What is Fenspiride hydrochloride?

Fenspiride hydrochloride (1-Oxa-3,8-diazaspiro[4.5]decan-2-one, 8-(2-phenylethyl)-, monohydrochloride; 1-Oxa-3,8-diazaspiro[4.5]decan-2-one, 8-phenethyl-, monohydrochloride; 8-Phenethyl-1-oxa-3,8-diazaspiro[4.5]decan-2-one hydrochloride; Decaspir; Decaspiride; Erespal; Fluiden; JP 428; NAT 333; NDR 5998A; Pneumorel; Tegencia; Viarespan) [1] is an oxazolidinone spiro compound with a molecular formula of C15H20N2O2. HCl, which is a non-steroidal compound with a number of modes of action and end-organ effects. As an α adrenergic and H1 histamine receptor antagonist, Fenspiride has been shown to be antiinflammatory, anti-allergic and antioxidant. Fenspiride inhibited SO2-induced goblet cell hyperplasia in rats, with concomitant inhibition of increased hexose and fucose, indicative of mucus hypersecretion, in lavage fluid [2]. Fenspiride also exhibits neuronal inhibitory activity. For example, in guinea pigs, it reverses capsaicin-induced and citric acid-induced bronchoconstriction and cough [3], and inhibits cholinergic and non-adrenergic, non-cholinergic (NANC) neural contraction of isolated bronchi [4].

Fenspiride hydrochloride is a bronchodilator, which was used as a drug in the treatment of certain respiratory diseases. Finsecbili hydrochloride against serotonin, dilating bronchial smooth muscle, the intensity of action is between isoproterenol and theophylline, in addition to reducing the resistance of air movement in the lungs, experiments have shown that this product has dilated bronchial smooth muscle, antitussive, antipyretic and analgesic effects. Suitable for chronic bronchitis, bronchial asthma and chronic respiratory insufficiency. [5]. In Russia it was approved for the treatment of acute and chronic inflammatory diseases of ENT organs and the respiratory tract, as well as for maintenance treatment of asthma (like rhinopharyngitis, laryngitis, tracheobronchitis, otitis and sinusitis) [6].

Taking fensapride hydrochloride can cause dizziness, insomnia, and the like. The European Union's Drug Administration (EMA) recently announced that it will suspend the use of fensopril (Fispiri) in the EU due to the potential risk of heart rhythm problems. The decision was based on the recent non-clinical study (hERG channel binding and in vitro a nimal model studies) and showed that fensopril (fensilel) may prolong the QT interval in patients. Fenspiride (Fins Billy) has been approved for use in children and adults to relieve cough caused by lung disease. The FDA's Pharmacovigilance Risk Assessment Committee (PRAC), after review, concluded that the drug may prolong the QT interval and induce life-threatening ventricular arrhythmias (tipped torsade ventricular tachycardia), Causes sudden cardiac death. Previously, patients who continued to take fensopril (fensamine) reported a heart rhythm problem. In order to explore the possible links between the two, the researchers took the lead in conducting animal experiments, and the results showed that fensopril (Fispiri) has the potential to prolong the human QT interval, and ultimately prompted the EU to suspend patients to use this type of the decision of the drug [7].

References

[1] https://www.chemicalbook.com/ProductChemicalPropertiesCB7295887_EN.htm

[2] Broillet A, White R, Ventrone R, Giessinger N. Efficacy of fenspiride in alleviating SO2 induced chronic bronchitis in rats and allergic rhinitis in guinea pigs. Rhinol Suppl 1988; 4: 75–83.

[3] Laude E. A., Bee D, Crambes O, Howard P. Antitussive and anti-broncho-constriction actions of fenspiride in guinea- pigs. Eur Resp J 1995; 8: 1699–1704.

[4] Girard V, Naline E, Crambes O, Malbezin M, Malmstrom R. E., Lundberg J. M., Advenier C. Pre- and postjunctional effects of fenspiride on guinea-pig bronchi. Eur Respir J 1997; 10: 1015–1020.

[5] https://www.chemsrc.com/en/cas/5053-08-7_1193126.html

[6] https://en.wikipedia.org/wiki/Fenspiride

[7] https://www.chemicalbook.com/ChemicalProductProperty_CN_CB7295887.htm