Codeine: General Introduction to It's Pharmacology

Name:- Ayan Das

University Roll No.:- 16401722005
Stream:- Bachelor of Optometry
Subject:- Pharmacology (General and Ocular)
Subject code:- BO-304

Introduction:
Codeine is an opiate and prodrug of morphine mainly used to treat pain, coughing, and
diarrhea. It is also commonly used as a recreational drug. It is found naturally in the sap of
the opium poppy, Papaver somniferum. It is typically used to treat mild to moderate degrees
of pain. Greater benefit may occur when combined with paracetamol (acetaminophen) or a
nonsteroidal anti-inflammatory drug (NSAID) such as aspirin or ibuprofen. Evidence does
not support its use for acute cough suppression in children or adults. In Europe, it is not
recommended as a cough medicine for those under 12 years of age. It is generally taken by
mouth. It typically starts working after half an hour, with maximum effect at two hours. Its
effects last for about four to six hours. Codeine exhibits abuse potential similar to other
opioid medications.[1]

[2]

Fig:-Codeine Oral Solution

Pharmacological Mechanism:
Codeine exerts its effects primarily through interactions with opioid receptors located in the
brain, spinal cord, and other parts of the body. It acts as a prodrug, which means it undergoes
metabolic conversion in the liver to its active form, morphine. Morphine is the compound
responsible for most of codeine's analgesic effects.
The primary pharmacological actions of codeine include:
1. Analgesia:Codeine and its active metabolite, morphine, bind to opioid receptors in the
brain, spinal cord, and peripheral tissues, leading to decreased perception of pain.
2. Cough Suppression:Codeine acts on the brainstem's cough center, reducing the urge to
cough. This property makes it useful in treating coughs, particularly in cases where the cough
is non-productive or irritating.[3]

[4]

Fig:-Codeine Molecular Structure

Pharmacokinetics:
Codeine is typically administered orally and is well-absorbed from the gastrointestinal tract.
Once absorbed, it undergoes metabolism in the liver, primarily by an enzyme called
CYP2D6. This enzyme converts codeine into morphine, its active metabolite. However, the
extent of this conversion can vary significantly among individuals due to genetic differences
in CYP2D6 activity. Some individuals are "ultra-rapid metabolizers" and may experience
higher levels of morphine and its effects.[5]

[6]

Fig:-Molecular Structure of Codeine

Clinical Uses:
Codeine is prescribed for various medical purposes, including:
1.Pain Relief: It is used to manage mild to moderate pain, such as after surgical procedures or
injury.
2.Cough Suppression: Codeine-containing cough syrups are used to suppress non-productive
coughs.

Risks and Side Effects:

Codeine use is associated with several risks:
1. Dependence and Addiction:Like other opioids, codeine has the potential for addiction and
dependence, particularly when used long-term or in higher doses.
2. Respiratory Depression: High doses of codeine or rapid conversion to morphine can lead to
slow and shallow breathing, which can be life-threatening.
3. Constipation: Opioids, including codeine, often cause constipation due to their effects on
the gastrointestinal tract.
4. Sedation and Drowsiness: Codeine can cause drowsiness and impair cognitive and motor
functions.[7]

[8]

Fig:-Codeine tablet

Conclusion:
Codeine is a valuable medication with analgesic and antitussive properties, often prescribed
for pain management and cough suppression. However, its use should be carefully monitored
due to the risk of dependence, addiction, and potential adverse effects. Clinicians should
consider individual variations in metabolism and weigh the benefits against the risks when
prescribing codeine-containing medications.[9]
 Reference

1-https://en.m.wikipedia.org/wiki/Codeine
2-https://paipharma.com/product/promethazine-vc-with-codeine-oral-solution/
3-Tripathi,K.D, Essentials of Medical Pharmacology,6th Edition
4-https://en.m.wikipedia.org/wiki/Codeine
5-Tripathi,K.D, Essentials of Medical Pharmacology,6th Edition
6-https://en.m.wikipedia.org/wiki/Codeine
7-Tripathi,K.D, Essentials of Medical Pharmacology,6th Edition
8-https://www.rehabguide.co.uk/codeine-addiction/
9-Tripathi,K.D, Essentials of Medical Pharmacology,6th Edition