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Eosinophils and New Antihistamines
Published in Gerald J. Gleich, A. Barry Kay, Eosinophils in Allergy and Inflammation, 2019
PAF- and LTB4-induced migration of guinea pig peritoneal eosinophils was used to study terfenadine in vitro. A full inhibition was observed for 10 µmol/L concentration of terfenadine (23). No other data were reported in this model.
Pharmacokinetic-Pharmacodynamic Correlations of Antihistamines
Published in Hartmut Derendorf, Günther Hochhaus, Handbook of Pharmacokinetic/Pharmacodynamic Correlation, 2019
Eric Snoeck, Achiel Van Peer, Jos Heykants
In two separate studies, the pharmacokinetics and pharmacodynamics of terfenadine were investigated in 13 children with allergic rhinitis78 and in 8 healthy elderly female patients.58 In children and the elderly, the mean peak serum concentration of terfenadine metabolite I preceded the peak suppressive effect on wheal and flare by 2 to 3 h. The serum elimination half-life of metabolite I in children averaged 2.0 h and was shorter than the mean elimination half-life of 2.9 to 4.5 h in healthy young adults.77,79 On the other hand, the serum elimination half-life of metabolite I in the elderly was prolonged and averaged 8.7 h. In children, the wheal and flare areas were significantly inhibited from 2 to 8 h after intake and in the elderly the histamine-induced skin reactions were significantly suppressed from 2 to 24 h postdosing.
Formulary
Published in Sarah Bekaert, Alison White, Integrated Contraceptive and Sexual Healthcare, 2018
Sarah Bekaert, Alison White, Kathy French, Kevin Miles
Concomitant use of erythromycin with terfenadine or astemizole is likely to result in an enhanced risk of cardiotoxicity with these drugs. The metabolism of terfenadine and astemizole is significantly altered when either are taken concomitantly with erythromycin. Rare cases of serious cardiovascular events have been observed, including torsades de pointes, other ventricular arrhythmias and cardiac arrest. Death has been reported with the terfenadine/erythromycin combination.
The exploration of effect of terfenadine on Ca2+ signaling in renal tubular cells
Published in Journal of Receptors and Signal Transduction, 2019
He-Hsiung Cheng, Wei-Zhe Liang, Chun-Chi Kuo, Lyh-Jyh Hao, Chiang-Ting Chou, Chung-Ren Jan
Terfenadine acts as an antihistamine for treatment of allergic conditions [1]. Although terfenadine has been used by over 100 million patients worldwide as of 1990 [2], it was superseded by fexofenadine in the 1990s due to the risk of a particular type of disruption of the electrical rhythms of the heart [3]. In vitro, terfenadine also altered Ca2+ signaling in different models. It has been shown that terfenadine inhibited cytosolic Ca2+ dynamics in cultured guinea pig cardiomyocytes [4], and reduced Ca2+ influx, cyclic guanosine monophosphate (cGMP) formation, and N-methyl-D-aspartate (NMDA) receptor-dependent neurotoxicity following activation of L-type voltage sensitive Ca2+ channels in neurons [5]. Furthermore, terfenadine prevented L-type Ca2+ channel current in rat ventricular myocytes [6] and blocked time-dependent Ca2+, Na+, and K+ channels in guinea pig ventricular myocytes [7]. On the contrary, terfenadine-induced apoptosis in A375 human melanoma cells was mediated through elevation in cytosolic free Ca2+ levels ([Ca2+]i) [8]. Furthermore, terfenadine was reported to increase Ca2+ release in human atrial myocytes [9] and rat mast cells [10]. However, the effects of terfenadine on Ca2+ homeostasis in renal tubular cells have not been explored.
Bepotastine besilate for the treatment of perennial allergic rhinitis
Published in Expert Opinion on Pharmacotherapy, 2018
Ismael Carrillo-Martin, Alexei Gonzalez-Estrada, Ves Dimov
A phase III trial compared the effectiveness of 20 mg/day of BB or 120 mg/day of terfenadine in 239 patients that were included using the same inclusion criteria as in the previously described trials, and then randomized to receive either BB or terfenadine for 4 weeks [24]. Symptom improvement scores were significantly (p = 0.021) better for bepotastine than terfenadine. Also significantly (p = 0.011), 61% (n = 103) of the patients who received bepotastine had a final global moderate or greater improvement scores as opposed to those who received terfenadine (43.8%; n = 96) [24]. Nasal symptoms and nasal cavity findings also improved with bepotastine. Nasal symptoms showed an improvement in 59–70% of recipients of BB versus 49–60% of those who were treated with terfenadine. Nasal cavity findings were improved in over 80% of patients who received BB versus 63% of those who were treated with terfenadine [24].
Terfenadine t-butyl hydroxylation catalyzed by human and marmoset cytochrome P450 3A and 4F enzymes in livers and small intestines
Published in Xenobiotica, 2018
Shotaro Uehara, Yukako Yuki, Yasuhiro Uno, Takashi Inoue, Erika Sasaki, Hiroshi Yamazaki
Changes in the pharmacokinetics and electrocardiographic pharmacodynamics of terfenadine have been reported with concomitant administration of erythromycin or ketoconazole (Honig et al., 1992,1993) caused by P450 3A4-derived enzyme inhibition (Jurima-Romet et al., 1994; Yun et al., 1993). It has been suggested that roles of human P450 2J2 in the terfenadine oxidation may be an unrecognized participant in first-pass metabolism of terfenadine (Lee et al., 2010) but its contribution may be minor relative to that of P450 3A4. Marmoset and cynomolgus monkey P450 2J2 enzymes in small intestines and livers effectively metabolized human P450 2J2 probe substrates, astemizole and terfenadine (Uehara et al., 2016b). Marmoset P450 4F12 in small intestines and livers efficiently metabolized another anti-histaminic drug ebastine (Uehara et al., 2016c). Understanding the characteristics of marmoset or cynomolgus monkey P450 enzymes in extensive intestinal and hepatic clearances of terfenadine and its related P450 substrates would be important for non-human primates as preclinical drug metabolism research models.