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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 ?
Firstly, the report provides a basic overview of the Zafirlukast Market including its definition, applications and manufacturing technology.
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.
Silverman RA, Nowak RM, Korenblat PE, Skobeloff E, Chen Y, Bonuccelli CM, Miller CJ, Simonson SG: Zafirlukast treatment for acute asthma: evaluation in a randomised, double-blind, multicenter trial.
Montelukast, marketed under the brand name Singulair, and zafirlukast (Accolate) are the most popular of the LTRAs.
Zafirlukast tablets are indicated for the prophylaxis and chronic treatment of asthma in adults and children 5 years of age and older.
Par started shipping 10mg and 20mg strengths of zafirlukast tablets on Friday.
Zafirlukast ve diger lokotriyen inhibitorleri ile Churg-Strauss sendromu arasinda bir iliski saptanmis, ancak bu iliski montelukast ile gorulmemistir.
There are two other members of this class of medications, zafirlukast (Accolate) and zileuton (Zyflo).
The drugs affected by the FDA announcement include montelukast (Singulair), zafirlukast (Accolate) and zieuton (Zyflo and Zyflo CR).
The FDA, which issued the call in mid June, 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).
3A4/5 amiodarona, aprepitant, canabi-noides, cimetidina, claritromicina, eritromicina, fluconazol, gemfi-brozil, inhibidores de proteasa, itraconazol, jugo de toronja, ketoconazol, metronidazol, mibe-fradil, norfloxacina, omeprazol, pozaconazol, pristinamicina, quinina, sertralina, telitromicina, voriconazol, zafirlukast Tomados de: Relling MV, Giacomini KM (7) e Isaza MC, et al.