Codeine
Opiate prodrug of morphine used for pain and cough.
Codeine is an opioid drug and a precursor to morphine, prescribed for pain, cough, and diarrhea, and also used recreationally. It comes from the sap of the opium poppy, *Papaver somniferum*. The World Health Organization lists it as an essential medicine, and in 2013 it was the most widely used opioid.
For mild to moderate pain, codeine is often taken by mouth, with effects beginning within half an hour, peaking at two hours, and lasting four to six hours. Combining it with paracetamol (acetaminophen) or a nonsteroidal anti-inflammatory drug (NSAID) like aspirin or ibuprofen can provide greater relief. Evidence does not support its use for acute cough in children, and in Europe it is not recommended for cough in anyone under 12. It is also used for diarrhea and diarrhea-predominant irritable bowel syndrome, though other drugs like loperamide are more common for severe cases.
Common side effects include nausea, vomiting, constipation, itching, lightheadedness, and drowsiness. Serious risks include breathing difficulties and addiction. Its safety during pregnancy is unclear, and caution is needed during breastfeeding because it can cause opioid toxicity in infants. As of 2016, it is not recommended for children. The liver breaks codeine down into morphine, and the speed of this process varies by genetics, which affects both its effects and abuse potential. Like other opioids, codeine carries risks of dependence and overdose. Withdrawal symptoms—such as craving, runny nose, yawning, sweating, insomnia, stomach cramps, nausea, vomiting, diarrhea, muscle spasms, chills, irritability, and pain—can occur if use is stopped abruptly. Long-term users should taper off under medical supervision.
Codeine was discovered in 1832 by Pierre Jean Robiquet. In 2013, about 361,000 kg were produced and 249,000 kg used. It naturally makes up about 2% of opium. It is available as a single-ingredient drug or in combination products, such as with paracetamol (co-codamol), aspirin (co-codaprin), or ibuprofen (Nurofen Plus). Injectable forms exist for subcutaneous or intramuscular use only—intravenous injection is contraindicated due to risk of anaphylactoid reactions. Suppositories are also marketed in some countries.
- discovered_by
- Pierre Jean Robiquet
- field
- Pharmaceuticals, Opioids
- natural_source
- Opium poppy (Papaver somniferum)
- common_uses
- Pain, coughing, diarrhea
Lore & Background
Codeine is a naturally occurring opiate that constitutes approximately two percent of the sap of the opium poppy, *Papaver somniferum*. Discovered in 1832 by Pierre Jean Robiquet, it functions as a prodrug, meaning it is metabolized by the liver into morphine; the speed of this conversion varies based on an individual’s genetics. The substance is typically administered orally and begins to take effect within thirty minutes, reaching peak activity at two hours, with pain-relieving and other effects persisting for four to six hours. It is most often employed for mild to moderate pain, such as post-surgical dental pain, and its efficacy can be enhanced when combined with paracetamol or a nonsteroidal anti-inflammatory drug like aspirin or ibuprofen. Evidence does not support its use for acute cough suppression in children, and European guidelines advise against it as a cough remedy for those under twelve. Common side effects include nausea, vomiting, constipation, itchiness, lightheadedness, and drowsiness, while serious risks involve breathing difficulties, addiction, and potential toxicity in breastfed infants. As with other opiates, chronic use can lead to physical dependence and withdrawal symptoms. Injectable forms are available only for subcutaneous or intramuscular administration, as intravenous injection may trigger a dangerous anaphylactoid reaction.
Reader's Guide
Codeine is significant as a widely used opioid analgesic and antitussive, but its use is complicated by abuse potential, addiction risk, and genetic variability in metabolism. It works by being broken down by the liver into morphine; how quickly this occurs depends on a person's genetics. Life-threatening intoxication can develop in patients with multiple functional alleles of CYP2D6, resulting in ultrarapid metabolism. The American Academy of Pediatrics does not recommend its use in children due to side effects, and the FDA lists age under 12 years old as a contraindication. Codeine is on the World Health Organization's List of Essential Medicines, reflecting its global medical importance despite ongoing safety concerns.
Did You Know?
- Codeine occurs naturally and makes up about 2% of opium.
- Codeine is a prodrug; it is converted by the liver into morphine, which is ten times more potent against the μ-opioid receptor.
Frequently Asked Questions
What is Codeine?
Codeine is an opiate medication and prodrug that the body converts into morphine. It is primarily prescribed to manage pain, suppress coughing, and treat diarrhea.
How does Codeine work in the body?
As a prodrug, Codeine is metabolized into morphine, which then produces its therapeutic effects. This conversion is what gives it its analgesic and antitussive properties.
Is Codeine used recreationally?
Yes, Codeine is commonly used as a recreational drug in addition to its medical applications. Its opioid effects, including euphoria and sedation, make it a frequent subject in addiction discussions.
More in Addictive Substances & Medications 1-24
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