Pharmacological optimization of antihistamine profile
DOI: 10.32364/2587-6821-2022-6-2-92-97
E.N. Kareva
I.M. Sechenov First Moscow State Medical University (Sechenov University),
Moscow, Russian Federation
Pirogov Russian National Research Medical University, Moscow, Russian Federation
Antihistamines are the first-line treatment for allergic diseases. The optimization of pharmacological properties of these pharmacotherapeutics is provided by the synthesis of new molecules with better safety profile (no penetration via the blood-brain barrier or less risk of drug interactions) or more selective affinity to H1-receptors (active optical isomer). In real clinical practice, drugs with extrahepatic metabolism have an advantage, the effectiveness of which does not depend on concomitant therapy, and the maximum concentration is reached in the shortest possible time, which ensures a rapid onset of action. Comfort use and, therefore, adherence to treatment is also an essential aspect of pharmacotherapy. Current orodispersible H1-receptor antagonists have a clinically significant antihistamine effect and agree with patient expectations due to comfort use and no need to take them with water. As a result, these medications are suitable for specific categories of individuals, e.g., children, patients with difficulty of swallowing, and people practicing an active lifestyle.
Keywords: histamine, antihistamines, levocetirizine, pharmacokinetics, pharmacodynamics, orodispersible forms, compliance.
For citation: Kareva E.N. Pharmacological optimization of antihistamine profile. Russian Medical Inquiry. 2022;6(2):92–97 (in Russ.). DOI: 10.32364/2587-6821-2022-6-2-92-97.
Acknowledgments
The technical edition is supported by LLC "Dr. Reddy’s Laboratories".
About the author:
Elena N. Kareva — Dr. Sc. (Med.), professor of the Department of Pharmacology, Institute of Biodesign and Modeling of Complex Systems, I.M. Sechenov First Moscow State Medical University (Sechenov University); 13, Nikitskiy Blvd., Moscow, 119019, Russian Federation; professor of the Department of Molecular Pharmacology and Radiobiology, Pirogov Russian National Research Medical University; 1, Ostrovityanov str., Moscow, 117437, Russian Federation; ORCID iD 0000-0002-9441-3468.
Contact information: Elena N. Kareva, e-mail: kareva_e_n@staff.sechenov.ru.
Financial Disclosure: the author has no a financial or property interest in any material or method mentioned.
There is no conflict of interests.
Received 20.01.2022.
Revised 14.02.2022.
Accepted 14.03.2022.
2. Gushchin I.S. Prospects for improving the antiallergic action of H1-antihistamines. Lechaschi vrach. 2009;5:64–67 (in Russ.).
3. Yanai K., Yoshikawa T., Yanai A. et al. The clinical pharmacology of non-sedating antihistamines. Pharmacol Ther. 2017;178:148–156. DOI: 10.1016/j.pharmthera.2017.04.004.
4. Grant J.A., Danielson L., Rihoux J.P., DeVos C. A double-blind, single-dose, crossover comparison of cetirizine, ebastine, epinastine, fexofenadine, terfenadine, and loratadine versus placebo: suppression of histamine-induced wheal and flare response for 24 h in healthy male subjects. Allergy. 1999;54(7):700–707. DOI: 10.1034/j.1398-9995.1999.00032.x.
5. McConathy J., Owens M.J. Stereochemistry in Drug Action. Prim Care Companion J Clin Psychiatry. 2003;5(2):70–73. DOI: 10.4088/pcc.v05n0202.
6. García-Zepeda S., Estrada-Muñiz E., Elizondo G. et al. Levocetirizine inhibits migration of immune cells to lymph nodes and induces treg cells in a murine type I allergic conjunctivitis model. Open Ophthalmol J. 2012;6:129–136. DOI: 10.2174/1874364101206010129.
7. Mahmoud F., Arifhodzic N., Haines D., Novotney L. Levocetirizine modulates lymphocyte activation in patients with allergic rhinitis. J Pharmacol Sci. 2008;108(2):149–156. DOI: 10.1254/jphs.08037fp.
8. Bachert C., Maspero J. Efficacy of second-generation antihistamines in patients with allergic rhinitis and comorbid asthma. J Asthma. 2011;48(9):965–973. DOI: 10.3109/02770903.2011.616616.
9. Weber-Schoendorfer C., Schaefer C. The safety of cetirizine during pregnancy. A prospective observational cohort study. Reprod Toxicol. 2008;26(1):19–23. DOI: 10.1016/j.reprotox.2008.05.053.
10. Gillard M., Christophe B., Wels B. et al. H1 antagonists: receptor affinity versus selectivity. Inflamm Res. 2003;52 Suppl 1:S49–S50. DOI: 10.1007/s000110300050.
11. Dos Santos R.V., Magerl M., Mlynek A., Lima H.C. Suppression of histamine- and allergen-induced skin reactions: comparison of first- and second-generation antihistamines. Ann Allergy Asthma Immunol. 2009;102(6):495–499. DOI: 10.1016/S1081-1206(10)60123-8.
12. Kareva Ye.N. The choice of an antihistamine drug: a pharmacologist’s point of view. RMJ. 2016;12:811–816 (in Russ.).
13. Hussein Z., Pitsiu M., Majid O. et al. Retrospective population pharmacokinetics of levocetirizine in atopic children receiving cetirizine: the ETAC study. Br J Clin Pharmacol. 2005;59(1):28–37. DOI: 10.1111/j.1365-2125.2005.02242.x.
14. Parisi G.F., Leonardi S., Ciprandi G. et al. Antihistamines in children and adolescents: A practical update. Allergol Immunopathol (Madr). 2020;48(6):753–762. DOI: 10.1016/j.aller.2020.02.005.
15. Emel’ianov A.V., Kochergin N.G., Goriachkina L.A. The history and modern approaches to clinical use of antihistaminic drugs. Russian journal of clinical dermatology and venereology. 2010;8(4):62–70 (in Russ.).
16. Walsh G.M. The anti-inflammatory effects of levocetirizine — are they clinically relevant or just an interesting additional effect? Allergy Asthma Clin Immunol. 2009;5(1):14. DOI: 10.1186/1710-1492-5-14.
17. Simons F.E. Early Prevention of Asthma in Atopic Children (EPAAC) Study Group. Safety of levocetirizine treatment in young atopic children: An 18-month study. Pediatr Allergy Immunol. 2007;18(6):535–542. DOI: 10.1111/j.1399-3038.2007.00558.x.
18. Day J.H., Briscoe M.P., Rafeiro E., Ratz J.D. Comparative clinical efficacy, onset and duration of action of levocetirizine and desloratadine for symptoms of seasonal allergic rhinitis in subjects evaluated in the Environmental Exposure Unit (EEU). Int J Clin Pract. 2004;58(2):109–118. DOI: 10.1111/j.1368-5031.2004.0117.x.
19. Frossard N., Strolin-Benedetti M., Purohit A., Pauli G. Inhibition of allergen-induced wheal and flare reactions by levocetirizine and desloratadine. Br J Clin Pharmacol. 2008;65(2):172–179. DOI: 10.1111/j.1365-2125.2007.03009.x.
20. Snidvongs K., Seresirikachorn K., Khattiyawittayakun L., Chitsuthipakorn W. Sedative Effects of Levocetirizine: A Systematic Review and Meta-Analysis of Randomized Controlled Studies. Drugs. 2017;77(2):175–186. DOI: 10.1007/s40265-016-0682-0.
21. Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006. Levocetirizine. 2021 Sep 20. PMID: 30000658.
22. Middleton P.G., Gade E.J., Aguilera C. et al. ERS/TSANZ Task Force Statement on the management of reproduction and pregnancy in women with airways diseases. Eur Respir J. 2020;55(2):1901208. DOI: 10.1183/13993003.01208-2019.
23. Ferrer M. Pharmacokinetic evaluation of levocetirizine. Expert Opin Drug Metab Toxicol. 2011;7(8):1035–1047. DOI: 10.1517/17425255.2011.590131.
24. Oleneva E.V., Ryvkin P.V., Ladyzhenskiy M.Ya., Mosolov S.N. Orodispersible dosage forms: possibilities of application in psychiatry. Sovremennaya terapiya psikhicheskikh rasstroystv. 2018;4:31–39 (in Russ.). DOI: 10.21265/PSYPH.2018.47.21792.
25. Serpelloni M. Mouth-dispersed solid medicinal formulation. Patent for invention RU2317812C2. Published on 27.02.2008. Bulletin #6 (in Russ.).
26. Instructions for use of the medicinal product. Levocetirizine. (Electronic resource.) URL: https://grls.rosminzdrav.ru/Grls_View_v2.aspx?routingGuid=d8b3682d-9729–40b7-a890-cedeb90e9286&t= (access date: 02.10.2022) (in Russ.).
27. Nikiforova G.N., Svistushkin V.M., Slavskiy A.N., Pshonkina D.M. Possibilities of use of the modern antihistamine medicines in therapy of patients with allergic rhinitis. Medical council. 2017;8:92–99 (in Russ.). DOI: 10.21518/2079-701X-2017-8-92-98.
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