Zafirlukast: Difference between revisions
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== '''What is Zafirlukast?''' == | == '''What is Zafirlukast?''' == | ||
* Zafirlukast ('''Accolate''') is '''a leukotriene receptor antagonists''' (LTRAs) used for the [[chronic]] treatment of [[asthma]]. | * Zafirlukast ('''Accolate''') is '''a leukotriene receptor antagonists''' (LTRAs) used for the [[chronic]] treatment of [[asthma]]. | ||
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[[File:Zafirlukast 3D ball-and-stick.png|thumb|Zafirlukast 3D ball-and-stick]] | [[File:Zafirlukast 3D ball-and-stick.png|thumb|Zafirlukast 3D ball-and-stick]] | ||
<youtube> | <youtube> | ||
title='''{{PAGENAME}}''' | title='''{{PAGENAME}}''' | ||
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height=600 | height=600 | ||
</youtube> | </youtube> | ||
== '''What are the uses of this medicine?''' == | == '''What are the uses of this medicine?''' == | ||
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'''Limitations of use:''' | '''Limitations of use:''' | ||
* Do not take zafirlukast if you need relief right away for a sudden asthma attack. | * Do not take zafirlukast if you need relief right away for a sudden asthma attack. | ||
== '''How does this medicine work?''' == | == '''How does this medicine work?''' == | ||
* Zafirlukast (za" fir loo' kast) is '''a leukotriene receptor antagonist that binds to the CysLT1 and CysLT2 receptors''', thereby interfering with inflammatory pathways that are involved in the pathogenesis of [[asthma]] and [[allergic rhinitis]]. | * Zafirlukast (za" fir loo' kast) is '''a leukotriene receptor antagonist that binds to the CysLT1 and CysLT2 receptors''', thereby interfering with inflammatory pathways that are involved in the pathogenesis of [[asthma]] and [[allergic rhinitis]]. | ||
* Pretreatment with single oral doses of zafirlukast '''inhibits [[bronchoconstriction]] and the early-phase and part of the late-phase inflammatory reactions in asthma'''. | * Pretreatment with single oral doses of zafirlukast '''inhibits [[bronchoconstriction]] and the early-phase and part of the late-phase inflammatory reactions in asthma'''. | ||
* Cysteinyl leukotriene production and receptor occupation have been correlated with the pathophysiology of asthma, including airway [[edema]], smooth muscle constriction, and altered cellular activity associated with the inflammatory process, which contribute to the signs and symptoms of asthma. | * Cysteinyl leukotriene production and receptor occupation have been correlated with the pathophysiology of asthma, including airway [[edema]], smooth muscle constriction, and altered cellular activity associated with the inflammatory process, which contribute to the signs and symptoms of asthma. | ||
== '''Who Should Not Use this medicine ?''' == | == '''Who Should Not Use this medicine ?''' == | ||
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* are allergic to zafirlukast or any of the ingredients in zafirlukast. | * are allergic to zafirlukast or any of the ingredients in zafirlukast. | ||
* have problems with your liver. | * have problems with your liver. | ||
== '''What drug interactions can this medicine cause?''' == | == '''What drug interactions can this medicine cause?''' == | ||
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* Always have a short-acting [[Beta2-adrenergic agonist|beta2-agonist]] medicine (rescue inhaler) with you to treat sudden symptoms. If you do not have a rescue inhaler medicine, talk to your healthcare provider to have one prescribed for you. | * Always have a short-acting [[Beta2-adrenergic agonist|beta2-agonist]] medicine (rescue inhaler) with you to treat sudden symptoms. If you do not have a rescue inhaler medicine, talk to your healthcare provider to have one prescribed for you. | ||
* Take zafirlukast regularly, even if you do not have asthma symptoms. | * Take zafirlukast regularly, even if you do not have asthma symptoms. | ||
== '''What are the dosage forms and brand names of this medicine?''' == | == '''What are the dosage forms and brand names of this medicine?''' == | ||
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This medicine is available in fallowing brand namesː | This medicine is available in fallowing brand namesː | ||
* '''Accolate''' | * '''Accolate''' | ||
=='''What side effects can this medication cause?'''== | =='''What side effects can this medication cause?'''== | ||
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* Changes in behaviour or mood | * Changes in behaviour or mood | ||
* [[Hypersensitivity]] reactions | * [[Hypersensitivity]] reactions | ||
==''' What special precautions should I follow?''' == | ==''' What special precautions should I follow?''' == | ||
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* [[Neuropsychiatric]] events have been reported in adult, adolescent and pediatric patients taking zafirlukast. Patients should be instructed to notify their prescriber if these changes occur. | * [[Neuropsychiatric]] events have been reported in adult, adolescent and pediatric patients taking zafirlukast. Patients should be instructed to notify their prescriber if these changes occur. | ||
* Zafirlukast is excreted in breast milk. zafirlukast should not be administered to mothers who are breast-feeding. | * Zafirlukast is excreted in breast milk. zafirlukast should not be administered to mothers who are breast-feeding. | ||
== '''What to do in case of emergency/overdose?''' == | == '''What to do in case of emergency/overdose?''' == | ||
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* There were no acute toxic effects in humans that could be consistently ascribed to the administration of zafirlukast. | * There were no acute toxic effects in humans that could be consistently ascribed to the administration of zafirlukast. | ||
* It is reasonable to employ the usual supportive measures in the event of an overdose; eg, remove unabsorbed material from the [[gastrointestinal tract]], employ clinical monitoring, and institute supportive therapy, if required. | * It is reasonable to employ the usual supportive measures in the event of an overdose; eg, remove unabsorbed material from the [[gastrointestinal tract]], employ clinical monitoring, and institute supportive therapy, if required. | ||
== '''Can this medicine be used in pregnancy?''' == | == '''Can this medicine be used in pregnancy?''' == | ||
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* There are no adequate and well-controlled trials in pregnant women. | * There are no adequate and well-controlled trials in pregnant women. | ||
* Because animal reproductive studies are not always predictive of human response, zafirlukast should be used during pregnancy only if clearly needed. | * Because animal reproductive studies are not always predictive of human response, zafirlukast should be used during pregnancy only if clearly needed. | ||
=='''Can this medicine be used in children?'''== | =='''Can this medicine be used in children?'''== | ||
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* It is not known if zafirlukast is safe and effective when used in children under 5 years old. | * It is not known if zafirlukast is safe and effective when used in children under 5 years old. | ||
* The effect of zafirlukast on growth in children has not been determined. | * The effect of zafirlukast on growth in children has not been determined. | ||
== '''What are the active and inactive ingredients in this medicine?''' == | == '''What are the active and inactive ingredients in this medicine?''' == | ||
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* '''Active ingredient:''' zafirlukast | * '''Active ingredient:''' zafirlukast | ||
* '''Inactive ingredients:''' croscarmellose sodium, lactose, magnesium stearate, microcrystalline cellulose, povidone, hypromellose, and titanium dioxide. | * '''Inactive ingredients:''' croscarmellose sodium, lactose, magnesium stearate, microcrystalline cellulose, povidone, hypromellose, and titanium dioxide. | ||
== '''Who manufactures and distributes this medicine?''' == | == '''Who manufactures and distributes this medicine?''' == | ||
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* ACCOLATE is a registered trademark of Par Pharmaceutical, Inc. | * ACCOLATE is a registered trademark of Par Pharmaceutical, Inc. | ||
== '''What should I know about storage and disposal of this medication?''' == | == '''What should I know about storage and disposal of this medication?''' == | ||
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* Keep zafirlukast in a tight closed container and keep zafirlukast out of the light. | * Keep zafirlukast in a tight closed container and keep zafirlukast out of the light. | ||
* Keep zafirlukast and all medicines out of the reach of children. | * Keep zafirlukast and all medicines out of the reach of children. | ||
{{antiasthma drugs}} | {{antiasthma drugs}} | ||
{{coststubd}} | {{coststubd}} | ||
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{{AstraZeneca}} | {{AstraZeneca}} | ||
{{Portal bar | Medicine}} | {{Portal bar | Medicine}} | ||
[[Category:Leukotriene antagonists]] | [[Category:Leukotriene antagonists]] | ||
[[Category:Carbamates]] | [[Category:Carbamates]] | ||
Latest revision as of 01:14, 30 March 2025
What is Zafirlukast?[edit]
- Zafirlukast (Accolate) is a leukotriene receptor antagonists (LTRAs) used for the chronic treatment of asthma.
What are the uses of this medicine?[edit]
- Zafirlukast (Accolate) used to help prevent asthma attacks and for the long-term treatment of asthma symptoms in adults and children 5 years and older.
Limitations of use:
- Do not take zafirlukast if you need relief right away for a sudden asthma attack.
How does this medicine work?[edit]
- Zafirlukast (za" fir loo' kast) is a leukotriene receptor antagonist that binds to the CysLT1 and CysLT2 receptors, thereby interfering with inflammatory pathways that are involved in the pathogenesis of asthma and allergic rhinitis.
- Pretreatment with single oral doses of zafirlukast inhibits bronchoconstriction and the early-phase and part of the late-phase inflammatory reactions in asthma.
- Cysteinyl leukotriene production and receptor occupation have been correlated with the pathophysiology of asthma, including airway edema, smooth muscle constriction, and altered cellular activity associated with the inflammatory process, which contribute to the signs and symptoms of asthma.
Who Should Not Use this medicine ?[edit]
This medicine cannot be used in patients who:
- are allergic to zafirlukast or any of the ingredients in zafirlukast.
- have problems with your liver.
What drug interactions can this medicine cause?[edit]
- Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.
- Zafirlukast may affect the way other medicines work, and other medicines may affect how zafirlukast works.
Especially tell your healthcare provider if you take:
- warfarin sodium (Coumadin, Jantoven)
- erythromycin (ERYC, ERY-TAB, PCE)
- theophylline (Elixophyllin, Theo-24, Theochron, Theolair, Uniphyl)
- fluconazole (Diflucan)
Is this medicine FDA approved?[edit]
- Zafirlukast was approved for use in the treatment of asthma in the United States in 1996, and it continues to be widely used with more than 2 million prescriptions filled yearly.
- Other leukotriene receptor antagonists include montelukast and pranlukast, but only montelukast is also available in the United States.
How should this medicine be used?[edit]
Recommended dosage: Adults and Children 12 years of age and older:
- The recommended dose of zafirlukast in adults and children 12 years and older is 20 mg twice daily.
Pediatric Patients 5 through 11 years of age:
- The recommended dose of zafirlukast in children 5 through 11 years of age is 10 mg twice daily.
Patients with Hepatic Impairment:
- Zafirlukast is contraindicated in patients with hepatic impairment including hepatic cirrhosis.
Patients with Renal Impairment:
- Dosage adjustment is not required for patients with renal impairment.
Administration:
- Take your prescribed dose of zafirlukast by mouth at least 1 hour before or 2 hours after meals.
- Zafirlukast does not treat the symptoms of a sudden asthma attack.
- Always have a short-acting beta2-agonist medicine (rescue inhaler) with you to treat sudden symptoms. If you do not have a rescue inhaler medicine, talk to your healthcare provider to have one prescribed for you.
- Take zafirlukast regularly, even if you do not have asthma symptoms.
What are the dosage forms and brand names of this medicine?[edit]
This medicine is available in fallowing doasage form:
- As 10 and 20 mg tablets for oral administration.
This medicine is available in fallowing brand namesː
- Accolate
What side effects can this medication cause?[edit]
The most common side effects of this medicine include: The most common side effects of zafirlukast in people 12 years and older include:
The most common side effects of zafirlukast in children 5 to 11 years include:
- headache
- stomach pain
Zafirlukast may cause serious side effects, including:
- Severe liver problems
- Inflammation of your blood vessels
- Changes in behaviour or mood
- Hypersensitivity reactions
What special precautions should I follow?[edit]
- Cases of life-threatening hepatic failure have been reported in patients treated with zafirlukast. Physicians may consider the value of liver function testing. 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), zafirlukast should be discontinued.
- Zafirlukast is not indicated for use in the reversal of bronchospasm in acute asthma attacks, including status asthmaticus. Therapy with zafirlukast can be continued during acute exacerbations of asthma.
- Coadministration of zafirlukast with warfarin results in a clinically significant increase in prothrombin time (PT).
- Patients with asthma on zafirlukast may present with systemic eosinophilia, eosinophilic pneumonia. 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.
- Neuropsychiatric events have been reported in adult, adolescent and pediatric patients taking zafirlukast. Patients should be instructed to notify their prescriber if these changes occur.
- Zafirlukast is excreted in breast milk. zafirlukast should not be administered to mothers who are breast-feeding.
What to do in case of emergency/overdose?[edit]
Symptoms of overdosage may include:
- rash and upset stomach
Management of overdosage:
- There were no acute toxic effects in humans that could be consistently ascribed to the administration of zafirlukast.
- It is reasonable to employ the usual supportive measures in the event of an overdose; eg, remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring, and institute supportive therapy, if required.
Can this medicine be used in pregnancy?[edit]
- Pregnancy Category B.
- There are no adequate and well-controlled trials in pregnant women.
- Because animal reproductive studies are not always predictive of human response, zafirlukast should be used during pregnancy only if clearly needed.
Can this medicine be used in children?[edit]
- It is not known if zafirlukast is safe and effective when used in children under 5 years old.
- The effect of zafirlukast on growth in children has not been determined.
What are the active and inactive ingredients in this medicine?[edit]
- Active ingredient: zafirlukast
- Inactive ingredients: croscarmellose sodium, lactose, magnesium stearate, microcrystalline cellulose, povidone, hypromellose, and titanium dioxide.
Who manufactures and distributes this medicine?[edit]
Manufactured by:
- Par Pharmaceutical
- Chestnut Ridge, NY U.S.A.
- ACCOLATE is a registered trademark of Par Pharmaceutical, Inc.
What should I know about storage and disposal of this medication?[edit]
- Store zafirlukast at 68°F to 77°F(20°C -25°C ).
- Keep zafirlukast tablets dry.
- Keep zafirlukast in a tight closed container and keep zafirlukast out of the light.
- Keep zafirlukast and all medicines out of the reach of children.
Albuterol, Bitolterol, Formoterol, Metaproterenol, Pirbuterol, Salbutamol, Salmeterol, Terbutaline
Leukotriene Receptor Antagonists
Benralizumab, Mepolizumab, Omalizumab, Reslizumab
| Drugs for obstructive airway diseases: asthma/COPD (R03) | ||||||||||
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