Propacetamol
(Synonyms: 丙帕他莫) 目录号 : GC66258
A prodrug form of acetaminophen
Cas No.:66532-85-2
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
Propacetamol is a prodrug form of the analgesic and antipyretic agent acetaminophen .1 It is converted to acetaminophen by rat liver microsomes. Propacetamol reduces acetic acid-induced writhing in mice and LPS-induced pyresis in rats when administered at doses of 200 and 600 mg/kg, respectively.1,2 Propacetamol (1,200 mg/kg) induces hepatotoxicity, decreases hepatic glutathione (GSH), superoxide dismutase (SOD), and glutathione peroxidase (GPX) levels, increases hepatic malondialdehyde (MDA) and nitrotyrosine levels, and increases mortality in mice.3
1.Murie, V.E., Marques, L.M.M., Souza, G.E.P., et al.Acetaminophen prodrug: Microwave-assisted synthesis and in vitro metabolism evaluation by mass spectrometryJ. Braz. Chem. Soc.27(6)1121-1128(2016) 2.Zhang , Y., Du, L., Pan, H., et al.Enhanced analgesic effects of propacetamol and tramadol combination in rats and miceBiol. Pharm. Bull.34(3)349-353(2011) 3.Liou, G.-G., Hsieh, C.-C., Lee, Y.-J., et al.N-Acetyl cysteine overdose inducing hepatic steatosis and systemic inflammation in both propacetamol-induced hepatotoxic and normal miceAntioxidants (Basel)10(3)442(2021)
| Cas No. | 66532-85-2 | SDF | Download SDF |
| 别名 | 丙帕他莫 | ||
| 分子式 | C14H20N2O3 | 分子量 | 264.32 |
| 溶解度 | H2O : 100 mg/mL (378.33 mM; Need ultrasonic) | 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 | 3.7833 mL | 18.9165 mL | 37.8329 mL |
| 5 mM | 0.7567 mL | 3.7833 mL | 7.5666 mL |
| 10 mM | 0.3783 mL | 1.8916 mL | 3.7833 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。
Propacetamol in dogs: First description of its pharmacokinetics after intravenous and oral administration
Res Vet Sci 2022 May;144:11-17.PMID:35033846DOI:10.1016/j.rvsc.2022.01.002.
Propacetamol is a prodrug form of paracetamol (APAP) licensed for human use as a pain reliever in postoperative care. It is prescribed if APAP cannot be administered orally or rectally to a patient and for patients in whom nonsteroidal anti-inflammatory drugs are contraindicated. In this study, we aimed to quantify the pharmacokinetics of APAP and its metabolites, paracetamol sulfate (PS), paracetamol glucuronide (PG), and N-acetyl-p-benzoquinone imine (NAPQI), after a single oral and intravenous (IV) administration of 30 mg/kg of Propacetamol to six healthy adult Labrador dogs according to a 2 × 2 crossover study. The analyses were performed using a validated HPLC-MS/MS method. PS and PG exposures were higher than that of APAP, while NAPQI concentrations were constantly below the detection limit of the analytical method. IV Propacetamol administration produced 30% more APAP than oral administration. However, Propacetamol released a significantly lower amount of active moiety in dogs than in humans. The Propacetamol dose administered in this study did not produce plasma APAP concentrations above the threshold sufficient to provide analgesia in adult humans (4 μg/mL). In conclusion, direct IV injection of APAP instead of Propacetamol might be a better clinical option for pain relief in dogs.
Single dose intravenous Propacetamol or intravenous paracetamol for postoperative pain
Cochrane Database Syst Rev 2011 Oct 5;(10):CD007126.PMID:21975764DOI:10.1002/14651858.CD007126.pub2.
Background: Paracetamol (acetaminophen) is the most commonly prescribed analgesic for the treatment of acute pain. It may be administered orally or intravenously. The efficacy and safety of intravenous (IV) formulations of paracetamol, IV paracetamol and IV Propacetamol, compared with placebo and other analgesics, is unclear. Objectives: To assess the efficacy and safety of IV formulations of paracetamol for treatment of postoperative pain in both adults and children. Search strategy: We searched the Cochrane Central Register of Controlled Trials (CENTRAL) (The Cochrane Library 2010, Issue 2), MEDLINE (1950 to May 2010), EMBASE (1980 to 2010, Week 18), LILACS (1992 to May 2010) and reference lists of retrieved articles. Selection criteria: Randomized, double-blind, placebo- or active-controlled single dose clinical trials of IV Propacetamol or IV paracetamol for acute postoperative pain in adults or children. Data collection and analysis: Two review authors independently assessed the risk of bias and extracted data. We contacted study authors for additional information. We collected adverse event information from the studies. Main results: Thirty-six studies (3896 participants) were included. Thirty-seven percent of participants receiving IV Propacetamol/paracetamol experienced at least 50% pain relief over four hours compared with 16% of those receiving placebo (number needed to treat to benefit (NNT = 4.0; 95% confidence interval 3.5 to 4.8). The proportion of participants in IV Propacetamol/paracetamol groups experiencing at least 50% pain relief diminished over six hours, as reflected in a higher NNT of 5.3 (4.2 to 6.7). Participants receiving IV Propacetamol/paracetamol required 30% less opioid over four hours than those receiving placebo. However, this did not translate to a reduction in opioid-induced adverse events.Meta-analysis of efficacy comparisons between IV Propacetamol/paracetamol and active comparators (opioids or nonsteroidal anti-inflammatories (NSAIDs)) were either not statistically significant, not clinically significant, or both.Adverse events occurred at similar rates with IV Propacetamol or IV paracetamol and placebo. However, pain on infusion occurred more frequently in those receiving IV Propacetamol versus placebo (23% versus 1%).Meta-analysis did not demonstrate statistically significant differences between IV Propacetamol/paracetamol and active comparators for any adverse event except a reduction in the rate of hypotension versus NSAIDs and a reduction in the rate of gastrointestinal disorders versus opioids. Authors' conclusions: A single dose of both IV Propacetamol and IV paracetamol provides around four hours of effective analgesia for about 37% of patients with acute postoperative pain. Both formulations are associated with few adverse events, although patients receiving IV Propacetamol have a higher incidence of pain on infusion than both placebo and IV paracetamol.
[Propacetamol: from basic action to clinical utilization]
Ann Fr Anesth Reanim 1999 Mar;18(3):332-40.PMID:10228672DOI:10.1016/s0750-7658(99)80059-8.
Objective: To review pharmacology and therapeutic use of Propacetamol, an injectable prodrug of acetaminophen (paracetamol). Data sources: Extraction from the Medline database of French and English articles on pharmacology and clinical use of Propacetamol. Study selection: Articles providing new data into the mechanisms of the analgesic action of paracetamol. Selection of controlled studies (original articles and abstracts of oral communications on therapeutic trials with Propacetamol as a single agent or part of balanced analgesia protocols). Case reports and letters to the editor were not considered in this analysis. Data extraction: Clinical articles were selected for advantages and adverse effects of Propacetamol. Articles dealing with mechanisms of action of Propacetamol and paracetamol were selected for the more recent data, excluding those reporting outdated theories not confirmed or abandoned. Data synthesis and conclusion: Mechanisms of action of paracetamol differ from those of NSAIDs, giving account of a low risk of adverse renal, gastrointestinal and haematological effects. Thanks to their high therapeutic index, prescription of Propacetamol and paracetamol is quite simple and safe. Main indications of both drugs are painful conditions, especially but not exclusively in the postoperative period, not requiring opioids and also in combination with other analgesic drug and/or techniques (balanced or multimodal analgesia). Because of cost, IV Propacetamol is changed for oral paracetamol as soon as possible.
Single dose intravenous paracetamol or intravenous Propacetamol for postoperative pain
Cochrane Database Syst Rev 2016 May 23;2016(5):CD007126.PMID:27213715DOI:10.1002/14651858.CD007126.pub3.
Background: This is an updated version of the original Cochrane review published in Issue 10, 2011. Paracetamol (acetaminophen) is the most commonly prescribed analgesic for the treatment of acute pain. It may be administered orally, rectally, or intravenously. The efficacy and safety of intravenous (IV) formulations of paracetamol, IV paracetamol, and IV Propacetamol (a prodrug that is metabolized to paracetamol), compared with placebo and other analgesics, is unclear. Objectives: To assess the efficacy and safety of IV formulations of paracetamol for the treatment of postoperative pain in both adults and children. Search methods: We ran the search for the previous review in May 2010. For this update, we searched the Cochrane Central Register of Controlled Trials (CENTRAL 2016, Issue 1), MEDLINE (May 2010 to 16 February 2016), EMBASE (May 2010 to 16 February 2016), LILACS (2010 to 2016), a clinical trials registry, and reference lists of reviews for randomized controlled trials (RCTs) in any language and we retrieved articles. Selection criteria: Randomized, double-blind, placebo- or active-controlled single dose clinical trials of IV paracetamol or IV Propacetamol for acute postoperative pain in adults or children. Data collection and analysis: Two review authors independently extracted data, which included demographic variables, type of surgery, interventions, efficacy, and adverse events. We contacted study authors for additional information. We graded each included study for methodological quality by assessing risk of bias and employed the GRADE approach to assess the overall quality of the evidence. Main results: We included 75 studies (36 from the original review and 39 from our updated review) enrolling a total of 7200 participants.Among primary outcomes, 36% of participants receiving IV paracetamol/Propacetamol experienced at least 50% pain relief over four hours compared with 16% of those receiving placebo (number needed to treat to benefit (NNT) = 5; 95% confidence interval (CI) 3.7 to 5.6, high quality evidence). The proportion of participants in IV paracetamol/Propacetamol groups experiencing at least 50% pain relief diminished over six hours, as reflected in a higher NNT of 6 (4.6 to 7.1, moderate quality evidence). Mean pain intensity at four hours was similar when comparing IV paracetamol and placebo, but was seven points lower on a 0 to 100 visual analog scale (0 = no pain, 100 = worst pain imaginable, 95% CI -9 to -6, low quality evidence) in those receiving paracetamol at six hours.For secondary outcomes, participants receiving IV paracetamol/Propacetamol required 26% less opioid over four hours and 16% less over six hours (moderate quality evidence) than those receiving placebo. However, this did not translate to a clinically meaningful reduction in opioid-induced adverse events.Meta-analysis of efficacy comparisons between IV paracetamol/Propacetamol and active comparators (e.g., opioids or nonsteroidal anti-inflammatory drugs) were either not statistically significant, not clinically significant, or both.Adverse events occurred at similar rates with IV paracetamol or IV Propacetamol and placebo. However, pain on infusion occurred more frequently in those receiving IV Propacetamol versus placebo (23% versus 1%). Meta-analysis did not demonstrate clinically meaningful differences between IV paracetamol/Propacetamol and active comparators for any adverse event. Authors' conclusions: Since the last version of this review, we have found 39 new studies providing additional information. Most included studies evaluated adults only. We reanalyzed the data but the results did not substantially alter any of our previously published conclusions. This review provides high quality evidence that a single dose of either IV paracetamol or IV Propacetamol provides around four hours of effective analgesia for about 36% of patients with acute postoperative pain. Low to very low quality evidence demonstrates that both formulations are associated with few adverse events, although patients receiving IV Propacetamol have a higher incidence of pain on infusion than both placebo and IV paracetamol.
Single-dose intravenous paracetamol or Propacetamol for prevention or treatment of postoperative pain: a systematic review and meta-analysis
Br J Anaesth 2011 Jun;106(6):764-75.PMID:21558067DOI:10.1093/bja/aer107.
Paracetamol is the most commonly prescribed analgesic for the treatment of acute pain. The efficacy and safety of i.v. formulations of paracetamol is unclear. We performed a systematic search (multiple databases, bibliographies, any language, to May 2010) for single-dose, randomized, controlled clinical trials of Propacetamol or i.v. paracetamol for acute postoperative pain in adults or children. Thirty-six studies involving 3896 patients were included. For the primary outcome, 37% of patients (240/367) receiving Propacetamol or i.v. paracetamol experienced at least 50% pain relief over 4 h compared with 16% (68/527) receiving placebo (number needed to treat=4.0; 95% confidence interval, 3.5-4.8). The proportion of patients in Propacetamol or i.v. paracetamol groups experiencing at least 50% pain relief diminished over 6 h. Patients receiving Propacetamol or paracetamol required 30% less opioid over 4 h and 16% less opioid over 6 h than those receiving placebo. However, this did not translate to a reduction in opioid-induced adverse events (AEs). Similar comparisons between Propacetamol or i.v. paracetamol and active comparators were either not statistically significant, not clinically significant, or both. AEs occurred at similar rates with Propacetamol or i.v. paracetamol and placebo. However, pain on infusion occurred more frequently in those receiving Propacetamol compared with placebo (23% vs 1%). A single dose of either Propacetamol or i.v. paracetamol provides around 4 h of effective analgesia for about 37% of patients with acute postoperative pain. Both formulations are associated with few AEs, although patients receiving Propacetamol have a higher incidence of pain on infusion.