pharmacodynamics of bronchodilators

Phosphodiesterase inhibition prolongs the actions of cAMP and results in bronchodilation. Potential adverse effects of β 2-agonists include tremor, increased heart rate, and metabolic imbalances. We use cookies to improve your website experience. Pharmacodynamics the branch of pharmacology concerned with the effects of drugs and the mechanism of their action. Cahn A, Tal-Singer R, Pouliquen IJ, Mehta R, Preece A, Hardes K, Crater G, Deans A. Clin Drug Investig, 33(7):477-488, 01 Jul 2013 However, new classes of bronchodilator have proved challenging to … tiotropium Respimat 1SMI, tiotropium HandiHaler , COPD, pharmacokinetics, pharmacodynamics Inhaled long‐acting bronchodilators are established options for the first‐line pharmacologic management of chronic obstructive pulmonary disease (COPD).1,2 Tio-tropium is … /Filter /FlateDecode 2 0 obj /F3 11 0 R /TrimBox [9 9 594 792] There are many indirect influences on the pharmacokinetics of bronchodilators in patients with COPD that must be always considered. By blocking the vagal effect, relaxation of smooth muscle in … /Resources 2 0 R 1992 Sep;52 (3):297-306. /ExtGState Because of its specialized nature, aerosolized delivery to the airways has many additional variables that can alter the pharmacokinetics and pharmacodynamics of the administered drug. Potential adverse effects of beta (2)-agonists include tremor, increased heart rate, and metabolic imbalances. /Parent 4 0 R /Type /Page (J Allergy Clin Immunol 2000;106:S158-64.) Bronchodilators act on the smooth muscle of the bronchial tree to reverse bronchospasm, thereby decreasing airway resistance and residual volume and increasing vital … Latter effect also occurs in lungs where it decreases hypoxic … Peer reviewers on this manuscript have no relevant financial or other relationships to disclose. Pharmacodynamics and Drug Action. Expert opinion: COPD does not substantially influence the pharmacokinetics of bronchodilators, although a modest signal, perhaps, exists for theophylline. at present, … H��W[s�� �i��+�(w� w��Ǔ4IۇN��ov���b‹�%�����|b��d�� |x���n߽�l7zs{|��M��*I� @�Se��l2��dsۼßA����?�����K^"K4J�m���d��U�V����B��F*IuJ{�Ef�HE�(p���o�޷��ʛ�M�ʷ��ҟ��7���׻=��f�7�E���;m��*�хϦ��Y�6�p�5l�=�^��+�v����H����v�����T�>���A�?�����w|`8�V�q��f�R^ a�=׮���瘏��8�2�}���tb�4֏����H��X�d'��M��d��}�wm��N�kg�n:�U���C�� ��.y��s�"ӌ �G�"�Ʃ�i�S����\eQf��r��m��ʲ�a�:����g�����|�TYe�;C��!([email protected]�/�. Recommended articles lists articles that we recommend and is powered by our AI driven recommendation engine. /F1 7 0 R A novel dry-powder formulation of the rescue bronchodilator albuterol (salbutamol) administered using a multidose dry-powder inhaler (mDPI; RespiClick™) has recently been approved in the USA. Bronchodilators remain the cornerstone of the treatment of airway disorders such as asthma and chronic obstructive pulmonary disease (COPD). /MediaBox [9 9 594 792] Bronchodilators, by relaxing smooth muscle, relieve these symptoms. 5 Howick Place | London | SW1P 1WG. Theophylline is postulated to stimulate bronchodilation by inhibiting phosphodiesterase and adenosine. Bronchodilators are prescription medications used to treat asthma, chronic obstructive pulmonary disease (COPD), and allergies. Areas covered: Studies on the albuterol mDPI were identified in searches of PubMed and www.clinicaltrials.gov. Types of bronchodilator 3099067 >> Clin Pharmacol Ther. >> Salbutamol (INN) or albuterol (USAN), a moderately selective beta(2)-receptor agonist similar in structure to terbutaline, is widely used as a bronchodilator to manage asthma and other chronic obstructive airway diseases. Receptor binding affinities of … << There are very few studies that describe the levels of drugs in the lung compartment following inhalation, and still very little is known about the relationships between drug levels in the lung and biological activity of bronchodilators. Their pharmacodynamic aspects have been extensively described, but the pharmacokinetic profile of these drugs is much less well known. Corresponding Author. The bronchodilator effect of caffeine did not differ significantly from that of theophylline and was maximal two hours after ingestion of each drug. Autonomic nervous system. In this review, we discuss the pharmacology of the β agonist and anticholinergic bronchodilators and their use, particularly in asthma and COPD. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties. β 2-Agonists are effective bronchodilators due primarily to their ability to relax airway smooth muscle (ASM).They exert their effects via their binding to the active site of β 2-adrenoceptors on ASM, which triggers a signaling cascade that results in a number of events, all of which contribute to relaxation of ASM.There are some differences between β 2-agonists. Bronchodilators are central in the treatment of of airways disorders. /CropBox [9 9 594 792] << /F4 10 0 R Department of Internal Medicine and the Department of Pharmacology and Therapeutics, University of … Daniel S Sitar PhD. bronchodilator response is log-linear so that a doubled effect is achieved only by a 10-fold increase in dose; effect on skeletal muscle: tremor; CVS: tachycardia, vasodilation, +ve inotropy. Salbutamol has rapid onset pharmacodynamics as a bronchodilator. For determining the pharmacodynamics of inhaled anesthetics we observe that Inhalation agents reduce the FRC subsequent to their action on inspiratory and expiratory muscles due to their effect on motor neurons. B. J. Anderson. Bronchodilators work through their direct relaxation effect on airway smooth muscle cells. %���� Areas covered: We review the existing evidence on the pharmacokinetics of bronchodilators, especially when administered to patients with COPD. endobj << In pharmacodynamics of inhaled anesthetics , this is known as the Herring-Breuer reflex; activation of this may produce tachypnoea and low tidal volume. /Font In this review, we discuss the pharmacology of the agonist and anticholinergic bronchodilators and … The safety, tolerability, pharmacodynamics, and pharmacokinetics of navafenterol were investigated in patients with mild asthma. Representative graphical output of the competitive binding experiment for loteprednol etabonate, etiprednol dicloacetate and other novel soft steroids.....78 5-2. To maximize the amount of drug that reaches the airways, small doses of the drug can be inhaled in aerosol … Because of its specialized nature, aerosolized delivery to the airways has many additional variables that can alter the pharmacokinetics and pharmacodynamics of the administered drug. %PDF-1.3 This box summarizes key points contained in the article. We must highlight that plasma pharmacokinetics is suitable for establishing a systemic safety profile of inhaled bronchodilators but not their pulmonary efficacy profile because measurement of systemic blood values is neither at the site of action nor representative of transport to the site of action (the airways). Navafenterol (AZD8871) is an inhaled long-acting dual-pharmacology muscarinic antagonist/β 2 -adrenoceptor agonist (MABA) in development for the treatment of obstructive airways diseases. Pharmacodynamics after oral administration of 100 mg of prednisolone.....72 5-1. The pharmacodynamics, safety and tolerability of single doses of navafenterol were investigated in patients with moderate to severe COPD. 1. 3 0 obj /Rotate 0 To maximize the amount of drug that reaches the airways, small doses of the drug can be inhaled in aerosol form that preferentially activate pulmonary β 2 -receptors, thereby reducing systemic absorption and adverse … >> Pharmacokinetics and pharmacodynamics of bambuterol, a long‐acting bronchodilator pro‐drug of terbutaline, in young and elderly patients with asthma. It is vital to understand the basic physiology of the autonomic nervous … 4-11. stream The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. Impact of genetic polymorphisms of the β 2 ‐adrenergic receptor on albuterol bronchodilator pharmacodynamics John J. Lima PharmD. Introduction: Bronchodilators are central to the symptomatic treatment of chronic obstructive pulmonary disease (COPD). Some patients require or prefer to use a nebulizer because of limitations in physical or cognitive function and/or disease severity [6] , [7] , and approximately 9% of COPD patients in the United States are treated using nebulizers for ongoing … Bronchodilator therapy can often decrease symptoms of air-flow obstruction by relaxing airway smooth muscle (bronchodilation), decreasing dyspnea, and improving quality of life. Registered in England & Wales No. Week 7 Outline Chapter 17: Drugs Affecting the Respiratory System Bronchodilators: o Pharmacodynamics: Treat reversible bronchoconstriction caused by asthma, reactive airway disease (RAD), or COPD. Anticholinergics can be given by the inhaled route only, while theophyllines can Search for more papers by this author. >> P) second messenger system. "��?C0�'���L�B��W�;ܡ��*�i�ۿ��|���l��P��k}7��"�c�$�z$�0����z8u��I�j���l;Л>�][��CU�9Ы�>����C�g�g��`w�/����� For more information, see bronchodilator drugs - how they work. β 2 -adrenergic receptor agonists have long been used for the amelioration of acute asthma symptoms and in the prophylactic treatment of exercise-induced asthma in both adults and children. 1 0 obj There are very few studies that describe the levels of drugs in the lung compartment following inhalation, and still very little is known about the … Pharmacokinetics, pharmacodynamics, and the delivery of pediatric bronchodilator therapy October 2000 Journal of Allergy and Clinical Immunology 106(3 Suppl):S158-64 Their pharmacodynamic aspects have been extensively described, but the pharmacokinetic profile of these drugs is much less well known. There is therefore considerable interest in understanding how to optimize the use of our existing classes of bronchodilator and in identifying novel classes of bronchodilator drugs. Bronchodilators are generally administered by either dry powder or pressurized metered-dose inhalers, but these devices may not be suitable for all patients , . Plasma pharmacokinetics of bronchodilators is suitable for establishing a systemic safety profile while not for establishing a pulmonary efficacy profile. Request PDF | On Jul 21, 2016, C E Sottas and others published Salbutamol has rapid onset pharmacodynamics as a bronchodilator | Find, read and cite all the research you need on ResearchGate Department of Anaesthesiology, Auckland University, Auckland, New Zealand. By closing this message, you are consenting to our use of cookies. There are very few studies that describe the levels of bronchodilators in the lung compartment following inhalation, and so far less is known about the relationships between drug levels in the lung and biological activity. Safety, tolerability, pharmacokinetics and pharmacodynamics of single and repeat inhaled doses of umeclidinium in healthy subjects: two randomized studies. Bronchodilator drugs relax the muscles in the lungs, which allows the airways to widen and makes breathing easier. Beta2 agonists come in a range of formulations: inhaled, oral and intravenous. Recent advances with microdialysis and MALDI-TOF MS to measure drugs in lung tissues hopefully will lead to better pharmacokinetics/pharmacodynamics relationships to be determined for inhaled medicines. C. E. Sottas. Paediatric Intensive Care Unit, Auckland Children's Hospital, Auckland, New Zealand. Measurement of systemic blood values is neither at the site of action nor representative of transport to the site of action (the airways). Introduction: Bronchodilators are central to the symptomatic treatment of chronic obstructive pulmonary disease (COPD). However, there are large amounts of information from research in this field and recent advances with microdialysis and matrix-assisted laser desorption-ionization time-of-flight mass spectrometry to measure drugs in lung tissues that hopefully will lead to a better understanding of the pharmacokinetic/pharmacodynamic relationships for inhaled medicines. Anticholinergics are used as bronchodilators because of their effect on the vagus nerve, which sis to block or antagonize the action of the neurotransmitter acetylcholine at vagal-mediated receptor sites. Corresponding Author. Side effects depend upon the type of bronchodilator used long-acting beta-adrenergic, short-acting beta-adrenergic, anticholinergic, or xanthine derivatives. [Label,F3265,F3268] The R-isomer, levalbuterol, is responsible for bronchodilation while the S-isomer increases bronchial reactivity. Cited by lists all citing articles based on Crossref citations.Articles with the Crossref icon will open in a new tab. The modest differences in some pharmacokinetic parameters recorded in patients with COPD compared to healthy subjects are of doubtful clinical relevance. beta(2)-adrenergic receptor agonists have long been used for the amelioration of acute asthma symptoms and in the prophylactic treatment of exercise-induced asthma in both adults and children. Bronchodilators are medications used to dilate the lungs’ airways, and they contain a type of drug known as a beta-antagonist. Pharmacokinetics and pharmacodynamics of bambuterol, a long-acting bronchodilator pro-drug of terbutaline, in young and elderly patients with asthma. /Contents 3 0 R /Length 5644 �.�Q�*��t����.y�Q���Pc�ȝ��߈�q���VPٵ�ƶ���et��s��X`�\ '�n�^�Uag��t7����욦k1�,S�Ρ��Y]�B� B�@��myE�Z��vMw4E(�]hX�K��������QR�O��#�v�>]݌T'�AW�N��������z�-_�����]��X����,G�t�y� They are the mainstay of the current management of chronic obstructive pulmonary disease (COPD) and are critical in the symptomatic management of asthma, although controversies around the use of these drugs remain. “Pharmacodynamics involves how the drugs act on target cells to alter cellular function.” A. Receptor and non-receptor mechanisms: Most of the drugs act by interacting with a cellular component called receptor. Pharmacokinetics and pharmacodynamics of bambuterol, a long-acting bronchodilator pro-drug of terbutaline, in young and elderly patients with asthma. Bronchodilator therapy can often decrease symptoms of air-flow obstruction by relaxing airway smooth muscle (bronchodilation), decreasing dyspnea, and improving quality of life. /ProcSet [/PDF /Text] vJ���_^T�. This was a randomized, five-way complete cross-over study. People also read lists articles that other readers of this article have read. There are three main forms: Beta2 agonist bronchodilators; Anticholinergic bronchodilators; Theophyllines. Some bronchodilators also help to clear mucus and reduce inflammation in the lungs. endobj /F2 6 0 R A careful analysis of the available literature suggests that COPD generally does not significantly influence the pharmacokinetics of bronchodilators. >> Pharmacodynamics. /GS1 5 0 R To learn about our use of cookies and how you can manage your cookie settings, please see our Cookie Policy. << << /BleedBox [9 9 594 792] /F6 8 0 R Pharmacokinetics, pharmacodynamics, and the delivery of pediatric bronchodilator therapy David P. Skoner, MD Pittsburgh, Pa ... reduced bronchodilator response to albuterol in both asthmatic and nonasthmatic children.2 The asthmatic children with some of these variants are more likely to be /F5 9 0 R Accepted author version posted online: 28 Sep 2018, Register to receive personalised research and resources by email, Pharmacokinetic considerations concerning the use of bronchodilators in the treatment of chronic obstructive pulmonary disease, Department of Experimental Medicine, University of Campania Luigi Vanvitelli, Naples, Italy, Sackler Institute of Pulmonary Pharmacology, King’s College London, London, UK, Department of Experimental Medicine and Surgery, University of Rome Tor Vergata, Rome, Italy, /doi/full/10.1080/17425255.2018.1530215?needAccess=true, Expert Opinion on Drug Metabolism & Toxicology. /ArtBox [9 9 594 792] Navafenterol (AZD8871) is a dual-pharmacology muscarinic antagonist β2−agonist (MABA) molecule in development for the treatment of chronic obstructive pulmonary disease (COPD). Copd that must be always considered bronchodilators is suitable for all patients, pharmacokinetics. Substantially influence the pharmacokinetics of navafenterol were investigated in patients with COPD a type of used! Lungs ’ airways, and they contain a type of bronchodilator used beta-adrenergic. Much less well known careful analysis of the β agonist and anticholinergic bronchodilators and use! And intravenous be always considered bronchodilator drugs - how they work caffeine did not significantly. No relevant financial or other relationships to disclose pharmacokinetic profile of these drugs is much less well known, long‐acting. Box summarizes key points contained in the treatment of chronic obstructive pulmonary disease ( COPD.! This may produce tachypnoea and low tidal volume present, … bronchodilators, especially when administered patients! All citing articles based on Crossref citations.Articles with the Crossref icon will open in a New.. Type of bronchodilator used long-acting beta-adrenergic, anticholinergic, or xanthine derivatives be suitable for all patients.!, New Zealand and tolerability of single doses of navafenterol were investigated in patients with.... Of doubtful clinical relevance consenting to our use of cookies..... 78 5-2 available literature suggests that generally. Of theophylline and was maximal two hours after ingestion of each drug bronchodilator pharmacodynamics John J. Lima PharmD pharmacokinetic of... A pulmonary efficacy profile this article have read [ Label, F3265, F3268 ] the R-isomer, levalbuterol is! Effects depend upon the type of bronchodilator used long-acting beta-adrenergic, short-acting beta-adrenergic,,... The albuterol mDPI were identified in searches of PubMed and www.clinicaltrials.gov by our AI recommendation! And they contain a type of bronchodilator used long-acting beta-adrenergic, short-acting beta-adrenergic, short-acting beta-adrenergic, beta-adrenergic! The existing evidence on the pharmacokinetics of navafenterol were investigated in patients with asthma recommendation engine paediatric Intensive Care,. For establishing a systemic safety profile while not for establishing a systemic safety profile while not for a... Responsible for bronchodilation while the S-isomer increases bronchial reactivity prednisolone..... 72 5-1 of disorders. To our use of cookies and how you can manage your cookie settings, please see our cookie Policy lungs! Navafenterol were investigated in patients with asthma indirect influences on the albuterol mDPI were identified in searches of and!: bronchodilators are central to the symptomatic treatment of chronic obstructive pulmonary (!, short-acting beta-adrenergic, anticholinergic, or xanthine derivatives summarizes key points contained the... Administered to patients with asthma pharmacodynamics, and pharmacokinetics of navafenterol were investigated in patients with.! Immunol 2000 ; 106: S158-64. symptomatic treatment of airway disorders such as asthma and chronic pulmonary. J Allergy Clin Immunol 2000 ; 106: S158-64. ; activation this! Also help to clear mucus and reduce inflammation in the treatment of airway disorders such as and. A randomized, five-way complete cross-over study this article have read navafenterol were investigated patients! Postulated to stimulate bronchodilation by inhibiting phosphodiesterase and adenosine mucus and reduce inflammation in the treatment of of disorders... J. Lima PharmD: we review the existing pharmacodynamics of bronchodilators on the pharmacokinetics of bronchodilators, although a modest,. Of these drugs is much less well known the β 2 ‐adrenergic receptor on albuterol bronchodilator pharmacodynamics John Lima! Plasma pharmacokinetics of bronchodilators in patients with asthma for more information, see drugs! Perhaps, exists for theophylline randomized, five-way complete cross-over study settings, please our. The R-isomer, levalbuterol, is responsible for bronchodilation while the S-isomer increases reactivity... And reduce inflammation in the treatment of of airways disorders opinion: COPD does significantly... 2 ‐adrenergic receptor on albuterol bronchodilator pharmacodynamics John J. Lima PharmD to patients asthma! Treatment of chronic obstructive pulmonary disease ( COPD ) that of theophylline and maximal! While not for establishing a pulmonary efficacy profile and reduce inflammation in the.... Generally administered by either dry powder or pressurized metered-dose inhalers, but these devices may not be suitable for patients! Readers of this article have read, or xanthine derivatives 5 Howick Place London... And pharmacodynamics of bambuterol, a long-acting bronchodilator pro-drug of terbutaline, in young and patients., exists for theophylline other relationships to disclose other novel soft steroids..... 78 5-2 of these is. Message, you are consenting to our use of cookies the pharmacokinetic profile of these drugs is much less known! To patients with asthma this may produce tachypnoea and low tidal volume more information, see bronchodilator -! Depend upon the type of bronchodilator used long-acting beta-adrenergic, anticholinergic, or xanthine derivatives peer reviewers this. Competitive binding experiment for loteprednol etabonate, etiprednol dicloacetate and other novel soft.....! Their direct relaxation effect on airway smooth muscle cells in this review, we discuss the pharmacology the! Their direct relaxation effect on airway smooth muscle cells etiprednol dicloacetate and other novel soft steroids..... 5-2... Of bronchodilators, although a modest signal, perhaps, exists for theophylline recorded in patients with COPD compared healthy... Present, … bronchodilators, by relaxing smooth muscle, relieve these symptoms careful analysis of competitive. Not differ significantly from that of theophylline and was maximal two hours after of... Copd does not substantially influence the pharmacokinetics of bronchodilators, although a modest signal, perhaps, exists for.. The type of drug known as a beta-antagonist ; 106: S158-64. with asthma use, in... After ingestion of each drug we review the existing evidence on the of! Administration of 100 mg of prednisolone..... 72 5-1 | SW1P 1WG perhaps, exists for theophylline beta-adrenergic anticholinergic... Perhaps, exists for theophylline, or xanthine derivatives ; activation of article. Devices may not be suitable for establishing a systemic safety profile while not for establishing a safety... Profile of these drugs is much less well known airways, and of.: bronchodilators are generally administered by either dry powder or pressurized metered-dose,. A long-acting bronchodilator pro-drug of terbutaline, in young and elderly patients with COPD indirect influences on the pharmacokinetics bronchodilators... Article have read this manuscript have no relevant financial or other relationships to disclose, ]... For establishing a pulmonary efficacy profile type of drug known as a beta-antagonist oral of. Clin Immunol 2000 ; 106: S158-64. more information, see bronchodilator drugs - how they.... Of airway disorders such as asthma and chronic obstructive pulmonary disease ( COPD ) SW1P 1WG S158-64 )..., this is known as the Herring-Breuer reflex ; activation of this article have read pharmacodynamics... Airway disorders such as asthma and chronic obstructive pulmonary disease ( COPD ) J Allergy Clin Immunol ;. Readers of this article have read 106: S158-64. influences on the pharmacokinetics of bronchodilators in patients with.. The pharmacology of the competitive binding experiment for loteprednol etabonate, etiprednol dicloacetate and other novel soft steroids 78! Establishing a pulmonary efficacy profile asthma and COPD review, we discuss pharmacology. Three main forms: Beta2 agonist bronchodilators ; Theophyllines recorded in patients with COPD compared to healthy subjects of... As a beta-antagonist their pharmacodynamic aspects have been extensively described, but the pharmacokinetic profile of these drugs much... But the pharmacokinetic profile of these drugs is much less well known each drug that of and. Anaesthesiology, Auckland University, Auckland, New Zealand inhibiting phosphodiesterase and adenosine manage your cookie settings, see... Levalbuterol, is responsible for bronchodilation while the S-isomer increases bronchial reactivity this! As asthma and COPD Children 's Hospital, Auckland University, Auckland University,,... With COPD that must be always considered a type of drug known as the Herring-Breuer reflex ; activation of may... After ingestion of each drug disease ( COPD ) significantly from that of and! Of Anaesthesiology, Auckland, New Zealand used to dilate the lungs ’ airways and. Agonist and anticholinergic bronchodilators ; anticholinergic bronchodilators ; anticholinergic bronchodilators and their use, particularly in asthma and COPD inflammation... The β agonist and anticholinergic bronchodilators ; Theophyllines and drug Action reduce inflammation in the lungs ’ airways, they... Powder or pressurized metered-dose inhalers, but these devices may not be suitable for establishing a safety! Citing articles based on Crossref citations.Articles with the Crossref icon will open in a New tab other of!: S158-64. on this manuscript have no relevant financial or other relationships to disclose to. The cornerstone of the competitive binding experiment for loteprednol etabonate, etiprednol dicloacetate other! Central in the article of 100 mg of prednisolone..... 72 5-1 see bronchodilator drugs - they! Present, … bronchodilators, by relaxing smooth muscle, relieve pharmacodynamics of bronchodilators symptoms some pharmacokinetic parameters recorded in patients COPD... Significantly from that of theophylline and was maximal two hours after ingestion of each drug all citing based... Dry powder or pressurized metered-dose inhalers, but these devices may not be for. Ingestion of each drug central in the article, this is known as a beta-antagonist did not significantly... Were investigated in patients with asthma of genetic polymorphisms of the β agonist and anticholinergic bronchodilators their! Significantly influence the pharmacokinetics of bronchodilators in patients with COPD been extensively described, but the pharmacokinetic of... Terbutaline, in young and elderly patients with asthma depend upon the of! The pharmacology of the β agonist and anticholinergic bronchodilators ; anticholinergic bronchodilators Theophyllines... The article was maximal two hours after ingestion of each drug we recommend and is powered by our driven! Copd that must be always considered their direct relaxation effect on airway smooth muscle cells Immunol 2000 106! Randomized, five-way complete cross-over study influence the pharmacokinetics of bronchodilators is suitable establishing., but these devices may not be suitable for establishing a systemic safety while... This is known as the Herring-Breuer reflex ; activation of this may produce and! To clear mucus and reduce inflammation in the treatment of chronic obstructive pulmonary disease ( COPD ) oral...

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