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- Adverse drug reactions associated with asthma medications in children: systematic review of clinical trials.
- Aagaard L1, Hansen EH.Author information 1Faculty of Health Sciences, Institute of Public Health, University of Southern Denmark, J.B. Winsløws Vej 19, 5000, Odense C, Denmark, firstname.lastname@example.org.AbstractBackground Respiratory medications are frequently prescribed for use in children. Several studies have reported information on the safety of asthma medications in clinical studies in adults, but information about safety in children is scarce. Objective To review published clinical trials on the occurrence and characteristics of adverse drug reactions (ADRs) in children, reported for asthma medications licensed for paediatric use. Methods We systematically reviewed the literature following the Preferred Reporting Items for Systematic Reviews and Meta-Analyses statement guidelines. PubMed, Embase, Cochrane Library, PsycINFO, IPA, and CINAHLs databases were searched from origin until July 2013 for studies reporting ADRs for beta2-receptor agonists, inhaled corticosteroids, leukotriene receptor antagonists and combination products in children from birth to age 17. Information on ADR reporting rates, age and gender, type and seriousness of ADRs, design, setting, observation period, type of assessors, and funding sources was extracted from the articles. Results Literature searches resulted in 162 potential relevant articles. However only 12 of these studies were included in this review as they reported information about ADR rates from use of salmeterol, formoterol, fluticasone, montelukast, zafirlukast and budesonide/formoterol in children. The total population was approximately 3,000 children; the majority was 6- to 11-year-olds and two thirds of these were boys. The observation period varied from 1 to 22 months. The most frequently reported ADRs were exacerbation of asthma, respiratory tract infection, cough, fever and headache. Only few ADRs were rated as being serious, however a number of children dropped out of the clinical trials due to serious ADRs, and, therefore, the real number of serious ADRs is probably higher. Conclusions Few clinical trials reporting ADRs from use of asthma medications in children were identified in the literature. These studies reported only a few types of ADRs, the majority being non-serious.
- International journal of clinical pharmacy.Int J Clin Pharm.2014 Feb 23. [Epub ahead of print]
- Background Respiratory medications are frequently prescribed for use in children. Several studies have reported information on the safety of asthma medications in clinical studies in adults, but information about safety in children is scarce. Objective To review published clinical trials on the occu
- PMID 24562976
- Pranlukast inhibits renal epithelial cyst progression via activation of AMP-activated protein kinase.
- Pathomthongtaweechai N1, Soodvilai S1, Chatsudthipong V1, Muanprasat C2.Author information 1Department of Physiology and Research Center of Transport Protein for Medical Innovation, Faculty of Science, Mahidol University, Rama 6 Rd., Rajathevi, Bangkok 10400, Thailand.2Department of Physiology and Research Center of Transport Protein for Medical Innovation, Faculty of Science, Mahidol University, Rama 6 Rd., Rajathevi, Bangkok 10400, Thailand. Electronic address: email@example.com.AbstractCysteinyl leukotriene receptor 1 (CysLT1 receptor) antagonists were found to inhibit chloride secretion in human airway epithelial cells. Since chloride secretion in renal epithelial cells, which shares common mechanisms with airway epithelial cells, plays important roles in renal cyst progression in polycystic kidney disease (PKD), this study was aimed to investigate effects of drugs acting as CysLT1 receptor antagonists on renal cyst progression and its underlying mechanisms. Effects of CysLT1 receptor antagonists on renal cyst growth and formation were determined using Madine Darby canine kidney (MDCK) cyst models. Mechanisms of actions of CysLT1 receptor antagonists were determined using short-circuit current measurement, assays of cell viability and cell proliferation, and immunoblot analysis of signaling proteins. Of the three drugs acting as CysLT1 receptor antagonists (montelukast, pranlukast and zafirlukast) tested, pranlukast was the most promising drug that inhibited MDCK cyst growth and formation without affecting cell viability. Its effect was independent of the inhibition of CysLT1 receptors. Instead, it reduced cAMP-activated chloride secretion and proliferation of MDCK cells in an AMP-activated protein kinase (AMPK)-dependent manner and had no effect on CFTR protein expression. Interestingly, pranlukast enhanced AMPK activation via calcium/calmodulin-dependent protein kinase kinase beta (CaMKKβ) with consequent activation of acetyl-CoA carboxylase (ACC) and suppression of mammalian target of rapamycin (mTOR) pathway. These results indicate that pranlukast retards renal epithelial cyst progression by inhibiting cAMP-activated chloride secretion and cell proliferation via CaMKKβ-AMPK-mTOR pathway. Therefore, pranlukast represents a class of known drugs that may have potential utility in PKD treatment.
- European journal of pharmacology.Eur J Pharmacol.2014 Feb 5;724:67-76. doi: 10.1016/j.ejphar.2013.12.013. Epub 2013 Dec 17.
- Cysteinyl leukotriene receptor 1 (CysLT1 receptor) antagonists were found to inhibit chloride secretion in human airway epithelial cells. Since chloride secretion in renal epithelial cells, which shares common mechanisms with airway epithelial cells, plays important roles in renal cyst progression i
- PMID 24360935
- Simple and Rapid Determination of Zafirlukast in Plasma by Ultra-performance Liquid Chromatography Tandem Mass Spectrometric Method: Application into Pharmacokinetic Study in Rabbits.
- Iqbal M1, Ezzeldin E, Al-Rashood KA, Al-Khamees KI, Khan RM, Raish M, Anwer T.Author information 1Bioavailability Laboratory, College of Pharmacy, King Saud University, Riyadh, KSA.AbstractZafirlukast is a selective leukotriene receptor antagonist used for the prophylaxis and chronic treatment of asthma. The aim of the present study was to develop a simple sensitive ultra-performance liquid chromatography tandem mass spectroscopy method for rapid determination of zafirlukast in plasma. After a simple one step protein precipitation by acetonitrile, zafirlukast and montelukast (IS) were separated on Acquity UPLC BEHTM C18 column (50×2.1 mm, i.d. 1.7 µm, Waters, USA) using a mobile phase of acetonitrile:water containing 10 mM acetic acid (80:20, v/v) at a flow rate of 0.3 mL/min. Zafirlukast and IS were eluted at 0.51 and 1.1 min, respectively with a total run time of only 1.5 min. The mass spectrometric determination was carried out using an electrospray interface operated in the negative mode with multiple reactions monitoring mode. The precursor to product ion transitions of m/z 574.11>462.07 and m/z 584.2>472.1 were used to quantify zafirlukast and IS, respectively. The method was linear in the concentration range of 0.17-600 ng/mL with coefficients of determination greater than 0.996 and lower limit of quantitation of 0.17 ng/mL. Intra-day and inter-day accuracies were 88.3-113.9% and the precisions were ≤12.6%. Zafirlukast was found to stable under various storage and sample processing conditions as per guidelines of bio-analytical method validation. The method developed herein is simple and rapid, and was successfully applied for the pharmacokinetic study in rabbits.
- Drug research.Drug Res (Stuttg).2013 Nov 20. [Epub ahead of print]
- Zafirlukast is a selective leukotriene receptor antagonist used for the prophylaxis and chronic treatment of asthma. The aim of the present study was to develop a simple sensitive ultra-performance liquid chromatography tandem mass spectroscopy method for rapid determination of zafirlukast in plasma
- PMID 24258705
- 高齢者気管支喘息患者における追加治療法の選択 : ロイコトリエン受容体拮抗薬(ザフィルルカスト)と吸入ステロイド薬(フルチカゾンプロピオネート)との比較検討
- 長島 修,熱田 了,原田 紀宏 [他],牧野 文彦,伊藤 潤,梶山 雄一郎,十合 晋作,高橋 和久,福地 義之助
- 順天堂医学 = Juntendo medical journal 55(3), 303-308, 2009-09-30
- NAID 10029497363
- 高齢者気管支喘息患者における追加治療法の選択:-ロイコトリエン受容体拮抗薬 (ザフィルルカスト) と吸入ステロイド薬 (フルチカゾンプロピオネート) との比較検討-
- 長島 修,熱田 了,原田 紀宏,牧野 文彦,伊藤 潤,梶山 雄一郎,十合 晋作,高橋 和久,福地 義之助
- 順天堂医学 55(3), 303-308, 2009
- 目的: 高齢者気管支喘息患者に対する追加治療としての吸入ステロイドの増量治療とロイコトリエン受容体拮抗薬の追加投与治療を比較検討する.対象・方法: 気道過敏性が亢進している中等症持続型気管支喘息患者に対して本検討を行った. 全例フルチカゾンプロピオネート (fluticasone propionate dry powderinhaler: FDP) 400μgが投与されており, 65歳以上の高齢者 …
- NAID 130004712112
- Montelukast Is a Potent and Durable Inhibitor of Multidrug Resistance Protein 2-Mediated Efflux of Taxol and Saquinavir
- , , [他],
- Biological and Pharmaceutical Bulletin 32(12), 2002-2009, 2009
- … Using the MRP2 over-expressing Madin-Darby canine kidney cell line, MDCKII-MRP2, we evaluated whether the clinically approved LTRAs, e.g. montelukast (Singulair™) and zafirlukast (Accolate™), can similarly suppress MRP2-mediated efflux. … We compared the efficacy of increasing concentrations (20—100 μM) of MK-571, montelukast, and zafirlukast, in suppressing the efflux of calcein-AM, a fluorescent MRP substrate, and the radiolabeled [3H-] drugs, taxol and saquinavir. …
- NAID 130000116986
- Zafirlukast comes as a tablet to take by mouth. It is usually taken two times a day, 1 hour before or 2 hours after meals. Try to take zafirlukast at around the same times every day. Follow the directions on your prescription label ...
- Zafirlukast dosing information Usual Adult Dose for Asthma -- Maintenance:-20 mg orally twice a day, 1 hour before or 2 hours after meals Comments:-A dose of 20 mg twice daily was not associated with an increase in the overall ...
- アコレート Accolate