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a leukotriene receptor antagonist used in treatment of asthma, administered orally.
Miller-Keane Encyclopedia and Dictionary of Medicine, Nursing, and Allied Health, Seventh Edition. © 2003 by Saunders, an imprint of Elsevier, Inc. All rights reserved.



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.

McGraw-Hill Nurse's Drug Handbook, 7th Ed. Copyright © 2013 by The McGraw-Hill Companies, Inc. All rights reserved


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.
Farlex Partner Medical Dictionary © Farlex 2012


A drug, C31H33N3O6S, that acts as a leukotriene receptor antagonist, reduces the inflammatory process, and is used in the treatment of asthma.
The American Heritage® Medical Dictionary Copyright © 2007, 2004 by Houghton Mifflin Company. Published by Houghton Mifflin Company. All rights reserved.


A blocker of leukotriene D4 and E4 (LTD4 and LTE4) components of a slow-reacting substance of anaphylaxis (SRSA); used for prophylaxis of asthma.
Medical Dictionary for the Health Professions and Nursing © Farlex 2012

Zafirlukast (Accolate)

An inhibitor that prevents leukotrienes from binding to cell receptors; taken over time, zafirlukast can help reduce or prevent asthma symptoms.
Gale Encyclopedia of Medicine. Copyright 2008 The Gale Group, Inc. All rights reserved.
References in periodicals archive ?
A study was carried out by Singh et al., in 2005, which showed that Zileuton, 5-LOX inhibitor and cysteinyl LT receptor antagonists, montelukast, Zafirlukast inhibited the number of writhes in acetic acid-induced writhing method but did not show analgesic activity in tail flick and hot plate methods.
Firstly, the report provides a basic overview of the Zafirlukast Market including its definition, applications and manufacturing technology.
Invion and Hovione will collaborate to develop the proprietary novel technology a dry powder formulation of the compound INV104 (zafirlukast) delivered by Hovione's inhaler.
(13.) 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.
Effect of zafirlukast (Accolate) on cellular mediators of inflammation: Bronchoalveolar lavage fluid findings after segmental antigen challenge.
Wood-Dauphinee, "Effectiveness of the leukotriene receptor antagonist zafirlukast for mild-to-moderate asthma: a randomized, double-blind, placebo-controlled trial," Annals of Internal Medicine, vol.
Two others, montelukast and zafirlukast, were subsequently developed, receiving FDA approval in 1998 and 1999, respectively.
FDA-approved leukotriene inhibitors include montelukast (Singulair and generic) and zafirlukast (Accolate), both of which are prescription tablets.
Solifenacin levels increase in the body with possibility of toxicity when taken with CYP3A4 inhibitors (e.g., clarithromycin [Biaxin[R]], erythromycin, diltiazem [Cardizem[R]], fluconazole [Diflucan[R]]), and protease inhibitors (e.g., quinine, verapamil [Calan[R]], zafirlukast [Accolate[R]]).
Montelukast, marketed under the brand name Singulair, and zafirlukast (Accolate) are the most popular of the LTRAs.
LTRAs are sold under the brand names Singulair (montelukast) and Accolate (zafirlukast).