Carbinoxamine (Monograph)

Brand names: Arbinoxa, Palgic
Drug class: First Generation Antihistamines

Medically reviewed by Drugs.com on Jan 1, 2024. Written by ASHP.

Introduction

First generation antihistamine; an ethanolamine derivative.^{100 101}

Uses for Carbinoxamine

Acute Allergic Reactions

Amelioration of allergic reactions to blood or plasma.^{100 g}

Adjunct to epinephrine and other standard measures for management of anaphylaxis after acute symptoms have been controlled.^{100 g}

Allergic and Nonallergic Rhinitis

Symptomatic relief of seasonal (e.g., hay fever) or perennial (nonseasonal) allergic rhinitis or nonallergic (vasomotor) rhinitis.^{100 g}

Allergic Conjunctivitis

Symptomatic relief of allergic conjunctivitis caused by foods or inhaled allergens.^{100 g}

Allergic Skin Disorders

Symptomatic management of mild, uncomplicated allergic skin manifestations of urticaria and angioedema.^{100 g}

Treatment of dermatographism.^{100 g}

Regulations Governing Carbinoxamine-containing Preparations

Many unapproved carbinoxamine-containing preparations formerly on the US market contained inappropriate labeling that promoted unapproved uses (including management of congestion^{† [off-label]}, cough^{† [off-label]}, or the common cold^{† [off-label]}, and use in children <2^{† [off-label]} years of age), which posed serious health risks.^{101 102} (See Pediatric Use under Cautions and also see Preparations.)

Carbinoxamine Dosage and Administration

Administration

Oral Administration

Administer orally as tablets or oral solution on an empty stomach with water.¹⁰⁰

Dosage

Available as carbinoxamine maleate; dosage expressed in terms of the salt.¹⁰⁰

Individualize dosage according to patient’s response and tolerance.¹⁰⁰

Pediatric Patients

Allergic Conditions

Acute Allergic Reactions, Allergic and Nonallergic Rhinitis, Allergic Conjunctivitis, or Allergic Skin Disorders

Oral

Children ≥2 years of age: Usually, 0.2–0.4 mg/kg daily.¹⁰⁰

Children 2–3 years of age: 2 mg 3 or 4 times daily (as oral solution).¹⁰⁰

Children 3–6 years of age: 2–4 mg 3 or 4 times daily (as oral solution).¹⁰⁰

Children >6 years of age: 4–6 mg 3 or 4 times daily (as tablets or oral solution).¹⁰⁰

Adults

Allergic Conditions

Acute Allergic Reactions, Allergic and Nonallergic Rhinitis, Allergic Conjunctivitis, or Allergic Skin Disorders

Oral

Usually, 4–8 mg 3–4 times daily (as tablets or oral solution).¹⁰⁰

Special Populations

Geriatric Patients

Initiate at lower dosages and monitor closely.¹⁰⁰ (See Geriatric Use under Cautions.)

Cautions for Carbinoxamine

Contraindications

• Children <2 years of age.¹⁰⁰

• Women who are breast-feeding.¹⁰⁰

• Patients receiving MAO inhibitor therapy.¹⁰⁰

• Known hypersensitivity to carbinoxamine or any ingredient in the formulation.¹⁰⁰

Warnings/Precautions

Warnings

Anticholinergic Effects

Possible anticholinergic effects (e.g., dryness of mouth, nose, and throat; dysuria; urinary retention).^b Use with extreme caution, if at all, in patients with angle-closure glaucoma, prostatic hypertrophy, stenosing peptic ulcer, pyloroduodenal obstruction, or bladder neck obstruction.^{100 b}

General Precautions

Concomitant Diseases

Use with caution in patients with increased IOP, hyperthyroidism, or cardiovascular disease (e.g., hypertension).^{100 b}

Use of antihistamines generally not recommended in asthmatics who previously experienced a serious antihistamine-induced adverse bronchopulmonary effect.^{o p} Do not use to treat lower respiratory symptoms, including asthma.¹⁰⁰

CNS Effects

Risk of drowsiness.^{100 b} Caution when performing hazardous activities requiring mental alertness and motor coordination (e.g., driving a motor vehicle, operating machinery).^{100 b}

Possible excitability (especially in children).¹⁰⁰ (See Pediatric Use under Cautions.)

Concurrent use of other CNS depressants may have additive CNS depressant effects.^{100 b} (See Interactions.)

Specific Populations

Pregnancy

Category C.^{100 c}

Lactation

Discontinue nursing or the drug because of potential risk to nursing infants.¹⁰⁰

Pediatric Use

Risk of diminished mental alertness in children.¹⁰⁰

Possible paradoxical excitement (e.g., restlessness, insomnia, tremors, euphoria, nervousness, delirium, palpitation, seizures), particularly in young children.^{100 b}

Safety and efficacy not established in children <2 years of age;¹⁰¹ death reported in such patients, although causal relationship to carbinoxamine not established.^{101 102} Use contraindicated in children <2 years of age.¹⁰⁰

Geriatric Use

Possible increased risk of dizziness, sedation, and hypotension in patients ≥60 years of age.^{100 b} Confusion or oversedation also may occur.¹⁰⁰ (See Geriatric Patients under Dosage and Administration.)

Common Adverse Effects

Sedation,^{100 g} sleepiness,¹⁰⁰ dizziness,¹⁰⁰ disturbed coordination,¹⁰⁰ epigastric distress,¹⁰⁰ thickening of bronchial secretions.¹⁰⁰

Drug Interactions

Specific Drugs and Laboratory Tests

Carbinoxamine Pharmacokinetics

Absorption

Onset

Approximately 30 minutes.^g

Duration

Pharmacologic effects persist for approximately 4 hours.¹⁰⁰

Stability

Storage

Oral

Tablets and Oral Solution

Tight, light-resistant containers with child-resistant closures at 15–30°C.¹⁰⁰

Actions

• Blocks H₁-receptor sites and prevents the action of histamine on the cell.^{100 b g}

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

• Has anticholinergic and sedative effects.¹⁰⁰

• Exhibits some activities common to anticholinergics, ganglionic and adrenergic blocking agents, local anesthetics, and antispasmodics.^b

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

Advice to Patients

• Risk of drowsiness; avoid alcohol and use caution when engaging in activities requiring mental alertness or motor coordination (e.g., operating machinery, driving a motor vehicle).^{100 b}

• Importance of administering tablets or oral solution on an empty stomach with water.¹⁰⁰

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.¹⁰⁰

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.¹⁰⁰

• Importance of informing patients of other important precautionary information.¹⁰⁰ (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.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

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