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As a widely employed medication, codeine is recognized for its antitussive characteristics, making it especially effective in alleviating cough symptoms. It is an opioid, albeit a milder one, and works by suppressing the cough reflex in the brain. Doctors prescribe it for the treatment of acute and chronic cough, particularly when caused by respiratory tract infections.
Classification
- Drug Class: Opioid analgesic, Antitussive
- ATC Code: R05DA04 (Antitussive drugs, opioids)
- Formulations Available: Oral tablets, syrups, and liquid solutions.
Mechanism of Action of Codeine
Codeine exerts its effects by interacting with opioid receptors located in the central nervous system. These receptors, primarily located in the brainstem, are responsible for controlling the cough reflex. It alleviates the frequency and severity of coughing by engaging with these receptors.
Pharmacokinetics of Codeine
- Absorption: The gastrointestinal tract facilitates the effective absorption of it.
- Distribution:The distribution in body is broad, including penetration into the central nervous system.
- Metabolism: The liver metabolizes codeine primarily to morphine, which contributes to its analgesic effects, through the action of the enzyme CYP2D6.
- Half-life: 3–4 hours.
- Excretion: The body mainly excretes the drug in urine, with a small amount remaining unchanged.
Therapeutic Indications
Codeine is indicated for:
- Cough suppression: Primarily used in dry, non-productive coughs that irritate the throat.
- Pain management: Although more commonly used for cough, It is also prescribed for mild to moderate pain, typically in combination with other analgesics like acetaminophen.
Dosage and Administration
The dosage of Codeine depends on the form and indication:
- For Adults:
- Cough: 10-20 mg every 4-6 hours, up to a maximum of 120 mg per day.
- Pain: 15-60 mg every 4-6 hours as required.
- For Children (6-12 years):
- Cough: 5-10 mg every 4-6 hours, not more than 60 mg daily.
- For Children under 6 years: Codeine is generally contraindicated due to the risk of respiratory depression.
Side Effects of Codeine
Common side effects include:
- Drowsiness
- Constipation
- Nausea and vomiting
- Dizziness
- Respiratory depression (especially in high doses)
Serious adverse effects include allergic reactions (rash, itching), bradycardia, and hypotension. Use it with caution in individuals with a history of respiratory disorders or opioid dependence.
Precautions
- Pregnancy and Breastfeeding: It should be avoided during pregnancy, especially in the first trimester. It may be passed to the infant through breast milk and can cause respiratory depression.
- Renal and Hepatic Impairment: Dose adjustments may be necessary for patients with liver or kidney dysfunction.
- Drug Interactions: Caution is required when using Codeine with other CNS depressants, such as benzodiazepines, alcohol, or other opioids.
Contraindications
- Hypersensitivity to opioids
- Severe respiratory depression
- Acute bronchial asthma or other respiratory conditions where patient has compromised breathing
- Children under 12 years (due to respiratory risks).
Codeine in Combination Products
Codeine is often combined with other drugs, such as acetaminophen, for enhanced effects in pain management. Some popular combination products include:
- Codeine + Acetaminophen
- Codeine + Promethazine
- Codeine + Guaifenesin
Popular Brands of Codeine
Here is a table listing some well-known brands of Codeine manufactured by multinational pharmaceutical companies, along with their specifications.
| Brand Name | Manufacturer | Active Ingredients | Dosage Form | Strength (per unit) | Indications |
| Tussinex | Pfizer | Codeine Phosphate | Syrup | 10 mg/5 ml | Cough, Cold |
| Robitussin AC | Pfizer | Codeine Phosphate, Guaifenesin | Syrup | 10 mg/5 ml, 100 mg/5 ml | Cough, Chest Congestion |
| Paveral | Sanofi | Codeine Phosphate | Tablet | 30 mg | Cough, Pain Relief |
| Phenergan with Codeine | GlaxoSmithKline | Promethazine Hydrochloride, Codeine | Syrup | 6.25 mg/5 ml, 10 mg/5 ml | Cough, Allergies |
| Codral | Johnson & Johnson | Codeine Phosphate, Pseudoephedrine | Tablet | 15 mg, 30 mg | Cough, Nasal Congestion |
Codeine Abuse and Dependence
As an opioid, Codeine carries a risk for abuse and dependence. Regular use, especially at higher doses or in individuals with a history of substance abuse, may lead to tolerance and addiction. Codeine abuse can result in euphoria, which may encourage misuse.
Conclusion
Codeine is a valuable antitussive drug with a well-established role in treating cough and mild pain. It is available in various formulations and can be located in numerous over the counter and prescription combination products. However, due to its opioid nature, it must be used with caution, particularly in children and those with respiratory or substance abuse concerns.
Key Takeaways:
- Codeine is useful for alleviating dry coughs and managing mild pain.
- Its mechanism of action involves the suppression of the cough reflex within the brain.
- This medication is available in multiple formulations, such as syrup and tablets.
- Side effects like drowsiness and constipation are common.
- There is a risk of dependency and abuse, necessitating careful use.
Thus, by understanding its mechanism, dosages, and potential risks, healthcare providers can ensure that Codeine is used appropriately and effectively.
