Brompheniramine, dexbrompheniramine (monograph)

Brompheniramine, dexbrompheniramine (monograph)

Brompheniramine, dexbrompheniramine (monograph)

introduction

first generation antihistamines; Alkylamine (propylamine) derivatives.

Used for brompheniramine, dexbrompheniramine

Allergic rhinitis or other upper respiratory tract allergies

Only use fixed combination preparations if there are simultaneous symptoms that can be attributed to each ingredient.

A cold

Used in fixed combination with other active ingredients (e.g., phenylephrine, pseudoephedrine) for the temporary relief of rhinorrhea, sneezing, tearing, itchy 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 stomach irritation.

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

dosage

Brompheniramine: Available as brompheniramine maleate; Dosage expressed in salt.

Dexbrompheniramine: Available as dexprompheniramine maleate; Dosage expressed in salt. Dexbrompheniramine maleate is only available in fixed combination preparations.

Adjust dosage individually based on patient response and tolerance.

Individual dose titration is not possible with fixed combination preparations. When used in fixed combination with other active ingredients (e.g. dextromethorphan, guaifenesin, phenylephrine, pseudoephedrine), choose a dosage for each ingredient that is within the usual therapeutic range. Because combinations and dosage strengths vary for fixed combination preparations, consult the manufacturer's product labeling for the appropriate dosage of each preparation.

Pediatric patients

Allergic rhinitis, other upper respiratory allergies or cold

Brompheniramine maleate

Orally

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

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

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

Adult

Allergic rhinitis, other upper respiratory allergies or cold

Brompheniramine maleate

Orally

Self-medication: 4 mg every 4 hours.

Prescription Limits

Pediatric patients

Allergic rhinitis, other upper respiratory allergies or cold

Brompheniramine maleate

Orally

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

Children 6 to <12 years: Maximum 12 mg in 24 hours. If used for self-medication, therapy should be discontinued if symptoms last longer than 7 days or are accompanied by fever.

Children ≥12 years: Maximum of 24 mg in 24 hours. If used for self-medication, therapy should be discontinued if symptoms last longer than 7 days or are accompanied by fever.

Adult

Allergic rhinitis, other upper respiratory allergies or cold

Brompheniramine maleate

Orally

Maximum 24 mg in 24 hours. If used for self-medication, therapy should be discontinued if symptoms last longer than 7 days or are accompanied by fever.

Special populations

Geriatric patients

Patients ≥ 60 years: Select dosage with caution due to age-related deterioration in liver, kidney and/or cardiac function as well as concomitant medical conditions and drug therapy, starting at the lower end of the usual dosage range.

Cautions for brompheniramine, dexbrompheniramine

Contraindications

• Women who breastfeed.

• During or within 2 weeks of MAO inhibitor therapy.

• According to some manufacturers, it can cause angle-closure glaucoma, urinary retention, stomach ulcers and acute asthma attacks.

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

Warnings/Precautions

Warnings

Concomitant diseases

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

CNS effects

Risk of drowsiness. Concomitant use of other CNS depressants can cause additive CNS depressant effects. (See CNS depressants under “Interactions” and also information for patients.)

Possible excitability (especially in children). (See “Use in Children” under “Precautions.”)

General precautions

Anticholinergic effects

Possible anticholinergic effects (e.g. severe dryness of the 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 “Warnings.”)

Using fixed combinations

When used in fixed combination with other active ingredients (e.g. dextromethorphan, guaifenesin, phenylephrine, pseudoephedrine), the cautions, cautions and contraindications associated with the concomitant active ingredients should be observed.

Specific populations

pregnancy

Category C. Use in the third trimester is not recommended due to the risk of serious reactions (e.g., seizures) in newborns and premature infants.

lactation

It is not known whether brompheniramine is excreted in milk. Discontinue breast-feeding or taking the drug due to the risk to breast-fed infants. (See “Contraindications” under “Warnings.”)

Pediatric use

Possible paradoxical irritability or agitation (e.g., restlessness, insomnia, tremor, euphoria, nervousness, delirium, palpitations, seizures), particularly in children.

Brompheniramine maleate: Safety and efficacy of brompheniramine in fixed combination with pseudoephedrine and dextromethorphan in children less than 6 months of age have not been established. For self-medication, brompheniramine must not be used in a fixed combination with phenylephrine in children under 6 years of age.

Risk of overdose and toxicity (including death) in children younger than 2 years receiving over-the-counter preparations containing antihistamines, cough suppressants, expectorants, and nasal decongestants alone or in combination for relief of symptoms of an upper respiratory tract infection. Limited evidence for the effectiveness of these preparations in this age group; suitable dosages not established. Therefore, the FDA recommended that such preparations not be used in children younger than 2 years; Safety and effectiveness in older children in evaluation. Because children ages 2-3 are also at increased risk of overdose and toxicity, some manufacturers of oral, nonprescription cough and cold products have voluntarily agreed to revise product labeling to indicate that such products should not be used in children younger than 4 years. The FDA recommends that parents and caregivers follow the dosage instructions and warnings in the product labeling that accompanies the product and consult a doctor if they have any concerns. Physicians should ask caregivers about the use of non-prescription cough/cold medications to prevent overdose.

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. (See Geriatric Patients under Dosage and Administration.)

Common side effects

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

Interactions with other medications

Specific medications and laboratory tests

Brompheniramine, dexbrompheniramine pharmacokinetics

absorption

Bioavailability

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

Brompheniramine: Peak concentrations are generally reached within 2-5 hours after oral administration.

beginning

Brompheniramine: The antihistamine effect appears to be maximal within 3-9 hours. The antipruritic effect appears to be maximal within 9-24 hours.

Length of time

Brompheniramine: Suppression of the flare response may last for at least 48 hours.

distribution

extent

Brompheniramine: Distribution not fully characterized; seems to be widespread.

Elimination

metabolism

Brompheniramine: Metabolism and excretion behavior not fully understood. Undergoes N-dealkylation and other metabolic processes to produce multiple metabolites.

Elimination route

Brompheniramine: Excreted within 72 hours as unchanged active substance and metabolites in urine (approximately 40%) and feces (approximately 2%).

Half-life

Brompheniramine: 11.8-34.7 hours.

Dexbrompheniramine: Approximately 22 hours.

stability

storage

Orally

Brompheniramine maleate chewable tablets and oral solution

20-25°C.

Actions

• Blocks H1 receptor sites, preventing the effect of histamine on the effector cell.

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

• Suppresses bloating and itching associated with the endogenous release of histamine.

• Has an anticholinergic and calming effect.

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

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

Advice for patients

• risk of drowsiness or dizziness; Avoid driving, operating machinery, or performing other hazardous tasks if these adverse effects occur.

• Importance of avoiding alcoholic beverages during antihistamine therapy.

• It is important to inform physicians about existing or planned concomitant therapies, including prescription and over-the-counter medications, nutritional and herbal supplements, as well as any comorbidities. It is important that patients who are already receiving another CNS depressant (e.g. sedative, tranquilizer) do not self-medicate without first consulting a doctor.

• It is important for women to tell doctors if they are pregnant, plan to become pregnant, or want to breastfeed.

• It is important to inform patients of other important precautionary information. (See Precautions.)

Preparations

Excipients in commercial drug preparations may have clinically significant effects in some individuals; Details can be found on the respective product labeling.

For information about shortages of one or more of these drugs, visit the ASHP Drug Shortages Resource Center.

Brompheniramine maleate combinations

AHFS DI Essentials™. © Copyright 2024, Selected changes February 1, 2016. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

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