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Azatadine
Pronunciation
U.S. Brand Names
Generic Available
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(a ZA ta deen)

U.S. Brand Names
Optimine®

Generic Available

No


Synonyms
Azatadine Maleate

Pharmacological Index

Antihistamine


Use

Treatment of perennial and seasonal allergic rhinitis and chronic urticaria


Pregnancy Risk Factor

B


Contraindications

Hypersensitivity to azatadine or to other related antihistamines including cyproheptadine; patients taking monoamine oxidase inhibitors should not use azatadine


Warnings/Precautions

Sedation and somnolence are the most commonly reported adverse effects


Adverse Reactions

>10%:

Central nervous system: Slight to moderate drowsiness

Respiratory: Thickening of bronchial secretions

1% to 10%:

Central nervous system: Headache, fatigue, nervousness, dizziness

Gastrointestinal: Appetite increase, weight gain, nausea, diarrhea, abdominal pain, xerostomia

Neuromuscular & skeletal: Arthralgia

Respiratory: Pharyngitis

<1%: Palpitations, edema, depression, angioedema, photosensitivity, rash, hepatitis, myalgia, paresthesia, bronchospasm, epistaxis


Overdosage/Toxicology

Symptoms of overdose include CNS depression or stimulation, dry mouth, flushed skin, fixed and dilated pupils, apnea.

There is no specific treatment for an antihistamine overdose, however, most of its clinical toxicity is due to anticholinergic effects. Anticholinesterase inhibitors may be useful by reducing acetylcholinesterase; anticholinesterase inhibitors include physostigmine, neostigmine, pyridostigmine, and edrophonium. For anticholinergic overdose with severe life-threatening symptoms, physostigmine 1-2 mg (0.5 mg or 0.02 mg/kg for children) I.V., slowly may be given to reverse these effects.


Drug Interactions

Increased effect/toxicity: Procarbazine, CNS depressants, tricyclic antidepressants, alcohol


Mechanism of Action

Azatadine is a piperidine-derivative antihistamine; has both anticholinergic and antiserotonin activity; has been demonstrated to inhibit mediator release from human mast cells in vitro; mechanism of this action is suggested to prevent calcium entry into the mast cell through voltage-dependent calcium channels


Pharmacodynamics/Kinetics

Onset of effect: 1-2 hours

Absorption: Oral: Rapid and extensive

Half-life, elimination: ~8.7 hours

Elimination: ~20% of dose excreted unchanged in urine over 48 hours


Usual Dosage

Children >12 years and Adults: Oral: 1-2 mg twice daily


Dietary Considerations

Alcohol: Additive CNS effects, avoid use


Mental Health: Effects on Mental Status

Drowsiness is common; rare reports of depression


Mental Health: Effects on Psychiatric Treatment

Contraindicated with MAOIs; may produce additive CNS depressant effect with concurrent psychotropic use


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

This drug has atropine-like effects and the patient may experience drowsiness; dry mouth, nose, and throat


Patient Information

Take as directed; do not exceed recommended dose. Avoid use of other depressants, alcohol, or sleep-inducing medications unless approved by prescriber. You may experience drowsiness or dizziness (use caution when driving or engaging in tasks requiring alertness until response to drug is known); or dry mouth, abdominal pain, or nausea (frequent small meals, frequent mouth care, chewing gum, or sucking hard candy may help). Report persistent sore throat, difficulty breathing, or expectorating (thick secretions); excessive sedation or mental stimulation; frequent nosebleeds; unusual joint or muscle pain; or lack of improvement or worsening or condition. Breast-feeding precautions: Breast-feeding is not recommended.


Nursing Implications

Assist with ambulation


Dosage Forms

Tablet, as maleate: 1 mg


References

Joske DJ, "Dystonic Reaction to Azatadine," Med J Aust, 1984, 141(7):449.


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