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diclofenac (Oxa Gel / diclofenac, topical)

✓ Approved

Actavis · PTGS1 · 小分子

什么是 diclofenac?

diclofenac 是一种小分子,由Actavis研发。该药已获批,用于治疗相关适应症,给药途径:Transdermal。

药物档案

商品名Oxa Gel, diclofenac, topical
公司Actavis
药物类别小分子
分子靶点PTGS1, PTGS2
给药途径Transdermal
状态Approved

作用机制

分子靶点

diclofenac 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

diclofenac 针对 5 个适应症,涉及 3 个治疗领域。

治疗领域疾病/病症分期
Musculoskeletal and connective tissue disordersMusculoskeletal pain✓ Approved
Musculoskeletal and connective tissue disordersMyositis✓ Approved
Musculoskeletal and connective tissue disordersRheumatoid arthritis✓ Approved
Injury, poisoning and procedural complicationsTraumatic shock✓ Approved
Skin and subcutaneous tissue disordersActinic keratosisPhase III

相关研究文献

PubMedJournal of microencapsulation2026-09-11

Cross-linked alginate/pozzolan (Alg@PZ) microcapsules for sodium diclofenac removal as emerging contaminant.

Drai Ikram I, Bachir Cherifa C, Bailiche Zohra Z, Rodríguez Juan Francisco JF et al.

This study investigates the adsorption of sodium diclofenac (SDF) onto Alginate/Pozzolan (Alg@PZ) microcapsules to address pharmaceutical contamination in aquatic systems. The Alg@PZ composite was synthesised via CaCl2 cross-linking by varying the Sodium Alginate (S-Alg)/Pozzolan (PZ) mass ratio from 0.625 to 3.25. Successful PZ incorporation into the S-Alg matrix was confirmed by FTIR, XRD and SEM analyses, revealing hydrogen and electrostatic bonding alongside a near-uniform spherical porous morphology of 1.73 mm diameter. TGA revealed optimal PZ encapsulation of 63.87% at a S-Alg/PZ ratio of 0.625, with high thermal stability. Adsorption experiments in a shallow-bed system demonstrated rapid SDF removal, best described by a PSO kinetic model reaching equilibrium after 45 minutes, with a qmax= 21.85 mg.g - 1. Thermodynamic analysis showed that the reaction was spontaneous and exothermic. However, Alg@PZ0.625 represents a scalable, eco-friendly and cost-effective alternative to conventional adsorbents for removing persistent pharmaceutical compounds from aqueous systems.

PMID 42723228
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PubMedPlastic and reconstructive surgery. Global open2026-09-11

Successful Healing of a Chronic Distal Toe Ulcer with Tendon Exposure Using the Topical Macrophage Regulator ON101.

Huang Chao-Hsin CH, Lin I-Wen IW, Su Yu-Ting YT, Huang Shu-Hung SH

Diabetic foot ulcer (DFU) is one of the most challenging complications of diabetes mellitus. Chronic hyperglycemia contributes to impaired immune function, characterized by failure of macrophage polarization from the proinflammatory M1 to the prohealing M2 phenotype, together with increased release of inflammatory mediators. ON101 is a novel macrophage-regulating topical agent derived from botanical extracts, designed to suppress proinflammatory cytokines, restore M1/M2 macrophage balance, and promote collagen synthesis. We report the case of a 77-year-old man with diabetes mellitus who presented with a chronic, nonhealing ulcer of the right fifth toe with exposed tendon, persisting for 2 years despite conventional wound care and twice-daily Aquacel Ag+ extra dressing changes. The wound was accompanied by local inflammation, whereas angiographic evaluation suggested preserved distal runoff without evidence of critical macrovascular occlusion. ON101 topical therapy was initiated once daily under PolyMen dressing, leading to progressive granulation tissue formation, epithelial coverage of the tendon, and complete wound closure within 2 months. Notably, the total amount of ON101 used throughout the treatment course was less than 1 15-g tube. Given the chronicity of the wound, the presence of exposed tendon, and the difficulty of achieving durable healing in distal diabetic toe ulcers, this case suggests that ON101 may provide substantial therapeutic benefit in selected refractory cases.

PMID 42724883
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PubMedNarra J2026-09-11

Real-world effectiveness of a topical dihydroavenanthramide D formulation for chronic pruritus: A multicenter clinical study with molecular evidence of pruritogenic pathway modulation.

Ribero Simone S, Vaccaro Mario M, Borgia Francesco F, Mattozzi Carlo C et al.

Chronic pruritus is a prevalent and clinically burdensome condition that substantially impairs quality of life and is sustained by complex interactions between neuro-immune signaling and epidermal barrier dysfunction. Central mediators implicated in this pruritogenic network include interleukin-4 (IL-4), interleukin-13 (IL-13), interleukin-31 (IL-31), substance P encoded by TAC1, and nerve growth factor (NGF). The aim of this study was to evaluate the real-world effectiveness of a topical formulation containing dihydroavenanthramide D (DHAvD), a neurokinin-1 receptor inhibitor, in combination with barrier-repairing agents for reducing pruritus severity in patients with chronic pruritus of diverse etiologies. A supportive molecular sub-study was also performed to determine whether clinical improvement was accompanied by modulation of cutaneous pruritogenic gene expression. A prospective, single-arm, multicenter clinical study was conducted in 1,000 patients with chronic pruritus of diverse etiologies. The formulation was applied twice daily for 14 days, and pruritus severity was assessed using the 12-Item Pruritus Severity Scale (12-PSS; range 3-22). In a molecular sub-study, 20 patients with chronic idiopathic pruritus underwent paired skin biopsies from symptomatic areas before and after treatment, and cutaneous mRNA expression of IL4, IL13, IL31, TAC1, and NGF was quantified by qRT-PCR. The mean 12-PSS score decreased from 11.37±3.71 at baseline to 5.64±2.87 at day 14 (d=-1.72; p<0.001), and 55.4% of participants achieved a ≥50% reduction in pruritus severity. The reduction in symptom severity was consistent across etiological subgroups (p=0.787). A clinically meaningful reduction was also observed among patients treated with the cream as monotherapy, with 12-PSS scores decreasing from 10.44±3.78 to 5.06±2.62 (d=-1.53; p<0.001). In the molecular sub-study, significant downregulation of all five target genes was observed, with effect sizes ranging from d=-0.62 for IL4 (p=0.013) to d=-2.64 for NGF (p<0.001). In conclusion, topical DHAvD combined with barrier-repairing agents was associated with clinically meaningful real-world reduction in chronic pruritus severity and supportive molecular evidence of multi-target pruritogenic pathway modulation. These findings warrant confirmation in randomized vehicle-controlled trials.

PMID 42724128
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PubMedAnnals of medicine and surgery (2012)2026-09-11

Post-traumatic Blaschko-linear dermatitis following prostatectomy: a rare case report.

Katanji Salah Aldin SA, Kaurie Meri Abdul Masih MAM, Rayya Mohammad Zuhair MZ, Rayya Ali Zuhair AZ et al.

Blaschko-linear acquired inflammatory skin eruption includes lichen striatus and blaschkitis, which can be triggered by factors such as pregnancy and autoimmune diseases; a rare case in an elderly man post-prostatectomy illustrates the need for accurate diagnosis to prevent unnecessary treatment. A 69-year-old man developed a pruritic vesicular eruption along Blaschko's lines after undergoing prostatectomy. All laboratory tests for viruses were negative, and the biopsy result indicated post-traumatic Blaschkoid dermatitis. The patient was treated with topical corticosteroids and antihistamines, and he experienced remarkable improvement with no relapse three months later. Surgery-induced blaschkitis mimicking herpes zoster highlights the nonviral Koebner phenomenon, thereby preventing unnecessary antiviral use. Diagnosis of Blaschko-linear inflammatory eruptions should be made promptly to avoid misdiagnosis and prevent unnecessary use of antivirals. Further studies are needed on surgical trauma and cutaneous mosaicism.

PMID 42724915
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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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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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