Eperisone Hydrochloride
(Synonyms: 盐酸乙哌立松,(±)-Eperisone hydrochloride) 目录号 : GC35995
Eperisone hydrochloride is muscle relaxant agent with antispasmodic effects. It is widely used in the treatment of patients with muscular contractures, low back pain or spasticity.
Cas No.:56839-43-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Eperisone hydrochloride is muscle relaxant agent with antispasmodic effects. It is widely used in the treatment of patients with muscular contractures, low back pain or spasticity.
Eperisone has very low bioavailability after oral administration in rats and extensively high oral clearance in humans. It undergoes extensive first-pass metabolism after oral administration in rats and humans because absorption of the drug is very high. The bioavailabilities in the intestine were 0.176 and 0.0879 at administration rates of 100 and 25 mg/h/kg, respectively, whereas those in the liver were 0.532 and 0.486, respectively. Eperisone has high metabolic clearance in the small intestine[1].
[1] Mihara K, et al. Pharm Res. 2001, 18(8):1131-7
| Cas No. | 56839-43-1 | SDF | |
| 别名 | 盐酸乙哌立松,(±)-Eperisone hydrochloride | ||
| Canonical SMILES | O=C(C1=CC=C(CC)C=C1)C(C)CN2CCCCC2.[H]Cl | ||
| 分子式 | C17H26ClNO | 分子量 | 295.85 |
| 溶解度 | DMSO: 31.25 mg/mL (105.63 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3801 mL | 16.9005 mL | 33.8009 mL |
| 5 mM | 0.676 mL | 3.3801 mL | 6.7602 mL |
| 10 mM | 0.338 mL | 1.69 mL | 3.3801 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Eperisone hydrochloride-induced maculopapular rash
Indian J Pharmacol 2016 Sep-Oct;48(5):604-605.PMID:27721553DOI:10.4103/0253-7613.190765.
Here, we report a case of a 30-year-old male who was prescribed Eperisone Hydrochloride for body pain and loose stools after which he developed severe maculopapular rash. Eperisone Hydrochloride is an analgesic and antispastic drug used for spastic diseases such as spastic paralysis in cerebrovascular diseases, cervical spondylosis, and periarthritis. The drug is marketed in most of the Asian countries including India, but it is not licensed. Studies show the history of hypersensitivity in other countries, but this is the first reported case in India.
Serum concentration of Eperisone Hydrochloride correlates with QT interval
Am J Emerg Med 2014 Jan;32(1):75-7.PMID:24135462DOI:10.1016/j.ajem.2013.09.006.
Background: Eperisone Hydrochloride is a centrally acting muscle relaxant prescribed for muscle stiffness that acts by depressing the activities of α and γ efferent neurons in the spinal cord and supraspinal structures. Although a case of eperisone-induced severe QT prolongation had been reported, the relationship between serum eperisone concentration and QT interval remains obscure. Objective: The aim of this study was to investigate the relationship between serum eperisone concentration and QT interval. Methods: Four patients who overdosed on eperisone were admitted to our hospital between January 2010 and December 2011. We took simultaneous serial measurements of serum eperisone concentration and QT interval in the intensive care unit. In total, 22 measurement points were plotted for these patients. We analyzed the correlation between the serum eperisone concentration and corrected QT (QTc) interval. Results: Three men and one woman (mean age, 50 years) overdosed on eperisone with an average dose of 3087.5 mg (therapeutic dose, 150 mg/day). The mean QTc interval at arrival was 592 ms (range, 444-825 ms), and the mean serum eperisone concentration at arrival was 1257.5 ng/mL (range, 14.5-4120.0 ng/mL). The correlation coefficient was 0.833 between serum eperisone concentration and QTc interval (P < .001). Conclusion: Serum eperisone concentration correlates with QTc interval in patients who overdose on eperisone.
Effects of Eperisone Hydrochloride and Non-Steroid Anti-Inflammatory Drugs (NSAIDs) for Acute Non-Specific Back Pain with Muscle Spasm: A Prospective, Open-Label Study
Drug Healthc Patient Saf 2020 Nov 16;12:221-228.PMID:33235514DOI:10.2147/DHPS.S278467.
Background: Low back pain (LBP) occurs as a common condition and may harm the patient's quality-of-life. Non-steroid anti-inflammatory drugs (NSAIDs) and eperisone form a drug regiment that has been reported as effective in improving low back pain, yet the evidence for its efficacy and safety is lacking. Objective: The aim of this study was to evaluate the effect of Eperisone Hydrochloride and ibuprofen compared with ibuprofen alone in reducing symptoms of patients with acute non-specific back pain with a muscle spasm. Methods: This was an open-label, prospective study involving 100 subjects with symptoms of back pain and muscle spasm. Eligible participants were randomly allocated to an experimental group (54 patients) and a control group (46 patients). The experimental group received eperisone 50 mg three times daily + ibuprofen 400 mg twice daily, and the control group received ibuprofen 400 mg twice daily over a 4-week duration. The primary outcomes were measured with the visual analog scale (VAS), and finger-to-floor (FTF) distance at baseline, week 2, and week 4. Results: After 4 weeks of follow-up, results from 59 subjects were collected. In both groups, VAS and FTF were decreased compared to baseline. Clinically significant pain reduction (>50% than baseline) was observed to be higher in the experimental group compared with the control group in the fourth week (72.4% vs 46.7%, P<0.05). At the end of the study, pain reduction in the experimental group was more significant compared to the control group (28.13±24.72 vs 34.42±28.47) and participants mobility (FTF distance <10 cm) improved in both groups, especially in the experimental group (75.9% vs 70%). There was no difference in adverse events between groups (P>0.05). Conclusion: The combination of Eperisone Hydrochloride and ibuprofen effectively reduces pain and improves functional outcomes over ibuprofen alone with a similar safety profile in these patients with acute non-specific back pain with muscle spasm.
Pharmacokinetic interactions between Eperisone Hydrochloride and aceclofenac: a randomized, open-label, crossover study of healthy Korean men
Clin Ther 2013 Oct;35(10):1528-35.PMID:24050970DOI:10.1016/j.clinthera.2013.08.012.
Background: Eperisone Hydrochloride, a centrally acting muscle relaxant, is a calcium antagonist that causes vasodilation and antispastic actions. Aceclofenac, an anti-inflammatory analgesic and antipyretic drug, has similar efficacy and improved gastrointestinal tolerance compared with other nonsteroidal anti-inflammatory drugs, such as diclofenac. Although Eperisone Hydrochloride and aceclofenac are frequently coadministered, no published studies have reported on the pharmacokinetic interactions between these 2 drugs. Objective: The aim of this study was to investigate any pharmacokinetic interactions between Eperisone Hydrochloride and aceclofenac in healthy Korean men. Methods: This was a randomized, open-label, crossover study. Each participant was randomly assigned to 1 of 6 treatment sequences and received Eperisone Hydrochloride (3 doses of 50 mg each), aceclofenac (2 doses of 100 mg each), or both as a single dose with a 7-day washout period between each dose. Blood samples were collected ≤ 24 hours after dosing, and plasma Eperisone Hydrochloride and aceclofenac concentrations were determined using validated LC/MS-MS. Pharmacokinetic analyses were conducted using noncompartmental methods. A safety profile was determined using the measurement of vital signs, ECG, and clinical laboratory tests. Results: A total 24 of men were enrolled, and all completed the study. The geometric mean ratios (90% CIs) of the Cmax and AUC0-∞ values for eperisone were 1.18 (0.828-1.673) and 1.12 (0.836-1.507), respectively. The geometric mean ratios (90% CIs) of the Cmax and AUC0-∞ for aceclofenac were 0.93 (0.847-1.022) and 1.01 (0.979-1.036), respectively. A total of 7 adverse events were reported in 7 men. All adverse events were mild, and no significant differences were found between treatment groups. Conclusion: No clinically significant pharmacokinetic differences exist between 150 mg Eperisone Hydrochloride and 200 mg aceclofenac when administrated as a monotherapy or in combination.
Pharmacokinetic Interactions Between Pelubiprofen and Eperisone Hydrochloride: A Randomized, Open-label, Crossover Study of Healthy Korean Men
Clin Ther 2017 Jan;39(1):138-149.PMID:27989618DOI:10.1016/j.clinthera.2016.11.020.
Purpose: Pelubiprofen is a novel nonsteroidal anti-inflammatory, analgesic, and antipyretic drug with at least similar efficacy and better tolerability compared with other nonsteroidal anti-inflammatory, analgesic, and antipyretic drugs such as naproxen and aceclofenac. Eperisone Hydrochloride is a centrally acting muscle relaxant that performs by blocking calcium channels. The combined use of pelubiprofen and Eperisone Hydrochloride is increasingly anticipated to promote the clinical effectiveness of pelubiprofen in relieving musculoskeletal symptoms of osteoarthritis, rheumatoid arthritis, and low back pain. No published data are yet available, however, regarding the pharmacokinetic interactions between these 2 drugs when administered concurrently. The objective of this study was to evaluate any pharmacokinetic interactions between pelubiprofen and Eperisone Hydrochloride in healthy Korean male volunteers. Methods: This was a randomized, open-label, crossover study. Each participant was randomly assigned to 1 of 6 treatment sequences and orally received either 45-mg sustained-release pelubiprofen, 75-mg sustained-release Eperisone Hydrochloride, or both as a single dose in each treatment period, with a 7-day washout period between each treatment. Serial blood samples were collected over 24 hours after dosing, and plasma concentrations of each drug and the major active metabolite of pelubiprofen (trans-alcohol pelubiprofen) were determined by using a validated HPLC-MS/MS system. Pharmacokinetic analyses were conducted by using noncompartmental methods. Findings: A total of 24 men (mean ± standard deviation of: age, 29 ± 4 years; weight, 72.5 ± 7.8 kg; body mass index, 23.4 ± 1.9 kg/m2) were enrolled, and 23 participants completed the study. For pelubiprofen, the geometric mean ratios (90% CIs) of Cmax and AUC0-∞ were 1.02 (0.87-1.19) and 0.97 (0.88-1.07), respectively. For the major active metabolite of pelubiprofen (trans-alcohol pelubiprofen), the geometric mean ratios (90% CIs) of Cmax and AUC0-∞ were 1.05 (0.98-1.13) and 1.04 (1.01-1.07). For eperisone, the geometric mean ratios (90% CIs) of Cmax and AUC0-∞ were 0.87 (0.67-1.15) and 1.05 (0.85-1.30). None of the study participants experienced serious adverse events during the study. Implications: No clinically significant changes were noted in the pharmacokinetic interactions of pelubiprofen, the major active metabolite of pelubiprofen (trans-alcohol pelubiprofen), and Eperisone Hydrochloride between monotherapy and combination therapy with 45-mg sustained-release pelubiprofen and 75-mg sustained-release Eperisone Hydrochloride.