Drotaverine (hydrochloride)
(Synonyms: 盐酸屈他维林) 目录号 : GC43574
An antispasmodic
Cas No.:985-12-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Drotaverine is an alkaloid that has been described as an inhibitor of phosphodiesterase 4 and negative allosteric modulator of L-type Ca2+ channels. Formulations containing drotaverine are used as antispasmodics to help cervical dilation in the early stages of labor.
| Cas No. | 985-12-6 | SDF | |
| 别名 | 盐酸屈他维林 | ||
| Canonical SMILES | CCOC1=C(OCC)C=C(CCN/C2=C\C3=CC=C(OCC)C(OCC)=C3)C2=C1.Cl | ||
| 分子式 | C24H31NO4•HCl | 分子量 | 434 |
| 溶解度 | DMF: 1 mg/ml,DMF:PBS (pH 7.2) (1:5): 0.16 mg/ml,DMSO: 1 mg/ml,Ethanol: 0.5 mg/ml | 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 | 2.3041 mL | 11.5207 mL | 23.0415 mL |
| 5 mM | 0.4608 mL | 2.3041 mL | 4.6083 mL |
| 10 mM | 0.2304 mL | 1.1521 mL | 2.3041 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。
Compatibility of Drotaverine hydrochloride with Ibuprofen and Ketoprofen Nonsteroidal Anti-Inflammatory Drugs Mixtures
Materials (Basel) 2022 Feb 8;15(3):1244.PMID:35161188DOI:10.3390/ma15031244.
Formulations with two or more active pharmaceutical ingredients (APIs) are a researched trend due to their convenient use compared with multiple medications. Moreover, drug-drug combinations may have a synergistic effect. Drotaverine hydrochloride (D-HCl) is commonly used for its antispasmodic action. The combination of a spasmolytic and an analgesic drug such as ibuprofen (Ibu) or ketoprofen (Ket) could become the answer for the treatment of localized pain. D-HCl:Ibu and D-HCl:Ket drug-drug interactions leading to the formation of eutectic compositions with increased bioavailability, obtained by mechanosynthesis, a green, solvent-free method was explored for the first time. The compatibility of Ibuprofen, Ketoprofen, and Drotaverine hydrochloride was investigated using differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier-Transform Infrared spectroscopy (FTIR). Solid-liquid equilibrium (SLE) phase diagrams for the binary systems of active pharmaceutical ingredients were developed and the Tammann diagrams were designed to determine the eutectic compositions. The excess thermodynamic functions GE for the pre-, post-, and eutectic compositions were obtained using the computed activity coefficients data. Results show that drotaverine-based pharmaceutical forms for pain treatment may be obtained at 0.9 respectively 0.8 molar fractions of ibuprofen and ketoprofen which is advantageous because the maximum allowed daily dose of Ibu is about 6 times higher than those of D-HCl and Ket. The obtained eutectics may be a viable option for the treatment of pain associated with cancer therapy.
Drotaverine hydrochloride Superporous Hydrogel Hybrid System: a Gastroretentive Approach for Sustained Drug Delivery and Enhanced Viscoelasticity
AAPS PharmSciTech 2022 Apr 26;23(5):124.PMID:35471680DOI:10.1208/s12249-022-02280-2.
This study aims to prepare Drotaverine hydrochloride superporous hydrogel hybrid systems (DSHH systems) to prolong its residence time in the stomach, provide extended release and reduce its frequency of administration. Drotaverine hydrochloride (DRH) is a spasmolytic drug that suffers from brief residence due to intestinal hypermotility during diarrheal episodes associated with gastrointestinal colics resulting in low bioavailability and repeated dosing. Eight DSHH systems were prepared using gas blowing technique. The prepared DSHH systems were evaluated regarding their morphology, incorporation efficiency, density, porosity, swelling ratio, viscoelastic property, erosion percentage and release kinetics. The FH8 formula containing equal proportion of chitosan (3%) /polyvinyl alcohol (3%) as strengthener and crosslinked with tripolyphosphate showed the highest incorporation efficiency (91.83 ± 1.33%), good swelling ratio (28.32 ± 3.15% after 24 h), optimum viscoelastic properties (60.19 ± 3.82 kPa) and sustained release profile (88.03 ± 2.15% after 24 h). A bioequivalence study was done to compare the bioavailability of the candidate formula versus Spasmocure®. Statistical analysis showed significant (P < 0.05) increase in bioavailability 2.7 folds with doubled Tmax (4 h) compared to the marketed product (2 h). These results declared that the superporous hydrogel hybrid systems could be a potential gastroretentive approach for the sustained delivery of drugs with short residence time with enhanced viscoelasticity.
Drotaverine hydrochloride for augmentation of labor
Int J Gynaecol Obstet 2004 Jan;84(1):17-22.PMID:14698825DOI:10.1016/s0020-7292(03)00276-5.
Objectives: To study the use of Drotaverine hydrochloride for acceleration of labor and relief of labor pains. Methods: In this double-blind placebo-controlled randomized study, 100 primigravidas in uncomplicated spontaneous labor at term were given Drotaverine hydrochloride or placebo (distilled water) intramuscularly. Labor events, including pain (assessed by a visual analog scale and a verbal rating scale), neonatal outcome, and side effects of the drug were recorded. Student's t-test was used for analysis. Results: Forty-four patients in the drug group and 40 in the placebo group had complete data for analysis after decoding. In Drotaverine group, there was a mean 15% reduction in the duration of the first stage of labor and a mean 19% reduction in the second stage. The maximum shortening of the first stage (28%) was observed when Drotaverine was administered when cervical dilatation was 4 cm (P=0.044). There were no adverse fetal effects, but atonic postpartum hemorrhage was more common in the Drotaverine group. There was no relief of pain with the drug except in the fourth stage of labor. Conclusions: Drotaverine hydrochloride is safe and effective in accelerating labor, but not effective in lessening labor pain.
Drotaverine to shorten the duration of labour in primigravidas: a randomised, double-blind, placebo-controlled trial
Afr Health Sci 2022 Sep;22(3):108-116.PMID:36910347DOI:10.4314/ahs.v22i3.13.
Background: Drotaverine, a spasmolytic, has been found to have potential to achieve a reduction in the duration of labour and prevent prolonged labour. Objective: To compare the effects of intravenous Drotaverine hydrochloride with placebo for shortening the duration of active phase of labour in primigravidas. Methods: A double-blind, placebo-controlled randomized trial of 246 primigravidas in active phase of labour at term was conducted. They were randomly (1:1 ratio) administered intravenous 2 ml (40mg) of Drotaverine hydrochloride or 2 ml of Vitamin B complex as placebo. The primary outcome measure was the duration of active phase of labour. The secondary outcome measures were cervical dilatation rate, oxytocin augmentation rate, incidence of prolonged labour, labour pain scores, mode of delivery, maternal and neonatal outcomes. Results: The mean duration of active phase of labour (hour) was significantly lower in the Drotaverine group compared to the control (Drotaverine; 6.22 ± 2.41 vs placebo; 8.33 ± 3.56; p <0.001). Also, the cervical dilatation rate (cm/hr) was significantly faster in the Drotaverine arm (Drotaverine; 1.68 ± 1.02 versus placebo; 1.06 ± 0.53, p <0.001). There was a significantly higher probability of faster delivery among women who were given Drotaverine (log-rank test, p < 0.001). The oxytocin augmentation rate, incidence of prolonged labour, labour pain scores, mode of delivery, maternal and neonatal outcomes were not significantly different among the groups. Conclusions: Drotaverine hydrochloride is effective in shortening the duration of active phase of labour without adverse maternal and neonatal outcomes. However, more evidence is needed to explore its role in active phase of labour among primigravid women. Trial registration number: PACTR201810902005232.
Drotaverine hydrochloride vs. valethamate bromide in acceleration of labor
Int J Gynaecol Obstet 2001 Sep;74(3):255-60.PMID:11543749DOI:10.1016/s0020-7292(01)00448-9.
Objectives: To compare the efficacy and safety of Drotaverine hydrochloride and valethamate bromide in shortening the duration of labor. Methods: In a randomized controlled trial of 150 nulliparous women in established labor with cervical dilation of 4 cm, 50 women were given Drotaverine (group I), 50 women were given valethamate (group II) and another 50 women were not given any medication (group III). Duration of labor, mode of delivery, side effects, and neonatal outcome were measured in all cases. Appropriate non-parametric tests and chi(2) tests were used for assessment of statistical significance. Results: In the three groups, 100%, 96% and 46% women delivered within 6 h, respectively. The injection-to-delivery interval was significantly reduced in the Drotaverine group (193.96 min) in contrast to the valethamate group (220.68 min) and control group (412.84 min). The rate of cervical dilation was highest in the Drotaverine group (2.04 cm/h) compared with the valethamate bromide group (1.86 cm/h) and control group (1.01 cm/h). There were no major maternal or fetal adverse effects in any group, but minor side effects were more common in the valethamate group. Conclusion: Both intramuscular Drotaverine hydrochloride and valethamate bromide are effective in acceleration of labor; however, Drotaverine accelerates labor more rapidly and is associated with less side effects.