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Carbinoxamine Maleate

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

Introduction

First generation antihistamine; an ethanolamine derivative.100 101

Uses for Carbinoxamine Maleate

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

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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 remaining on the US market as of June 2006 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.101 102 (See Pediatric Use under Cautions and also see Preparations.)

Carbinoxamine Maleate 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 Maleate

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. 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

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.105 106 Limited evidence of efficacy for these preparations in this age group; appropriate dosages not established.105 Do not use such preparations in children <2 years of age;h safety and efficacy in older children currently 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 recently agreed to voluntarily revise the product labeling to state that such preparations should not be used in children <4 years of age. During the transition period, some preparations on pharmacy shelves will have the new recommendation (“do not use in children <4 years of age”), while others will have the previous recommendation (“do not use in children <2 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 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

Interactions for Carbinoxamine Maleate

Specific Drugs and Laboratory Tests

Drug or Test

Interaction

Comments

CNS depressants (alcohol, hypnotics, sedatives, tranquilizers)

Possible additive CNS depression100 b

Avoid alcohol;100 avoid concomitant use with other CNS depressants without consulting clinician100

MAO inhibitors

MAO inhibitors prolong and intensify anticholinergic effects of antihistamines100 b

Concomitant use contraindicated100

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 Maleate 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.

Many prescription cough, cold, and allergy preparations commercially available in the US have not been approved by the FDA.500 Because of the potentially serious health risks associated with unapproved preparations, FDA announced on March 3, 2011, that it would take enforcement action (e.g., seizure, injunction, other judicial or administrative proceeding) against any currently marketed and listed unapproved cough, cold, and allergy preparation manufactured on or after June 1, 2011 or shipped on or after August 30, 2011.500 For additional information and for a complete list of unapproved cough, cold, and allergy preparations affected by this FDA notice, see FDA website ().

* 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, 2004-2014, Selected Revisions January 11, 2012. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

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

References

Only references cited for selected revisions after 1984 are available electronically.

100. Pamlab, LLC. Palgic (4 mg carbinoxamine maleate) tablet and oral solution prescribing information. Covington, IA; 2006 Jun.

101. Food and Drug Administration. Carbinoxamine products: Enforcement action dates (Docket No. 2006N-0229). Fed Regist. 2006; 71:33462-5.

102. Food and Drug Administration. Questions and answers about unapproved drugs and FDA’s enforcement action against carbinoxamine products. Rockville, MD; 2006 Jun. From FDA website.

103. Anon. Dear Pamlab customer letter. Covington, LA: Pamlab, LLC; 2006 June 12. From Palgic website.

104. US Department of Health and Human Services and Food and Drug Administration Center for Drug Evaluation and Research (CDER). Guidance for FDA staff and industry: Marketed unapproved drugs–Compliance policy guide. 2006 Jun. From FDA web site.

105. Srinivasan A, Budnitz D, Shehab N et al. Infant deaths associated with cough and cold medications—two states, 2005. MMWR Morb Mortal Wkly Rep. 2007; 56:1-4. [PubMed 17218934]

106. Food and Drug Administration. Cough and cold medications in children less than two years of age. Rockville, MD; 2007 Jan 12. From FDA website.

107. PamLab, LLC. Palgic (carbinoxamine maleate) product description. Covington, LA; Undated. From Pamlab website.

108. Approved Drug Products with Therapeutic Equivalence Evaluations (Electronic Orange Book). Accessed 2011 Jun 29. From FDA website.

500. Food and Drug Administration. Drugs for human use; unapproved and misbranded oral drugs labeled for prescription use and offered for relief of symptoms of cold, cough, or allergy, enforcement action dates. Notice. [Docket No. FDA-2011-N-0100] Fed Regist. 2011; 76:11794-8.

b. AHFS Drug Information 2008. McEvoy GK, ed. Antihistamines General Statement. Bethesda, MD: American Society of Health-System Pharmacists; 2008:1-8.

c. Carbinoxamine. In: Briggs GG, Freeman RK, Yaffe SJ. Drugs in pregnancy and lactation. 7th ed. Philadelphia, PA: Lippincott Williams & Wilkins; 2005:229.

g. PamLab, LLC. Palgic (carbinoxamine maleate) product description. Covington, LA; Undated. From Pamlab website.

h. Food and Drug Administration. FDA news: FDA releases recommendations regarding use of over-the-counter cough and cold products. Rockville, MD; 2008 Jan 17. From the FDA web site.

i. Richwine L. U.S. panel against cold drugs for kids under 6. Reuters, 2007 Oct 19. From Reuters website.

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