Antiemetic Effects of Lerisetron in Radiation-induced Emesis in the Dog

Segura, Ignacio A. Gomez de; Grande, A. García; Miguel, Enrique de

doi:10.1080/028418698430160

Cited by 7 publications

(3 citation statements)

References 13 publications

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“…Lerisetron also reverses the gastric distention induced by a single dose of cisplastin (5 mg/kg, ip) in rats with an ED 50 value of 152 μg/kg, ip 7. In an emesis model in the dog, in which emesis is induced by irradiation, the ED 50 of lerisetron for suppressing vomiting was 63 ± 18 μg/kg, which is less than the corresponding dose of ondansetron of 178 ± 151 μg/kg 8…”

Section: Introductionmentioning

confidence: 79%

Pharmacokinetics and Pharmacological Effect of Lerisetron, a New 5‐HT3 Antagonist, in Rats

Jauregizar

Calvo

Súárez

et al. 2002

Journal of Pharmaceutical Sciences

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Section: Introductionmentioning

confidence: 79%

Pharmacokinetics and Pharmacological Effect of Lerisetron, a New 5‐HT3 Antagonist, in Rats

Jauregizar

Calvo

Súárez

et al. 2002

Journal of Pharmaceutical Sciences

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“…These emesis occurring within 24 hours, is now known to be mediated via 5-hydroxythriptamin3 (5-HT3) receptors and thus can be controlled with the specific 5-HT3 receptor antagonists (Grunberg 1993;Hsu 2010). Granisetron, ondansetron, andtropisetron, having been considered the most powerful antiemetics so far, have been proven at least equally efficacious as conventional treatments (Chevallier 1993;Gomez-de-Segura et al 1998;Gregory and Ettinger 1998;Hsu 2010;Janelsins et al 2013;Schnell 2003).…”

Section: Introductionmentioning

confidence: 99%

A clinical survey on the electrocardiogram after intravenous granisetron hydrochloride administration in clinically normal dogs

Ghaemi

Sedigh

Ghaffari

2021

J Hellenic Vet Med Soc

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Cardiac side effect of 5-hydroxytryptamine-3 receptor antagonists has been a concern for clinicians. There is a substantial need for greater clarity about the safety of granisetron hydrochloride, an antiemetic agent of this class used in oncological and parvoviral gastroenteritis with acute vomiting in dogs. This study aimed to assess the electrocardiographic effects of a single dose of intravenous granisetron. We randomly assigned 16 adult crossbreed female healthy dogs into two groups of intervention and control and injected them intravenously with granisetron and normal saline, respectively, at a dose of 0.5 ml/kg over one minute. Standard electrocardiography (ECG) was recorded at the baseline, as well as 5, 15, 30, 60, 120, 360, and 720 minutes after the intervention. Heart rate and ECG parameters (PR intervals, QRS duration, ST-segment, T-wave amplitudes, QT, JT, QTc and JTc intervals) were evaluated in lead II.No significant difference was observed between the intervention and the control groups in any of the measured variables at any of the time-points. Mean values of measured parameters showed no significant difference compared with baseline values in the control group, while the granisetron group saw statistically significant but clinically asymptomatic changes in heart rate, PR, QRS, QT, JT, and QTc at different time-points, compared to the baseline values (P<0.05). In conclusion, Granisetron administration was not associated with clinically significant adverse effects on ECG variables or heart rate. Thus, it can be regarded as a relatively safe drug.

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“…than granisetron and tropisetron [4]. Lerisetron improved cisplatin-induced gastric distension in rats and mice and also inhibited cisplatin-induced emesis in dogs [5]. A study using a radiation-induced emesis model in the dog has shown that lerisetron is more potent and shows less individual variability than ondansetron while having an equally effective anti-emetic action [6].…”

Section: Introductionmentioning

confidence: 99%

Effects of Lerisetron, a New 5-HT3 Receptor Antagonist, on Ipecacuanha- induced Emesis in Healthy Volunteers

Cooper¹,

Sologuren

Valiente

et al. 2011

Arzneimittelforschung

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The purpose of these studies was to evaluate the effect of lerisetron (1-phenyl-methyl-2-piperazinyl-1H-benzimidazole hydrochloride, CAS 143257-98-1, F-0930-RS2), a new 5-HT3 receptor antagonist, on ipecacuanha-induced nausea and vomiting. The ipecacuanha model of emesis has been used to test the anti-emetic activity of several different 5-HT3 antagonists and the anti-emetic doses that were effective in the ipecacuanha model have been found to correlate well with the clinically effective doses. Study 1 investigated oral doses of lerisetron from 4 mg to 40 mg. Study 2 evaluated the duration of effect of a single dose of 20 mg oral lerisetron. Study 3 evaluated intravenous doses of 18 mg and 12 mg lerisetron. In Study 1, the 40 mg dose of oral lerisetron inhibited emesis in all test subjects. The percentage of subjects who experienced an emetic episode increased as the dose of lerisetron decreased. At the lowest dose level tested five of six subjects had an emetic episode compared with four out of five in the placebo group. In Study 2, 20 mg oral lerisetron was effective up to 12 h after administration. When ipecacuanha was administered at 18 h post-dose three of seven subjects had an emetic episode and at 24 h post-dose the incidence of emesis was similar to the placebo treatment groups in the previous study. Study 3 demonstrated the effectiveness of intravenous doses of lerisetron. The 18 mg intravenous dose reduced the number of patients experiencing emetic episodes by 75% compared with placebo, doses below 12 mg i.v. were not evaluated because of the reduced efficacy of the compound at this dose level. In conclusion, lerisetron has been shown to be effective in the treatment of ipecacuanha-induced nausea and vomiting at intravenous doses of 18 mg and at oral doses of 20 mg for up to 12 hours.

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Antiemetic Effects of Lerisetron in Radiation-induced Emesis in the Dog

Cited by 7 publications

References 13 publications

Pharmacokinetics and Pharmacological Effect of Lerisetron, a New 5‐HT3 Antagonist, in Rats

Pharmacokinetics and Pharmacological Effect of Lerisetron, a New 5‐HT3 Antagonist, in Rats

A clinical survey on the electrocardiogram after intravenous granisetron hydrochloride administration in clinically normal dogs

Effects of Lerisetron, a New 5-HT3 Receptor Antagonist, on Ipecacuanha- induced Emesis in Healthy Volunteers

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