Pulmonology Book

http://www.fpnotebook.com/

Leukotriene Receptor Antagonist

Aka: Leukotriene Receptor Antagonist, Leukotriene Synthesis Inhibitor, Accolate, Zafirlukast, Montelukast, Singulair, Zileuton, Zyflo
  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
      2. Wechsler (2005) Am J Respir Crit Care Med 172(1): 12-8
  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
    2. (2000) Med Lett Drugs Ther 42:22-3
    3. Scow (2007) Am Fam Physician 75:65-70
    4. Wilson (2001) Chest 119:2021-6

Accolate (C0526502)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C062735
English Accolate, accolate, AstraZeneca brand of zafirlukast, Zeneca brand of zafirkulast
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Singulair (C0595724)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C093875
English Singulair, singulairs, singulair, Cahill May Roberts brand of montelukast sodium, Merck Frosst brand of montelukast sodium, Merck Sharp & Dohme brand of montelukast sodium, Merck brand of montelukast sodium
Sources
Derived from the NIH UMLS (Unified Medical Language System)


montelukast (C0298130)

Definition (NCI) The active ingredient in a drug used to treat symptoms of asthma, such as trouble breathing, tight chest, wheezing, coughing, and runny nose. Montelukast blocks the action of a substance that causes airways in the lungs to narrow and causes other symptoms of asthma. It is a type of leukotriene receptor antagonist and a type of antiasthmatic agent.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C093875
SnomedCT 320883008, 373728005, 108619008, 373734003
English MONTELUKAST, montelukast (medication), montelukast, montelukast [Chemical/Ingredient], Montelukast product, Montelukast, Montelukast (substance), Montelukast product (product), Montelukast (product), Montelukast agent (substance), Montelukast agent, Montelukast product (substance)
Spanish montelucast, producto (producto), montelukast (producto), montelucast, producto, montelukast, montelukast (sustancia), montelucast, producto (sustancia), agente con montelukast, agente con montelukast (sustancia)
Sources
Derived from the NIH UMLS (Unified Medical Language System)


zileuton (C0081408)

Definition (NCI) A substance that is used to prevent asthma symptoms and that is being studied in the prevention of lung cancer. It belongs to the family of drugs called leukotriene blockers.
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)
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)
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C063449
SnomedCT 386180009, 108617005
English N-(1-benzo(b)thien-2-ylethyl)-N-hydroxyurea, zileuton, (+-)-N-Hydroxy-N-(1-benzo[b]thien-2-ylethyl)-urea, N-(1-Benzo[b]thien-2-ylethyl)-N-hydroxyurea, zileuton (Zyflo), zileuton (medication), ZILEUTON, zileuton [Chemical/Ingredient], Zileuton (product), Zileuton (substance), Zileuton, ZLT
Spanish zileutona, zileutón, zileutón (producto), zileutona (sustancia), zileutona (producto), zileutón (sustancia)
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Zyflo (C0724508)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C063449
English Zyflo, zyflo, Abbott brand of zileuton
Sources
Derived from the NIH UMLS (Unified Medical Language System)


zafirlukast (C0378466)

Definition (NCI) A drug used to prevent and treat symptoms of asthma. It blocks substances that cause inflammation in the lungs. It is a type of antiasthmatic agent and a leukotriene receptor antagonist.
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.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C062735
SnomedCT 320888004, 108614003, 386880006
English 4-(5-cyclopentyloxycarbonylamino-2-methylindol-3-yl-methyl)-3-methoxy-N-O-tolylsulfonylbenzamide, zafirlukast, Carbamic Acid,(3-((2-methoxy-4-((((2-methylphenyl)sulfonyl)amino)carbonyl)phenyl)methyl)-1-methyl-1H-indol-5-yl)-, Cyclopentyl Ester, Cyclopentyl 3-(2-methoxy-4-((o-tolylsulfonyl)carbamoyl)benzyl)-1-methylindole-5-carbamate, zafirlukast (medication), zafirlukast [Chemical/Ingredient], ZAFIRLUKAST, Zafirlukast, Zafirlukast (product), Zafirlukast (substance)
Spanish Zafirlukast, zafirlukast (producto), zafirlukast (sustancia), zafirlukast
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Navigation Tree