Brompheniramine, Dexbrompheniramine (Monograph)

Drug class: First Generation Antihistamines

Introduction

First generation antihistamines; alkylamine (propylamine) derivatives.

Uses for Brompheniramine, Dexbrompheniramine

Allergic Rhinitis or Other Upper Respiratory Allergies

Used in fixed combination with other agents (e.g., dextromethorphan, guaifenesin, phenylephrine, pseudoephedrine) for relief of rhinorrhea, sneezing, lacrimation, itching eyes, oronasopharyngeal itching, and/or other symptoms (e.g., nasal/sinus congestion, cough) associated with allergic rhinitis (e.g., hay fever) or other upper respiratory allergies.

Use fixed-combination preparations only when symptoms amenable to each ingredient are present concurrently.

Common Cold

Used in fixed combination with other agents (e.g., phenylephrine, pseudoephedrine) for temporary relief of rhinorrhea, sneezing, lacrimation, itching eyes, oronasopharyngeal itching, and/or other symptoms associated with the common cold (e.g., nasal congestion).

Brompheniramine, Dexbrompheniramine Dosage and Administration

Administration

Oral Administration

Administer orally with food, water, or milk to minimize gastric irritation.

Brompheniramine maleate oral solution: Use only the measuring device (e.g., calibrated dropper, cup, spoon) provided by the manufacturer.

Dosage

Brompheniramine: Available as brompheniramine maleate; dosage expressed in terms of the salt.

Dexbrompheniramine: Available as dexprompheniramine maleate; dosage expressed in terms of the salt. Dexbrompheniramine maleate available only in fixed-combination preparations.

Individualize dosage according to patient’s response and tolerance.

Fixed-combination preparations do not permit individual titration of dosages. When used in fixed combination with other agents (e.g., dextromethorphan, guaifenesin, phenylephrine, pseudoephedrine), select a dosage that is within the usual therapeutic range for each ingredient. Because combinations and dosage strengths vary for fixed-combination preparations, consult manufacturer’s product labeling for appropriate dosage of the specific preparation.

Pediatric Patients

Allergic Rhinitis, Other Upper Respiratory Allergies, or the Common Cold

Brompheniramine Maleate

Oral

Children 2 to <6 years of age: 1 mg every 4 hours.

Self-medication in children 6 to <12 years of age: 2 mg every 4 hours.

Self-medication in children ≥12 years of age: 4 mg every 4 hours.

Adults

Allergic Rhinitis, Other Upper Respiratory Allergies, or the Common Cold

Brompheniramine Maleate

Oral

Self-medication: 4 mg every 4 hours.

Prescribing Limits

Pediatric Patients

Allergic Rhinitis, Other Upper Respiratory Allergies, or the Common Cold

Brompheniramine Maleate

Oral

Children 2 to <6 years of age: Maximum 6 mg in 24 hours.

Children 6 to <12 years of age: Maximum 12 mg in 24 hours. When used for self-medication, discontinue therapy if symptoms persist for >7 days or are accompanied by fever.

Children ≥12 years of age: Maximum 24 mg in 24 hours. When used for self-medication, discontinue therapy if symptoms persist for >7 days or are accompanied by fever.

Adults

Allergic Rhinitis, Other Upper Respiratory Allergies, or the Common Cold

Brompheniramine Maleate

Oral

Maximum 24 mg in 24 hours. When used for self-medication, discontinue therapy if symptoms persist for >7 days or are accompanied by fever.

Special Populations

Geriatric Patients

Patients ≥60 years of age: Select dosage with caution, starting at the lower end of the usual dosage range, because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.

Cautions for Brompheniramine, Dexbrompheniramine

Contraindications

• Women who are breast-feeding.

• During or within 2 weeks of MAO-inhibitor therapy.

• Angle-closure glaucoma, urinary retention, peptic ulcer disease, and acute asthmatic attack, according to some manufacturers.

• Known hypersensitivity to brompheniramine, other antihistamines, or any ingredient in the formulation.

Warnings/Precautions

Warnings

Concomitant Diseases

Use with caution in patients with increased IOP, bronchial asthma, hyperthyroidism, diabetes mellitus, cardiovascular disease (e.g., hypertension, ischemic heart disease), or prostatic hypertrophy.

CNS Effects

Risk of drowsiness. Concurrent use of other CNS depressants may have additive CNS depressant effects. (See CNS Depressants under Interactions and also see Advice to Patients.)

Possible excitability (especially in children). (See Pediatric Use under Cautions.)

General Precautions

Anticholinergic Effects

Possible anticholinergic effects (e.g., severe dryness of mouth, nose, and throat; dysuria; urinary retention). Use with caution, if at all, in patients with prostatic hypertrophy, pyloroduodenal obstruction, or bladder neck obstruction. (See Contraindications under Cautions.)

Use of Fixed Combinations

When used in fixed combination with other agents (e.g., dextromethorphan, guaifenesin, phenylephrine, pseudoephedrine), consider the cautions, precautions, and contraindications associated with the concomitant agent(s).

Specific Populations

Pregnancy

Category C. Use not recommended during the third trimester because of risk of severe reactions (e.g., seizures) in neonates and premature infants.

Lactation

Not known if brompheniramine is distributed into milk. Discontinue nursing or the drug because of potential risk to nursing infants. (See Contraindications under Cautions.)

Pediatric Use

Possible paradoxical irritability or excitement (e.g., restlessness, insomnia, tremors, euphoria, nervousness, delirium, palpitation, seizures), especially in children.

Brompheniramine maleate: Safety and efficacy of brompheniramine in fixed combination with pseudoephedrine and dextromethorphan not established in children <6 months of age. For self-medication, do not use brompheniramine in fixed combination with phenylephrine in children <6 years of age.

Risk of overdosage and toxicity (including death) in children <2 years of age receiving OTC preparations containing antihistamines, cough suppressants, expectorants, and nasal decongestants alone or in combination for relief of symptoms of upper respiratory tract infection. Limited evidence of efficacy for these preparations in this age group; appropriate dosages not established. Therefore, FDA recommended not to use such preparations in children <2 years of age; safety and efficacy in older children under evaluation. Because children 2–3 years of age also are at increased risk of overdosage and toxicity, some manufacturers of oral nonprescription cough and cold preparations agreed to voluntarily revise the product labeling to state that such preparations should not be used in children <4 years of age. FDA recommends that parents and caregivers adhere to dosage instructions and warnings on the product labeling that accompanies the preparation and consult a clinician about any concerns. Clinicians should ask caregivers about use of nonprescription cough/cold preparations to avoid overdosage.

Geriatric Use

Possible increased risk of confusion, dizziness, sedation, hypotension, hyperexcitability, and anticholinergic effects (e.g., dry mouth, urinary retention [particularly in men]) in patients ≥60 years of age. (See Geriatric Patients under Dosage and Administration.)

Common Adverse Effects

Sedation (e.g., drowsiness, dizziness), CNS stimulation (e.g., restlessness, insomnia, anxiety, tension, nervousness), vertigo, weakness, confusion, blurred vision, nausea, dry mouth, cardiac palpitations, flushing, increased thickening of bronchial secretions.

Drug Interactions

Specific Drugs and Laboratory Tests

Brompheniramine, Dexbrompheniramine Pharmacokinetics

Absorption

Bioavailability

Brompheniramine and dexbrompheniramine appear to be well absorbed from the GI tract.

Brompheniramine: Peak concentrations generally occur within 2–5 hours following oral administration.

Onset

Brompheniramine: Antihistamine effect appears to be maximal within 3–9 hours. Antipruritic effect appears to be maximal within 9–24 hours.

Duration

Brompheniramine: Suppression of the flare response may persist for up to at least 48 hours.

Distribution

Extent

Brompheniramine: Distribution not fully characterized; appears to be widely distributed.

Elimination

Metabolism

Brompheniramine: Metabolic and excretory fate not fully characterized. Undergoes N-dealkylation and other metabolic processes to several metabolites.

Elimination Route

Brompheniramine: Excreted in urine (about 40%) and feces (about 2%) as unchanged drug and metabolites within 72 hours.

Half-life

Brompheniramine: 11.8–34.7 hours.

Dexbrompheniramine: Approximately 22 hours.

Stability

Storage

Oral

Brompheniramine Maleate Chewable Tablets and Oral Solution

20–25°C.

Actions

• Blocks H₁-receptor sites, thereby preventing the action of histamine on the effector cell.

• Antagonizes the allergic response (vasodilation, increased vascular permeability, increased mucus secretion) of nasal tissue.

• Suppresses flare and pruritus that accompany the endogenous release of histamine.

• Has anticholinergic and sedative effects.

• Causes less drowsiness than some other first-generation antihistamines.

• Antihistamines do not block the stimulating effect of histamine on gastric acid secretion, which is mediated by H₂-receptors of the parietal cells.

Advice to Patients

• Risk of drowsiness or dizziness; avoid driving, operating machinery, or engaging in other hazardous tasks if these adverse effects occur.

• Importance of avoiding alcoholic beverages during antihistamine therapy.

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant illnesses. Importance of patients already receiving another CNS depressant (e.g., sedative, tranquilizer) not undertaking self-medication without first consulting a clinician.

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

• Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

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