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Benzydamine
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Benzydamine is an indazole non-steroidal anti-inflammatory drug with analgesic, antipyretic, and anti-edema properties. Available as a liquid mouthwash, spray for mouth and throat, topical cream, and vaginal irrigation (formerly also available in tablets, suppositories and intramuscular injections), benzydamine is most frequently employed for the relief of painful inflammatory conditions of the mouth and the musculoskeletal system, respectively. It is also said to promote healing. In pharmaceutical products, benzydamine is employed as benzydamine hydrochloride (CAS number 132-69-4, EC number 205-076-0, molecular formula C19H24ClN3O) (1).
Oral problems
Published in Mervyn Dean, Juan-Diego Harris, Claud Regnard, Jo Hockley, Symptom Relief in Palliative Care, 2018
Mervyn Dean, Juan-Diego Harris, Claud Regnard, Jo Hockley
Some topical agents can offer mucosal protection. Carmellose (Orabase) paste is an effective protective for local lesions. There is no evidence that benzydamine, sucralfate or chlorhexidine ease oral pain.48–50 Choline salicylate gel can help but can cause pain on application. In the US, gel preparation can be obtained via a Compounding Pharmacy. Lidocaine (cream, gel or spray) can help acutely painful lesions at the expense of numbness, but toxicity has been reported with frequent use.51 In very severe pain, systemic analgesia is required. Topical opioids may help, but in very severe pain systemic opioids are required. Ketamine may have a role in extensive mucositis.64
Wrong administration route of medications in the domestic setting: a review of an underestimated public health topic
Published in Expert Opinion on Pharmacotherapy, 2021
Maria Rosaria Gualano, Giuseppina Lo Moro, Gianluca Voglino, Dario Catozzi, Fabrizio Bert, Roberta Siliquini
A report from Ballesteros et al. [31] in 2009 studied the in-depth ingestion of benzydamine-containing vaginal preparations through calls addressed to the Spanish Poison Control Center (SPCC) from 1991 to 2003. As mentioned above [10], people who use these gynecological formulations might make administration route errors by ingesting these medications. Indeed, 724 cases were recognized: 94.3% occurred in a home setting, and 52.9% occurred in a general public setting with no health-care professional involved as an intermediary figure. Specifically, 86.2% of the patients were older than 14 years of age; among these, 80.9% were female. These errors are probably associated with the confounding effect of finding the same active substance in OTC solutions for oropharyngeal diseases. In particular, the authors reported that female adults (80.9% of adults) confused the route of administration of the drug, whereas male patients confused the medication with the oral antiseptic with the same active substance but different doses. The clinical effect of benzydamine poisoning was mild: 72.9% of cases were considered asymptomatic with minor symptoms, 25.7% with a moderate presentation, and 1.4% with severe symptomatology, none of which resulted in death [31].
Functional assessment of rat pulmonary flavin-containing monooxygenase activity
Published in Xenobiotica, 2019
Yildiz Yilmaz, Gareth Williams, Nenad Manevski, Markus Walles, Stephan Krähenbühl, Gian Camenisch
Benzydamine and benzydamine N-oxide blood concentrations were quantified following i.v. and i.a. administration of benzydamine to Sprague-Dawley rats and the pharmacokinetic parameters and concentration-time profiles are shown in Figure 6 and Table 3, respectively. Benzydamine was rapidly eliminated following i.v. and i.a. with blood clearances estimated to be 173 and 182 mL/min/kg, respectively (approximately three-fold higher than hepatic blood flow). The data showed that the benzydamine exposures achieved via the two administration routes were comparable and that there was no indication of significant pulmonary extraction under the conditions described here. The mean benzydamine N-oxide exposure obtained following i.v. dosing was slightly higher than after i.a. dosing (72 ± 4 and 61 ± 7 h × ng/mL respectively). However, this may likely be due to analytical or inter-animal variability rather than a reflection of pulmonary extraction.
Human plasma metabolic profiles of benzydamine, a flavin-containing monooxygenase probe substrate, simulated with pharmacokinetic data from control and humanized-liver mice
Published in Xenobiotica, 2018
Miho Yamazaki-Nishioka, Makiko Shimizu, Hiroshi Suemizu, Megumi Nishiwaki, Marina Mitsui, Hiroshi Yamazaki
The nonsteroidal anti-inflammatory drug benzydamine is used topically, in oral rinses or systematically to treat inflammation (Baldock et al., 1990; Schoenwald et al., 1987). Benzydamine is also a typical probe substrate for flavin-containing monooxygenases (FMO; EC 1.14.13.8). Benzydamine is used during drug discovery and development (Stormer et al., 2000; Yeung et al., 2000), because it undergoes FMO-dependent oxygenation to a stable N-oxide (Figure 1B). A different metabolic pathway involving benzydamine N-demethylation (Figure 1C) in human liver microsomes mediated mainly by cytochromes P450 (P450; EC 1.14.14.1) has also been reported (Stormer et al., 2000; Taniguchi-Takizawa et al., 2015).