Chlorpheniramine Stats & Data
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DrugBankDescription
A histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than promethazine.
Mechanism of Action
Chlorpheniramine binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine.
Pharmacodynamics
In allergic reactions an allergen interacts with and cross-links surface IgE antibodies on mast cells and basophils. Once the mast cell-antibody-antigen complex is formed, a complex series of events occurs that eventually leads to cell-degranulation and the release of histamine (and other chemical mediators) from the mast cell or basophil. Once released, histamine can react with local or widespread tissues through histamine receptors. Histamine, acting on H1-receptors, produces pruritis, vasodilatation, hypotension, flushing, headache, tachycardia, and bronchoconstriction. Histamine also increases vascular permeability and potentiates pain. Chlorpheniramine, is a histamine H1 antagonist (or more correctly, an inverse histamine agonist) of the alkylamine class. It competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract. It provides effective, temporary relief of sneezing, watery and itchy eyes, and runny nose due to hay fever and other upper respiratory allergies.
Metabolism
Primarily hepatic via Cytochrome P450 (CYP450) enzymes.
Absorption
Well absorbed in the gastrointestinal tract.
Toxicity
Oral LD50 (rat): 306 mg/kg; Oral LD50 (mice): 130 mg/kg; Oral LD50 (guinea pig): 198 mg/kg Registry of Toxic Effects of Chemical Substances. Ed. D. Sweet, US Dept. of Health & Human Services: Cincinatti, 2010. Also a mild reproductive toxin to women of childbearing age.
Indication
For the treatment of rhinitis, urticaria, allergy, common cold, asthma and hay fever.
Effect Profile
Curated + 6 ReportsModerate visuals with mild auditory effects and body load, low headspace
Tolerance & Pharmacokinetics
drugs.wikiExperience Report Analysis
ErowidDemographics
Gender Distribution
Age Distribution
Reports Over Time
Effect Analysis
ErowidEffects aggregated from 6 experience reports (6 Erowid)
Effect Sentiment Distribution
Confidence Distribution
Positive Effects 1
Adverse Effects 1
Real-World Dose Distribution
62K DosesFrom 45 individual dose entries
Oral (n=36)
Common Combinations
Most co-occurring substances in experience reports
Harm Reduction
drugs.wikiHarm-reduction points and cautions: 1) First-generation antihistamines have central anticholinergic effects; high doses can cause confusion, agitation, hallucinations, urinary retention, blurred vision, tachycardia, and potentially dangerous hyperthermia. Seek urgent care for severe agitation, delirium, hot/dry skin, or urinary retention. 2) Chlorpheniramine has a long elimination half-life (about 21–27 hours), so next-day drowsiness, slowed reaction time, and impaired coordination may persist beyond the 4–6 hour symptom-relief window; avoid driving or operating machinery if sedated. 3) Do not combine with dextromethorphan-containing ‘CCC/Triple C’ products: chlorpheniramine inhibits the serotonin transporter and is a CYP2D6 inhibitor/substrate; with DXM (a serotonergic CYP2D6 substrate), this raises the risk of serotonin syndrome and delirium. 4) Avoid co-use with MAOIs (or within 14 days of stopping one) due to severe interaction risk, especially if any serotonergic medicine (including DXM) is also present. 5) Additive CNS and respiratory depression occur with alcohol, opioids, benzodiazepines, and other sedatives; if accidental co-use occurs, keep doses low, avoid re-dosing, and ensure a sober monitor. 6) In hot environments or exertion (festivals, clubs), anticholinergic reduction of sweating increases overheating risk; hydrate, rest in shade, and stop use if feeling hot, confused, or unwell. 7) Older adults and those with glaucoma, prostatic hypertrophy/BPH, or a history of urinary retention are more sensitive to anticholinergic effects; consider non-sedating antihistamines instead and consult a clinician. 8) Overdose management is medical: there is no at-home antidote; in hospital, physostigmine may be considered for severe anticholinergic delirium by trained clinicians. 9) Product labels differ; many multi-symptom cold remedies already include chlorpheniramine—avoid double-dosing by checking ‘active ingredients’ on all concurrent OTCs. 10) Clinically significant hepatotoxicity is rare with chlorpheniramine-class drugs, but report unexplained jaundice, dark urine, or right-upper-quadrant pain if they occur after repeated dosing.
References
Drugs.wiki References
- DrugBank DB01114: mechanism/targets, half-life, product strengths, categories
- DrugBank DB01114 BioInteractions: CYP2D6 substrate/inhibitor flags
- NCBI StatPearls: Dextromethorphan risks (serotonin syndrome, MAOIs/SSRIs)
- TripSit DXM tool warning to avoid antihistamines in DXM products
- Erowid DXM basics/dosage: specific warning about Coricidin/CPM (CCC)
- NCBI StatPearls: Antihistamines (class adverse effects, anticholinergic toxicity; QTc caution)
- NCBI StatPearls: Diphenhydramine toxicity (anticholinergic delirium, hyperthermia)
- NCBI LiverTox: Brompheniramine/chlorpheniramine hepatotoxicity rare