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Journal of Pharmacology and Therapeutic Research
Volume 1 Issue 1 Clinical Pharmacy 2017
Notes:
Page 16
December 07-09, 2017 | Rome, Italy
7th World Congress on
Clinical Pharmacy and Pharmacy Practice
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, China
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 (eg, 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 has 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 has worked in different
London Teaching Hospitals for 16 years. In the last 12 years in UK, she has
specialized in Pediatrics (especially in PICU and Pediatric Liver), Obstetrics and
Gynecology. She published two articles relating to drugs use in pediatric 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. She delivers lectures
to the Master and Undergraduate Pharmacy students relating to drugs use in
Pediatrics, Obstetrics and Gynecology.
Christina Yuen Ki Leung, J Pharmacol Ther Res 2017