Therapeutic Uses of Codeine in Pediatric Patients

Marcia L. Buck, PharmD, FCCP

Pediatr Pharm. 2004;10(4) 

In This Article

Introduction

The combination of acetaminophen and codeine is one of the most commonly used preparations for the treatment of moderate pain in children. Codeine is also used in a variety of antitussive preparations.[1,2] Despite the frequency of its use, there have been relatively few studies of codeine in the pediatric population. This issue of Pediatric Pharmacotherapy will review the pharmacology of codeine and highlight recent publications of its use in children.

Mechanism of Action

Codeine, also known as methylmorphine, is a naturally occurring alkaloid produced by the poppy plant, Papaver somniferum. It was first isolated from opium by the French pharmacist Robiquet in 1833. Although it may be obtained directly from the plant source, it is more commonly produced as a semisynthetic agent from the 3-O-methylation of morphine. Codeine is one of the phenanthrene opioids, a group with also includes morphine, hydrocodone, hydromorphone, oxycodone, oxymorphone, and levorphanol.[1,3]

Like other opioids, codeine binds to mu-opioid receptors to produce analgesia and euphoria, as well as respiratory depression, miosis, and reduced gastric motility. It also binds to kappa opioid receptors, producing spinally-mediated analgesia. Codeine has a low affinity for opioid receptors, however, making it a relatively weak analgesic with approximately 1/6th to 1/10th the potency of morphine.[3,4]

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