Evolución, mecanismo de acción y uso clínico de tres generaciones de antihistamínicos

Autores/as

  • Maria Zofia Lisiecka National Medical Institute of the Ministry of the Interior and Administration

DOI:

https://doi.org/10.15649/2346075X.3651

Palabras clave:

Alérgico, Rinitis, Asma, Receptores H1, Alergias, Efecto sedante

Resumen

Introducción. Esta revisión analiza la evolución, mecanismos de acción y aplicaciones clínicas de tres generaciones de antihistamínicos. Materiales y métodos: Se realizó una búsqueda sistemática en bases de datos como PubMed, MEDLINE, Web of Science y Scopus, utilizando términos clave y términos MeSH, abarcando literatura científica publicada entre 1985 y 2023. Resultados y discusión: El estudio revela que el desarrollo de antihistamínicos se originó en la investigación de los mecanismos de anafilaxia y alergia, identificando la histamina como mediador clave. Esto condujo a la síntesis de sustancias antihistamínicas y al surgimiento de tres generaciones de fármacos. Estos fármacos bloquean los receptores H1 de histamina para aliviar los síntomas alérgicos. La primera generación, aunque eficaz, presenta efectos secundarios como sedación debido a su acción no selectiva. Las generaciones posteriores, más selectivas para los receptores H1 periféricos, ofrecen mejor perfil de seguridad. La tercera generación, como metabolitos activos de la segunda, destaca por su eficacia y seguridad. Los antihistamínicos de primera generación se utilizan en situaciones agudas y para alergias locales, mientras que los de segunda y tercera generación son preferidos para la rinitis alérgica estacional y crónica. Conclusiones: La importancia del estudio radica en la posible aplicación de sus resultados en la práctica clínica de los alergólogos. 

Referencias

Gumieniczek A, Lejwoda K, Data N. Chemical stability study of H1 antihistaminic drugs from the first and the second generations, diphenhydramine, azelastine and bepotastine, in pure APIs and the presence of two excipients, citric acid and polyvinyl alcohol. Molecules. 2022;27(23):8322.https://doi.org/10.3390/molecules27238322

Emeryk A. Blastine - A modern antihistamine. Alergoprofil. 2023;19(2):3-7. https://doi.org/10.24292/01.AP.192160623

Mehta P, Miszta P, Filipek S. Molecular modeling of histamine receptors - Recent advances in drug discovery. Molecules. 2021;26(6):1778. https://doi.org/10.3390/molecules26061778

Marko M, Pawliczak R. Pharmacotherapy and immunotherapy of allergic rhinitis induced by house dust mite, grass, and birch pollen allergens: A meta-analysis of randomized clinical trials. Exp Rev Resp Med. 2023;17(7):607-621. https://doi.org/10.1080/17476348.2023.2241364

Arcimowicz M. Allergic rhinitis – Effective treatment according to the latest recommendations. Polish J Otolaryng. 2022;76(6):45-59. https://doi.org/10.5604/01.3001.0016.1488

Walkiewicz G, Jankowska M, Pawliczak R. The effect of drugs used in allergic rhinitis on the central nervous system. Polish J Allerg. 2020;7(4):190-196. https://doi.org/10.5114/pja.2020.102085

Krzystanek M, Krysta K, Pałasz A. First-generation antihistaminic drugs used in the treatment of insomnia-superstitions and evidence. Pharm Psych Neurol. 2020;36(1):33-40. https://doi.org/10.33450/fpn.2020.04.003

Frankiewicz T. Dimenhydrinate – A drug to prevent motion sickness. Med Życ. 2023;10(1-4):28-31. https://journalsmededu.pl/index.php/medycyna_i_zycie/article/view/2905

Richet G. The discovery of anaphylaxis, a brief but triumphant encounter of two physiologists (1902). Hist Sci Méd. 2003;37(4):463-469. https://pubmed.ncbi.nlm.nih.gov/14989211/

Bergmann KC. Milestones in the 20th century. In: History of Allergy. Ettlingen: Karger Medical and Scientific Publishers; 2014. p. 27-45. https://doi.org/10.1159/000358478

Figueroa K, Shankley N. One hundred years of histamine research. In: Histamine in Inflammation. Boston: Springer; 2010. p. 1-9. https://doi.org/10.1007/978-1-4419-8056-4_1

Tan J, Jeffries S, Carr R. A review of histamine-2 receptor antagonist and proton pump inhibitor therapy for gastroesophageal reflux disease in neonates and infants. Paediatric Drugs. 2023;25(5):557-576. https://doi.org/10.1007/s40272-023-00580-z

Nishio Y, Hara M, Oshita K, Jotaki S, Murotani K, Hiraki T. Relationship between Tryptase and Hypotension in Anaphylaxis during Anesthesia. Kurume Med J. 2024;70(12):19-27. https://doi.org/10.2739/kurumemedj.ms7012012

Zhang P, Wan Y, Li H, Lin X. Relationship between perioperative anaphylaxis and history of allergies or allergic diseases: A systematic review and meta-analysis with meta-regression. J Clin Anesth. 2024;94:111408. https://doi.org/10.1016/j.jclinane.2024.111408

Klimek L, Mullol J, Ellis AK. Current management of allergic rhinitis. J Allergy Clin Immunol Pract. 2024;12(6):1399-1412. https://doi.org/10.1016/j.jaip.2024.03.023

Duman N, Duman R, Vurmaz A. Effects of second-generation H1-antihistamine drugs on angiogenesis in in vivo chick chorioallantoic membrane model. Cutan Ocular Toxicol. 2023;42(1):8-11. https://doi.org/10.1080/15569527.2022.2152040

Lieberman P. The basics of histamine biology. Ann Allergy Asthma Immun. 2011;106(2):S2-S5. https://doi.org/10.1016/j.anai.2010.08.005

Chaudhari R, Gosavi S, Bornare P, Sonawane S, Ahire T. An overview of antihistamines and their properties used for treatment of different diseases. Antiinflamm Antiallergy Agents Med Chem. 2023;22(4):220-229. https://doi.org/10.2174/0118715230259623231111165759

Kim JH, Cha HR, Ha EK. Association between first-generation antihistamine use in children and cardiac arrhythmia and ischemic heart disease: a case-crossover study. Pharmaceuticals. 2023;16(8):1073. https://doi.org/10.3390/ph16081073

Linton S, Hossenbaccus L, Ellis AK. Evidence-based use of antihistamines for treatment of allergic conditions. Ann Allergy Asthma Immunol. 2023;131(4):412-420. https://doi.org/10.1016/j.anai.2023.07.019

World Health Organization. Core health indicators in the WHO European Region 2017. Special focus: 2030 Sustainable Development Agenda. Available from: https://www.who.int/europe/publications/i/item/WHO-EURO-2017-4788-44551-63102. Accessed March 15, 2024.

Jacob E, Uthra KT, Gupta S, Chitra V, Damodharan N, Pazhani GP. An emerging antihistamine drug with multiple therapeutic benefits: Bilastine. Pharm Sci Asia. 2024;51(1):1-9. https://doi.org/10.29090/psa.2024.01.23.1200

Bernstein JA, Bernstein JS, Makol R, Ward S. Allergic Rhinitis. JAMA. 2024;331(10):866. https://doi.org/10.1001/jama.2024.0530

Hall-Landers RJ, Morton-Jones ME, Plexico LW, Spray GJ, Sandage MJ. First-Generation OTC antihistamine use and voice function in individuals with allergic rhinitis: a preliminary report of clinically impactful findings. J Voice. 2024. https://doi.org/10.1016/j.jvoice.2024.06.013

Chaudhari R, Gosavi S, Bornare P, Sonawane S, Ahire T. An overview of antihistamines and their properties used for treatment of different diseases. Antiinflamm Antiallergy Agents Med Chem. 2023;22(4):220-229. https://doi.org/10.2174/0118715230259623231111165759

Wang D, Guo Q, Wu Z. Molecular mechanism of antihistamines recognition and regulation of the histamine H1 receptor. Nature Commun. 2024;15(1):84. https://doi.org/10.1038/s41467-023-44477-4

Kim MJ, Kulkarni V, Goode MA, Sivesind TE. Exploring the interactions of antihistamine with retinoic acid receptor beta (RARB) by molecular dynamics simulations and genome-wide meta-analysis. J Mol Graph Model. 2023;124:108539. https://doi.org/10.1016/j.jmgm.2023.108539

Akimoto H, Uesawa Y, Hishinuma S. Molecular determinants of the kinetic binding properties of antihistamines at the histamine H1 receptors. Int J Mol Sci. 2021;22(5):2400. https://doi.org/10.3390/ijms22052400

Nieto A, Nieto M, Mazón Á. The clinical evidence of second-generation H1-antihistamines in the treatment of allergic rhinitis and urticaria in children over 2 years with a special focus on rupatadine. Expert Opin Pharmacother. 2021;22(4):511-519. https://doi.org/10.1080/14656566.2020.1830970

Li L, Liu R, Peng C, Chen X, Li J. Pharmacogenomics for the efficacy and side effects of antihistamines. Exp Dermatol. 2022;31(7):993-1004. https://doi.org/10.1111/exd.14602

Yanai K, Yoshikawa T, Church MK. Efficacy and safety of non-brain penetrating H1-antihistamines for the treatment of allergic diseases. In: The Functional Roles of Histamine Receptors. Cham: Springer; 2021. p. 193-214. https://doi.org/10.1007/7854_2021_265

Miller DW, Lin S, Safa NA, Zhang Y. Blood-brain barrier transporters and central nervous system drug response and toxicity. In: Transporters and Drug‐Metabolizing Enzymes in Drug Toxicity. Hoboken: John Wiley & Sons; 2021. p. 377-412. https://doi.org/10.1002/9781119171003.ch12

Pham L, Baiocchi L, Kennedy L, Sato K, Meadows V, Meng F, Huang CK, Kundu D, Zhou T, Chen L, Alpini G, Francis H. The interplay between mast cells, pineal gland, and circadian rhythm: Links between histamine, melatonin, and inflammatory mediators. J Pineal Res. 2021;70(2):e12699. https://doi.org/10.1111/jpi.12699

Kordulewska NK, Topa J, Rozmus D, Jarmołowska B. Effects of osthole on inflammatory gene expression and cytokine secretion in histamine-induced inflammation in the caco-2 cell line. Int J Mol Sci. 2021;22(24):13634. https://doi.org/10.3390/ijms222413634

Sakur AA, Nashed D, Noureldin I. Green potentiometric determination of some of the third-generation antihistamines: Fexofenadine, desloratadine, and levocetirizine by using new carbon paste electrodes. Talanta Open. 2022;5:100116. https://doi.org/10.1016/j.talo.2022.100116

Song Y, Dan K, Yao Z, Yang X, Chen B. Hao F. Altered gut microbiota in H1-antihistamine-resistant chronic spontaneous urticaria associates with systemic inflammation. Front Cell Infect Microbiol. 2022;12:831489. https://doi.org/10.3389/fcimb.2022.831489

Wolfson AR, Wong D, Abrams EM, Waserman S, Sussman GL. Diphenhydramine: Time to move on? J Allergy Clin Immunol Pract. 2022;10(12):3124-3130. https://doi.org/10.1016/j.jaip.2022.07.018

Hamano H, Ikeda Y, Goda M, Fukushima K, Kishi S, Chuma M, Michiko Y, Niimura T, Takechi K, Imanishi M, Zamami Y, Horinouchi Y, Izawa-Ishizawa Y, Miyamoto L, Ishizawa K, Fujino H, Tamaki T, Aihara K, Tsuchiya K. Diphenhydramine may be a preventive medicine against cisplatin-induced kidney toxicity. Kidney Int. 2021;99(4):885-899. https://doi.org/10.1016/j.kint.2020.10.041

Parisi GF, Leonardi S, Ciprandi G, Corsico A, Licari A, Miraglia Del Giudice M, Peroni D, Salpietro C and Marseglia GL. Cetirizine use in childhood: An update of a friendly 30-year drug. Clin Mol Allergy. 2020;18(1):2. https://doi.org/10.1186/s12948-020-00118-5

DuToit G, Smith P, Muraro A. Identifying patients at risk of anaphylaxis. World Allergy Org J. 2024;17(6):100904. https://doi.org/10.1016/j.waojou.2024.100904

Fujimura R, Asada A, Aizawa M, Kazama I. Cetirizine more potently exerts mast cell-stabilizing property than diphenhydramine. Drug Discov Therap. 2022;16(5):245-250. https://doi.org/10.5582/ddt.2022.01067

Zhang L, Cheng L, Hong J. The clinical use of cetirizine in the treatment of allergic rhinitis. Pharmacology. 2013;92(1-2):14-25. https://doi.org/10.1159/000351843

Renko A, Cortese T, Karagiannis P, Salzman M. Unintentional cetirizine overdose causing anticholinergic syndrome. Am J Emerg Med. 2022;52:270.e1-270.e3. https://doi.org/10.1016/j.ajem.2021.08.062

AlMasoud N, Bakheit AH, Alshammari MFM, Abdel-Aziz HA, AlRabiah H. Loratadine. In: Profiles of Drug Substances, Excipients and Related Methodology. Amsterdam: Elsevier; 2022. p. 55-90. https://doi.org/10.1016/bs.podrm.2021.10.002

Hong D, Weng J, Ye M, Liu Y. Efficacy of different oral H1 antihistamine treatments on allergic rhinitis: A systematic review and network meta-analysis of randomized controlled trials. Braz J Otorhinolaryngol. 2023;89(4):101272. https://doi.org/10.1016/j.bjorl.2023.03.009

Iriarte Sotés P, Armisén M, Usero-Bárcena T, Rodriguez Fernández A, Otero Rivas MM, Gonzalez MT, Meijide Calderón A, Veleiro B. Efficacy and safety of up-dosing antihistamines in chronic spontaneous urticaria: A systematic review of the literature. J Investig Allergol Clin Immunol. 2020;31(4):282-291. https://doi.org/10.18176/jiaci.0649

Chen X, Xiang H, Yang M. Topical cetirizine for treating androgenetic alopecia: A systematic review. J Cosm Dermatol. 2022;21(11):5519-5526. https://doi.org/10.1111/jocd.15309

Mahdy AM, Webster NR. Histamine and antihistamines. Anaesth Intensive Care. 2011;12(7):324-329. https://doi.org/10.1016/j.mpaic.2011.04.012

Ayaz M, Anwar F, Saleem U, Shahzadi I, Ahmad B, Mir A, Ismail T. Parkinsonism attenuation by antihistamines via downregulating the oxidative stress, histamine, and inflammation. ACS Omega. 2022;7(17):14772-14783. https://doi.org/10.1021/acsomega.2c00145

Naicker P, Anoopkumar-Dukie S, Grant GD, Kavanagh JJ. The effects of antihistamines with varying anticholinergic properties on voluntary and involuntary movement. Clin Neurophys. 2013;124(9):1840-1845. https://doi.org/10.1016/j.clinph.2013.04.003

Wang H, Zhang J, You S, Ao Y, Bai Y, Shi H, Ji L, Jia J, Zhang Y, Jia H. Diagnosis and clinical characteristics of patients with non-allergic rhinitis. Chinese J Otorhinol Head Neck Surg. 2014;49(6):501-505. https://europepmc.org/article/med/25241870

Ganga NP. The therapeutic applications of cough medicines in respiratory diseases. Int J Pharm Phytopharm Res. 2021;11(3):6-10. https://doi.org/10.51847/DM6GuOGsgq

Hao J, Brosse L, Bonnet C, Ducrocq M, Padilla F, Penalba V, Desplat A, Ruel J, Delmas P. The widely used antihistamine mepyramine causes topical pain relief through direct blockade of nociceptor sodium channels. The FASEB J. 2021;35(12):e22025. https://doi.org/10.1096/fj.202100976RR

Bachert C, Maspero J. Efficacy of second-generation antihistamines in patients with allergic rhinitis and comorbid asthma. J Asthma. 2011;48(9):965-973. https://doi.org/10.3109/02770903.2011.616616

Milsmann E, Rohdewald P. Placebo-controlled study of the efficacy of topical antihistaminics against histamine-induced pruritus. Dermatologica. 1985;170(5):230-234. https://doi.org/10.1159/000249538

Giallongo A, Parisi, GF, Licari A, Pulvirenti G, Cuppari C, Salpietro C, Marseglia GL, and Leonardi S. Novel therapeutic targets for allergic airway disease in children. Drug Cont. 2019;8:212590. https://doi.org/10.7573/dic.212590

Wesselhoeft R, Rasmussen L, Jensen PB, Jennum PJ, Skurtveit S, Hartz I, Reutfors J, Damkier P, Bliddal M, Pottegård A. Use of hypnotic drugs among children, adolescents, and young adults in Scandinavia. Acta Psych Scand. 2021;144(2):100-112. https://doi.org/10.1111/acps.13329

Chaudhry SK, Susser LC. Considerations in treating insomnia during pregnancy: A literature review. Psychosomatics. 2018;59(4):341-348. https://doi.org/10.1016/j.psym.2018.03.009

Burgazli CR, Rana KB, Brown JN, Tillman F. Efficacy and safety of hydroxyzine for sleep in adults: Systematic review. Human Psychopharm Clin Exp. 2023;38(2):e2864. https://doi.org/10.1002/hup.2864

Simons FE, and Akdis CA. Histamine and H1-antihistamines: celebrating a century of progress. J Allergy Clin Immunol. 2020;146(6):1139-1157. https://doi.org/10.1016/j.jaci.2011.09.005

Wang, L., Wang, C., Lou, H., & Zhang, L. Antihistamine premedication improves safety and efficacy of allergen immunotherapy. Annals of allergy, asthma & immunology. 2021;127(3), 363–371.e1. https://doi.org/10.1016/j.anai.2021.05.023

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2024-08-16

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Lisiecka, M. Z. (2024). Evolución, mecanismo de acción y uso clínico de tres generaciones de antihistamínicos. Innovaciencia, 12(1). https://doi.org/10.15649/2346075X.3651

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