CARBINOXAMINE MALEATE tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

CARBINOXAMINE MALEATE (UNII: 02O55696WH) (CARBINOXAMINE - UNII:982A7M02H5)

Available from:

Foxland Pharmaceuticals, Inc.

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

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. 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 ).

Product summary:

Carbinoxamine maleate tablets, USP, 6 mg are supplied as a white, round tablet, debossed "404" on one side and "ADG" on the other side, in bottles of 20 tablets, NDC 69067-240-20. Store at 20° to 25°C (68° to 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.

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

CARBINOXAMINE MALEATE- CARBINOXAMINE MALEATE TABLET
FOXLAND PHARMACEUTICALS, INC.
----------
CARBINOXAMINE MALEATE
TABLETS, USP 6 MG
DESCRIPTION
Carbinoxamine maleate is a histamine-H
receptor blocking agent.
Each tablet contains 6 mg carbinoxamine maleate and the following
inactive ingredients:
anhydrous lactose, magnesium stearate, microcrystalline cellulose, and
sodium starch
glycolate.
Carbinoxamine maleate is freely soluble in water. Its structure is:
2-[(4-chlorophenyl)-2-pyridinylmethoxy]-N, N-dimethylethanamine
(Z)-2-butenedioate
(1:1)
C
H
ClN
O∙C
H
O
MW=406.86
CLINICAL PHARMACOLOGY
MECHANISM OF ACTIONS
Carbinoxamine maleate, an ethanolamine derivative, is an antihistamine
with
anticholinergic (drying) and sedative properties. Carbinoxamine
appears to compete with
histamine (type H1) for receptor sites on effector cells in the
gastrointestinal tract, blood
vessels and respiratory tract.
PHARMACOKINETICS AND METABOLISM
Carbinoxamine is well absorbed from the GI tract and appears to be
extensively
metabolized by the liver, and excreted in the urine as inactive
metabolites within 24
hours. Virtually no intact drug is extended in the urine.
1
16
19
2
4
4
4
In a study comparing a controlled release suspension and a solution of
carbinoxamine,
healthy volunteers were administered a single dose of 8 mg
carbinoxamine. A time to
maximum concentration (Tmax) was between 1.5 hours to 5 hours, a peak
plasma
concentration (Cmax) of about 24 ng/mL was observed, and extent of
exposure (AUC)
was about 286 ng hr/mL. The serum half-life is reported to be 10 to 20
hours.
DRUG/FOOD INTERACTIONS
Carbinoxamine should not be used in patients with hypersensitivity to
carbinoxamine.
Carbinoxamine may increase the effects of other drugs such as
barbiturates, TCAs,
MAO inhibitors such as Phenelzine (Nardil), Tranylcypromine (Parnate),
or Selegiline
(Eldepryl), alcohol, other antihistamines, and CNS depressants.
Carbinoxamine can be
taken with or without food.
CARDIOVASCULAR EFFECTS
Cardiac effects, including prolongation of QT int