Concepts of Phenylpiperidine Derivatives Use in the Treatment of Acute and Chronic Pain: A New Avenue

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Concepts of Phenylpiperidine Derivatives Use in the Treatment of Acute and Chronic Pain: A New Avenue

Acute pain usually starts suddenly and is an intense sensation. Chronic pain is ongoing and lasts longer than 6 months, often continue after an injury has healed. Phenylpiperidines derivatives can be used to obtain relief from acute and chronic pain. It plays an essential function in many aspects of medicine like anaesthesia and pain medicine. These agents belong to a chemical class of drugs with a phenyl moiety directly attached to piperidine.

The present study aimed to focus on phenylpiperidine derivatives and their use in current anaesthesia and perioperative medicine practice. Second generation synthetic phenylpiperidine which is a series of opioid such as meperidine, fentanyl, was synthesized and introduced as fentanyl citrate into clinical anaesthesia practice in 1968. Fentanyl- mediated or modulated responses enhance the pain threshold and provide both analgesic and sedative effects. It acts as an agonist at mu-opioid receptor, at the dorsal horn inhibiting ascending pain pathways in the rostral ventral medulla. As fentanyl is metabolized mainly via CYP3A4, there is a possibility that adverse effects may occur with concomitant use of any drug which affects CYP3A4 activity. Stopping the use of CYP3A4 inducers can also increase fentanyl plasma concentration. The routes to administer fentanyl-based formulations could be intravenous, intramuscular, transdermal, transmucosal, and neuraxial routes. Remifentanil which 2 times potent than fentanyl, can be used as ultra-short-acting analgesic.

The newer formulations of sufentanil, which is an analog and 5 to 10 times potent than fentanyl, currently being evaluated for acute pain management. We examine the routes of administration and clinical considerations, including the role of opioids such as fentanyl as a natural killer cell suppressive agent and it has also been shown to potentiate propagation of infection and cancer with other opioids.

In recent years, fentanyl and other phenylpiperidine formulations have been developed and successfully marketed for chronic pain management. Due to complex physiological responses and potential drug-drug interactions of opioids, clinicians should recognize all the aspects of this drug class and consider all available options in appropriate clinical settings.

Source:

Pain Physician

Link to the source:

http://www.painphysicianjournal.com/current/pdf?article=NDIwOQ%3D%3D

Original title of article:

Current Concepts of Phenylpiperidine Derivatives Use in the Treatment of Acute and Chronic Pain

Authors:

Nidal Elbaridi, Alan David Kaye et al.

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