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Chlorpheniramine

CHLOR-TRIMETON

Pronunciation: klor-fen-IR-a-meen

Chlorpheniramine ballicule: receptor binding, kinetics and half-life diagram
Mechanism of action: Chlorpheniramine ballicule

What it isFirst-generation H1 antagonist; allergic rhinitis and cold remedies.

Why this oneIt is less sedating than diphenhydramine but remains common in multi-ingredient cold products.

What limits itAnticholinergic burden and sedation make it poor for older adults and unsafe before driving.

Chlorpheniramine molecular structure (skeletal formula)
Molecular structure: Chlorpheniramine

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
Temporary relief of hay fever/upper respiratory allergy symptoms (sneezing, runny nose, itchy watery eyes, itchy nose/throat)Adults & children ≥12 y1 tablet (4 mg) q4–6h PRN1 tablet (4 mg) q4–6h PRN6 tablets (24 mg)/24 h
Temporary relief of hay fever/upper respiratory allergy symptomsChildren 6 to <12 y1/2 tablet (2 mg) q4–6h PRN (break tablet in half)1/2 tablet (2 mg) q4–6h PRN3 whole tablets (12 mg)/24 h

Renal Undefined

Hepatic Undefined

Dose no more often than every 4 to 6 hours; do not exceed the stated 24-hour tablet limit.

Instructions

Available strengths

Contraindications

Cautions

Adverse reactions

Pregnancy If pregnant, ask a health professional before use (OTC drug-facts statement).

Lactation If breast-feeding, ask a health professional before use (OTC drug-facts statement).

Cost

Chlorpheniramine (CHLOR-TRIMETON)
Strength#/mogeneric $/unitCostPlus
12 mgER tabper unitnot offered
NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Chlorpheniramine is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

NO BOXED WARNINGS

Principal riskAnticholinergic burden and sedation, so it is poor in the elderly

Classes and tags

Clinical profile

Therapeutic safety burden1 / 4
Sedation liability2 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism1 / 4
Embryofetal risk1 / 4

Serotonin and MAOI

Provisional washout figures

SRI significance2 / 4
Serotonin release0 / 4

Evidence confidenceModerate

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