their breathing after 3 minutes, administer
another dose of Naloxone and continue rescue breathing.
If the second dose of Naloxone does still not revive the person,
something else may be wrong (either the heart has already stopped,
there are no opioids in their system, non-opioid drugs are the cause of
the overdose, or the opioid drugs were too strong for the Naloxone)
Step 5: Monitor the person
Stay with the person until emergency responders arrive.
If you must leave them alone for any length of time, or if they are
unconscious, position them in the recovery position so their airway is
clear and they are less likely to choke on their own vomit, as they could
aspirate and die if left on their back.
If the person revives they will likely be in full opioid withdrawal and
want to use.
Use every effort to persuade them not to.
Key messaging
Key messages to reduce risk of death from opioid overdose include:
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Do not use alone
Use safer routes (i.e. not injecting)
Do a test hit first
Know the signs and symptoms of an OD
Do not mix drugs
Carry Naloxone
Call 911 if someone is overdosing
Know where to find resources
Naloxone reverses overdoses but does not treat addiction.
Availability of Naloxone
To date, Naloxone is not available over the counter, meaning it requires
a prescription.
Take-home Naloxone kits are available with both a prescription and
training on its administration.
Health Canada is putting forward an amendment to the prescription
drug list to allow non-prescription use of naloxone specifically for
emergency use for opioid overdose outside hospital settings.
Naloxone Take Home Kit
A Naloxone take home kit would
include:
◦ 2 glass ampoules of 0.4 mg/ml of
naloxone wrapped in gauze inside a
pill bottle for protection. Label
includes information.
◦ 2 rectangle VanishPoint® safety
syringes: 3cc-25g X 1
◦ 2 alcohol swabs
◦ 2 latex gloves
◦ One-way rescue breathing barrier
mask
◦ THN Administration information form
with Kit identifier information
◦ Steps to respond to opioid overdose
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Naloxone Training
Training and education on Naloxone include:
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Learning the signs of opioid overdose
How to perform rescue breathing
How to put someone in the recovery position
How to administer injectable Naloxone
Research has shown that with basic training, almost anybody would be
able to recognize an overdose and successfully administer.
AHS Online Naloxone Training
Alberta Health Services has made a Take Home Nalaxone online training
available to non-AHS health professionals. The training includes helpful
resources for download.
To take this training visit: http://cdm.absorbtraining.ca/#/login
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Complete sign-up as non-AHS learner. Login to account
Click ‘Catalogue’, then click ‘Chronic Disease Management’, then click
‘Addictions and Mental Health’
Choose the Take Home Naloxone Training by selecting ‘Open’.
Ensure Pop-up Blocking is turned off, then click ‘Launch’
Website Resources & References
Brands, B., Sproule, B., & Marshman, J. (eds) (1998). Drugs & drug abuse
(3rd ed.). Canada: Centre for Addiction and Mental Health
Drugs Fool (Alberta Health Services campaign):
◦ http://www.albertahealthservices.ca/drugsfool.asp
Harm Reduction Coalition:
◦ http://harmreduction.org/issues/overdose-prevention/overview/overdosebasics/responding-to-opioid-overdose/administer-naloxone/
Toward the Heart:
◦ Website: http://towardtheheart.com
◦ Overdose survival guide:
http://towardtheheart.com/assets/uploads/files/OD_Survival_Guide_Tips_to_Sa
ve_a_Life_2012.08.29_upright_for_website.pdf
Know Your Source:
◦ http://knowyoursource.ca
Contact Info
Sue Howard
Landline: (604) 535-2124
Cell: (250) 809-1066
Email:
sue@suehowardconsulting.
ca
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