Carbinoxamine

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Carbinoxamine
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Sree Teja Yelamanchili, MBBS [2]

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Overview

Carbinoxamine is a H1-blocking agent that is FDA approved for the treatment of seasonal and perennial allergic rhinitis, vasomotor rhinitis, allergic conjunctivitis due to inhalant allergens and foods, mild uncomplicated allergic skin manifestations of urticaria and angioedema, and dermatographism. Common adverse reactions include epigastric pain, coordination problem, dizziness, sedation, somnolence, and excessive bronchial secretions.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Indications

Dosage

DOSAGE SHOULD BE INDIVIDUALIZED ACCORDING TO THE NEEDS AND THE RESPONSE OF THE PATIENT.

Carbinoxamine maleate dosage should be based on the severity of the condition and the response of the patient. The drug is well tolerated in adult doses as high as 24 mg daily, in divided doses, over prolonged periods. On the other hand, some patients respond to as little as 4 mg daily.

Clinical experience suggests the following dosage schedules:

Tablets

Usual Adult Dosage:

  • 1 or 2 tablets (4 to 8 mg) 3 to 4 times daily.

Oral Solution

Usual Adult Dosage:

  • 1 or 2 teaspoonfuls (4 to 8 mg) 3 to 4 times daily.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Carbinoxamine in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Carbinoxamine in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

Indications

  • Seasonal and perennial allergic rhinitis.
  • Vasomotor rhinitis.
  • Allergic conjunctivitis due to inhalant allergens and foods.
  • Mild, uncomplicated allergic skin manifestations of urticaria and angioedema.
  • Dermatographism.
  • As therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the acute manifestations have been controlled.
  • Amelioration of the severity of allergic reactions to blood or plasma.

Dosage

Tablets

Usual Child’s Dosage:

  • Six to eleven years – 1/2 to 1 tablet (2 to 4 mg) 3 to 4 times daily.

Oral Solution

Usual Child’s Dosage:

  • Approximately 0.2 to 0.4 mg/kg/day, divided into 3 to 4 doses
  • Six to eleven years – 1/2 to 1 teaspoonful (2 to 4 mg) 3 to 4 times daily.

Dosing for children 2 to 5 years of age should be based on weight whenever possible. The usual dosage for children 2 to 5 years of age is approximately 0.2 to 0.4 mg/kg/day, divided into 3 to 4 daily doses. In general, this corresponds to a dose of 1/4 to 1/2 teaspoonful (1 to 2 mg) 3 to 4 times daily.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Carbinoxamine in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Carbinoxamine in pediatric patients.

Contraindications

Carbinoxamine maleate is contraindicated in:

  • Children younger than 2 years of age.
  • Nursing mothers.
  • Patients who are hypersensitive to the drug or on monoamine oxidase inhibitor therapy.

Warnings

Deaths have been reported in children less than 2 years of age who were taking antihistamines, including carbinoxamine-containing drug products, therefore, carbinoxamine maleate is contraindicated in children younger than 2 years of age.

Antihistamines should be used with considerable caution in patients with: narrow angle glaucoma, stenosing peptic ulcer, symptomatic prostatic hypertrophy, bladder neck obstruction, pyloroduodenal obstruction.

Adverse Reactions

Clinical Trials Experience

There is limited information regarding Carbinoxamine Clinical Trials Experience in the drug label.

Postmarketing Experience

Body as a Whole: Urticaria, drug rash, anaphylactic shock, photosensitivity, excessive perspiration, chills, dryness of mouth, nose and throat.

Cardiovascular: Hypotension, headache, palpitations, tachycardia, extrasystoles.

Hematologic: Hemolytic anemia, thrombocytopenia, agranulocytosis.

Central Nervous System: Sedation, sleepiness, dizziness, disturbed coordination, fatigue, confusion, restlessness, excitation, nervousness, tremor, irritability, insomnia, euphoria, paresthesia, blurred vision, diplopia, vertigo, tinnitus, acute labyrinthitis, hysteria, neuritis, convulsions.

Gastrointestinal: Epigastric distress, anorexia, nausea, vomiting, diarrhea, constipation.

Urogenital: Urinary frequency, difficult urination, urinary retention, early menses.

Respiratory: Thickening of bronchial secretions, tightness of chest and wheezing, nasal stuffiness.

Drug Interactions

Monoamine oxidase inhibitors prolong and intensify the anticholinergic (drying) effects of antihistamines.

Carbinoxamine maleate has additive effects with alcohol and other CNS depressants (hypnotics, sedatives, tranquilizers, etc.).

Interactions of carbinoxamine maleate with other drugs and the possibility of cardiac conduction effects on the QT interval have not been studied.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): C Animal reproductive studies have not been conducted with carbinoxamine maleate. It is also not known whether carbinoxamine maleate can cause fetal harm when administered to a pregnant woman or can affect reproductive capacity.

Carbinoxamine maleate should be given to a pregnant woman only if clearly needed.
Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Carbinoxamine in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Carbinoxamine during labor and delivery.

Nursing Mothers

Because of the higher risk of antihistamines for infants generally and for newborns and prematures in particular, use of carbinoxamine maleate is contraindicated in nursing mothers.

Pediatric Use

Carbinoxamine maleate is contraindicated in children younger than 2 years of age.

Carbinoxamine maleate may diminish mental alertness in children. In the young child, particularly, they may produce excitation.

Geriatic Use

Carbinoxamine maleate is more likely to cause dizziness, sedation, and hypotension in elderly patients (approximately 60 years or older). Sedating drugs may also cause confusion and over sedation in the elderly. Therefore, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic renal, or cardiac function, and of concomitant disease or other drug therapy.

Gender

There is no FDA guidance on the use of Carbinoxamine with respect to specific gender populations.

Race

There is no FDA guidance on the use of Carbinoxamine with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Carbinoxamine in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Carbinoxamine in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Carbinoxamine in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Carbinoxamine in patients who are immunocompromised.

Administration and Monitoring

Administration

  • Oral

Monitoring

Vital signs (including respiration, pulse, blood pressure, and temperature) and EKG should be monitored in carbinoxamine overdosage.

IV Compatibility

There is limited information regarding the compatibility of Carbinoxamine and IV administrations.

Overdosage

Manifestations

Antihistamine overdosage reactions may vary from central nervous system depression to stimulation. Stimulation is particularly likely in children. Atropine-like signs and symptoms – dry mouth; fixed, dilated pupils; flushing; and gastrointestinal symptoms may also occur. Especially in infants and children, antihistamine overdosage may cause hallucinations, convulsions, or death.

The oral LD50 of carbinoxamine maleate in guinea pigs is 411 mg/kg.

Treatment

The treatment of overdosage with carbinoxamine maleate is essentially symptomatic and supportive. Vital signs (including respiration, pulse, blood pressure, and temperature) and EKG should be monitored. Induction of vomiting is not recommended. Activated charcoal should be given and gastric lavage should be considered after ingestion of a potentially life-threatening amount of drug.

In the presence of severe anticholinergic effects, physostigmine may be useful. Vasopressors may be used to treat hypotension.

Pharmacology

Carbinoxamine.png
Carbinoxamine
Systematic (IUPAC) name
2-[(4-Chlorophenyl)-pyridin-2-yl-methoxy]-N,N-
dimethyl-ethanamine
Identifiers
CAS number 486-16-8
ATC code R06AA08
PubChem 2564
DrugBank DB00748
Chemical data
Formula C16H19ClN2O 
Mol. mass 290.788 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability ?
Metabolism ?
Half life 10 to 20 hours
Excretion ?
Therapeutic considerations
Pregnancy cat.

C

Legal status

4 mg is FDA approved

Routes Oral: 4 mg tablet or 4 mg/5 mL liquid

Mechanism of Action

Carbinoxamine maleate is an antihistamine with anticholinergic (drying) and sedative properties. Antihistamines appear to compete with histamine for receptor sites on effector cells.

Structure

Carbinoxamine maleate is a histamine-H1 receptor blocking agent.

Each tablet contains 4 mg carbinoxamine maleate.

Inactive ingredients: anhydrous lactose, magnesium stearate, microcrystalline cellulose, and sodium starch glycolate.

Each 5 mL (teaspoonful) of oral solution contains 4 mg carbinoxamine maleate.

Inactive ingredients: artificial banana bubble gum flavor, citric acid (anhydrous), glycerin, purified water, sodium benzoate and sorbitol solution.

Carbinoxamine maleate is freely soluble in water.

Its structure is:

This image is provided by the National Library of Medicine.

Pharmacodynamics

There is limited information regarding Carbinoxamine Pharmacodynamics in the drug label.

Pharmacokinetics

The pharmacological effects of carbinoxamine maleate after oral absorption have been shown to last approximately 4 hours.

Nonclinical Toxicology

There is limited information regarding Carbinoxamine Nonclinical Toxicology in the drug label.

Clinical Studies

There is limited information regarding Carbinoxamine Clinical Studies in the drug label.

How Supplied

Carbinoxamine Maleate Tablets USP, 4 mg are supplied as white, round tablets scored and debossed “B” bisected “P” on one side and “605” on the other side, and supplied in bottles of 100 tablets, NDC 64376-605-01.

Carbinoxamine Maleate Oral Solution, 4 mg/5 mL is supplied as clear, colorless liquid with a banana bubble gum flavor, and is supplied in 4 oz bottles NDC 64376-612-40 and 16 oz bottles NDC 64376-612-16.

Manufactured for:

Boca Pharmacal, LLC

Coral Springs, FL 33065

www.bocapharmacal.com

1-800-354-8460

Rev. 08/13

Storage

Store at 20°-25°C (68°-77°F). [See USP Controlled Room Temperature].

Dispense in a tight, light-resistant container with a child-resistant closure as defined in the official compendium.

Images

Drug Images

Arbinoxa NDC 637170870.jpg

Drug Name: Arbinoxa
Ingredient(s): CARBINOXAMINE MALEATE[CARBINOXAMINE]
Imprint: CYP;870
Dosage: 4 mg
Color(s): White
Shape: Round
Size (mm): 7
Score: 2
NDC:637170870

Drug Label Author: Hawthorn Pharmaceuticals, Inc.

This pill image is provided by the National Library of Medicine's PillBox.
Carbinoxamine Maleate NDC 643760605.jpg

Drug Name: Carbinoxamine Maleate
Ingredient(s): CARBINOXAMINE MALEATE[CARBINOXAMINE]
Imprint: BP;605
Dosage: 4 mg
Color(s): White
Shape: Round
Size (mm): 7
Score: 2
NDC:643760605

Drug Label Author: Boca Pharmacal, LLC

This pill image is provided by the National Library of Medicine's PillBox.

Package and Label Display Panel

This image is provided by the National Library of Medicine.
This image is provided by the National Library of Medicine.
This image is provided by the National Library of Medicine.
This image is provided by the National Library of Medicine.

Patient Counseling Information

There is limited information regarding Carbinoxamine Patient Counseling Information in the drug label.

Precautions with Alcohol

  • Alcohol may increase the drowsiness effect.
  • Avoid alcoholic beverages while taking this product.
  • Carbinoxamine maleate has additive effects with alcohol and other CNS depressants (hypnotics, sedatives, tranquilizers, etc.).

Brand Names

  • Histex PD
  • Histex I/E
  • Histex CT
  • Pediox
  • Carbihist
  • Histuss PD
  • Carboxine
  • Mintex PD

Look-Alike Drug Names

There is limited information regarding Carbinoxamine Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.


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