Names and pronunciation
(za-feer′loo-cast) Accolate
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Drug reference
(za-feer′loo-cast) Accolate
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Func. class.: Bronchodilator
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Chem. class.: Leukotriene receptor antagonist
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Do not confuse: Accolate/Accupril/Accutane
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ACTION: Antagonizes the contractile action of leukotrienes (LTD4, LTE4) in airway smooth muscle; inhibits broncho constriction caused by antigens
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USES: Prophylaxis and chronic treatment of asthma in adults/children >5 yr
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CONTRAINDICATIONS: Hyper sensitivity, hepatic encephalopathy Precautions: Pregnancy, breastfeeding, children, geriatric patients, hepatic dis ease, Churg-Strauss syndrome, acute bronchospasm
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SIDE EFFECTS CNS: Headache, dizziness, suicidal ide- ation, insomnia, fever GI: Nausea, diarrhea, abdominal pain, vomiting, dyspepsia, hepatic failure, hepatitis HEMA: Agranulocytosis OTHER: Infections, pain, asthenia, myal gia, fever, increased ALT, urticaria, rash, angioedema
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INTERACTIONS Increase: plasma levels of zafirlukast— aspirin, acetaminophen Increase: bleeding risk—warfarin, moni tor INR closely Decrease: plasma levels of zafirlukast— erythromycin, theophylline Drug/Food Decrease: bioavailability
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DOSAGE AND ROUTES • Adult/child ≥12 yr: PO 20 mg bid • Child 5-11 yr: PO 10 mg bid
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Available forms: Tabs 10, 20 mg
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Administer: • 1 hr before or 2 hr after meals
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Assess: • Churg-Strauss syndrome (rare): eo- sinophilia, vasculitic rash, worsening pul- monary symptoms, cardiac complications, neuropathy; may be caused by reducing oral corticosteroids • Respiratory rate, rhythm, depth; aus cultate lung fields bilaterally; notify pre scriber of abnormalities; not to be used for acute bronchospasm in acute asthma • Hepatic dysfunction: right upper quadrant abdominal pain, nausea/vomit ing, fatigue, lethargy, pruritus, jaundice, and flulike symptoms, discontinue; moni tor LFTs; should be measured immediately and the patient managed if needed • Pregnancy/breastfeeding: use only if clearly needed; do not breastfeed, ex- creted in breast milk
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Evaluate: • Therapeutic response: ability to breathe more easily
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To check OTC medications, current pre scription medications that may increase stimulation, do not stop other asthma med ications unless instructed to do so • To avoid hazardous activities because dizziness may occur • That if GI upset occurs, to take prod uct with 8 oz water; to take 1-2 hr after a meal; to avoid taking with food if possible because absorption may be decreased Z • To notify prescriber of nausea, vomit- ing, diarrhea, abdominal pain, fatigue, jaundice, anorexia, flulike symptoms (he- patic dysfunction) • Not to use for acute asthma episodes • To take even if symptom free • Not to take if breastfeeding HIGH ALERT
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PHARMACOKINETICS Rapidly absorbed, peak 3 hr, 99% pro tein binding (albumin), extensively metabolized, inhibits CYP2C9 and 3A4 enzyme systems, excreted in feces, clear ance reduced in geriatric patients, hepatic impairment, half-life 10 hr
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• Adult/child ≥12 yr: PO 20 mg bid
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