(1)zafirlukast will increase the level or effect of sunitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.tacrolimusMonitor Closely (1)zafirlukast will increase the level or effect of tacrolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.tadalafilMonitor Closely (1)zafirlukast will increase the level or effect of tadalafil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.tamoxifenMonitor Closely (1)zafirlukast, tamoxifen. affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor. CYP2C9/10 inhibition decreases tamoxifen metabolism to active metabolites.tazemetostatMonitor Closely (1)zafirlukast will increase the level or effect of tazemetostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.temsirolimusMonitor Closely (1)zafirlukast will increase the level or effect of temsirolimus by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.theophyllineMonitor Closely (1)zafirlukast will increase the level or effect of theophylline by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.Minor (1)theophylline decreases levels of zafirlukast by unknown mechanism. Minor/Significance Unknown.tinidazoleMonitor Closely (1)zafirlukast will increase the level or effect of tinidazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.tipranavirMonitor Closely (1)zafirlukast will increase the level or effect of tipranavir by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.tolbutamideMinor (1)zafirlukast will increase the level or effect of tolbutamide by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.tolterodineMonitor Closely (1)zafirlukast will increase the level or effect of tolterodine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.tolvaptanSerious - Use Alternative (1)zafirlukast will increase the level or effect of tolvaptan by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.trazodoneMinor (1)zafirlukast will increase the level or effect of trazodone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.triamcinolone acetonide injectable suspensionMonitor Closely (1)zafirlukast will increase the level or effect of triamcinolone acetonide injectable suspension by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.triazolamMonitor Closely (1)zafirlukast will increase the level or effect of triazolam by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.vardenafilMonitor Closely (1)zafirlukast will increase the level or effect of vardenafil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.verapamilMonitor Closely (1)zafirlukast will increase the level or effect of verapamil by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.vilazodoneMonitor Closely (1)vilazodone increases levels of zafirlukast by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No dose adjustment needed with mild CYP3A4 inhibitors.vinblastineMinor (1)zafirlukast will increase the level or effect of vinblastine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.vincristineMinor (1)zafirlukast will increase the level or effect of vincristine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.vincristine liposomalMinor (1)zafirlukast will increase the level or effect of vincristine liposomal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.vinorelbineMinor (1)zafirlukast will increase the level or effect of vinorelbine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.voriconazoleMinor (1)zafirlukast will increase the level or effect of voriconazole by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.warfarinMonitor Closely (1)zafirlukast will increase the level or effect of warfarin by affecting hepatic enzyme CYP2C9/10 metabolism. Use Caution/Monitor.zavegepant intranasalSerious - Use Alternative (1)zafirlukast will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. NTCP inhibitors may result in a significant increase in systemic exposure of zavegepant (a NTCP substrate).ziprasidoneMinor (1)zafirlukast will increase the level or effect of ziprasidone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.zolpidemMinor (1)zafirlukast will increase the level or effect of zolpidem by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.zonisamideMinor (1)zafirlukast will increase the level or effect of zonisamide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown. >10% headache (12.9% in age >12 yr) 1-10% Abdominal pain (1.8%) Infection (3.5%) Nausea (3.1%) Diarrhea (2.8%) Generalized pain (1.8%) Vomiting (1.5%) Dyspepsia/gastritits (1.3%) Increased ALT (1.5%) Infection (4%) Back pain (2%) Weakness (2%) Myalgia (2%) Frequency Not Defined Eosinophilia Eosinophilic pneumonia Vasculitis Malaise Bleeding Bruising Contraindications Hypersensitivity Hepatic impairment, including cirrhosis; Cmax and AUC ~50-60% greater than those of normal adults Cautions Increased risk of infection if age >55 yr Not indicated for use in the reversal of bronchospasm in acute asthma attacks, including status asthmaticus; therapy can be continued during acute exacerbations of asthma Coadministration of zafirlukast with warfarin results in a clinically significant increase in prothrombin time (PT); patients on oral warfarin anticoagulant therapy and this drug should have their prothrombin times monitored closely and anticoagulant dose adjusted accordingly Indicated for the chronic treatment of asthma; should be taken regularly as prescribed, even during symptom-free periods; this drug is not a bronchodilator and should not be used to treat acute episodes of asthma Patients receiving therapy should be instructed not to decrease the dose or stop taking any other antiasthma medications unless instructed by a physician Patients should be instructed to notify their physician if neuropsychiatric events occur while using this drug; women who are breast-feeding should be instructed not to take this medication; alternative antiasthma medication should be considered in such patients Bioavailability of this medication may be decreased when taken with food; patients should be instructed to take the medication at least 1 hour before or 2 hours after meals Eosinophillic conditions In rare cases, patients with asthma on this medication may present with systemic eosinophilia, eosinophilic pneumonia, or clinical features of vasculitis consistent with Churg-Strauss syndrome, a condition which is often treated with systemic steroid therapy; physicians should be alert to eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy presenting in their patients These events have usually, but not always, been associated with reductions and/or withdrawal of steroid therapy; the possibility that this medication may be associated with emergence of Churg-Strauss syndrome can neither be excluded nor established Neuropsychiatric events Neuropsychiatric events have been reported in adult, adolescent and pediatric patients taking this medication; post-marketing reports include insomnia and depression The clinical details of some post-marketing reports involving this medication appear consistent with a drug-induced effect; patients and prescribers should be alert for neuropsychiatric events; patients should be instructed to notify their prescriber if these changes occur Prescribers should carefully evaluate the risks and benefits of continuing treatment with this medication if such events occur Hepatotoxicity Cases of life-threatening hepatic failure reported; cases of liver injury without other attributable cause reported from post-marketing adverse event surveillance of patients who have received recommended dose (40 mg/day) In most, but not all post-marketing reports, the patient’s symptoms abated and the liver enzymes returned to normal or near-normal after stopping therapy In rare cases, patients have either presented with fulminant hepatitis or progressed to hepatic failure, liver transplantation and death; in rare post-marketing cases, no clinical symptoms or signs suggestive of liver dysfunction were reported to precede the latter observations Physicians may consider the value of liver function testing.; periodic serum transaminase testing has not proven to prevent serious injury but it is generally believed that early detection of drug-induced hepatic injury along with immediate withdrawal of the suspect drug enhances likelihood for recovery Patients should be advised to be alert for signs and symptoms of liver dysfunction (eg, right upper quadrant abdominal pain, nausea, fatigue, lethargy, pruritus, jaundice, flu-like symptoms, and anorexia) and to contact their physician immediately if they occur; ongoing clinical assessment of patients should govern physician interventions, including diagnostic evaluations and treatment If liver dysfunction is suspected based upon clinical signs or symptoms (eg, right upper quadrant abdominal pain, nausea, fatigue, lethargy, pruritus, jaundice, flu-like symptoms, anorexia, and enlarged liver), should be discontinued Liver function tests, in particular serum ALT, should be measured immediately and the patient managed accordingly; if liver function tests are consistent with hepatic dysfunction, therapy should not be resumed; patients in whom therapy was withdrawn because of hepatic dysfunction where no other attributable cause is identified should not be re-exposed to the drug Pregnancy No teratogenicity was observed at oral doses up to 1600 mg/kg/day in mice (approximately 160 times maximum recommended daily oral dose in adults on mg/m2 basis), up to 2000 mg/kg/day in rats (approximately 410 times the maximum recommended daily oral dose in adults on mg/m2 basis) and up to 2000 mg/kg/day in cynomolgus monkeys (which resulted in approximately 20 times the exposure to drug plus metabolites compared to that from the maximum recommended daily oral dose in adults based on comparison of the AUC values) At an oral dose of 2000 mg/kg/day in rats, maternal toxicity and deaths were seen with increased incidence of early fetal resorption; spontaneous abortions occurred in cynomolgus monkeys at the maternally toxic oral dose of 2000 mg/kg/day; there are no adequate and well-controlled trials in pregnant women; because animal reproduction studies are not always predictive of human response, this medication should be used during pregnancy only if clearly needed Lactation This medication is excreted in breast milk; following repeated 40 mg twice-a-day dosing in healthy women, average steady-state concentrations in breast milk were 50 ng/mL compared to 255 ng/mL in plasma; because of potential for tumorigenicity shown in mouse and rat studies and the enhanced sensitivity of neonatal rats and dogs to adverse effects of this medication should not be administered to mothers who are breast-feedingPregnancy Categories A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk. B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available. Mechanism of Action Inhibits bronchoconstriction as competitive receptor antagonist of leukotrienes D4 & E4; receptor occupation and cysteinyl leukotriene production has been associated with the pathophysiology of ashtma Pharmacokinetics Half-Life: 8-16 hr Onset: 3-14 days Peak plasma concentration: 326 ng/mL (healthy subjects); 568 ng/mL (asthmatics) Peak plasm time: 3 hr (healthy subjects); 3.5 hr (asthmatics) Clearance: 20 L/hr; significantly decreased in cirrhosis and age 65 yr Protein bound: 99% Vd: 70 L Bioavailability: Reduced 40% with food Metabolism: Hepatic CYP2C9 Excretion: Feces (90%); urine (10%) Enzymes inhibited: Hepatic CYP2C9, CYP3A4 BRAND FORM. UNIT PRICE PILL IMAGE Accolate oral- 20 mg tabletAccolate oral- 10 mg tabletzafirlukast oral- 20 mg tabletzafirlukast oral- 10 mg tabletzafirlukast oral- 20 mg tabletzafirlukast oral- 10 mg tabletzafirlukast oral- 10 mg tabletzafirlukast oral- 10 mg tabletzafirlukast oral- 20 mg tabletCopyright © 2010 First DataBank, Inc.Print Patient Educationzafirlukast oral ZAFIRLUKAST - ORAL (ZA-fir-LOO-kast) COMMON BRAND NAME(S): Accolate USES: Zafirlukast is used to control and prevent symptoms (such as wheezing and shortness of breath) caused by asthma. Controlling symptoms of asthma helps you maintain your normal activities and cuts down on time lost from work or school.This medication must be used regularly to be effective. It does not work right away and should not be used to relieve sudden asthma attacks. If an asthma attack occurs, use your quick-relief inhaler (such as albuterol, salbutamol) as prescribed. HOW TO USE: Read the Patient Information Leaflet if available from your pharmacist before you start taking zafirlukast and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth without food as directed by your doctor, usually 2 times daily. Take zafirlukast on an empty stomach at least 1 hour before or 2 hours after meals. The dosage is based on your age.Use this medication regularly to get the most benefit from it. To help you remember, take it at the same times each day. Keep taking this medication even if you feel well. Do not increase your dose, use this drug more often, or stop using it without first consulting your doctor.Get medical help right away if your asthma symptoms worsen or if you are using your quick-relief inhaler more than usual or more often than prescribed. SIDE EFFECTS: Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: mental/mood changes (such as trouble sleeping, agitation, hallucinations, depression, thoughts of suicide), signs of infection (such as sore throat that doesn't go away, fever, cough), numbness/tingling of arms/legs, chest pain, coughing up blood, worsening shortness of breath, muscle/joint pain, swelling ankles/feet.This drug may rarely cause serious (possibly fatal) liver disease. Get medical help right away if you have any symptoms of liver