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paracetamol (paracetamol, EFVDAS)

✓ Approved

Elan · PTGS1 · 小分子

什么是 paracetamol？

paracetamol 是一种小分子，由Elan研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名paracetamol, EFVDAS
公司Elan
药物类别小分子
分子靶点PTGS1, PTGS2
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Elan

作用机制

分子靶点

paracetamol 作用于 2 个分子靶点：

PTGS1prostaglandin-endoperoxide synthase 1 (COX3, PCOX1)
PTGS2prostaglandin-endoperoxide synthase 2 (GRIPGHS, hCox-2)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

paracetamol 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Gastrointestinal disordersAbdominal pain✓ Approved

相关研究文献

PubMedChemMedChem2026-09-11

Phosphorylated Analogs of Paracetamol and Their Anti-Inflammatory Potential.

Cruz Osvaldo León de la OL, Gutiérrez-Rebolledo Gabriel Alfonso GA, Castro Carlos Zepactonal Gómez CZG, Juárez Ángel Daniel Campos ÁDC et al.

Paracetamol is a widely used analgesic and antipyretic agent; however, its use is limited by minimal anti-inflammatory activity and the risk of hepatotoxicity from prolonged oral use or in acute overdose. To address these limitations, four novel phosphorylated paracetamol analogs (2a-2d) were synthesized via a UV-radical methodology and evaluated through integrated in silico, in vitro, and in vivo for anti-inflammatory dermal approaches. Molecular docking suggested plausible binding interactions with COX-1 and COX-2 for all analogs. In vitro cytotoxicity assays in THP-1 cells showed that 2a and 2b did not affect cell viability at 100 μM over 24 h. In a TPA-induced acute ear edema model in CD1 male mice, 2a produced about 50% inhibition of edema at the lowest tested quantity (0.5 mg/ear), representing a fourfold potency advantage over indomethacin at the same amount, while 2b displayed significant anti-inflammatory and vasoregulatory activity at higher quantities. Computational ADME profiling indicated that all analogs satisfy Lipinski's drug-likeness criteria and exhibit low predicted hERG channel risk. These results support N-phosphorylation of 4-aminophenol as a viable strategy to improve the topical anti-inflammatory efficacy of paracetamol analogs.

PMID 42723329
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PubMedNanoscale advances2026-09-11

Development of Co and Cu-based metal-organic frameworks for electrochemical sensing of Pb ions and paracetamol.

Akter Farzana F, Khan Sanjida S, Islam Suravi S, Chowdhury A M Sarwaruddin AMS et al.

The present study investigates charge-transfer activity in electrochemistry using a metal-organic framework (MOF) to detect pharmaceutical contaminants (organic substances) along with toxic metals (inorganic pollutants). These contaminants constitute a major threat to human health as well as to the environment because of their persistence, adverse effects, and bioaccumulation. The MOFs (Cu MOF, Cu-Co MOF, and Co MOF) were produced via solvothermal synthesis. They were analyzed by a variety of methods, such as X-ray diffraction (XRD) and Fourier transform infrared (FTIR) spectroscopy. The range of crystalline size of the synthesized MOFs using the Debye-Scherrer equation was 80-92 nm. The thermal resistance of the MOFs was examined using thermogravimetric analysis (TGA). In this study, a bimetallic Cu-Co MOF-modified electrode was developed and systematically evaluated as an electrochemical sensing material. In comparison with the monometallic Cu MOF and Co MOF, the Cu-Co MOF exhibited enhanced electrochemical performance, which could be attributed to the synergistic effect of the two metal centers. Furthermore, the Cu-Co MOF served as a dual-electrode system for detecting two analytes (paracetamol and Pb), highlighting its potential as a versatile sensing platform for pharmaceutical and environmental monitoring. For paracetamol, the limit of detection (LOD) and limit of quantitation (LOQ), based on the oxidation current, were 1.98 and 6.59 ppm, respectively. Similarly, based on the reduction current, the calculated LOD and LOQ were 0.20 ppm and 0.68 ppm, respectively. For a heavy metal (Pb), the estimated LOD and LOQ were 0.09 and 0.31 ppm, respectively.

PMID 42724898
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PubMedJournal of the Chinese Medical Association : JCMA2026-09-11

2026 Taiwan guidelines for the acute pharmacologic treatment of migraine in adults.

Lau Chi Ieong CI, Chen Wei-Ta WT, Hou Tsung-Wei TW, Liaw Yi-Chia YC et al.

Since the publication of the Taiwan Headache Society's 2022 Guidelines for the Acute Treatment of Migraine Attacks, advances in headache medicine and the approval of new drugs in Taiwan have necessitated an update. To address clinical needs, the Guideline Committee of the Taiwan Headache Society reviewed evidence for pharmacological and non-pharmacological acute treatments using evidence-based principles. Drawing from the latest European, American, and international guidelines, and through expert consensus, this revision updates treatment roles, grades of recommendation, efficacy, and adverse-effect profiles. Currently, a broad range of medications is available in Taiwan for acute migraine management, categorised into "specific" and "non-specific" agents. Specific treatments include oral and intranasal triptans, and gepants, i.e., oral calcitonin gene-related peptide (CGRP) receptor antagonists. Non-specific agents include acetaminophen and non-steroidal anti-inflammatory drugs (NSAIDs: diclofenac, ibuprofen, naproxen). Injectable prochlorperazine is also strongly recommended. Ergotamine/caffeine combinations are less effective and are second-line agents, while high-dose aspirin is limited by gastrointestinal risk. Considering the potential risk of dependency, tramadol or tramadol/paracetamol combinations should be reserved until all other agents fail, and should be limited to oral forms. Other opioids, such as morphine, butorphanol, etc., lack evidence and are not recommended. Treatment should follow the principle of stratified care: oral NSAIDs for mild disability, with combination analgesics or parenteral NSAIDs as alternatives, and oral or intranasal triptans for moderate to severe disability, ideally administered early. Antiemetics may be added, and combining triptans with NSAIDs enhances efficacy. Rimegepant can be considered a first-line therapy, particularly for patients who are unresponsive or intolerant to triptans, have cardiovascular contraindications, or are at risk of developing medication overuse. In status migrainosus, parenteral corticosteroids with intravenous fluids are advised. Acetaminophen remains first-line for children and pregnant women. To prevent medication-overuse headache, acute treatments, including NSAIDs, acetaminophen, triptans, ergot derivatives, and combination analgesics, should not exceed two days per week, probably with the exception of rimegepant.

PMID 42723131
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PubMedFrontiers in oral health2026-09-11

Comparative effectiveness of therapeutic ultrasound and pharmacotherapy in the management of muscular temporomandibular disorders: a randomized clinical trial.

Subhikshaa M M, Shetty Prathima P, Veena K M KM, Shenoy Prashanth P et al.

Temporomandibular disorders (TMDs) of muscular origin are a common cause of chronic orofacial pain and functional limitation. Conservative management includes pharmacotherapy and physiotherapeutic modalities such as therapeutic ultrasound. However, evidence directly comparing their effectiveness remains limited. This randomized clinical trial compared therapeutic ultrasound and pharmacotherapy in reducing pain intensity and improving mandibular function in patients with muscular TMDs. A prospective, parallel-group randomized clinical trial was conducted among 36 patients diagnosed with muscular TMDs according to Group I of the Research Diagnostic Criteria for Temporomandibular Disorders (RDC/TMD). Following ethical approval (YEC-1/2024/038) and CTRI registration (CTRI/2024/12/077788), participants were randomly allocated into two groups (n = 18). Group A received ibuprofen (400 mg), paracetamol (325 mg), and chlorzoxazone (250 mg) twice daily for seven days. Group B received therapeutic ultrasound (1 MHz, 1.0 W/cm², continuous mode) for 10 min daily for seven days. Pain intensity was assessed using the Numerical Rating Scale (NRS), and maximum mouth opening was measured using a Vernier calliper. Data were analysed using paired and independent Student's t-tests (p < 0.05). All participants completed the study. Both groups showed significant reductions in pain intensity and improvements in maximum mouth opening (p < 0.05). Mean NRS scores decreased from 6.31 ± 1.35 to 2.94 ± 1.06 in the pharmacotherapy group and from 5.56 ± 1.97 to 1.69 ± 1.08 in the therapeutic ultrasound group. Mean mouth opening increased from 40.31 ± 3.63 mm to 41.44 ± 2.94 mm and from 40.75 ± 3.55 mm to 43.63 ± 2.55 mm, respectively. Therapeutic ultrasound achieved significantly greater pain reduction (p = 0.002) and greater improvement in mouth opening (p = 0.032). No adverse events were reported. Both treatments were effective for muscular temporomandibular disorders; however, therapeutic ultrasound was associated with greater short-term improvements in pain intensity and maximum mouth opening than pharmacotherapy under the conditions of this study. https://ctri.nic.in/Clinicaltrials/login.php, identifier CTRI/2024/12/077788.

PMID 42723852
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PubMedFrontiers in pharmacology2026-09-09

The interaction between paracetamol and ethanol during the early development of zebrafish.

Małkowska Anna A, Wieczorek Karolina K, Pawlak Kacper K, Bonder Julia Elżbieta JE

The issue of drug-alcohol interactions is a major concern in drug therapy and can endanger patient safety. Paracetamol is one of the most widely used analgetic drugs, while ethanol is commonly consumed addictive substance. This study investigated the toxic effects of paracetamol, ethanol, and their mixture at different concentrations on the embryonic development of zebrafish (Danio rerio, D. rerio). Zebrafish embryos (20 embryos per group, 3 biological replicates for each concentration or combination of concentrations) were exposed for 72 h post-fertilization to paracetamol (0.5, 1.0, 2.0, 3.0, 5.0, and 10.0 mM), ethanol (85.5, 171.0, 256.5, 342.0, 513.0, 855.0) or their combinations. Additionally, combinations of paracetamol and ethanol were examined to assess the type of interaction (0.5:85.5; 1.0:171.0; 1.5:256.5; 2.0:342.0; 3.0:513.0; and 5.0: 855.0 mM). The combination of the drug and alcohol resulted in a higher incidence of developmental defects compared to the effects of either substance used alone. The most frequently observed changes included decreased larval pigmentation, pericardial and sac edema or increased larval mortality compared to control (e.g., 2-4 fold increase over control). Notably, there was a statistically significant reduction in both eye size and body length of the larvae. Furthermore, the severity of the defects increased proportionally with dose. Additionally, analysis using the Chou-Talalay method revealed the synergism in this interaction, with a combination index below 1. These findings demonstrate that exposure to paracetamol and ethanol exerts a synergistic toxic effect on early zebrafish development, emphasising the potential risks associated with drug-alcohol co-exposure.

PMID 42713147
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PubMedHuman reproduction open2026-09-09

Fetal exposure to paracetamol is associated with altered markers of ovarian development and reduced uterine volume in girls: the COPANA study.

Fischer Margit B MB, Mola Gylli G, Sundberg Karin K, Scheel Lone L et al.

Is fetal exposure to paracetamol associated with markers of ovarian function in infancy? Mild to moderate doses of prenatal paracetamol exposure, assessed by detailed maternal reports and urinary measurements, are associated with ovarian morphology and activity as well as reduced size of estrogen-responsive tissues in infant girls. Maternal use of paracetamol is widespread. Across multiple independent animal studies, fetal exposure consistently impairs the formation of primordial ovarian follicles, causing subfertility and premature estropause in female offspring. The Copenhagen Analgesic study (COPANA) is a single-center, prospective, observational cohort study conducted at a university hospital (March 2020 to November 2022). From 3425 eligible participants, 685 healthy singleton pregnant women of Caucasian origin, were enrolled in the first trimester of pregnancy, and 302 infant daughters were examined at follow-up. Exclusion criteria included maternal diabetes or thyroid disease, pre- or post-term delivery, or severe infant illness. Pregnant women reported paracetamol use biweekly and provided first-trimester urinary samples which were analyzed for paracetamol levels (LC-MS/MS) and adjusted for urinary osmolarity (n = 299). Girls were classified by timing of initial exposure: early fetal life (<17 weeks, n = 92), mid-late fetal life (≥17 weeks, n = 67), or unexposed controls (n = 143). Of the 92 girls initially exposed in early fetal life, a subgroup was exposed exclusively in early fetal life (n = 22).In an independent confirmatory cohort, 1210 girls were followed from infancy to adolescence. Their exposure was maternal self-reported (any) use of paracetamol during pregnancy and reported early in the third trimester (yes/no). Early fetal exposure was associated with reduced ovarian volume (-0.11 cm3, 95% CI -0.19 to -0.03) and reduced uterine volume (-0.18 cm3, -0.35 to -0.01), whereas mid-late fetal exposure was associated with fewer ovarian follicles (-1.05 follicles, -1.71 to -0.39) compared to unexposed girls. AMH levels were lower in girls exposed exclusively in early fetal life (-0.45 SDS, -0.87 to -0.03) compared to unexposed girls. Maternal urinary paracetamol concentrations were inversely associated with ovarian and uterine volume as well as breast tissue diameter. In the independent confirmatory cohort, fetal paracetamol exposure was associated with reduced uterine volume at puberty (-4.11 cm3, -7.29 to -0.92) and smaller ovarian volume during adolescence (-2.76 cm3, -4.82 to -0.70). The observational design of the study allows evaluation of exposure outcome associations, while the causality interpretation is supported by consistency with experimental models demonstrating comparable effects. Residual confounding by indication for paracetamol use cannot be completely excluded, although the results were robust after accounting for fever and other maternal factors. The analytic design of the current study limited our ability to evaluate whether frequency or patterns of paracetamol use influenced the observed associations. In this prospective cohort study of infant girls, prenatal exposure to paracetamol was associated with differences in several markers of ovarian development, including ovarian volume, follicle number, and circulating AMH, as well as uterine volume and breast tissue diameter. The associations with reduced ovarian and uterine size were also observed in a confirmatory cohort followed to adolescence. Whether these early-life differences have long-term clinical relevance, including effects on reproductive lifespan, remains uncertain and requires analyses in studies with extended follow-up. This research was supported by Rigshospitalets Research Council under grant (E-22717-21), Læge Sofus Carl Emil Friis og hustru Doris Friis'Legat (F-23936-01), Aase og Ejnar Danielsens Foundation (20-10-0367), Helsefonden (20-B-0388), Axel Muusfeldt Foundation (2020-0385), and The Danish Centre for Endocrine Disrupting Substances (CeHoS) (2022-23219). The funders had no role in considering the study design or in the collection, analysis, interpretation of data, writing of the report, or decision to submit the article for publication. The publication was completed as part of the MERLON project under grant agreement No. 101137411. The MERLON project is funded by the European Union. Views and opinions expressed are, however, those of the authors only and do not necessarily reflect those of the European Union or the European Health and Digital Executive Agency (HADEA). Neither the European Union nor HADEA can be held responsible for them. All authors declare no support from any organization for the submitted work, no financial relationships with any organizations that might have an interest in the submitted work in the previous 3 years, and no other relationships or activities that could appear to have influenced the submitted work. One author (MA) is a government official. ClinicalTrials.gov ID: NCT0436922.

PMID 42713612
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