What Is Codeine?

Codeine is an opioid often prescribed to reduce coughing but also used to treat mild to moderate pain. It can be prescribed by itself, in combination with acetaminophen, or in prescription cough medications.

Codeine is available in tablet, capsule, and liquid form and in combination with several other medications. When taken orally, it is absorbed readily and reaches maximum concentration within an hour. For pain relief in an average adult, it is dosed between 15 milligrams and 60 milligrams every four to six hours. The dose for cough suppression is lower, usually between 10 milligrams to 20 milligrams every four to six hours as needed.

Codeine Drug Schedule

Codeine is unique in that it can be categorized into different controlled substance risk levels depending on how it is prescribed.

Schedule II

Codeine is a Schedule II controlled substance when prescribed by itself due to its risks of physical dependence and abuse. Before prescribing codeine, clinicians should complete an assessment of the patient involving their risk of substance abuse or misuse. Schedule II controlled substances are medications that have been determined to have a high potential for abuse, which may lead to severe psychological or physical dependence.

Schedule III

Codeine becomes a Schedule III controlled substance when it is combined with acetaminophen (such as Tylenol). A Schedule III substance has a lower potential for abuse than a Schedule II. If misused, these medications have a moderate or low physical dependence or high psychological dependence.

Schedule V

Codeine becomes a Schedule V controlled substance when it is available in cough suppressant medication. Substances in this category have low potential for abuse and have limited quantities of narcotics present.

How Does Codeine Work?

In the US, codeine is usually produced by chemical modification of morphine. When it is metabolized in the body, a small amount (approximately less than 10%) is converted to morphine. Due to this, codeine is only a tenth as potent as morphine for pain relief, resulting in limited analgesic effects.

After ingestion, approximately 80% of codeine is metabolized into Codeine-6-glucuronide (C6G), an agent that has very little pain-relieving activity. Codeine is considered a weak agonist at the main pain receptors in the central nervous system.

Codeine is a known cough suppressant and is most effective in reducing a cough that occurs due to short-term illness. This happens due to binding at the mu-opioid receptor in the brain, which acts on the cough center located in the brainstem.

Some animal models suggest codeine, and other opioids, affect the raphe nuclei in the brain, depressing the cough reflex activity. There is some evidence that binding to the kappa opioid receptor may also contribute to the cough suppressant activity.

For the treatment of diarrhea, opioids bind to receptors throughout the gut, which control motility and secretion. Codeine causes an increased amount of intestinal absorption, leading to decreased stool volume overall. This is done by slowing the rate of passage of fluids. In addition, there is a slowing or stopping of the natural peristalsis of the intestine, which delays or inhibits bowel movements.

Genetic Factors

Codeine is metabolized to morphine through a pathway called cytochrome P450 2D6 (or CYP2D6). There is some evidence that patients with different genetic alterations may only feel pain relief from codeine if they are able to complete this metabolic breakdown.

A small percentage of the population metabolizes codeine poorly, which may result in poor pain relief. Conversely, a person who is an ultrarapid metabolizer of codeine can metabolize it to morphine rapidly, leading to potentially fatal respiratory depression at normal doses.

Featured Centers Offering Treatment for Codeine Addiction

Side Effects

Codeine has several of the same side effects as other opioids. Mental sedation and fatigue are common. Constipation is also one of the most common side effects reported. Nausea or vomiting, as well as itching, urinary retention, sexual dysfunction, hallucinations, and blurry vision are also regularly reported side effects.

When codeine is used in combination with benzodiazepines, alcohol, or other substances, a cumulative effect of respiratory depression, sedation, coma, and death can occur. The effects of chronic codeine cough syrup (CCS) abuse have been found to cause brain damage and alterations in blood flow patterns in the brain.

An overdose of codeine may result in any of these symptoms:

  • Delayed or shallow breathing
  • Fainting
  • Slow heartbeat
  • Extreme sleepiness
  • Difficulty breathing
  • Cold and clammy skin
  • Small pupils
  • Blue-tinted fingertips or lips

An overdose can happen even if a person takes the amount of codeine prescribed. If you suspect an overdose, call 911 immediately.

Dependance And Misuse

In late 2018, the U.S. Food and Drug Administration published an alert that changed how cough and cold medications containing codeine could be prescribed. This alert required labeling changes to limit the use of codeine and hydrocodone-containing cough medications to adults aged 18 and older. In addition, warnings about the risk of misuse, abuse, addiction, overdose, and death, as well as slowed or difficult breathing, were added.

When abused, codeine can produce feelings of euphoria, elation, and extreme happiness, which can make a person taking it use larger doses or take the drug more frequently to maintain the high. The increase in codeine prescription drug abuse has been linked to an increase in social acceptability and a potential false belief that prescription medications are safer than street drugs.

Codeine withdrawal can be uncomfortable and produce moderate to severe symptoms, such as fever, headaches, and insomnia, when people try to quit or taper off the drug. People may fall back into using codeine to avoid these withdrawals symptoms, contributing to the cycle of misuse.

Abuse In Young Adults

The abuse of cough syrups containing codeine has been rising in young adults. This has been the result of availability, a false sense of safety, and social popularity. Mixing codeine in cough syrup form with alcohol is considered polysubstance abuse, and this is the basis for the slang term “Lean” or “purple drank”. Sometimes, it is combined with candy and soda.

Treatment For Codeine Addiction

An addiction to codeine can lead to serious and life-threatening side-effects for those who misuse and abuse the drug. Young adults are particularly vulnerable to misuse due to its prevalence in popular culture.

If you or a loved one is seeking support for codeine addiction, help is available. Reach out to a treatment provider today to explore your treatment options, risk-free.