Bioanalysis of antihistamines for clinical or forensic purposes

Abstract

Antihistamines are a class of drugs that inhibit the action of histamine and are used to alleviate symptoms associated with allergic reactions, but some of them can cause side effects, the most unpleasant and dangerous of which are the sedative effects that may hinder important psychological functions and impair skilled performance. These side effects could decrease safety in certain common and critical tasks, such as driving or operating machinery, leading to accidents. Antihistamines can also cause intoxications, sometimes lethal, especially when co-administered with alcohol or other sedative drugs. Thus, the development of analytical methods for their determination in biological fluids is considered to be useful for the investigation of clinical and forensic cases. These methodologies could also be used for pharmacokinetic studies. Several liquid and a few gas chromatographic methods have been developed for the determination of antihistamines in biological matrices after proper pretreatment procedures. This article reviews the published analytical methodologies that were gathered through the search in PubMed database and the recent developments on isolation or determination of antihistamines in biological materials. Current trends and future perspectives on bioanalysis of antihistamines are also discussed. Copyright © 2016 John Wiley & Sons, Ltd.

Microliquid/Liquid Interfacial Sensors: Biomimetic Investigation of Transmembrane Mechanisms and Real-Time Determinations of Clemastine, Cyproheptadine, Epinastine, Cetirizine, and Desloratadine

“…In addition, since the optimum pH of the internal environment in the brain should be 7.4, we examined the existing species of the five antihistamines at pH = 7.4 and figured out their partition coefficients in the w/DCE phase, which are summarized in Table . It can be seen that under pH = 7.4, CYP has the strongest lipophilicity, which is consistent with the first-generation antihistamines; EPI and CET have relatively weak lipophilicity, so they are second-generation antihistamines that cannot easily cross the BBB. However, CLE and DSL show a significant discrepancy between their partition coefficients and their ability to cross the BBB.…”

“…Antihistamines are a class of drugs that work by blocking the binding of histamine to the H 1 receptor and are used in clinical practice mainly to alleviate symptoms associated with allergic reactions, such as eczema, urticaria, and allergic rhinitis. , Understanding the nature of the ionized and neutral forms of antihistamines is essential for studying the mechanism of the transmembrane behaviors of the drug and pharmacokinetics . Until now, antihistamines have been developed in three generations.…”

“…Until now, antihistamines have been developed in three generations. The first-generation antihistamines have serious sedative side effects due to their high lipophilicity, which increases their ability to cross the blood–brain barrier (BBB), , and poor receptor selectivity, thus leading to the emergence of the second- and third-generation antihistamines. Despite the relatively high therapeutic index of antihistamines, their acute toxicity is not negligible, depending on the dose of the drug used. , When antihistamines are coadministered with other therapeutic drugs, significant interactions may occur, which can be life-threatening in severe cases, and are now the subject of widespread concern. , Besides, the therapeutic effects of drugs are closely related to the transmembrane mechanism, the pH of the medium, metabolism, absorption, and the physical and chemical properties of the drug, i.e., lipophilicity, p K a , and solubility, especially the lipophilicity which determines and influences the rate of drug transport across membranes. , …”

Flow injection–chemiluminescence determination of cetirizine dihydrochloride in pharmaceuticals using tris(2,2′‐bipyridyl)ruthenium (II)–Ag(III) complex reaction

“…CTZH has been determined quantitatively in biological samples and pharmaceutical formulations employing analytical techniques such as spectrophotometry, [ 7–10 ] spectrofluoremtry, [ 11 ] potentiometry, [ 5 ] conductometry, [ 12 ] voltammetry, [ 13–15 ] inductively coupled plasma‐atomic emission spectrometry, [ 16 ] capillary zone electrophoresis, [ 3,17 ] high‐performance liquid chromatography (HPLC), [ 17–22 ] high‐performance thin layer chromatography (HPTLC), [ 4 ] gas chromatography–mass spectrometry (GC–MS), [ 23 ] chemiluminescence, [ 24–26 ] and electro‐chemiluminescence (ECL). [ 27 ] However, some of these techniques are relatively sensitive in addition to selective, but are usually time consuming during the samples pretreatment steps, and require complex devices with excessive cost, high consumption of toxic solvents; require highly trained personnel, have the possibility of interfering substances in real samples and low sensitivity especially in spectroscopic methods.…”

High performance liquid chromatography associated with resonance Rayleigh scattering for synchronous determination of three antihistamines and mechanism study

“…Therefore, it is necessary to detect antihistamines in water sources and increase the safety level of the drug. Hence, massive analytical techniques such as high performance liquid chromatography (HPLC), gas chromatography‐mass spectrometry (GC‐MS), liquid chromatography tandem mass spectrometry (LC‐MS/MS), ultraviolet (UV), capillary electrophoresis, HPLC‐UV, HPLC‐diode array detector (DAD), thin layer chromatography (TLC), gas chromatography (GC), flame ionization (FID), electron capture detection (ECD), GC coupled with mass spectrometry (MS), radioimmunoassay (RIA) and enzyme‐linked immunosorbent assay (ELISA) have been put forward to detect antihistamines.…”