Carbinoxamine Maleate

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 angio-edema. 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 AND ADMINISTRATION Carbinoxamine maleate is contraindicated in children younger than 2 years of age (see CONTRAINDICATIONS). Carbinoxamine maleate 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 bebased on the severity of the condition and the response of the patient. The drug is well tolerated in adults 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 followingdosage schedules: Tablets Usual Adult Dosage: 1 or 2 tablets (4 to 8 mg) 3 to 4 times daily. Usual Child’s Dosage: Six to eleven years – 1⁄2 to 1 tablet (2 to 4 mg) 3 to 4 times daily.

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).

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. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or Tripoint Therapeutics at AE_PC@tripointtherapeutics.com.

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.).

Mechanism of Actions Carbinoxamine maleate, an ethanolamine derivative, is an antihistamine with anticholinergic (drying) and sedative properties. Carbinoxamine appears to compete with histamine (type H 1 ) for receptor sites on effector cells in the gastrointestinal tract, blood vessels and respiratory tract.

DESCRIPTION Carbinoxamine maleate is a histamine-H 1 receptor blocking agent. Each immediate release tablet contains 6 mg carbinoxamine maleate for oral administration and the following inactive ingredients: anhydrous lactose, colloidal silicon dioxide, magnesium stearate, microcrystalline cellulose, and sodium starch glycolate. Carbinoxamine maleate is very soluble in water, freely soluble in alcohol and in chloroform. Its structure is: Ethanamine,2-[(4-chlorophenyl)-2-pyridinylmethoxy]-N, N-dimethyl-, (Z)-2-butenedioate (1:1) C 20 H 23 ClN 2 O 5 MW= 406.86 FDA approved dissolution test specifications differ from USP. Chemical Structure

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 LD 50 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.

HOW SUPPLIED Carbinoxamine Maleate Tablets USP, 6 mg are supplied as white to off-white, round tablet, debossed with “LP” over “239” on one side and plain on the other side, in bottles of 100 tablets, NDC 69315-239-01 Store at 20° to 25°C (68° to 77°F); excursions permitted between 15°C and 30°C (between 59°F and 86°F) [See USP Controlled Room Temperature]. Dispense in a tight, light-resistant container with a child-resistant closure as defined in the official compendium. Rx only Manufactured and Distributed by: Leading Pharma, LLC 3 Oak Rd, Fairfield, New Jersey (NJ) 07004 United States (USA) Rev. 04 07/25