Abstract
Hydrocodone is one of the most prescribed oral analgesic drugs and it is one of the most abused drugs in general population. It is a mu-opioid agonist predominantly metabolized to the O-demethylated product hydromorphone and to the N-demethylated product norhydrocodone. The purpose of the study is to summarize the preclinical and clinical characteristics of hydrocodone. Pharmacokinetic aspect (terminal half-life, maximum serum concentration, and time to maximum serum concentration) of hydrocodone and the influence of metabolic genetic polymorphism in analgesic response to hydrocodone are also illustrated and commented. Literature on experimental preclinical pharmacology investigating analgesic activity in laboratory animals is furtherly discussed. Moreover, the authors discuss and comment on the updated data regarding safety profile and effectiveness of hydrocodone in the treatment of chronic pain. A bibliographic research was carried out (from February 01, 2018 to August 28, 2018) independently by two researchers (blinded to the authors and initially on results) in the major scientific databases and research engines of peer-reviewed literature on life sciences and biomedical topics, starting from January 1990 to August 2018. Analysis of results of clinical studies suggests that abuse-deterrent extended-release (ER) hydrocodone formulations can be effective and they are well tolerated in the treatment of chronic low back pain. Weaker is the evidence of the analgesic effectiveness of ER hydrocodone on other chronic pain syndromes and non-cancer non-neuropathic chronic pain. In these conditions, hydrocodone showed to have positive effects in non-controlled open studies and needs to be further studied to assess the real strength of results.
Highlights
Opioids are the most potent drugs producing analgesia and their use is fundamental for the clinical pain management (Mercadante et al, 2014)
Objective of this review is to summarize the principal preclinical and clinical characteristics of the opioid drug hydrocodone
Hydrocodone produces its analgesic effects by activating mu-opioid receptors (MORs), it is a μ-opioid receptor agonist analgesic, even though when higher concentrations are reached it can bind with different opioid receptors
Summary
Opioids are the most potent drugs producing analgesia and their use is fundamental for the clinical pain management (Mercadante et al, 2014). The largest part of prescriptions regarding pain relievers opioid drugs are oxycodone, hydrocodone, morphine, codeine, methadone and transdermal morphine and fentanyl (Graziani and Nisticò, 2016). Objective of this review is to summarize the principal preclinical and clinical characteristics of the opioid drug hydrocodone. The investigators used the following keywords or combination of keywords: “hydrocodone,” “hydrocodone” and “chronic pain,” “hydrocodone” and “opioids.” The analysis included all articles written in English language, published in peer-reviewed scientific journals, describing preclinical findings and clinical applications of hydrocodone. All the authors reviewed all the eligible articles and resolved by discussion any uncertainty regarding the content about hydrocodone to be discussed
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