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Pain Management 2018
Internal Medicine 2018 International Journal of Anesthesiology & Pain Medicine
ISSN: 2471-982X Page 48
March 26-28, 2018
Vienna, Austria
JOINT EVENT
7 t h E d i t i o n o f I n t e r n a t i o n a l C o n f e r e n c e o n
Internal Medicine and Patient Care
&
6 t h E d i t i o n o f I n t e r n a t i o n a l C o n f e r e n c e o n
Pain Management
Volume 4
Buprenorphine and Fentanyl transdermal patches are used for
the management of chronic intractable pain in both malignant
and nonmalignant patients. Both buprenorphine and fentanyl
are potent opioids, but they have different pharmacology and
toxicology properties. It is important to understand the difference
in these properties as this information is useful for clinicians and
pharmacists to use the opioid patches safely and effectively.
Opioid analgesics mimic endogenous opioid peptides by causing
a prolonged activation of opioid receptors (usually μ receptor).
This receptor medicates analgesia, respiratory depression,
euphoria and sedation. Fentanyl is potent, highly lipid soluble,
rapidly acting μ-opioid receptor full agonist. Buprenorphine
is a highly lipophilic semisynthetic opioid. It has complex
pharmacology which is different from Fentanyl. Buprenorphine is
a partial μ-opioid receptor agonist which binds to and activates a
receptor, but has only partial efficacy compared to a full agonist.
This means that it may have ceiling effect and demonstrate
both agonist and antagonist effects. In human studies using
clinical effective analgesia doses, buprenorphine does not have
a ceiling effect to analgesia. However, buprenorphine does have
a ceiling effect for respiratory depression. Hence, higher doses
can be given with fewer respiratory depression side effect
compared with higher doses of fentanyl. The primary side effects
of buprenorphine are similar to fentanyl (e.g. nausea, vomiting,
and constipation), but the intensity of these side effects is
reduced significantly compared to full agonist, fentanyl. The
most severe and serious adverse reaction associated with opioid
use is respiratory depression, the mechanism is behind fatal
overdose. Buprenorphine behaves differently than fentanyl in this
respect, as it shows a ceiling effect for respiratory depression.
Buprenorphine has slowed off rate (half-life of association/
dissociation is 2–5 hours). The slow dissociation from μ-receptor
accounts for its prolonged therapeutic effect for treatment of
pain. Respiratory depression is rare with buprenorphine, but if
occurs, it can be reversed by Naloxone, often larger doses are
required than fentanyl because buprenorphine dissociates slowly
from the receptors. In conclusions, the pharmacology profile
of buprenorphine is complex but unique, and contributes to its
distinct safety and efficacy when it is used under appropriate
clinical indications.
Biography
Christina Yuen Ki Leung completed two Bachelor’s Degrees in England, BSc
Management Sciences Degree followed by the BPharm Pharmacy Degree.
Following the registration as a pharmacist in the UK, she worked in different
London Teaching Hospitals, UK for 16 years. In the last 12 years in UK, she
specialized in Pediatrics (especially in PICU and Paediatric Liver), Obstetrics
and Gynaecology. She published two articles relating to drugs use in pedi-
atric liver diseases in the UK Children Liver Diseases Magazine. She is also
a Registered Pharmacist in Hong Kong. Since 2012, she has been working
as the Senior Pharmacist (Clinical Pharmacy in Charge) at the HKU-SZH in
China. She is also the Honorary Tutor at the University of Hong Kong, Hong
Kong. She delivers lectures to theMaster and Undergraduate Pharmacy stu-
dents relating to drugs use in Pediatrics, Obstetrics and Gynaecology.
Understanding the pharmacology and toxicology properties of
transdermal buprenorphine and fentanyl to ensure the safety
and efficacy of drugs use
Christina Yuen Ki Leung
The University of Hong Kong - Shenzhen Hospital, China
Christina Yuen Ki Leung, Int J Anesth Pain Med 2018, Volume 4
DOI: 10.21767/2471-982X-C1-002