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a leukotriene receptor antagonist used in treatment of asthma, administered orally.



Pharmacologic class: Leukotriene receptor antagonist

Therapeutic class: Antiasthmatic, bronchodilator

Pregnancy risk category B


Antagonizes activity of three leukotrienes at specific receptor sites in airway smooth muscle, inhibiting inflammation


Tablets (coated): 10 mg, 20 mg

Indications and dosages

Prophylaxis and long-term treatment of asthma

Adults and children ages 12 and older: 20 mg P.O. b.i.d.

Children ages 5 to 11: 10 mg P.O. b.i.d.

Off-label uses

• Exercise-induced bronchospasm
• Chronic urticaria


• Hypersensitivity to drug or its components
• Hepatic impairment, including hepatic cirrhosis


Use cautiously in:
• acute asthma attacks
• concurrent use of warfarin
• patients older than age 55
• pregnant patients
• breastfeeding patients (use not recommended)
• children younger than age 5 (safety not established).


• Give at least 1 hour before or 2 hours after a meal.

Adverse reactions

CNS: headache, dizziness, asthenia, insomnia, depression (especially in children and adolescents)

GI: nausea, vomiting, diarrhea, abdominal pain, dyspepsia

Hepatic: hepatic dysfunction including liver failure and death (rare)

Musculoskeletal: joint or back pain, myalgia

Other: fever, infection, pain


Drug-drug.Aspirin: increased zafirlukast blood level

Erythromycin, theophylline: decreased zafirlukast blood level

Warfarin: increased warfarin effects, greater risk of bleeding

Drug-food.Any food: decreased rate and extent of zafirlukast absorption

Patient monitoring

• Assess patient's respiratory status to help evaluate drug efficacy.

Monitor liver function tests closely; watch for signs and symptoms of liver dysfunction.

Patient teaching

• Tell patient to take at least 1 hour before or 2 hours after a meal.
• Advise patient to take exactly as prescribed, even if he is symptom-free.

Tell patient to immediately report asthma attack. Advise him not to use drug for rapid relief of bronchospasm.
• Instruct patient to continue taking other asthma drugs unless prescriber directs otherwise.

Instruct patient to immediately report signs and symptoms of liver dysfunction (nausea, anorexia, fatigue, lethargy, pruritus, jaundice, flulike symptoms, or right upper quadrant abdominal pain).
• Instruct patient or caregiver to report insomnia or depression.
• Instruct female patient to consult prescriber if she plans to breastfeed.
• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs and foods mentioned above.


A blocker of leukotriene D4 and E4 (LTD4 and LTE4) components of a slow-reacting substance of anaphylaxis (SRSA); used for the prophylaxis of asthma attacks.


/za·fir·lu·kast/ (zah-fir´loo-kast) a leukotriene receptor antagonist used as an antiasthmatic agent.


A drug, C31H33N3O6S, that acts as a leukotriene receptor antagonist, reduces the inflammatory process, and is used in the treatment of asthma.


a leukotriene receptor antagonist interfering with substances that cause swelling and tightening of the airway.
indications This drug is used for prophylaxis and chronic treatment of asthma in children and adults.
contraindications Known hypersensitivity to this drug prohibits its use.
adverse effects Adverse effects of this drug include headache, dizziness, nausea, diarrhea, abdominal pain, vomiting, infections, pain, asthenia, myalgia, fever, dyspepsia, and increased ALT.


A blocker of leukotriene D4 and E4 (LTD4 and LTE4) components of a slow-reacting substance of anaphylaxis (SRSA); used for prophylaxis of asthma.

Zafirlukast (Accolate)

An inhibitor that prevents leukotrienes from binding to cell receptors; taken over time, zafirlukast can help reduce or prevent asthma symptoms.
References in periodicals archive ?
The collaboration extends from fully integrated scale-up and manufacture of phase appropriate cGMP Zafirlukast Dry Powder Inhaler for non-clinical and clinical studies to further secure for Hovione the exclusive rights to manufacture commercial supplies of Zafirlukast DPI.
The leukotriene-receptor antagonists montelukast and zafirlukast are also alternatives for treatment of mild persistent asthma.
Animal studies and post-marketing surveillance for zafirlukast and montelukast are reassuring.
She was medicated at home with theophylline, prednisone, albuterol, and zafirlukast.
Accolate, also known as Zafirlukast, is one of a new class of "preventer" medicines called leukotriene modifiers which block the effects of leukotriene - natural substances which trigger inflammation and mucus secretion and cause constriction in the lungs leading to an asthma attack.
Zileuton and zafirlukast are a more recent type of long-term-control medicine.
Of 146 asthmatics who used inhalers as needed, those who also took zafirlukast (sold as Accolate) daily for 13 weeks had 90 percent more days without asthma symptoms and 98 percent more days without episodes of asthma that disturbed their sleep or limited their activity than those who took placebo instead of zafirlukast.
The zafirlukast agreement ends all litigation related to the product and allows Dr.
The agency said the reported neuropsychiatric events included cases of agitation, aggression, anxiety, dream abnormalities and hallucinations, depression, insomnia, irritability, restlessness, suicidal ideation and behavior, and tremor in patients using montelukast (Singulair), zafirlukast (Accolate), and zileuton (Zyflo, Zyflo CR).
Montelukast and zafirlukast are LTRAs that block the actions of leukotrienes, thereby preventing airway hypersensitivityincreased mucus secretion, and increased vascular permeability by alleviating airway inflammation.
2]-agonists * Beclomethasone * Salmeterol * Budesonide * Formoterol * Ciclesonide * Fluticasone Leukotriene receptor antagonists Sustained-release theophylline * Montelukast preparations * Zafirlukast Oral corticosteroids * Prednisone * Prednisolone * Methylprednisone * Methylprednisolone RELIEVERS For quick relief of symptoms and use in acute attacks as when required (PRN) dosage only Short-acting [[beta].
Montelukast and zafirlukast are two examples of anti-leukotriene medications.