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Pronunciation |
|
(a
ZA ta
deen) |
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U.S. Brand
Names |
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Optimine® |
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Generic
Available |
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No |
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Synonyms |
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Azatadine Maleate |
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Pharmacological Index |
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Antihistamine |
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|
Use |
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Treatment of perennial and seasonal allergic rhinitis and chronic
urticaria |
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Pregnancy Risk
Factor |
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B |
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Contraindications |
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Hypersensitivity to azatadine or to other related antihistamines including
cyproheptadine; patients taking monoamine oxidase inhibitors should not use
azatadine |
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Warnings/Precautions |
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Sedation and somnolence are the most commonly reported adverse
effects |
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Adverse
Reactions |
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>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 |
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Overdosage/Toxicology |
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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. |
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|
Drug
Interactions |
|
Increased effect/toxicity: Procarbazine, CNS depressants, tricyclic
antidepressants, alcohol |
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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 |
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|
Pharmacodynamics/Kinetics |
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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
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Usual Dosage |
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Children >12 years and Adults: Oral: 1-2 mg twice
daily |
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Dietary
Considerations |
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Alcohol: Additive CNS effects, avoid use |
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Mental Health: Effects
on Mental Status |
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Drowsiness is common; rare reports of depression |
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Mental Health:
Effects on Psychiatric
Treatment |
|
Contraindicated with MAOIs; may produce additive CNS depressant effect with
concurrent psychotropic use |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
|
This drug has atropine-like effects and the patient may experience
drowsiness; dry mouth, nose, and throat |
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Patient
Information |
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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. |
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Nursing
Implications |
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Assist with ambulation |
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Dosage Forms |
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Tablet, as maleate: 1 mg |
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References |
|
Joske DJ, "Dystonic Reaction to Azatadine," Med J Aust, 1984,
141(7):449. |
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