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Drugs, Supplies and Delivery

Chlorpheniramine Maleate

Chlorpheniramine Maleate remains a cornerstone for managing allergic conditions due to its potent H₁-blocking activity. However, its sedative and anticholinergic effects necessitate cautious use in vulnerable populations. Adherence to BNF guidelines, awareness of drug interactions, and patient education on side effects are crucial for safe therapy.

Chlorpheniramine Maleate is a first-generation antihistamine that competitively blocks histamine H₁ receptors, preventing histamine-mediated allergic responses. Its key actions include:

  1. Peripheral Effects: Inhibits histamine-induced vasodilation, bronchoconstriction, and mucous secretion.
  2. Central Nervous System (CNS) Effects: Crosses the blood-brain barrier, causing sedation by blocking H₁ receptors in the brain (Lippincott).
  3. Anticholinergic Activity: Blocks muscarinic receptors, leading to dry mouth, blurred vision, and urinary retention.

Chlorpheniramine is indicated for:

  1. Allergic Conditions:
    • Allergic rhinitis (hay fever).
    • Urticaria (hives) and pruritus (itching).
    • Conjunctivitis due to allergies.
  2. Adjunctive Therapy:
    • Anaphylaxis (combined with adrenaline and steroids).
  3. Symptomatic Relief:
    • Common cold (to reduce rhinorrhea and sneezing).

Adults:

  • Oral: 4 mg every 4–6 hours; maximum 24 mg/day (BNF).
  • Parenteral (Rare): 10–20 mg intramuscularly or intravenously under medical supervision.

Children:

  • 1–2 years: 1 mg twice daily.
  • 2–6 years: 1 mg every 4–6 hours (max 6 mg/day).
  • 6–12 years: 2 mg every 4–6 hours (max 12 mg/day).

Special Populations:

  • Renal/Hepatic Impairment: Use with caution; consider dose reduction.
  • Elderly: More susceptible to anticholinergic effects; lower doses advised.
  • Common: Drowsiness, dry mouth, blurred vision, dizziness, constipation.
  • Serious (Rare):
    • Hypotension, palpitations.
    • Urinary retention (risk in prostatic hypertrophy).
    • CNS depression (confusion, hallucinations).
    • Severe allergic reactions (e.g., rash, anaphylaxis).
  1. Contraindications:
    • Angle-closure glaucoma.
    • Severe urinary retention or pyloroduodenal obstruction.
    • Concurrent use of MAO inhibitors (BNF).
  2. Pregnancy/Lactation:
    • Category B: Use only if clearly needed; limited human data.
    • Excreted in breast milk; may cause sedation in infants.
  3. Activities Requiring Alertness: Avoid driving or operating machinery.
  • CNS Depressants: Alcohol, benzodiazepines, opioids—enhanced sedation.
  • MAO Inhibitors: Increased anticholinergic and CNS effects (avoid combination).
  • Anticholinergics: Atropine, tricyclic antidepressants—additive dry mouth/urinary retention.
  • Hypertensive Agents: May counteract efficacy of certain blood pressure medications.
  • Generic: Chlorpheniramine Maleate.
  • Brand Names:
    • UK: Piriton® (combination with other agents).
    • US: Chlor-Trimeton®, Aller-Chlor®.
    • Others: Avil® (India), Polaramine® (varies by region).

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