Is Quifenadine an antihistamine of the first generation? Do we know everything…

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Abstract

Quifenadine was developed in the 1970s in the laboratory of M.D. Mashkovsky and is one of the first examples of the creation of a new class of non-sedative antihistamine with polyfunctional action that combines high selective activity to block histamine receptor type 1 and the ability to block serotonin action and increase tissue histaminase activity.

There is a large experience in the use of quifenadine (based on scientific clinical studies and real clinical practice). The total number of patients involved in the trials reached approximately 2000. The studies evaluated the quifenadipharmacokinetics, pharmacodynamics, clinical efficacy, and safety of the grug. The results of a clinical study of quiphenadine showed high therapeutic efficacy in a variety of allergic diseases (allergic rhinitis, atopy and atom-atopic dermatitis, chronic urticaria).

Quiphenadine meets the current requirements for antihistamines, however, the question remains open, which generation of drugs can be classified as quinuclidine, taking into account all its characteristics and clinical effects.

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About the authors

Dmitry A. Sychev

Russian Medical Academy of Continuous Professional Education

Email: sychevda@rmapo.ru
ORCID iD: 0000-0002-4496-3680
SPIN-code: 4525-7556
Scopus Author ID: 7801389135

MD, Dr. Sci. (Med.), Professor, Academician of the Russian Academy of Sciences

Russian Federation, 2/1 Barrikadnaya street, 125993 Moscow

Natalia M. Nenasheva

Russian Medical Academy of Continuous Professional Education

Email: 1444031@gmail.com
ORCID iD: 0000-0002-3162-2510
SPIN-code: 3363-6170

MD, Dr. Sci. (Med.), Professor

Russian Federation, 2/1 Barrikadnaya street, 125993 Moscow

Oksana V. Sebekina

Russian Medical Academy of Continuous Professional Education; City Clinical Hospital No. 24

Email: Sebekin1@mail.ru
ORCID iD: 0000-0002-3508-9602
SPIN-code: 2922-9398
Scopus Author ID: 6503913655

MD, Cand. Sci. (Med.)

Russian Federation, 2/1 Barrikadnaya street, 125993 Moscow; Moscow

Marina Yu. Peredelskaya

Russian Medical Academy of Continuous Professional Education; City Clinical Hospital No. 24

Author for correspondence.
Email: concy1984@gmail.com
ORCID iD: 0000-0003-2682-8108
SPIN-code: 3363-5507
Scopus Author ID: 57210586164

MD, Cand. Sci. (Med.)

Russian Federation, 2/1 Barrikadnaya street, 125993 Moscow; Moscow

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Supplementary files

Supplementary Files
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1. Fig. 1. Overview of the main functions of histamine receptors (adapted from [1]).

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2. Fig. 2. The level of sedative effect of antihistamines according to the Stanford Sleepiness Scale (adapted from [14]).

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3. Fig. 3. The average concentration of the drug in different modes of taking the drug. Mode 1 ― a single oral dose of 10 mg of hifenadine (Fencarol); mode 2 ― a single oral dose of hifenadine (Fencarol) at a dose of 50 mg; mode 3 ― oral intake of one tablet of 50 mg with 200 ml of water, provided ingestion twice a day for four days (Taking the drug lasted until the morning of the fifth day, 9 doses in total). Adapted from [21].

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