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Carbinoxamine

Class: First Generation Antihistamines
ATC Class: R06AA08
VA Class: AH102
CAS Number: 3505-38-2
Brands: Arbinoxa, Palgic

Medically reviewed by Drugs.com on Jan 3, 2022. Written by ASHP.

Introduction

First generation antihistamine; an ethanolamine derivative.

Uses for Carbinoxamine

Acute Allergic Reactions

Amelioration of allergic reactions to blood or plasma.

Adjunct to epinephrine and other standard measures for management of anaphylaxis after acute symptoms have been controlled.

Allergic and Nonallergic Rhinitis

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

Allergic Conjunctivitis

Symptomatic relief of allergic conjunctivitis caused by foods or inhaled allergens.

Allergic Skin Disorders

Symptomatic management of mild, uncomplicated allergic skin manifestations of urticaria and angioedema.

Treatment of dermatographism.

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, cough, or the common cold, and use in children <2 years of age), which posed serious health risks. (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.

Dosage

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

Individualize dosage according to patient’s response and tolerance.

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.

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

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

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

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).

Special Populations

Geriatric Patients

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

Cautions for Carbinoxamine

Contraindications

  • Children <2 years of age.

  • Women who are breast-feeding.

  • Patients receiving MAO inhibitor therapy.

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

Warnings/Precautions

Warnings

Anticholinergic Effects

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

General Precautions

Concomitant Diseases

Use with caution in patients with increased IOP, hyperthyroidism, or cardiovascular disease (e.g., hypertension).

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

CNS Effects

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

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

Concurrent use of other CNS depressants may have additive CNS depressant effects. (See Interactions.)

Specific Populations

Pregnancy

Category C.

Lactation

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

Pediatric Use

Risk of diminished mental alertness in children.

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

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

Geriatric Use

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

Common Adverse Effects

Sedation, sleepiness, dizziness, disturbed coordination, epigastric distress, thickening of bronchial secretions.

Interactions for Carbinoxamine

Specific Drugs and Laboratory Tests

Drug or Test

Interaction

Comments

CNS depressants (alcohol, hypnotics, sedatives, tranquilizers)

Possible additive CNS depression

Avoid alcohol; avoid concomitant use with other CNS depressants without consulting clinician

MAO inhibitors

MAO inhibitors prolong and intensify anticholinergic effects of antihistamines

Concomitant use contraindicated

Test, antigen or histamine

Inhalation-challenge testing with histamine or antigen: Possible suppression of test response

Antigen skin testing: Possible suppression of wheal and flare reactions

Carbinoxamine Pharmacokinetics

Absorption

Onset

Approximately 30 minutes.

Duration

Pharmacologic effects persist for approximately 4 hours.

Stability

Storage

Oral

Tablets and Oral Solution

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

Actions

  • Blocks H1-receptor sites and prevents the action of histamine on the cell.

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

  • Has anticholinergic and sedative effects.

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

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

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).

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

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

  • 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.

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

Carbinoxamine Maleate

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Solution

4 mg/5 mL*

Arbinoxa

Hawthorn

Carbinoxamine Maleate Solution

Palgic

Pamlab

Tablets

4 mg*

Arbinoxa

Hawthorn

Carbinoxamine Maleate

Palgic

Pamlab

AHFS DI Essentials™. © Copyright 2022, Selected Revisions January 11, 2012. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

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