montelukast (Singulair)
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Introduction
Tradename: Singulair. Generic August 2012[10]
Indications
- prophylaxis & chronic treatment of asthma in adults & children over 2 years of age
- adjunctive therapy for patients with asthma inadequately controlled on inhaled steroids[5]
- exercise-induced asthma[7]
- bronchospasm
- seasonal allergic rhinitis in adults & children over 2 years of age[4]
Contraindications
* considered safe in pregnancy[11]
Dosage
Tabs: 4, 5 & 10 mg chewable tablets.
Pharmacokinetics
- metabolized in liver by cyt P450 2C9 & 3A4
elimination via liver
1/2life = 2.7-5.5 hours
Adverse effects
- uncommon (< 2%)
- rare
- other
- agitation, aggression, anxiousness, abnormal dreams, hallucinations, depression, insomnia, irritability, restlessness, tremor[9]
- possible association between the use of Singulair & behavior/mood changes, suicidality (suicidal thinking & behavior) & suicide[8][9]
- increased risk for neuropsychiatric disorder (RR=1.1)[13]
- highest risk for anxiety disorder (RR=1.2)[13]
Toxicity:
- no mortality in single doses of 5000 mg/kg in mice & rats.
Drug interactions
- phenobarbital (no dose adjustment recommended)
- any drug which inhibits cyt P450 2C9 or 3A4 can increase montelukast levels
- any drug which induces cyt P450 2C9 or 3A4 can diminish montelukast levels
Mechanism of action
leukotriene D4 receptor inhibitor
More general terms
Additional terms
- allergic angiitis & granulomatosis of Churg-Strauss; eosinophilic granulomatosis with polyangiitis (EGPA)
- cysteinyl leukotriene receptor (LTC4 receptor, LTD4 receptor)
- cytochrome P450 2C9; cytochrome P450 BP-1; cytochrome P450 MP-4; S-mephenytoin-4-hydroxylase; limonene 6-monooxygenase; limonene 7-monooxygenase (CYP2C9, CYP2C10)
- cytochrome P450 3A4 (cytochrome P450 C3, nifedipine oxidase, P450-PCN1, NF-25, CYP3A4)
References
- ↑ Merck & Company
- ↑ Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220233&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 3.0 3.1 Journal Watch 21(19):154, 2001 Knorr et al, Pediatrics 108:e48, 2001
- ↑ 4.0 4.1 Singulair (Montelukast) for Seasonal Allergic Rhinitis Prescriber's Letter 10(2):9 2003 Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=190210&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 5.0 5.1 Journal Watch 23(24):192, 2003 Bjermer L et al, BMJ 327:891, 2003 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/14563743 <Internet> http://bmj.bmjjournals.com/cgi/content/full/327/7420/891
- ↑ Department of Veterans Affairs, VA National Formulary
non formulary drug request - ↑ 7.0 7.1 7.2 Prescriber's Letter 14(7): 2007 Montelukast (Singulair) for Exercise-induced Bronchospasm Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=230707&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 8.0 8.1 FDA MedWatch http://www.fda.gov/medwatch/safety/2008/safety08.htm#Singulair
Prescriber's Letter 15(5): 2008 Singulair (Montelukast) and Suicide Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=240507&pb=PRL (subscription needed) http://www.prescribersletter.com - ↑ 9.0 9.1 9.2 FDA Safety Alert 6/12/2009 Updated Information on Leukotriene Inhibitors: Montelukast (marketed as Singulair), Zafirlukast (marketed as Accolate), and Zileuton (marketed as Zyflo and Zyflo CR) http://www.fda.gov/Drugs/DrugSafety/PostmarketDrugSafetyInformationforPatientsandProviders/DrugSafetyInformationforHeathcareProfessionals/ucm165489.htm
- ↑ 10.0 10.1 Prescriber's Letter 19(4): 2012 CHART: Anticipated Availability of First-Time Generics Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=280401&pb=PRL (subscription needed) http://www.prescribersletter.com
FDA News Release: Aug. 3, 2012 FDA approves first generic versions of Singulair to treat asthma, allergies http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm314436.htm - ↑ 11.0 11.1 Medical Knowledge Self Assessment Program (MKSAP) 17. 18, American College of Physicians, Philadelphia 2015, 2018.
- ↑ 12.0 12.1 Brooks M FDA Adds Boxed Warning to Montelukast Over Mental Health Risks. Medscape - Mar 04, 2020. https://www.medscape.com/viewarticle/926271
- ↑ 13.0 13.1 13.2 Paljarvi T, Forton J, Luciano S et al Analysis of Neuropsychiatric Diagnoses After Montelukast Initiation. JAMA Netw Open. 2022;5(5):e2213643 PMID: https://www.ncbi.nlm.nih.gov/pubmed/35608857 Free article https://jamanetwork.com/journals/jamanetworkopen/fullarticle/2792596
Database
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5311297
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5284590
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=60950
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=60951
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=4248
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5281040
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5281041