The effect of ivermectin on convulsions in rats produced by lidocaine and strychnine
Само за регистроване кориснике
2007
Чланак у часопису (Објављена верзија)
Метаподаци
Приказ свих података о документуАпстракт
Ivermectin is one of the most commonly used drugs in pharmacotherapy of parasitic diseases in domestic and wild animals caused by parasitic nematodes and arthropods. However, ivermectin and other avermectins very often produce side-effects in hosts. The most dominant clinical symptom of ivermectin toxicity in domestic and wild animals is CNS depression. In nematodes, the target site of ivermectins action is glutamate-gated chloride-channel receptor and GABA receptor. The depressive effect of ivermectin in mammals might include more than one mechanism; therefore, the anticonvulsive effect of ivermectin against convulsions caused by lidocaine and strychnine was evaluated. Ivermectin antagonized lidocaine- and strychnine-induced convulsions in rats, although these have different mechanisms. In the present study, the anticonvulsive ED50 of ivermectin for lidocaine-induced convulsions was 2.44 mg/kg (95% CL 1.67 to 3.57 mg/kg), whereas for convulsions induced by strychnine it was higher at ...4.25 mg/kg (95% CL 2.32 to 3.78 mg/kg). At the same time, both anticonvulsive doses are significantly lower then the observed LD50 of ivermectin (18.20 mg/kg). Furthermore, flumazenil (0.1 and 0.2 mg/kg), an antagonist of benzodiazepine receptors, antagonizes just one part of these anticonvulsive effects of ivermectin. Our results show the significant anticonvulsive properties of ivermectin and support the findings that ivermectin in the CNS of mammals produces multiple inhibitory effects, probably through participation in the function of GABA-sensitive and GABA-insensitive chloride channels.
Кључне речи:
ivermectin / convulsions / GABA / glycineИзвор:
Veterinary Research Communications, 2007, 31, 7, 863-872Издавач:
- Springer, Dordrecht
Финансирање / пројекти:
- Испитивање механизама резистенције и токсичности антихелминтика-ГАБА и никотинских агониста (RS-145026)
DOI: 10.1007/s11259-007-0050-3
ISSN: 0165-7380
PubMed: 17308985
WoS: 000247738300007
Scopus: 2-s2.0-34447258393
Колекције
Институција/група
Fakultet veterinarske medicineTY - JOUR AU - Trailović, Saša AU - Varagić, Vladislav M. PY - 2007 UR - https://vet-erinar.vet.bg.ac.rs/handle/123456789/450 AB - Ivermectin is one of the most commonly used drugs in pharmacotherapy of parasitic diseases in domestic and wild animals caused by parasitic nematodes and arthropods. However, ivermectin and other avermectins very often produce side-effects in hosts. The most dominant clinical symptom of ivermectin toxicity in domestic and wild animals is CNS depression. In nematodes, the target site of ivermectins action is glutamate-gated chloride-channel receptor and GABA receptor. The depressive effect of ivermectin in mammals might include more than one mechanism; therefore, the anticonvulsive effect of ivermectin against convulsions caused by lidocaine and strychnine was evaluated. Ivermectin antagonized lidocaine- and strychnine-induced convulsions in rats, although these have different mechanisms. In the present study, the anticonvulsive ED50 of ivermectin for lidocaine-induced convulsions was 2.44 mg/kg (95% CL 1.67 to 3.57 mg/kg), whereas for convulsions induced by strychnine it was higher at 4.25 mg/kg (95% CL 2.32 to 3.78 mg/kg). At the same time, both anticonvulsive doses are significantly lower then the observed LD50 of ivermectin (18.20 mg/kg). Furthermore, flumazenil (0.1 and 0.2 mg/kg), an antagonist of benzodiazepine receptors, antagonizes just one part of these anticonvulsive effects of ivermectin. Our results show the significant anticonvulsive properties of ivermectin and support the findings that ivermectin in the CNS of mammals produces multiple inhibitory effects, probably through participation in the function of GABA-sensitive and GABA-insensitive chloride channels. PB - Springer, Dordrecht T2 - Veterinary Research Communications T1 - The effect of ivermectin on convulsions in rats produced by lidocaine and strychnine VL - 31 IS - 7 SP - 863 EP - 872 DO - 10.1007/s11259-007-0050-3 ER -
@article{ author = "Trailović, Saša and Varagić, Vladislav M.", year = "2007", abstract = "Ivermectin is one of the most commonly used drugs in pharmacotherapy of parasitic diseases in domestic and wild animals caused by parasitic nematodes and arthropods. However, ivermectin and other avermectins very often produce side-effects in hosts. The most dominant clinical symptom of ivermectin toxicity in domestic and wild animals is CNS depression. In nematodes, the target site of ivermectins action is glutamate-gated chloride-channel receptor and GABA receptor. The depressive effect of ivermectin in mammals might include more than one mechanism; therefore, the anticonvulsive effect of ivermectin against convulsions caused by lidocaine and strychnine was evaluated. Ivermectin antagonized lidocaine- and strychnine-induced convulsions in rats, although these have different mechanisms. In the present study, the anticonvulsive ED50 of ivermectin for lidocaine-induced convulsions was 2.44 mg/kg (95% CL 1.67 to 3.57 mg/kg), whereas for convulsions induced by strychnine it was higher at 4.25 mg/kg (95% CL 2.32 to 3.78 mg/kg). At the same time, both anticonvulsive doses are significantly lower then the observed LD50 of ivermectin (18.20 mg/kg). Furthermore, flumazenil (0.1 and 0.2 mg/kg), an antagonist of benzodiazepine receptors, antagonizes just one part of these anticonvulsive effects of ivermectin. Our results show the significant anticonvulsive properties of ivermectin and support the findings that ivermectin in the CNS of mammals produces multiple inhibitory effects, probably through participation in the function of GABA-sensitive and GABA-insensitive chloride channels.", publisher = "Springer, Dordrecht", journal = "Veterinary Research Communications", title = "The effect of ivermectin on convulsions in rats produced by lidocaine and strychnine", volume = "31", number = "7", pages = "863-872", doi = "10.1007/s11259-007-0050-3" }
Trailović, S.,& Varagić, V. M.. (2007). The effect of ivermectin on convulsions in rats produced by lidocaine and strychnine. in Veterinary Research Communications Springer, Dordrecht., 31(7), 863-872. https://doi.org/10.1007/s11259-007-0050-3
Trailović S, Varagić VM. The effect of ivermectin on convulsions in rats produced by lidocaine and strychnine. in Veterinary Research Communications. 2007;31(7):863-872. doi:10.1007/s11259-007-0050-3 .
Trailović, Saša, Varagić, Vladislav M., "The effect of ivermectin on convulsions in rats produced by lidocaine and strychnine" in Veterinary Research Communications, 31, no. 7 (2007):863-872, https://doi.org/10.1007/s11259-007-0050-3 . .