zafirlukast

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A drug that acts as a leukotriene receptor antagonist, reduces the inflammatory process, and is used to treat the signs and symptoms of asthma.

[zafir-, of unknown origin + -lukast, leukotriene receptor antagonist suff. (from rearrangement of (anti)as(thmatic) l(e)uk(otriene receptor antagonis)t).]

Brand names: Accolate®

Chemical formula:

Drug Forms:
• Zafirlukast tablets (below)
• Zafirlukast Oral tablet

Español:
• Tabletas de zafirlukast
• Zafirlukast, Tableta oral

Zafirlukast tablets

What is zafirlukast?

ZAFIRLUKAST (Accolate®) helps to reduce asthma symptoms (coughing, wheezing, shortness of breath, or chest tightness) and control your asthma. It does not provide instant relief and cannot be used to treat a sudden asthma attack. It works only when used on a regular basis to help reduce inflammation and prevent asthma attacks. Zafirlukast is effective in adults and older children. Generic zafirlukast tablets are not yet available.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• an acute asthma attack
• are on corticosteroid therapy, like prednisone or inhalers
• liver disease, like hepatitis
• an unusual or allergic reaction to zafirlukast, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I use this medicine?

Take zafirlukast by mouth (i.e., swallowed) on an empty stomach. This means you should take this medicine at least 1 hour before or 2 hours after a meal. Follow the directions on the prescription label. You should take zafirlukast every day, even when you are not having asthma symptoms. Do not take your medicine more often than directed.

Contact your pediatrician or health care professional regarding the use of this medicine in children under the age of 5 years old. Special care may be needed.

What drug(s) may interact with zafirlukast?

• alprazolam
• aspirin
• astemizole
• carbamazepine
• cilostazol
• cisapride
• clarithromycin
• cyclosporine
• diazepam
• diltiazem
• dofetilide
• doxercalciferol
• erythromycin
• paricalcitol
• phenytoin
• sildenafil
• some medicines for lowering cholesterol (examples: lovastatin, simvastatin)
• some medicines for lowering heart rate or blood pressure (examples: diltiazem, felodipine, nifedipine, quinidine, verapamil)
• terfenadine
• theophylline
• tolbutamide
• voriconazole
• warfarin

Tell your prescriber or health care professional about all other medicines that you are taking, including non-prescription medicines. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What should I watch for while taking zafirlukast?

Zafirlukast is only used to help prevent asthma attacks; it is not used as a "quick-relief" medicine to treat an asthma attack. Therefore, you should always have your "quick-relief" medicine with you to treat an asthma attack. Talk with your prescriber about what you should do if you have an acute asthma attack.

Tell your prescriber or health care professional if your symptoms do not improve or if your asthma gets worse while you are using zafirlukast. If you find that your medicines become less effective in treating your asthma, you should contact your health care professional as soon as possible.

Do not to stop taking or decrease the use of your other asthma treatments, including steroids, when starting zafirlukast unless otherwise directed by their health care prescriber. Follow your prescriber's directions exactly.

Zafirlukast works best if you use it regularly even when you do not have asthma symptoms. Do not stop using your medication without your prescriber's advice.

If you are going to have surgery, tell your health care professional that you take zafirlukast.

What side effects may I notice from using zafirlukast?

Side effects that you should report to your prescriber or health care professional as soon as possible:
• wheezing or continued coughing

Rare or uncommon-signs of allergic reactions:
• skin rash and itching (hives)
• swelling of face, lips, or eyelids
• difficulty breathing

Rare- signs of liver problems:
• brown or dark urine
• fatigue
• loss of appetite
• nausea and vomiting
• severe itching
• yellowing of the eyes or skin

Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• cough, sore throat
• headache
• indigestion or mild stomach ache
• runny or stuffy nose

Where can I keep my medicine?

Keep out of the reach of young children.

Store at room temperature; do not freeze. Protect from light and moisture. Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

Zafirlukast
Systematic (IUPAC) name
cyclopentyl {3-​[2-​methoxy-​4-​({[(2-​methylphenyl)​sulfonyl]​amino}​carbonyl)​benzyl]-​1-​methyl-​1H-​indol-​5-​yl}​carbamate
Identifiers
CAS number	107753-78-6
ATC code	R03DC01
PubChem	5717
DrugBank	APRD00377
Chemical data
Formula	C31H33N3O6S
Mol. mass	575.676 g/mol
Pharmacokinetic data
Bioavailability	Unknown
Protein binding	99%
Metabolism	Hepatic (CYP2C9-mediated)
Half life	10 hours
Excretion	Biliary
Therapeutic considerations
Pregnancy cat.	B1 (Au), B (U.S.)
Legal status	POM (UK)
Routes	Oral

Zafirlukast is an oral leukotriene receptor antagonist (LTRA) for the maintenance treatment of asthma, often used in conjunction with an inhaled steroid and/or long-acting bronchodilator. It is available as a tablet and is usually dosed twice daily. Another leukotriene receptor antagonist is montelukast (Singulair), taken once daily. Zyflo, also used in the treatment of asthma via its inhibition of 5-lipoxygenase, is taken four times per day.

Zafirlukast blocks the action of the cysteinyl leukotrienes on the CysLT1 receptors, thus reducing constriction of the airways, build-up of mucus in the lungs and inflammation of the breathing passages.

Zafirlukast is marketed by Astra-Zeneca with the brand names Accolate, Accoleit, and Vanticon. It was the first LTRA to be marketed in the USA and is now approved in over 60 countries, including the UK, Japan, Taiwan, Italy, Spain, Canada, Brazil, China and Turkey.

A letter was submitted to the FDA by Zeneca Pharmaceuticals on July 22, 1997, notifying them of a change in product labeling that includes the following potential reaction in patients undergoing a dosage reduction of oral steroids who are currently taking zafirlukast:

PRECAUTIONS-Eosinophilic Conditions: The reduction of the oral steroid dose, in some patients on ACCOLATE therapy, has been followed in rare cases by the occurrence of eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy sometimes presenting as Churg Strauss Syndrome, a systemic eosinophilic vasculitis. Although a causal relationship with ACCOLATE has not been established, caution is required when oral steroid reduction is being considered.¹

1- http://www.fda.gov/medWatch/safety/1997/accola.htm

External links

• Accolate, Accoleit, Vanticon (manufacturer's website)
• Zafirlukast (patient information)

v • d • e Drugs for obstructive airway diseases: asthma/COPD (R03) Adrenergics, inhalants Short acting β2-agonists Salbutamol/Levosalbutamol • Fenoterol • Terbutaline • Pirbuterol • Procaterol • Bitolterol • Rimiterol • Carbuterol • Tulobuterol • Reproterol Long acting β2-agonists (LABA) Arformoterol • Bambuterol • Clenbuterol • Formoterol • Salmeterol Ultra LABA: Indacaterol other Epinephrine • Hexoprenaline • Isoprenaline (Isoproterenol) • Orciprenaline (Metaproterenol) Glucocorticoids Beclometasone • Budesonide • Ciclesonide • Fluticasone • Mometasone Anticholinergics/ muscarinic antagonist Ipratropium • Tiotropium Mast cell stabilizers Cromoglicate • Nedocromil Xanthines Doxofylline • Theobromine • Theophylline/Aminophylline Eicosanoid inhibition Leukotriene antagonists Montelukast • Pranlukast • Zafirlukast Lipoxygenase inhibitor Zileuton Thromboxane receptor antagonists Ramatroban • Seratrodast Combination products Budesonide/formoterol • Fluticasone/salmeterol • Ipratropium/salbutamol

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