Rx Drugs Info

carbinoxamine maleate (Carbinoxamine Maleatetablet 
carbinoxamine maleate (Carbinoxamine Maleatesolution 
[Pamlab, L.L.C.]

Rx only

Code 838A00

DESCRIPTION

Carbinoxamine maleate is a histamine-H1 receptor blocking agent.

Each tablet contains 4 mg carbinoxamine maleate and the following inactive ingredients: anhydrous lactose, magnesium stearate, microcrystalline cellulose, and sodium starch glycolate.

Each 5 mL (teaspoonful) of oral solution contains 4 mg carbinoxamine maleate and the following inactive ingredients: artificial bubble gum flavor, citric acid (anhydrous), glycerin, methylparaben, propylene glycol, propylparaben, purified water, sodium citrate (hydrous) and sorbitol solution.

Carbinoxamine maleate is freely soluble in water. Its structure is:

Image from Drug Label Content

2-[(4-chlorophenyl)-2-pyridinylmethoxy]-N, N-dimethylethanamine (Z)-2-butenedioate (1:1)

C16H19CIN2O• C4H4O4                                                                                          MW = 406.86

CLINICAL PHARMACOLOGY

Carbinoxamine maleate is an antihistamine with anticholinergic (drying) and sedative properties.

Antihistamines appear to compete with histamine for receptor sites on effector cells.

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

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

INDICATIONS AND USAGE

Carbinoxamine maleate is effective for the symptomatic 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.

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.

CONTRAINDICATIONS

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

Carbinoxamine maleate is contraindicated in nursing mothers.

Carbinoxamine maleate is contraindicated in patients who are hypersensitive to the drug or on monoamine oxidase inhibitor therapy. (See Drug Interactions section.)

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 (see CONTRAINDICATIONS).

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

PRECAUTIONS

As many other antihistamines, carbinoxamine maleate has an atropine-like action and, therefore, should be used with caution in patients with: increased intraocular pressure, hyperthyroidism, cardiovascular disease, hypertension.

Antihistamines such as carbinoxamine maleate should not be used to treat lower respiratory tract symptoms, including asthma.

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

Carbinoxamine maleate is more likely to cause dizziness, sedation, and hypotension in elderly patients (approximately 60 years or older).

Information for Patients

Carbinoxamine maleate may cause drowsiness; alcohol, sedatives, and tranquilizers may increase the drowsiness effect. Avoid alcoholic beverages while taking this product. Do not take this product if you are taking sedatives or tranquilizers, without first consulting your doctor. Use caution when driving a motor vehicle or operating machinery.

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.).

Carcinogenesis, Mutagenesis, Impairment of Fertility

No long-term studies in animals have been performed to determine the possible effects of carbinoxamine maleate on carcinogenesis, mutagenesis, and fertility.

Pregnancy 

Pregnancy Category 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.

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 (see CONTRAINDICATIONS section).

Pediatric Use

Carbinoxamine maleate is contraindicated in children younger than 2 years of age (see CONTRAINDICATIONS).

Geriatric Use

Sedating drugs may cause confusion and over-sedation in the elderly; elderly patients generally should be started on lower doses of carbinoxamine maleate and observed closely.

ADVERSE REACTIONS

The most frequent adverse reactions are underlined:

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.

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.

DOSAGE AND ADMINISTRATION

Carbinoxamine maleate is contraindicated in children younger than 2 years of age (see CONTRAINDICATIONS).

Carbinoxamine maleate tablets should be taken on an empty stomach with water.

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 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

Usual Child’s Dosage:

 
Over six years – 1 to 1½ tablets (4 to 6 mg) 3 or 4 times daily.

Oral Solution

Usual Adult Dosage:

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

Usual Child’s Dosage (approximately 0.2 – 0.4 mg/kg/day):

 
Two to three years –½ teaspoonful (2 mg) 3 or 4 times daily.
 
Three to six years –½ teaspoonful to 1 teaspoonful (2 to 4 mg) 3 or 4 times daily
 
Over six years - 1 to 1½ teaspoonfuls (4 to 6 mg) 3 or 4 times daily.

HOW SUPPLIED

Carbinoxamine Maleate Tablets, USP 4 mg are supplied as white, round, scored tablets, debossed “PAL” on one side and score “4” on the other side, and are supplied in bottles of 100 tablets, NDC 0525-6748-01 and bottles of 500 tablets, NDC 0525-6748-05.

Carbinoxamine Maleate Oral Solution, 4 mg/5 mL is supplied as clear, colorless liquid with a bubble gum aroma, and is supplied in 4 oz bottles NDC 0525-6752-04 and 16 oz bottles NDC 0525-6752-16.

Store at controlled room temperature, 15°C to 30°C (59°F to 86°F) [See USP].

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

Manufactured for:

Pamlab, L.L.C.

Covington, LA 70433

Manufactured by:

MIKART, INC.

Atlanta, GA 30318

Rev. 05/06                                                                                                                     Code 838A00


Carbinoxamine Maleate (Carbinoxamine Maleate)
PRODUCT INFO
Product Code 0525-6748 Dosage Form TABLET
Route Of Administration ORAL DEA Schedule
INGREDIENTS
Name (Active Moiety) Type Strength
CARBINOXAMINE MALEATE (CARBINOXAMINE) Active 4 MILLIGRAM  In 1 TABLET
ANHYDROUS LACTOSE Inactive  
MAGNESIUM STEARATE Inactive  
MICROCRYSTALLINE CELLULOSE Inactive  
SODIUM STARCH GLYCOLATE Inactive  
IMPRINT INFORMATION
Characteristic Appearance Characteristic Appearance
Color WHITE (WHITE) Score 2
Shape ROUND (ROUND) Symbol false
Imprint Code PAL;4 Coating false
Size 7mm
PACKAGING
# NDC Package Description Multilevel Packaging
1 0525-6748-01 100 TABLET In 1 BOTTLE, PLASTIC None
2 0525-6748-05 500 TABLET In 1 BOTTLE, PLASTIC None

Carbinoxamine Maleate (Carbinoxamine Maleate)
PRODUCT INFO
Product Code 0525-6752 Dosage Form SOLUTION
Route Of Administration ORAL DEA Schedule
INGREDIENTS
Name (Active Moiety) Type Strength
CARBINOXAMINE MALEATE (CARBINOXAMINE) Active 4 MILLIGRAM  In 5 MILLILITER
ARTIFICIAL BUBBLE GUM FLAVOR Inactive  
CITRIC ACID Inactive  
GLYCERIN Inactive  
METHYLPARABEN Inactive  
PROPYLENE GLYCOL Inactive  
PROPYLPARABEN Inactive  
WATER Inactive  
SODIUM CITRATE Inactive  
SORBITOL SOLUTION Inactive  
IMPRINT INFORMATION
Characteristic Appearance Characteristic Appearance
Color Score
Shape Symbol
Imprint Code Coating
Size
PACKAGING
# NDC Package Description Multilevel Packaging
1 0525-6752-04 118 MILLILITER In 1 BOTTLE, PLASTIC None
2 0525-6752-16 473 MILLILITER In 1 BOTTLE, PLASTIC None

Revised: 05/2006Pamlab, L.L.C.

Data are from FDA and U.S. National Library of Medicine.