chlorcyclizine/codeine

Action and Spectrum

Actions and Spectrum: 

• chlorcyclizine binds to and blocks H1 histamine receptors on cells in various tissues, including the respiratory tract, blood vessels, and skin. Doing so prevents histamine from binding to these receptors and causing the typical allergic response. This leads to a reduction in the symptoms of allergy, such as itching, inflammation, and nasal congestion. 
• chlorcyclizine primarily targets histamine receptors and is effective against symptoms caused by histamine release, such as allergies. It is not effective against other types of pain or inflammation. 
• codeine works by binding to opioid receptors in the brain and spinal cord. These receptors are part of the body’s pain control system. When codeine binds to these receptors, it reduces the transmission of pain signals and modifies how the brain perceives pain. codeine is mainly used for pain relief and cough suppression. It is not effective against allergic reactions or other allergy-related symptoms like chlorcyclizine. Due to its opioid properties, codeine has a broader spectrum of activity than chlorcyclizine, but it has a higher risk of side effects and potential for misuse. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Respiratory depression 

Vomiting 

Dizziness 

Nausea 

Hypotension 

Urinary retention 

Blurred vision 

Black Box Warning

Black box warning: 

None 

Contraindication / Caution

Contraindications/caution: 

• Hypersensitivity or Allergy: Individuals allergic to chlorcyclizine, codeine, or other medication components should not take products containing these substances. 
• Respiratory Depression: codeine is an opioid, and like other opioids, it can cause respiratory depression (slowed breathing) in high doses or individuals sensitive to its effects. Individuals with severe respiratory disorders or conditions that affect breathing should avoid using medications containing codeine. 
• Asthma and Other Respiratory Conditions: codeine can cause bronchial constriction in some individuals, particularly those with asthma. Therefore, caution should be exercised when using codeine-containing medications in individuals with a history of asthma or other respiratory conditions. 
• Central Nervous System Depression: The combination of chlorcyclizine and codeine can have additive soothing effects on the central nervous system. Individuals taking other medications that depress the central nervous system, such as sedatives, tranquilizers, or alcohol, should use these medications with caution. 
• Monoamine Oxidase Inhibitors (MAOIs): The combination of chlorcyclizine and codeine should be avoided in individuals taking monoamine oxidase inhibitors (MAOIs) or those taking MAOIs within the past 14 days. MAOIs can interact with codeine, leading to serious side effects, including serotonin syndrome. 

Pregnancy / Lactation

Pregnancy consideration: Insufficient data available 

Lactation: Excretion of the drug(codeine) in human breast milk is known. 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

The combination of chlorcyclizine and codeine provides a dual approach to symptom relief: 

• Allergy Relief: chlorcyclizine’s antihistamine action helps alleviate allergic symptoms by blocking histamine receptors. This can help reduce itching, sneezing, nasal congestion, and other allergy-related symptoms. 
• Cough Suppression and Pain Relief: codeine, as an opioid, acts on mu-opioid receptors to suppress the cough reflex and provide mild analgesia. It can help alleviate coughing and relieve pain, such as sore throat associated with a persistent cough. 

Pharmacokinetics: 

Absorption 

It is well absorbed from the gastrointestinal tract after oral administration. 

Distribution 

Both chlorcyclizine and codeine are distributed throughout the body via the bloodstream. They can cross the blood-brain and other biological barriers, allowing them to exert their effects on various tissues and organs. 

Metabolism 

chlorcyclizine undergoes metabolism in the liver, primarily through oxidation and conjugation reactions. The metabolites are then excreted in the urine and feces. 

codeine is metabolized in the liver primarily by the enzyme CYP2D6. It is converted to its active metabolite, morphine, contributing to its analgesic effects. The metabolism of codeine can vary widely among individuals due to genetic differences in CYP2D6 activity. Some individuals are “poor metabolizers” and may experience reduced analgesic effects from codeine. 

Elimination and Excretion 

Metabolized chlorcyclizine and its metabolites are excreted primarily in the urine and, to a lesser extent, in the feces. 

After the metabolism of codeine to morphine, the active metabolite is excreted primarily in the urine. Unmetabolized codeine is also excreted in the urine. 

Adminstartion

Administration: 

Oral administration 

Syrup 

• Shake the syrup well before use to ensure proper mixing of the ingredients. 
• Use the measuring device provided with the medication to measure the prescribed dose accurately. 
• Syrup is usually taken orally, with or without food, as directed. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: chlorcyclizine/codeine 

Why do we use chlorcyclizine/codeine? 

The combined medication containing chlorcyclizine and codeine is used primarily to relieve allergic symptoms and cough. It takes advantage of the antihistamine properties of chlorcyclizine to alleviate allergy symptoms, while codeine acts as a cough suppressant and mild analgesic.  

• Allergic Rhinitis and Allergy Symptoms: As an antihistamine, chlorcyclizine helps alleviate symptoms associated with allergic rhinitis (hay fever) and other allergic reactions. These symptoms include sneezing, itching, runny nose, and watery eyes. 
• Cough Suppression: codeine is an opioid antitussive, meaning it helps suppress coughing. This is particularly useful in persistent, non-productive coughs, such as those associated with colds, upper respiratory infections, or irritation due to allergens. 
• Mild Pain Relief: codeine, as an opioid, provides mild analgesic effects and can offer some relief from pain associated with conditions such as sore throat, muscle aches, or headaches. 
• Symptomatic Relief: The combined medication provides symptomatic relief by addressing both allergic symptoms and coughing, helping to improve the overall quality of life during periods of discomfort.