- What is zafirlukast, and how does it work (mechanism of action)?
- What is zafirlukast used for?
- What are the side effects of zafirlukast?
- What is the dosage for zafirlukast?
- Which drugs or supplement interactions occur with this drug?
- What brand names are available for zafirlukast?
- Is this medication safe to use during pregnancy or while breastfeeding?
- What else should you know about zafirlukast?
What is zafirlukast, and how does it work (mechanism of action)?
- Zafirlukast is an oral leukotriene receptor antagonist used for treating asthma. Leukotrienes are a group of chemicals manufactured in the body from arachidonic acid. Release of leukotrienes within the body, for example, by allergic reactions, promotes inflammation in many diseases such as asthma, a disease in which inflammation occurs in the lungs. Zafirlukast blocks the binding of leukotriene types D4 (LTD4), and E4 (LTE4) and the promotion of inflammation.
- Accolate is the brand name for zafirlukast.
- Zafirlukast is available in generic form. You need a prescription for zafirlukast.
What is zafirlukast used for?
- Accolate is an FDA approved prescription drug used for the medical treatment of chronic asthma.
- It also is effective in preventing exercise-induced asthma and in relieving the symptoms of allergic rhinitis.
- For the treatment of asthma, it starts working only after 3 to 14 days of therapy. Therefore, it should not be used for the treatment an acute asthma attack because immediate relief is needed.
What are the side effects of zafirlukast?
The most common health side effects include:
Other health side effects and adverse effects include:
What is the dosage for zafirlukast?
- The recommended dose for the treatment of asthma is 10 mg twice daily for children 5-11 years of age and 20 mg twice daily for individual 12 years of age and older.
- Food reduces the absorption of this medicine.
- Therefore, it should be taken either 1 hour before or 2 hours after meals.
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Which drugs or supplement interactions occur with this drug?
Accolate inhibits the activity of cytochrome isozymes CYP 3A4 and CYP 2C9. The CYP 3A4 isozyme is responsible for metabolism (elimination) of many drugs. Thus far, data in humans are very limited. In one small study, zafirlukast was shown to interact with warfarin (Coumadin, Jantoven), resulting in increased "thinning" of blood and a decreased ability of blood to clot. This can increase the risk of bleeding.
Until more data are available, this medication should be used very cautiously in patients taking drugs metabolized by CYP3A4 including:
- alprazolam (Xanax)
- carbamazepine (Tegretol)
- cyclosporine (Neoral, Sandimmune)
- calcium channel blockers
- felodipine (Plendil)
- isradipine (Dynacirc)
- nicardipine (Cardene)
- nifedipine (Procardia, Adalat)
- nimodipine (Nimotop)
- amlodipine (Norvasc)
- diltiazem (Cardizem; Tiazac; Dilacor)
- lovastatin (Mevacor)
- quinidine (Quinidex, Quinaglute)
- simvastatin (Zocor)
- triazolam (Halcion)
- verapamil (Calan, Isoptin, Verelan, Covera-HS)
Erythromycin reduces the absorption of zafirlukast, potentially reducing its effect.
What brand names are available for zafirlukast?
- Accolate is the brand name available for this medication.
Is this medication safe to use during pregnancy or while breastfeeding?
- Safe use of Accolate for prevention and medical treatment for asthma during pregnancy has not been established. Doctors or other health care professionals may prescribe it during pregnancy if it is felt that its benefits outweigh the potential unknown risks.
- It is secreted into breast milk and should not be used by women who are breastfeeding.
What else should you know about zafirlukast?
- Accolate is available in tablets of 10 mg and 20 mg.
- Keep the medication tablets stored at room temperature, between 15 C and 30 C (59 F and 86 F).
- This medication was approved by the FDA in September 1996.
- If you have questions about this medicine seek medical advise from your doctor or pharmacist.
Zafirlukast (Accolate) is a drug prescribed for the treatment of chronic asthma, preventing exercise-induced asthma, and the symptoms of allergic rhinitis (hay fever). It is not prescribed for acute asthma attacks. Common side effects include nausea, diarrhea, abdominal pain, sore throat, respiratory infections, rhinitis, Drug interactions, dosing, uses, and pregnancy and breastfeeding safety information should be reviewed prior to taking this medication.
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Related Disease Conditions
Asthma is a condition in which hyperreactive airways constrict and result in symptoms like wheezing, coughing, and shortness of breath. Causes of asthma include genetics, environmental factors, personal history of allergies, and other factors. Asthma is diagnosed by a physician based on a patient's family history and results from lung function tests and other exams. Inhaled corticosteroids (ICS) and long-acting bronchodilators (LABAs) are used in the treatment of asthma. Generally, the prognosis for a patient with asthma is good. Exposure to allergens found on farms may protect against asthma symptoms.
Hay Fever (Allergic Rhinitis)
Hay fever (allergic rhinitis) is an irritation of the nose caused by pollen and is associated with the following allergic symptoms: nasal congestion, runny nose, sneezing, eye and nose itching, and tearing eyes. Avoidance of known allergens is the recommended treatment, but if this is not possible, antihistamines, decongestants, and nasal sprays may help alleviate symptoms.
Neutropenia is a marked decrease in the number of neutrophils, neutrophils being a type of white blood cell (specifically a form of granulocyte) filled with neutrally-staining granules, tiny sacs of enzymes that help the cell to kill and digest microorganisms it has engulfed by phagocytosis. Signs and symptoms of neutropenia include gum pain and swelling, skin abscesses, recurrent ear and sinus infections, sore mouth, low-grad fever, pneumonia-like symptoms, and pain and irritation around the rectal area. Neutropenia has numerous causes, for example, infections (HIV, TB, mono); medications (chemotherapy); vitamin deficiencies (anemia); bone marrow diseases (leukemias), radiation therapy, autoimmune destruction of neutrophils, and hypersplenism. Treatment of neutropenia depends upon the cause and the health of the patient.
Chronic Rhinitis and Post-Nasal Drip
Chronic rhinitis and post-nasal drip symptoms include an itchy, runny nose, sneezing, itchy ears, eyes, and throat. Seasonal allergic rhinitis (also called hay fever) usually is caused by pollen in the air. Perennial allergic rhinitis is a type of chronic rhinitis and is a year-round problem, often caused by indoor allergens, such as dust, animal dander, and pollens that may exist at the time. Treatment of chronic rhinitis and post nasal drip are dependent upon the type of rhinitis condition.
Asthma: Over the Counter Treatment
Patients who have infrequent, mild bouts of asthma attacks may use over-the-counter (OTC) medications to treat their asthma symptoms. OTC asthma medicines are limited to epinephrine and ephedrine. These OTC drugs are best used with the guidance of a physician, as there may be side effects and the drugs may not be very effective.
There are many unusual symptoms of asthma, including sighing, difficulty sleeping, anxiety, chronic cough, recurrent walking pneumonia, and rapid breathing. These symptoms may vary from individual to individual. These asthma complexities make it difficult to accurately diagnose and treat asthma.
Asthma in Children
Asthma in children manifests with symptoms such as coughing and wheezing. Rates of asthma in children are increasing. Asthma in children is usually diagnosed based on the description of symptoms. Lung function tests may also be used. A variety of medications are used for the treatment of childhood asthma.
Adult-onset asthma is asthma that is diagnosed in people over 20 years of age. Symptoms include wheezing, coughing, shortness of breath and difficulty breathing. Treatment may involve anti-inflammatory medications or bronchodilators.
Exercise-induced asthma is asthma triggered by vigorous exercise. Symptoms include coughing, shortness of breath, chest tightness, wheezing, and fatigue while exercising. Preventing exercise-induced asthma attacks involves using inhaled medicines before exercising, performing warm-up exercises and cooling down afterward, avoiding exercising outdoors when pollen counts are high, restricting exercise when you have a viral infection, and wearing a mask over your nose and mouth when exercising in cold weather.
There are two types of asthma medications: long-term control with anti-inflammatory drugs and quick relief from bronchodilators. Asthma medicines may be inhaled using a metered-dose inhaler or nebulizer or they may be taken orally. People with high blood pressure, diabetes, thyroid disease, or heart disease shouldn't take OTC asthma drugs like Primatene Mist and Bronkaid.
Occupational asthma is a type of asthma caused by exposure to a substance in the workplace. Symptoms and signs include wheezing, chest tightness, and shortness of breath. The usual treatment for occupational asthma involves removal from exposure and the use of bronchodilators and inhaled anti-inflammatory medicines.
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