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    Home > Health Library > Encyclopedia

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    Chlorpheniramine

    Table of Contents > Drugs >

    Chlorpheniramine

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    Pronunciation

    U.S. Brand Names

    Synonyms

    Generic Available

    Canadian Brand Names

    Use

    Pregnancy Risk Factor

    Contraindications

    Warnings/Precautions

    Adverse ReactionsDrug Interactions

    Ethanol/Nutrition/HerbInteractions

    Stability

    Mechanism of Action

    Pharmacodynamics/Kinetics

    Dosage

    Administration

    Dietary Considerations

    Patient Education

    Nursing Implications

    Additional Information

    Dental Health: Effects on DentalTreatmentDental Health:Vasoconstrictor/Local Anesthetic

    PrecautionsMental Health: Effects on MentalStatusMental Health: Effects onPsychiatric Treatment

    Dosage Forms

    International Brand Names

    Pronunciation

    (klor fen IR a meen)

    U.S. Brand Names

    Aller-Chlor [OTC]; Chlorphen [OTC]; Chlor-Trimeton [OTC]; Diabetic Tussin Allergy Relief

    [OTC]; Teldrin HBP [OTC]

    Synonyms

    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    Chlorpheniramine Maleate; CTM

    Generic AvailableYes

    Canadian Brand Names

    Chlor-Tripolon; Novo-Pheniram

    Use

    Perennial and seasonal allergic rhinitis and other allergic symptoms including urticaria

    Pregnancy Risk Factor

    B

    Contraindications

    Hypersensitivity to chlorpheniramine maleate or any component of the formulation; narrow-angle

    glaucoma; bladder neck obstruction; symptomatic prostate hypertrophy; during acute asthmatic

    attacks; stenosing peptic ulcer; pyloroduodenal obstruction. Avoid use in premature and term

    newborns due to possible association with SIDS.

    Warnings/Precautions

    Causes sedation, caution must be used in performing tasks which require alertness (eg,

    operating machinery or driving). Sedative effects of CNS depressants or ethanol are potentiated.

    Use with caution in patients with angle-closure glaucoma, pyloroduodenal obstruction (including

    stenotic peptic ulcer), urinary tract obstruction (including bladder neck obstruction and

    symptomatic prostatic hyperplasia), hyperthyroidism, increased intraocular pressure, and

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    cardiovascular disease (including hypertension and tachycardia). High sedative and

    anticholinergic properties, therefore may not be considered the antihistamine of choice for

    prolonged use in the elderly. May cause paradoxical excitation in pediatric patients, and can

    result in hallucinations, coma, and death in overdose.

    Adverse Reactions

    >10%:

    Central nervous system: Slight to moderate drowsiness

    Respiratory: Thickening of bronchial secretions

    1% to 10%:

    Central nervous system: Headache, excitability, fatigue, nervousness, dizziness

    Gastrointestinal: Nausea, xerostomia, diarrhea, abdominal pain, appetite increase, weight gain

    Genitourinary: Urinary retention

    Neuromuscular & skeletal: Arthralgia, weakness

    Ocular: Diplopia

    Renal: Polyuria

    Respiratory: Pharyngitis

    Drug Interactions

    Substrate of CYP2D6 (minor), 3A4 (major); Inhibits CYP2D6 (weak)

    Increased toxicity (CNS depression): CNS depressants, MAO inhibitors, tricyclic antidepressants,

    phenothiazines

    CYP3A4 inhibitors: May increase the levels/effects of chlorpheniramine. Example inhibitors

    include azole antifungals, ciprofloxacin, clarithromycin, diclofenac, doxycycline, erythromycin,

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    imatinib, isoniazid, nefazodone, nicardipine, propofol, protease inhibitors, quinidine, and

    verapamil.

    Ethanol/Nutrition/Herb Interactions

    Ethanol: Avoid ethanol (may increase CNS depression).

    Stability

    Protect from light

    Mechanism of Action

    Competes with histamine for H1-receptor sites on effector cells in the gastrointestinal tract, blood

    vessels, and respiratory tract

    Pharmacodynamics/Kinetics

    Half-life elimination, serum: 20-24 hours

    Dosage

    Children: Oral: 0.35 mg/kg/day in divided doses every 4-6 hours

    2-6 years: 1 mg every 4-6 hours, not to exceed 6 mg in 24 hours

    6-12 years: 2 mg every 4-6 hours, not to exceed 12 mg/day or sustained release 8 mg at bedtime

    Children >12 years and Adults: Oral: 4 mg every 4-6 hours, not to exceed 24 mg/day or sustained

    release 8-12 mg every 8-12 hours, not to exceed 24 mg/day

    Elderly: Oral: 4 mg once or twice daily. Note: Duration of action may be 36 hours or more when

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    serum concentrations are low.

    Hemodialysis: Supplemental dose is not necessary

    Administration

    Timed release oral forms are to be swallowed whole, not crushed or chewed.

    Dietary Considerations

    May be taken with food or water.

    Patient Education

    May cause drowsiness; swallow whole, do not crush or chew sustained release product; avoid

    alcohol, may impair coordination and judgment

    Nursing Implications

    Raise bed rails, institute safety measures, assist with ambulation.

    Additional Information

    Not effective for nasal stuffiness.

    Dental Health: Effects on Dental Treatment

    Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon

    discontinuation). Chronic use of antihistamines will inhibit salivary flow, particularly in elderly

    patients; this may contribute to periodontal disease and oral discomfort.

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