II. Preparations
- Zafirlukast (Accolate)
- Montelukast (Singulair)
- Zileuton (Zyflo)
III. Mechanism
- Attenuates bronchoconstriction and inflammation
- Leukotriene Receptor Antagonists
- Zafirlukast (Accolate)
- Montelukast (Singulair)
- Leukotriene Synthesis Inhibitor
- Zileuton (Zyflo)
IV. Indication: Adjunctive in Asthma and Allergic Rhinitis
V. Dosing: Zafirlukast (Accolate)
- Leukotriene Receptor Antagonist
- Avoid at mealtime
- Take 1 hour before or 2 hours after meals
- Dose
- Age >11 years old: 20 mg orally twice daily
- Child 7-11 years old: 10 mg orally twice daily
VI. Dosing: Montelukast (Singulair)
- Leukotriene Receptor Antagonist
- Dose
- Adults: 10 mg orally at bedtime
- Child age 6 to 14 years: 5 mg orally at bedtime
- Child age 2-5 years: 4 mg orally at bedtime
VII. Dosing: Zileuton (Zyflo)
- Leukotriene Synthesis Inhibitor
- Indicated only in age 12 and over
- Dosing
- Dose: 600 mg orally four times daily
- Risks
- Hepatotoxicity in 5% (Monitor liver enzymes q3 months)
- Drug Interactions: Warfarin, Theophylline, Propranolol
- Expensive ($273 per month)
VIII. Efficacy
- Modestly effective for maintenance management
- Inhaled Steroids are preferred over leukotriene agents
- Used as adjunctive therapy in Asthma
- Benefit may be limited to patients with the 5-LO and LTC4 polymorphisms
IX. Adverse Effects
- Multiple P450 Drug Interactions
- Potentiates Warfarin
- Potentiates Theophylline
- Potentiates Propranolol
- Some association with Churg-Strauss Syndrome
- Systemic Eosinophilic Vasculitis
- Vasculitic rash
- Pulmonary and cardiac conditions
- Hepatotoxicity with Zileuton (Zyflo)
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| zafirlukast (on 2/22/2017 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| ZAFIRLUKAST 10 MG TABLET | Generic | $1.31 each |
| ZAFIRLUKAST 20 MG TABLET | Generic | $1.30 each |
| montelukast (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| MONTELUKAST SOD 10 MG TABLET | Generic | $0.10 each |
| MONTELUKAST SOD 4 MG GRANULES | Generic | $3.25 each |
| MONTELUKAST SOD 4 MG TAB CHEW | Generic | $0.18 each |
| MONTELUKAST SOD 5 MG TAB CHEW | Generic | $0.17 each |
| singulair (on 6/8/2017 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| SINGULAIR 10 MG TABLET | Generic | $0.10 each |
| SINGULAIR 4 MG GRANULES | Generic | $3.25 each |
| SINGULAIR 4 MG TABLET CHEW | Generic | $0.18 each |
| SINGULAIR 5 MG TABLET CHEW | Generic | $0.17 each |
| zyflo (on 12/1/2016 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| ZYFLO CR 600 MG TABLET | $28.51 each | |
Ontology: zileuton (C0081408)
| Definition (NCI_NCI-GLOSS) | 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 | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| 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) |
Ontology: montelukast (C0298130)
| Definition (NCI_NCI-GLOSS) | 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 | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | C093875 |
| SnomedCT | 320883008, 108619008, 373734003, 373728005 |
| LNC | LP171622-6 |
| English | montelukast (medication), montelukast, montelukast [Chemical/Ingredient], Montelukast agent, Montelukast (product), Montelukast agent (substance), MONTELUKAST, Montelukast product, Montelukast, Montelukast (substance), Montelukast product (product), Montelukast product (substance) |
| Spanish | montelucast, producto (producto), montelukast (producto), montelucast, producto, agente con montelukast (sustancia), agente con montelukast, montelucast, producto (sustancia), montelukast (sustancia), montelukast |
Ontology: zafirlukast (C0378466)
| Definition (NCI_NCI-GLOSS) | 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 | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| 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 (producto), zafirlukast (sustancia), zafirlukast |
Ontology: Accolate (C0526502)
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | C062735 |
| English | Accolate, accolate, AstraZeneca brand of zafirlukast, Zeneca brand of zafirkulast |
Ontology: Singulair (C0595724)
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | C093875 |
| English | Singulair, 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 |
Ontology: Leukotriene Antagonists (C0595726)
| Definition (MSH) | A class of drugs designed to prevent leukotriene synthesis or activity by blocking binding at the receptor level. |
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | D020024 |
| SnomedCT | 108616001, 372517002 |
| Swedish | Leukotrienblockerare |
| English | ANTAG LEUKOTRIENE, LEUKOTRIENE ANTAG, RECEPT ANTAG LEUKOTRIENE, LEUKOTRIENE RECEPT ANTAG, Leukotriene receptor antagnist, Antagonists, Leukotriene, Antagonists, Leukotriene Receptor, Leukotriene Receptor Antagonists, Receptor Antagonists, Leukotriene, leukotriene inhibitors (medication), leukotriene inhibitors, Leukotriene Antagonists, inhibitors leukotriene receptor, leukotriene antagonist, leukotriene antagonists, leukotriene receptor antagonist, leukotriene receptor antagonists, Leukotriene receptor antagonist, Leukotriene receptor inhibitor (product), Leukotriene receptor inhibitor (substance), Leukotriene receptor inhibitor, Antileukotrienes |
| Czech | leukotrieny - antagonisté, receptory leukotrienů - antagonisté |
| Finnish | Leukotrieeniantagonistit |
| Russian | LEIKOTRIENA ANTAGONISTY, RETSEPTOROV LEIKOTRIENA ANTAGONISTY, ЛЕЙКОТРИЕНА АНТАГОНИСТЫ, РЕЦЕПТОРОВ ЛЕЙКОТРИЕНА АНТАГОНИСТЫ |
| Polish | Antagoniści receptorów leukotrienowych, Antagoniści leukotrienów, Leki antyleukotrienowe |
| Japanese | ロイコトリエン拮抗剤, ロイコトリエンアンタゴニスト, ロイコトリエンレセプターアンタゴニスト, ロイコトリエン受容体アンタゴニスト, ロイコトリエン受容体拮抗剤, ロイコトリエン受容体拮抗物質, ロイコトリエン受容体拮抗薬, ロイコトリエン拮抗物質, ロイコトリエン拮抗薬 |
| Norwegian | Leukotrienantagonister, Leukotrienhemmere, Leukotrienreseptorantagonister |
| Spanish | inhibidor del receptor de leucotrieno (sustancia), inhibidor del receptor de leucotrienos (producto), inhibidor del receptor de leucotrienos (sustancia), inhibidor del receptor de leucotrienos, inhibidor del receptor de leucotrieno, Antagonistas de Leucotrieno, Antagonistas de Receptor de Leucotrieno |
| German | Leukotrien-Antagonisten, Leukotrien-Rezeptor-Antagonisten |
| Italian | Antagonisti dei leucotrieni |
| Portuguese | Antagonistas de Leucotrienos, Antagonistas dos Receptores de Leucotrienos |
| French | Antagonistes des leucotriènes, Antagonistes des récepteurs aux leucotriènes, Antagonistes des récepteurs des leucotriènes |
Ontology: Zyflo (C0724508)
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | C063449 |
| English | Zyflo, zyflo, Abbott brand of zileuton |
