Proparacaine Hydrochloride (Proxymetacaine Hydrochloride)
目录号 : GC33729
Proparacaine盐酸盐是电压门控钠离子通道拮抗剂，ED50为3.4mM。
Cas No.:5875-06-9
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
Proparacaine Hydrochloride is a voltage-gated sodium channels antagonist with ED50 of 3.4 mM.IC50 Value: 3.4 mM(ED50) [1]Target: Sodium Channelin vitro: Proparacaine is more potent and less toxic than cocaine [1]. Proparacaine significantly increases in FHV-1 (P < 0.01), C. felis, and 28S rDNA Ct values when fusidic acid is used [2].in vivo: Proparacaine inhibits corneal epithelial migration and adhesion through alteration of the actin cytoskeleton [3]. Proparacaine acts like bupivacaine or lidocaine and produces dose-related spinal blockades of motor function, proprioception and nociception. Intrathecal proxymetacaine also produces longer sensory blockade than motor blockade [4].
[1]. Grant, R.L. and D. Acosta, Comparative toxicity of tetracaine, proparacaine and cocaine evaluated with primary cultures of rabbit corneal epithelial cells. Exp Eye Res, 1994. 58(4): p. 469-78. [2]. Segarra, S., K. Papasouliotis, and C. Helps, The in vitro effects of proxymetacaine, fluorescein, and fusidic acid on real-time PCR assays used for the diagnosis of Feline herpesvirus 1 and Chlamydophila felis infections. Vet Ophthalmol, 2011. 14 Suppl 1: [3]. Dass, B.A., H.K. Soong, and B. Lee, Effects of proparacaine on actin cytoskeleton of corneal epithelium. J Ocul Pharmacol, 1988. 4(3): p. 187-94. [4]. Hung, C.H., et al., Intrathecal oxybuprocaine and proxymetacaine produced potent and long-lasting spinal anesthesia in rats. Neurosci Lett, 2009. 454(3): p. 249-53.
| Cas No. | 5875-06-9 | SDF | |
| Canonical SMILES | O=C(OCCN(CC)CC)C1=CC=C(OCCC)C(N)=C1.[H]Cl | ||
| 分子式 | C16H27ClN2O3 | 分子量 | 330.85 |
| 溶解度 | DMSO: 50 mg/mL (151.13 mM); Water: 33.33 mg/mL (100.74 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 | 3.0225 mL | 15.1126 mL | 30.2252 mL |
| 5 mM | 0.6045 mL | 3.0225 mL | 6.045 mL |
| 10 mM | 0.3023 mL | 1.5113 mL | 3.0225 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。
Prolonged corneal anaesthesia by Proxymetacaine Hydrochloride detected by a thermal cooling stimulus
Cont Lens Anterior Eye 2009 Apr;32(2):84-7; quiz 99-100.PMID:19181566DOI:10.1016/j.clae.2008.12.006.
Purpose: To assess the duration, depth and recovery time of anaesthesia produced by 0.5% Proxymetacaine Hydrochloride (proparacaine), using a thermal cooling stimulus. Methods: Seventeen non-contact lens-wearing subjects were recruited (mean age=26+/-3.6 years, range=23-39; blue iris=8, brown iris=9). Central corneal sensitivity was measured in the right eye of each patient to establish a baseline, before 20microl of either 0.5% Proxymetacaine Hydrochloride (p) or 0.9% unpreserved saline (s) was instilled under four experimental conditions (right eye-left eye): p-p, p-s, s-p, s-s. Corneal sensitivity was re-measured at 2, 5, 10, 15, 20, 30, 45 and 60min post-instillation. Results: The onset of anaesthesia was observed at 2min (Wilcoxon, p<0.001), with the maximum anaesthesia occurring at 15min (Wilcoxon, p<0.001). Recovery of corneal sensitivity to baseline levels did not occur by 60min (Wilcoxon, p<0.001). No difference in onset time, depth of anaesthesia, or recovery time was noted between the blue and brown iris subjects (Mann-Whitney, p>0.05). Conclusions: Although the anaesthetic effect of 0.5% Proxymetacaine Hydrochloride continues for more than 60min, this finding does not alter current clinical practice. The extended duration, however, is of relevance to studies that use corneal anaesthesia to investigate the role of corneal nerves in the blink mechanism.
Identification, synthesis and structural confirmation of process-related impurities in Proparacaine Hydrochloride
J Pharm Biomed Anal 2020 Oct 25;190:113497.PMID:32798917DOI:10.1016/j.jpba.2020.113497.
Proparacaine Hydrochloride is an ester-type local anesthetic agent that is extensively used in ophthalmic operations. The process-related impurities of Proparacaine Hydrochloride were investigated, and seven impurities were detected in the reaction solution of the last step at the level of 0.03-1.08 % by a newly developed HPLC method. Based on the synthetic process and the results of LC-HRMS, the structures of five impurities were proposed as 3-amino-4-propoxybenzoic acid (Imp-A), ethyl 3-amino-4-propoxybenzoate (Imp-B), 2-(ethylamino)ethyl 3-amino-4-propoxybenzoate hydrochloride (Imp-C), 2-(diethylamino)ethyl 3-nitro-4-propoxybenzoate hydrochloride (Imp-F), and 3-nitro-4-propoxybenzoic acid (Imp-G). And the structures were confirmed by synthesis, followed by varieties of spectral and chromatographic analyses. The structures of two impurities with almost same molecular weight in LC-HRMS were elucidated as 2-(diethylamino)ethyl 3-(ethylamino)-4-propoxy-benzoate hydrochloride (Imp-D) and 2-(diethylamino)ethyl 3-formamido-4-propoxybenzoate hydrochloride (Imp-E) by NMR and IR. An HPLC-based method was developed, and validation study demonstrated that the approach was precise, accurate, and sensitive. The impurities information of Proparacaine Hydrochloride can be used for the quality control of intermediate, raw material drug and its commercial products.
Degree of corneal anaesthesia after topical application of 0.4% oxybuprocaine hydrochloride and 0.5% Proparacaine Hydrochloride ophthalmic solution in clinically normal cattle
Aust Vet J 2016 Jun;94(6):181-5.PMID:27237118DOI:10.1111/avj.12443.
Objectives: The use of corneal anaesthesia is necessary for a range of clinical purposes. Therefore, we assessed and compared the efficacy of corneal anaesthesia after application of 0.4% oxybuprocaine hydrochloride and 0.5% Proparacaine Hydrochloride ophthalmic solution in clinically normal cattle. Methods: The 24 clinically normal cows were allocated into two groups. Cows in group 1 (n = 12) received 0.2 mL of 0.4% oxybuprocaine hydrochloride with fluorescein ophthalmic solution in one eye and 0.2 mL of sterile saline (0.9% NaCl) with fluorescein in the contralateral eye (control). Group 2 (n = 12) received 0.2 mL of 0.4% oxybuprocaine hydrochloride with fluorescein ophthalmic solution in one eye and 0.2 mL of 0.5% Proparacaine Hydrochloride with fluorescein in the contralateral eye (control). In each group, corneal touch threshold was determined by Cochet-Bonnet aesthesiometer for both eyes immediately prior to topical administration of solutions, at 1 min and 5 min after administration of topical solutions and every 5 min thereafter for a total of 75 min. Results: Significant corneal anaesthesia was noted immediately following topical application of both oxybuprocaine and proparacaine as compared with controls, with maximal corneal anaesthesia noted 1 min after administration. Both oxybuprocaine and proparacaine produced significant corneal anaesthesia for the duration of the 75-min study. Neither oxybuprocaine hydrochloride nor Proparacaine Hydrochloride treatment resulted in visible adverse effects. Conclusion: There are limited data available demonstrating the efficacy and duration of corneal anaesthetic agents in cattle. Both oxybuprocaine hydrochloride and Proparacaine Hydrochloride should be considered practical options for providing corneal anaesthesia in cattle in a clinical setting.
A single drop of 0.5% Proparacaine Hydrochloride for uncomplicated clear corneal phacoemulsification
Middle East Afr J Ophthalmol 2013 Jul-Sep;20(3):221-4.PMID:24014985DOI:10.4103/0974-9233.114795.
Purpose: The purpose of this study was to compare the efficacy of a single drop of 0.5% Proparacaine Hydrochloride in uncomplicated cataract surgery with phacoemulsification. Materials and methods: Two hundred and ninety five patients scheduled for the phacoemulsification were divided into 2 groups based on the anesthetic agents they were to receive: 146 patients who received a single drop of 0.5% proparacaine 2 min before the start of the surgery (proparacaine group) and; 149 patients who received supplementation of 0.5% intracameral preservative free xylocaine (xylocaine group). A single surgeon performed all surgeries. Intraoperative and post-operative pain scores were evaluated on a visual analog scale. The surgeon noted his subjective impression of corneal clarity, discomfort while performing the surgery any supplemental anesthesia required and intraoperative complications. An anesthetist noted vital parameters and the need for intravenous sedation. Total surgical time was noted. Comparison of parameters was performed with the Chi-square test, and A P value less than 0.05 was considered as statistically significant. Results: No statistically significant difference was seen in the intraoperative (P = 0.24) and post-operative (P = 0.164) pain scores between groups. There was no pain (0 score) in 41.8% of patients in the proparacaine group and 46.3% of patients in the xylocaine group. The average surgical time (P = 0.279) and surgeon discomfort (P = 0.07) were not statistically significantly different between groups. No patients required supplemental anesthesia. There were no surgical complications that could compromise the visual outcome. An equal number of patients in both groups preferred same type of anesthetic technique for the fellow eye cataract surgery (89.11% for the proparacaine group and 90.18% for the xylocaine group). No patients in either group had changes in vital parameters or required intravenous sedation. Conclusion: A single drop pre-operatively, of Proparacaine Hydrochloride was comparable to the intracameral supplementation of preservative free xylocaine for phacoemulsification in uncomplicated cataract surgery without compromising the visual outcome. However, we recommend individualizing the anesthetic technique according to the requirements of the surgeon.
Proparacaine Hydrochloride topical drop and intracameral 0.5% lignocaine for phacotrabeculectomy in patients with primary open angle glaucoma
Middle East Afr J Ophthalmol 2014 Jul-Sep;21(3):210-5.PMID:25100903DOI:10.4103/0974-9233.134669.
Aim: To compare the efficacy and safety of 0.5% intracameral lignocaine to 1% intracameral lignocaine prior to phacotrabeculectomy. Study design: Prospective, comparative, observational, and interventional study. Setting: Tertiary eye care center in central India. Materials and methods: This study was comprised of 79 patients (79 eyes) with primary open angle glaucoma scheduled for phacotrabeculectomy. Patients were assigned to 1 of 2 Groups receiving proparacaine 0.5% eye drops and 1% intracameral lignocaine just prior to phacotrabeculectomy (Group 1, n = 39) and 0.5% intracameral lignocaine after completion of phacoemulsification just prior to trabeculectomy (Group 2, n = 40). The visual analogue scale was used to record intraoperative and postoperative pain. Patient comfort, intraoperative painful sensations perceived by the patient, supplemental anesthesia, complications, and surgeon discomfort were noted. An anesthetist also noted the vital parameters and the requirement for intravenous medications. Results: There was no significant difference in the intraoperative pain score (P = 0.0733) or supplemental anesthesia (P = 0.372) between Groups. Postoperative pain score was statistically significant in Group 2 (P < 0.0001). The overall operating conditions in both Groups were comparable (P = 0.7389). A greater number of patients in Group 2 (88.57%) preferred the same anesthetic technique for combined surgery in the fellow eye. There was no difference in inadvertent eye movements and lid squeezing between Groups and they did not interfere with surgery. Conclusion: Topical anesthetic drops supplemented with 0.5% intracameral lignocaine before performing trabeculectomy is as effective as 1% intracameral lignocaine given at the beginning of phacotrabeculectomy for primary open angle glaucoma.