Devi Akash, Khanwelkar Chitra
Pharmacology and Therapeutics, Krishna Vishwa Vidyapeeth (Deemed to Be University), Karad, IND.
Pharmacology, Krishna Vishwa Vidyapeeth (Deemed to Be University), Karad, IND.
Cureus. 2024 Sep 16;16(9):e69513. doi: 10.7759/cureus.69513. eCollection 2024 Sep.
Introduction Thiocolchicoside (THC) is a semi-synthetic derivative of colchicoside and a naturally occurring compound in the seeds of the plant. At present, it is used as a skeletal muscle relaxant. It is used to treat rheumatic arthritis, orthopaedic conditions, and trauma. Topically, it is used to relieve excruciating spasms in the muscles. It is also used to treat a wide range of conditions, which include surgical pain, cervicobrachial neuralgia, acute to chronic torticollis, Parkinson's disease, drug-induced Parkinsonism, spastic hemiplegia, tooth soreness, acute lower back pain, etc. THC is used in conjunction with non-steroidal anti-inflammatory drugs (NSAIDs), muscle relaxants, and analgesics. By downregulating and inhibiting the synthesis of NF-κB-regulated gene products, it possesses anti-inflammatory properties. To prevent aneuploidy, the European Medical Agency has placed restrictions on the use of THC, stating that it should not be injected for five days or taken orally for longer than seven days. This is because its metabolism in the body may lead to the production of the metabolite M2. When used during pregnancy, the growing fetus is more negatively impacted. It has also been connected to infertility in men. Aim To study the skeletal muscle relaxant effects of THC in Wistar rats in comparison with standard drugs. Materials and methods The skeletal muscle relaxant activity level was measured using the rotarod apparatus. There were five groups of Wistar rats (n = 6). Group I received 0.9% normal saline (NS) as a control. Group II (test group) received THC 2 mg/kg intraperitoneally (ip). Group III (test group) received THC 4 mg/kg (ip). Group IV diazepam (DIZ) 3 mg/kg (ip) which is the standard treatment group. Group V received a combination of THC 2 mg/kg and DIZ 3 mg/kg. After treatment, retention time was noted at intervals of 30, 60, and 120 minutes. Results Group I (control), Group II (THC 2 mg/kg) and Group III (THC 4 mg/kg) did not demonstrate any skeletal muscle relaxant activity. Group IV (DIZ 3 mg/kg) and Group V (THC 2 mg/kg + DIZ 3 mg/kg) showed statistically significant skeletal muscle relaxant activity when compared to control. However, there was no statistically significant difference between the skeletal muscle relaxant activity of these two groups. This indicates that the addition of THC did not potentiate the skeletal muscle relaxant activity of DIZ. Conclusion THC didn't show skeletal muscle relaxant properties in both doses and did not potentiate the activity of DIZ.
引言
硫代秋水仙碱(THC)是秋水仙碱的半合成衍生物,是植物种子中的一种天然存在的化合物。目前,它被用作骨骼肌松弛剂。用于治疗风湿性关节炎、骨科疾病和创伤。局部使用时,它可缓解肌肉剧烈痉挛。它还用于治疗多种病症,包括手术疼痛、颈臂神经痛、急性至慢性斜颈、帕金森病、药物性帕金森综合征、痉挛性偏瘫、牙痛、急性下背痛等。THC与非甾体抗炎药(NSAIDs)、肌肉松弛剂和镇痛药联合使用。通过下调和抑制NF-κB调节的基因产物的合成,它具有抗炎特性。为防止非整倍体,欧洲药品管理局对THC的使用进行了限制,规定不得注射五天以上或口服超过七天。这是因为它在体内的代谢可能导致代谢物M2的产生。在怀孕期间使用时,发育中的胎儿受到的负面影响更大。它还与男性不育有关。
目的
比较THC与标准药物对Wistar大鼠的骨骼肌松弛作用。
材料和方法
使用转棒仪测量骨骼肌松弛活性水平。将Wistar大鼠分为五组(n = 6)。第一组接受0.9%生理盐水(NS)作为对照。第二组(试验组)腹腔注射(ip)2 mg/kg的THC。第三组(试验组)腹腔注射4 mg/kg的THC。第四组腹腔注射3 mg/kg的地西泮(DIZ),为标准治疗组。第五组接受2 mg/kg的THC和3 mg/kg的DIZ的组合。治疗后,每隔30、60和120分钟记录停留时间。
结果
第一组(对照组)、第二组(2 mg/kg的THC)和第三组(4 mg/kg的THC)未表现出任何骨骼肌松弛活性。与对照组相比,第四组(3 mg/kg的DIZ)和第五组(2 mg/kg的THC + 3 mg/kg的DIZ)表现出统计学上显著的骨骼肌松弛活性。然而,这两组的骨骼肌松弛活性之间没有统计学上的显著差异。这表明添加THC并未增强DIZ的骨骼肌松弛活性。
结论
两种剂量的THC均未表现出骨骼肌松弛特性,也未增强DIZ的活性。