Q&A: Why is the illicit use of Fentanyl so dangerous?

TORONTO
– Toronto Public Health Officials are sounding
the alarm on the
illicit use of ‘Fentanyl,’
a painkiller 750 times more powerful than codeine and 100 times more powerful
than morphine.

According
to Public Health officials, some
users
are scraping the drug-containing gel from the patch and injecting it,
causing
a much higher
dosage that takes effect instantly.

Global
News spoke to Michelle Arnot, a lecturer at the University of Toronto’s
Department of Pharmacology and Toxicology,
about how Fentanyl works, why it is so potent, and possible side effects
associated with its
injection.

How
does Fentanyl work? 

The
drug works similar to morphine in that it binds and interacts with the mu opioid
receptor- which is one of the main receptors that modulates pain. Part of
modulation of pain is euphoria which is also associated with the activation of
this receptor however (i.e. think of how good you feel with a runners high- now
multiply that exponentially).

Why
is it more dangerous than other opiates? 

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It
is more fat soluble than morphine- so its onset of action is faster as it
reaches the brain faster- this makes it more potent (i.e. less drug is needed
for the intended effect). This fat solubility also makes it ideal for
transdermal application- where it sits under the skin and slowly diffuses to the
brain. 

Why
is Fentanyl more addictive than other drugs? 

It
is addictive because it is more fat soluble and readily crosses into the brain.
The reasons that make it a good clinical drug are some of the reasons why it is
misused. Fast onset, fast euphoria, stronger addictive profile (fast on and fast
off).  When used as a patch this onset is slowed…clinical effects take about
12 hours.

Why
is it so dangerous for people to inject Fentanyl? 

Injection
from transdermal patches are dangerous for a number of
reasons:

1. It
   is more potent. Less drug is required for euphoria and less drug is required for
   respiratory depression and death.
2. The
   dose in the patch can be 10-50 times more than what is given clinically in a
   Fentanyl injection. Extraction does not allow for quantification of active
   ingredient- so it is unknown what dose the individual is injecting and difficult
   to repeat exactly every time it is extracted.
3. Contaminants
   and ethanol and cellulose in the formulation can also cause their own adverse
   effects

 What
are some side effects of Fentanyl? 

As
for adverse effects- the big one that results in death due to Fentanyl overdose,
is respiratory depression (the drive to breath is inhibited) and without medical
treatment- death.