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RESPIRATORY SYSTEM › ANTIHISTAMINES FOR SYSTEMIC USE › ANTIHISTAMINES FOR SYSTEMIC USE › Substituted ethylene diamines
chloropyramine
R06AC03
Forms & Strengths
- Tablets 2 mg
- Tablets 4 mg
- Syrup 0.5 mg/mL
- Injectable solution 10 mg/mL
Adult Dosing
- Allergic rhinitis/urticaria: 4 mg PO 2‑3 times daily (max 12 mg/day)
- Severe pruritus: 6‑8 mg PO 3 times daily (max 24 mg/day)
- Acute anaphylaxis adjunct: 10 mg IV/IM single dose, repeat after 30 min if needed
Pediatric Dosing
- >1 yr: 0.5 mg/kg PO 2‑3 times daily (max 6 mg/day)
- 6‑12 yr: 1‑2 mg PO 2‑3 times daily
- <1 yr: not recommended
Indications
- Seasonal and perennial allergic rhinitis
- Acute and chronic urticaria
- Allergic conjunctivitis
- Pruritic dermatoses (e.g., insect bites)
- Mild‑moderate anaphylactic reactions (adjunct therapy)
- Angioedema
Mechanism of Action
- Competitive reversible H1‑receptor antagonist
- Blocks peripheral and central histamine actions
- Exhibits anticholinergic and sedative activity due to CNS penetration
Contraindications
- Hypersensitivity to chloropyramine or other first‑generation antihistamines
- Narrow‑angle glaucoma
- Severe hepatic or renal impairment
- Neonates and infants <6 months
- Pregnancy category C – avoid unless benefit outweighs risk
Adverse Reactions
- Sedation and somnolence
- Dry mouth (xerostomia)
- Constipation or gastrointestinal upset
- Urinary retention, especially in men with BPH
- Blurred vision, mydriasis
- Tachycardia or palpitations
- Hypotension
- Skin rash or photosensitivity
- Rare extrapyramidal symptoms
Drug Interactions
- Additive CNS depression with alcohol, opioids, benzodiazepines, barbiturates, other antihistamines
- Increased anticholinergic effects with anticholinergic drugs (e.g., tricyclic antidepressants, atropine)
- Cimetidine may raise chloropyramine plasma levels
- MAO inhibitors may potentiate anticholinergic and sedative effects
- Concurrent QT‑prolonging agents – monitor cardiac rhythm
- Avoid simultaneous use with other H1 antagonists to prevent overdose
Curated Content: Needs Vetting Before Put to Clinical Use