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Drugs and Medicinal Substances

Codeine

Nervous System Agents

Codeine is an opiate and a prodrug of morphine, used to treat mild to moderate pain, coughing and diarrhea, and it works better against pain when combined with another analgesic such as paracetamol or an NSAID. The liver enzyme CYP2D6 converts codeine into morphine, a far more potent opioid, which then binds to mu-opioid receptors in the central nervous system to reduce pain signaling. French chemist Pierre Jean Robiquet discovered codeine in 1832; the compound occurs naturally in the opium poppy, making up roughly two percent of raw opium, and most codeine used today is produced by chemically modifying morphine.

Facts
Drug Class
Opiate, prodrug of morphine 1
Mechanism of Action
Prodrug of morphine; binding of codeine or morphine to the mu-opioid receptor hyperpolarizes the neuron and inhibits release of nociceptive neurotransmitters, causing an analgesic effect 1
Approved Use
Pain, coughing and diarrhea 1
First Approved / Isolated Year
1832 1
Significant Risk
Breathing difficulties and addiction 1
Classification
Approval Status
Approved 1
ATC ClassSourced to the subject's own account
N: Nervous System 2
Route of Administration
Oral 1
WHO Essential MedicineSourced to the subject's own account
Core List 3
Sources
1. Codeine - Wikipedia
  • Lead section, first sentence (drug class)
    Codeine is an opiate and prodrug of morphine
  • Article body, sentence beginning 'Binding of codeine or morphine to the μ-opioid receptor'
    Binding of codeine or morphine to the μ-opioid receptor results in hyperpolarization of the neuron leading to the inhibition of the release of nociceptive neurotransmitters, causing an analgesic effect
  • Lead section, first sentence (medical use)
    mainly used to treat pain, coughing, and diarrhea
  • Article body, sentence beginning 'Codeine was first isolated in 1832'
    Codeine was first isolated in 1832 in France by Pierre Robiquet
  • Lead section, sentence beginning 'Serious side effects may include'
    Serious side effects may include breathing difficulties and addiction.
  • Lead section, route-of-administration statement
    It is generally taken orally.
  • Regulatory approval status
View the Source
2. Anatomical Therapeutic Chemical Classification System (Wikipedia)
WikipediaFirst-level anatomical group codes, Code N
Quote, First-level anatomical group codes, Code N
Nervous system
View the Source
3. WHO Model List of Essential Medicines (Wikipedia)
WikipediaWHO Model List of Essential Medicines, Opioid analgesics section
Quote, WHO Model List of Essential Medicines, Opioid analgesics section
Codeine
View the Source
Frequently Asked Questions

Why is codeine described as a prodrug rather than a painkiller in its own right?

Codeine is classed as a prodrug of morphine: the body converts codeine into morphine, and it is the resulting morphine that actually relieves pain.

Codeine is an opiate and a prodrug of morphine, mainly used to treat pain, coughing and diarrhea. Being a prodrug means codeine itself is not the compound that produces the effect; the body converts codeine into morphine, a far more potent opioid, and it is that morphine which acts on the central nervous system to relieve pain.
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