AZATADINE MALEATE
(a-za'ta-deen)
Optimine, Trinalin
Classifications: antihistamine (h1-receptor antagonist)
Prototype: Diphenhydramine
Pregnancy Category: B
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1 mg tablets
Long-acting antihistamine that acts by competitively antagonizing the stimulating effects of histamine at H1-receptor sites on smooth muscle of blood vessels and respiratory and GI tract.
The effect is to block or reduce intensity of allergic responses associated with histamine release, such as vasodilation,
capillary permeability and tissue edema, and itching.
Symptomatic relief of hay fever (seasonal allergic rhinitis), perennial (or nonseasonal) allergic rhinitis, and chronic urticaria.
Hypersensitivity to azatadine or to other H1-receptor antagonists; MAO INHIBITOR therapy. Safety during pregnancy (category B), lactation, or in children <12 y is not established.
Increased intraocular pressure, narrow-angle glaucoma; pyloroduodenal obstruction, stenosing peptic ulcer; prostatic hypertrophy,
bladder neck obstruction; hyperthyroidism; hypertension, cardiovascular disease; convulsive disorders; history of asthma or
COPD.
Allergic Rhinitis
Adult: PO 1–2 mg b.i.d.
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Oral
- Give drug with food or milk to minimize GI adverse effects.
- Store at 2°–30° C (36°–86° F) in tightly closed container, unless otherwise directed.
CNS:
Drowsiness, sedation, dizziness, disturbed coordination, fatigue, confusion, euphoria, excitation, nervousness, restlessness, insomnia,
tremor, irritability. CV: Hypotension, palpitation, tachycardia, extrasystoles. GI:
Dry mouth, epigastric distress, nausea, vomiting, anorexia, diarrhea, or constipation. Urogenital: Urinary retention, early menses. Hematologic:
Hemolytic anemia, thrombocytopenia, agranulocytosis. Respiratory: Thickening of bronchial secretions. Special Senses: Nasal stuffiness; dryness of nose and throat; tinnitus, blurred vision.
As a general rule, H1-receptor antagonists are discontinued about 4 d before skin testing procedures are to be performed since they may produce false-negative results.
Drug:
Alcohol,
cns depressants add to sedation, drowsiness; mao inhibitors may prolong anticholinergic effects of azatadine; tricyclic antidepressants augment anticholinergic effects.
Absorption: Readily absorbed from GI tract. Peak: 4 h. Distribution: Probably crosses blood–brain barrier; crosses placenta; distribution into breast milk unknown. Metabolism: Partially metabolized in liver. Elimination: 50% excreted in urine in 5 d. Half-Life: 9–12 h.
Assessment & Drug Effects
- Monitor for sedation, dizziness, hypotension, and confusion which are more common in older adults. Advise patient to report
these effects. Reduction in dosage may be indicated.
- Monitor mental status. There may be additive CNS depression with alcohol and other CNS depressants (e.g., sedatives, tranquilizers,
sleep medications).
Patient & Family Education
- Do not drive or engage in potentially hazardous activities until response to drug is known. This drug commonly causes drowsiness,
sedation, and dizziness.
- Avoid concurrent use of alcohol because of potential for additive CNS depression.
- Avoid prolonged exposure to sunlight or to artificial ultraviolet light. Photosensitivity is a possible adverse effect.
- Relieve dry mouth with frequent rinses with tepid water. Avoid mouthwashes, which contain alcohol that enhances drying.
- Do not breast feed while taking this drug without consulting physician.
1%)
Canadian drug name; 
Prototype drug