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Leukotriene Receptor AntagonistAka: Leukotriene Synthesis Inhibitor, Accolate, Zafirlukast, Montelukast, Singulair, Zileuton, Zyflo

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  1. Preparations
    1. Zafirlukast (Accolate)
    2. Montelukast (Singulair)
    3. Zileuton (Zyflo)
  2. Mechanism
    1. Attenuates bronchoconstriction and inflammation
    2. Leukotriene receptor antagonists
      1. Zafirlukast (Accolate)
      2. Montelukast (Singulair)
    3. Leukotriene Synthesis Inhibitor
      1. Zileuton (Zyflo)
  3. Indication: Adjunctive in Asthma and Allergic Rhinitis
    1. Moderate Persistent Asthma
    2. Severe Persistent Asthma
    3. Moderate Chronic Obstructive Pulmonary Disease
    4. Aspirin-induced Asthma
    5. Exercise-Induced Bronchospasm
    6. Allergic Rhinitis
  4. Dosing: Zafirlukast (Accolate)
    1. Leukotriene Receptor Antagonist
    2. Avoid at mealtime
      1. Take 1 hour before or 2 hours after meals
    3. Dose
      1. Age >11 years old: 20 mg PO bid
      2. Child 7-11 years old: 10 mg PO bid
  5. Dosing: Montelukast (Singulair)
    1. Leukotriene Receptor Antagonist
    2. Dose
      1. Adults: 10 mg PO qhs
      2. Child age 6 to 14 years: 5 mg PO qhs
      3. Child age 2-5 years: 4 mg PO qhs
  6. Dosing: Zileuton (Zyflo)
    1. Leukotriene Synthesis Inhibitor
    2. Indicated in age only 12 and over
    3. Dose: 600 mg orally four times daily
    4. Hepatotoxicity in 5% (Monitor liver enzymes q3 months)
    5. Drug interactions: Warfarin, theophylline, Propranolol
    6. Expensive ($273 per month)
  7. Efficacy
    1. Modestly effective for maintenance management
    2. Inhaled Steroids are preferred over leukotriene agents
    3. Used as adjunctive therapy in Asthma
    4. Benefit may be limited to patients with the 5-LO and LTC4 polymorphisms
      1. Sampson (2004) RT J Respir Care Practitioners 17:30
      2. Wechsler (2005) Am J Respir Crit Care Med 172(1):12
  8. Adverse Effects
    1. Multiple P450 drug interactions
      1. Potentiates Warfarin
      2. Potentiates Theophylline
      3. Potentiates Propranolol
    2. Some association with Churg-Strauss Syndrome
      1. Systemic Eosinophilic Vasculitis
      2. Vasculitic rash
      3. Pulmonary and cardiac conditions
    3. Hepatotoxicity with Zileuton (Zyflo)
  9. Cost
    1. Among most expensive agents in Asthma
    2. Accolate and Singulair: $90-100 per month
    3. Zyflo: $270 per month
  10. References
    1. (1996) Med Lett Drugs Ther 38:111
    2. (2000) Med Lett Drugs Ther 42:22
    3. Scow (2007) Am Fam Physician 75:65
    4. Wilson (2001) Chest 119:2021

zileuton (C0081408)

Definition (PDQ)A synthetic derivative of hydroxyurea with antiasthmatic properties. The leukotriene inhibitor zileuton blocks 5-lipoxygenase, which catalyzes the formation of leukotrienes from arachidonic acid; causes bronchodilation; decreases bronchial mucous secretion and edema; and may prevent or decrease the symptoms of asthma. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=285649&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=285649&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C26667" NCI Thesaurus)
Definition (NCI)A synthetic derivative of hydroxyurea with antiasthmatic properties. The leukotriene inhibitor zileuton blocks 5-lipoxygenase, which catalyzes the formation of leukotrienes from arachidonic acid; causes bronchodilation; decreases bronchial mucous secretion and edema; and may prevent or decrease the symptoms of asthma. (NCI04)
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC063449
Englishzileuton, ZILEUTON PREPARATION, ZLT
Spanishzileutona
Parent ConceptsLipooxygenase Inhibitor (C1517903), hydroxyurea (C0020402), [RE108] ANTIASTHMA, ANTILEUKOTRIENES (C0973620), Respiratory smooth muscle relaxant (C0304440), 5-lipoxygenase inhibitor (C1289971), Leukotriene Antagonists (C0595726)
SourcesMSH, MTHSPL, NCI, NDFRT, PDQ, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF
Derived from the NIH UMLS (Unified Medical Language System)


montelukast (C0298130)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC093875
Englishmontelukast, Montelukast agent, MONTELUKAST PREPARATION, Montelukast product
Spanishagente con montelukast, montelukast
Parent ConceptsBronchodilator Agents (C0006280), Acetates (C0000979), Quinolines (C0034424), [RE109] ANTIASTHMA, OTHER (C0973621), Leukotriene Antagonists (C0595726), Duplicate concept (C1274013)
SourcesMSH, NCI, NDFRT, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF
Derived from the NIH UMLS (Unified Medical Language System)


zafirlukast (C0378466)

Definition (NCI)A toyl compound with anti-asthmatic property. Zafirlukast selectively and competitively binds and blocks the cysteinyl leukotriene 1 receptor , thereby preventing potent proinflammatory mediators leukotriene C4, D4 and E4 from binding. This prevents leukotriene-mediated actions, including enhanced migration of eosinophils and neutrophils, increased adhesion of leukocytes, increased monocyte and neutrophil aggregation, increased airway edema, inflammation, capillary permeability and bronchoconstriction.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC062735
Englishzafirlukast, ZAFIRLUKAST PREPARATION
Spanishzafirlukast
Parent ConceptsAnti-Asthmatic Agents (C0282556), Tosyl Compounds (C0040493), [RE108] ANTIASTHMA, ANTILEUKOTRIENES (C0973620), Leukotriene Antagonists (C0595726), Duplicate concept (C1274013)
SourcesMSH, MTHSPL, NCI, NDFRT, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF
Derived from the NIH UMLS (Unified Medical Language System)


Accolate (C0526502)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC062735
EnglishAccolate, AstraZeneca brand of zafirlukast, Zeneca brand of zafirkulast
SourcesMSH, NCI, RXNORM
Derived from the NIH UMLS (Unified Medical Language System)


Singulair (C0595724)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC093875
EnglishCahill May Roberts brand of montelukast sodium, Merck brand of montelukast sodium, Merck Frosst brand of montelukast sodium, Merck Sharp & Dohme brand of montelukast sodium, Singulair
SourcesMSH, NCI, RXNORM
Derived from the NIH UMLS (Unified Medical Language System)


Zyflo (C0724508)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC063449
EnglishAbbott brand of zileuton, Zyflo
SourcesMSH, NCI, PDQ, RXNORM
Derived from the NIH UMLS (Unified Medical Language System)



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