Abstract

Several over-the-counter (OTC) drugs are known to be misused. Among them are opioids such as codeine, dihydrocodeine, and loperamide. This work elucidates their pharmacology, interactions, safety profiles, and how pharmacology is being manipulated to misuse these common medications, with the aim to expand on the subject outlined by the authors focusing on abuse prevention and prevalence rates. The reviewed literature was identified in several online databases through searches conducted with phrases created by combining the international non-proprietary names of the drugs with terms related to drug misuse. The results show that OTC opioids are misused as an alternative for illicit narcotics, or prescription-only opioids. The potency of codeine and loperamide is strongly dependent on the individual enzymatic activity of CYP2D6 and CYP3A4, as well as P-glycoprotein function. Codeine can also be utilized as a substrate for clandestine syntheses of more potent drugs of abuse, namely desomorphine (“Krokodil”), and morphine. The dangerous methods used to prepare these substances can result in poisoning from toxic chemicals and impurities originating from the synthesis procedure. OTC opioids are generally safe when consumed in accordance with medical guidelines. However, the intake of supratherapeutic amounts of these substances may reveal surprising traits of common medications.

Highlights

  • Over-the-counter (OTC) drugs are medicines sold without medical prescription to treat common and temperate medical conditions

  • Most of the opioids used in clinical practice, including those available as OTC medicines, are agonists of opioid receptors that are predominantly selective for μ type receptors

  • While it is generally agreed upon that this problem concerns mainly prescription-only opioids and illicit narcotics, the involvement of OTC opioids should not be overlooked as there is sound evidence that such substances are being misused

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Summary

Introduction

Over-the-counter (OTC) drugs are medicines sold without medical prescription to treat common and temperate medical conditions. The misconception that OTC drugs are devoid of any harm to users has become established as a commonly held belief. Due to the acknowledged misuse liability, or associated health risks, some countries have already restricted access to several. OTC drugs by introducing an intermediate category of pharmacy-only (or pharmacist-only) medicines (POMs). While the purchase of POMs does not require a prescription from a physician, they may only be purchased in a pharmacy. Other restrictions, such as age limit or maximal purchase quotas, may be in place for the sale of POMs and OTC drugs

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