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Pronunciation
(brome fen IR a meen)
Generic Available (U.S.)
Yes: Chewable tablet, timed release tablet
Index Terms
Brand Names: U.S.
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Symptomatic relief of perennial and seasonal allergic rhinitis, vasomotor rhinitis, and other respiratory allergies
Pregnancy Risk Factor
C
Pregnancy Considerations
There are no adequate and well-controlled studies in pregnant women. Use in pregnancy only when clearly needed. May cause severe reactions (convulsions) in newborns and premature infants; avoid use in 3rd trimester.
Lactation
Excretion in breast milk unknown/not recommended
Breast-Feeding Considerations
Some antihistamines are excreted in breast milk. Premature infants and newborns have a higher risk of intolerance to antihistamines. Use while breast-feeding is contraindicated by the manufacturer.
Contraindications
Hypersensitivity to brompheniramine or any component of the formulation; use with or within 14 days of MAO inhibitor therapy; narrow-angle glaucoma; urinary retention; peptic ulcer disease; during acute asthmatic attacks; breast-feeding; newborn or premature infants
Warnings/Precautions
Concerns related to adverse effects:
• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
Disease-related concerns:
• Asthma: Use with caution in patients with a history of asthma.
• Cardiovascular disease: Use with caution in patients with cardiovascular disease (including hypertension and ischemic heart disease).
• Increased intraocular pressure: Use with caution in patients with increased intraocular pressure.
• Prostatic hyperplasia/urinary obstruction: Use with caution in patients with prostatic hyperplasia and/or GU obstruction.
• Thyroid dysfunction: Use with caution in patients with thyroid dysfunction.
Concurrent drug therapy issues:
• Sedatives: Effects may be potentiated when used with other sedative drugs or ethanol.
Special populations:
• Elderly: Use with caution in the elderly; may be more sensitive to adverse effects.
• Pediatrics: Antihistamines may cause excitation in young children.
Dosage form specific issues:
• Tartrazine: Some products may contain tartrazine.
Adverse Reactions
Frequency not defined.
Cardiovascular: Angina, blood pressure increased, chest tightness, circulatory collapse, extrasystoles, hypotension, palpitation, tachycardia
Central nervous system: Anxiety, chills, confusion, coordination impaired, dizziness, drowsiness, euphoria, excitation, fatigue, headache, hysteria, insomnia, irritability, nervousness, neuritis, restlessness, sedation, seizure, stimulation, tension, vertigo
Dermatologic: Photosensitivity, rash, urticaria
Endocrine & metabolic: Early menses
Gastrointestinal: Abdominal cramps, anorexia, constipation, diarrhea, dry throat, epigastric distress, heartburn, nausea, vomiting, xerostomia
Genitourinary: Dysuria, polyuria, urinary retention
Hematologic: Agranulocytosis, hemolytic anemia, hypoplastic anemia, thrombocytopenia
Neuromuscular & skeletal: Paresthesia, tremor, weakness
Ocular: Blurred vision, diplopia, mydriasis
Otic: Labyrinthitis (acute), tinnitus
Respiratory: Dry nose, nasal congestion, thickening of bronchial secretions, wheezing
Miscellaneous: Anaphylactic shock, diaphoresis
Metabolism/Transport Effects
None known.
Drug Interactions
Acetylcholinesterase Inhibitors (Central): Anticholinergics may diminish the therapeutic effect of Acetylcholinesterase Inhibitors (Central). Acetylcholinesterase Inhibitors (Central) may diminish the therapeutic effect of Anticholinergics. If the anticholinergic action is a side effect of the agent, the result may be beneficial. Risk C: Monitor therapy
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
Amphetamines: May diminish the sedative effect of Antihistamines. Risk C: Monitor therapy
Anticholinergics: May enhance the adverse/toxic effect of other Anticholinergics. Exceptions: Levocabastine (Nasal); Paliperidone. Risk C: Monitor therapy
Benzylpenicilloyl Polylysine: Antihistamines may diminish the diagnostic effect of Benzylpenicilloyl Polylysine. Management: Suspend systemic H1 antagonists for benzylpenicilloyl-polylysine skin testing and delay testing until systemic antihistaminic effects have dissipated. A histamine skin test may be used to assess persistent antihistaminic effects. Risk D: Consider therapy modification
Betahistine: Antihistamines may diminish the therapeutic effect of Betahistine. Risk C: Monitor therapy
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Exceptions: Levocabastine (Nasal). Risk C: Monitor therapy
Droperidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (e.g., opioids, barbiturates) with concomitant use. Risk D: Consider therapy modification
HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. Risk D: Consider therapy modification
Pramlintide: May enhance the anticholinergic effect of Anticholinergics. These effects are specific to the GI tract. Risk D: Consider therapy modification
Selective Serotonin Reuptake Inhibitors: CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Ethanol: May increase CNS depression; monitor for increased effects with coadministration. Caution patients about effect.
Storage
Store between 15°C to 30°C (59˚F to 86°F). Protect from light.
Mechanism of Action
Competes with histamine for H1-receptor sites on effector cells
Pharmacodynamics/Kinetics
Distribution: Vd: Children: ~20 L/kg (Simons, 1999); Adults: ~12 L/kg (Simons, 1982)
Protein binding: 39% to 49% (Martínez-Gómez, 2007)
Metabolism: Hepatic (Simons, 2004)
Half-life, elimination: Children: ~12 hours (Simons, 1999); Adults: ~25 hours (Simons, 1982)
Time to peak, serum: Children: 3-3.5 hours (Simons, 1999); Adults: 2-4 hours (Simons, 1982)
Excretion: Urine (Bruce, 1968)
Dosage
Oral: Allergic rhinitis, allergic symptoms, vasomotor rhinitis:
Children 6-12 years (LoHist-12): One tablet every 12 hours (maximum: 2 tablets/day)
Children >12 years (Bromax, LoHist-12): Refer to adult dosing
Adults:
Bromax: One tablet twice daily
LoHist-12: 1-2 tablets every 12 hours (maximum: 4 tablets/day)
Administration: Oral
Extended release tablets are to be swallowed whole; do not crush or chew.
Test Interactions
May interfere with urine detection of amphetamine/methamphetamine (false-positive). May interfere with skin tests using allergen extracts.
Dietary Considerations
May be taken with food, water, or milk.
Patient Education
Follow dosing guidelines closely; measure dosage carefully, especially in pediatric patients. Avoid alcohol. You may experience drowsiness or dizziness. Report persistent sedation, confusion, agitation, blurred vision, or respiratory difficulty.
Geriatric Considerations
Anticholinergic action may cause significant confusional symptoms, constipation, or problems voiding urine. If an antihistamine is indicated, a second generation nonsedating antihistamine would be a more appropriate choice.
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.
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
May cause agitation, confusion, dizziness, drowsiness, or fatigue. May cause paradoxical excitation in pediatric patients; may cause hallucinations in overdose.
Mental Health: Effects on Psychiatric Treatment
Concurrent use with psychotropics may produce additive anticholinergic and/or sedative effects; monitor
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Tablet, chewable, oral, as tannate: 12 mg [DSC]
Tablet, extended release, oral, as maleate:
Bromax: 11 mg [DSC] [dye free]
LoHist-12: 6 mg [DSC] [scored; dye free]
Tablet, timed release, oral, as maleate: 6 mg [DSC]
References
Bruce RB, Turnbull LB, Newman JH, et al, "Metabolism of Brompheniramine," J Med Chem, 1968, 11(5):1031-4.
Martínez-Gómez MA, Villanueva-Camañas RM, Sagrado S, et al, "Evaluation of Enantioselective Binding of Antihistamines to Human Serum Albumin by ACE," Electrophoresis, 2007, 28(15):2635-43.
Olsen KM, Gulliksen M, and Christophersen AS, “Metabolites of Chlorpromazine and Brompheniramine May Cause False-Positive Urine Amphetamine Results with Monoclonal EMIT D.A.U. Immunoassay,” Clin Chem, 1992, 38(4):611-2.
Simons FE, "Advances in H1-Antihistamines," N Engl J Med, 2004, 351(21):2203-17.
Simons FE, Frith EM, and Simons KJ, "The Pharmacokinetics and Antihistaminic Effects of Brompheniramine," J Allergy Clin Immunol, 1982, 70(6):458-64.
Simons FE, Roberts JR, Gu X, et al, "The Clinical Pharmacology of Brompheniramine in Children," J Allergy Clin Immunol, 1999, 103(2 Pt 1):223-6.
International Brand Names
Lexi-Comp.com
Last full review/revision February 2012
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