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piroxicam suppositories (Riacen)

✓ Approved

Chiesi Farmaceutici S.p.A. · PTGS1 · 小分子

什么是 piroxicam suppositories？

piroxicam suppositories 是一种小分子，由Chiesi Farmaceutici S.p.A.研发。该药已获批，用于治疗相关适应症，给药途径：Rectal。

药物档案

商品名Riacen
公司Chiesi Farmaceutici S.p.A.
药物类别小分子
分子靶点PTGS1, PTGS2
给药途径Rectal
状态Approved
来源： ClinicalTrials.gov, Chiesi Farmaceutici S.p.A.

作用机制

分子靶点

piroxicam suppositories 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

piroxicam suppositories 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
Hepatobiliary disordersHepatitis✓ Approved

相关研究文献

PubMedFrontiers in pharmacology2026-08-08

Piroxicam accelerates diabetic foot ulcer healing via ERα-dependent mitochondrial protection and oxidative stress relief.

Liao Qing-Qing QQ, Chen Li-Ping LP, Zheng Jia-Qi JQ, Yang Yu-Jie YJ et al.

The pathology of diabetic foot ulcer (DFU) is characterized by keratinocyte dysfunction, non-resolving inflammation, and oxidative stress. We aim to investigate the effects and mechanisms of piroxicam on DFU healing through regulating mitochondrial function and suppressing inflammation. DFU was established in male C57BL/6 J mice and ovariectomized female mice. Piroxicam (1% or 0.33%) solution or saline was then applied for 9 days. HaCaT cells were induced with high glucose (HG) and subsequently incubated with piroxicam (0, 1.2, 3.7, 11, 33, 100 nM). Piroxicam significantly promoted DFU healing and inhibited the fibrosis in male diabetic mice at a low dose. Consistently, piroxicam enhanced proliferation and migration, and inhibited inflammation, fibrosis, and cellular senescence in HG-induced HaCaT cells. Mechanistically, piroxicam alleviated HG-induced mitochondrial dysfunction by stabilizing the mitochondrial respiratory chain, increasing biogenesis, and enhancing mitophagy. These effects further attenuated oxidative stress and inhibited the cGAS-STING-NF-κB inflammatory pathway, thereby reducing the release of pro-inflammatory factors. Furthermore, molecular docking revealed that piroxicam bound to ERα, a finding further confirmed by a cellular thermal shift assay. HG induced a significant decrease in nuclear ERα protein levels, which was reversed by piroxicam, especially at 11 and 33 nM. Additionally, piroxicam's pro-healing and anti-inflammation effects were attenuated in ovariectomized female DFU mice. Piroxicam's protection of mitochondrial function and suppression of oxidative stress was also abolished upon blocking ERα by tamoxifen. In conclusion, piroxicam alleviates mitochondrial dysfunction and suppresses inflammatory responses by binding to ERα, which ultimately promotes DFU healing at low doses.

PMID 42568976
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PubMedBMJ open2026-07-31

Clinical efficacy of Mepilex Lite dressings combined with indomethacin suppositories in the treatment of acute radiation dermatitis caused by rectal cancer radiotherapy: a study protocol for a randomised controlled trial.

Shang Heli H, Yang Yanwei Y, Cao Hailan H, Wu Yan Y et al.

Acute radiation dermatitis is a common adverse reaction in radiotherapy, especially in patients with rectal cancer undergoing radiotherapy. At present, acute radiation dermatitis of the perianal skin has received widespread attention; however, acute radiation skin injury of the anal canal skin has not received sufficient attention. These patients mainly complain of anal pain, which seriously affects their quality of life. Mepilex Lite dressings have been recommended for the treatment of acute radiation dermatitis and have a definite effect. However, there is limited research on the use of this dressing for the treatment of acute radiation-induced dermatitis of the anal canal skin and its clinical efficacy and safety in this context need further verification. This study is an assessor-blinded randomised controlled trial designed to evaluate the efficacy and safety of Mepilex Lite dressings combined with indomethacin suppositories for the treatment of acute radiation dermatitis of the anal canal skin. A total of 274 eligible patients from the tumour radiotherapy ward of the First Affiliated Hospital of Shandong First Medical University will be randomly assigned to either the experiment or control group (1:1). The control group will be given 30 mg of indomethacin suppositories for rectal administration, and the experiment group will be given Mepilex Lite dressings in addition to the measures taken by the control group. The 5 cm × 5 cm dressing will be inserted into the anal canal for 3 cm through the anus and exposed for 2 cm. The main outcome indicator is the treatment efficiency of the acute radiation dermatitis of the anal canal skin on the 14th day after the intervention. The secondary outcome indicator is the treatment efficiency of the acute radiation dermatitis of the anal canal skin on the seventh and 21st days after the intervention. Concurrently, the Numeric Rating Scale, Hospital Anxiety and Depression Scale, Pittsburgh Sleep Quality Index and Skin Disease Patient Quality of Life Scale-16 will be used to assess patient pain, depression and anxiety, sleep quality and quality of life, respectively. A table questionnaire survey will be conducted at baseline and on 7, 14 and 21 days after intervention. The research protocol has obtained ethical approval from the Ethics Committee of the First Affiliated Hospital of Shandong First Medical University (approval number: YXLL-KY-2024 (162)). The results will be published in peer-reviewed journals and abstracts will be submitted to domestic and international conferences to disseminate our research findings. NCT06837831.

PMID 42532557
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PubMedBritish journal of clinical pharmacology2026-07-29

Pharmacometric evaluation of pre-referral rectal artesunate in children with severe malaria.

Adehin Ayorinde A, Onyamboko Marie A MA, Fanello Caterina C, White Nicholas J NJ et al.

Parenteral artesunate is the preferred first-line treatment for severe malaria. Pre-referral rectal artesunate suppositories are recommended where parenteral treatment is inaccessible. In this study, we compared dihydroartemisinin exposure and model-predicted early parasite clearance following rectal artesunate and intravenous artesunate in African children with severe malaria. A total of 82 African children with severe malaria participated in a randomized crossover study in Democratic Republic of Congo. Forty children received rectal artesunate (10 mg/kg) while the other 42 received intravenous artesunate (2.4 mg/kg) as the first intervention, and then the other route of administration for the second dose. Blood samples were drawn for drug quantification, and nonlinear mixed-effects modelling was used to evaluate the pharmacokinetic properties of intravenous and rectal artesunate and to simulate expected parasite clearance associated with these routes of administration. The mean individually estimated rectal bioavailability of artesunate was 21% but was highly variable (IQR: 8%-35%). Plasma exposure to dihydroartemisinin-the principal and bioactive metabolite of artesunate-did not differ significantly between rectal and intravenous administration. Predicted parasite reduction over the first 12 h was similar for both routes, consistent with previously reported clinical benefits of rectal artesunate. These findings support the 10-mg/kg dose of rectal artesunate as a pre-referral intervention, which should be more widely deployed in malaria-endemic areas.

PMID 42522584
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PubMedBulletin of experimental biology and medicine2026-07-28

Effects of Melatonin in Original Rectal Suppositories on the Neurological Status and Mucosa-Associated and Luminal Microbiota of the Distal Colon in Wistar Rats with Experimental Acute Cerebral Ischemia.

Shishkova Yu S YS, Osikov M V MV, Boyko M S MS, Shelomentsev A V AV et al.

We analyzed the effects of melatonin (MT) administered via rectal suppositories on the composition of the mucosa-associated and luminal microbiota of the distal colon and neurological status of Wistar rats under conditions of experimental acute ischemic stroke (EAIS). The animals received original 100-mg rectal suppositories containing 2.5 mg of MT every 24 h for 3 days. Neurological status was assessed using the Garcia scale and the limb placing test, while microbiota composition in the distal colon was determined using real-time PCR. In rats with EAIS, neurological deficit was observed, characterized by a significant decrease in the Garcia and limb placing scores. In parallel, changes in the colon microbiota were observed: appearance of Clostridioides difficile, Fusobacterium nucleatum, Enterobacter spp., and the disappearance of Enterococcus spp. The administration of original MT-containing rectal suppositories led to partial recovery of neurological deficit, as manifested by in an increase in the Garcia score and limb placing test performance, which was accompanied by the appearance of Bacteroides thetaiotaomicron and the disappearance of Cl. difficile in the colon microbiota. Correlation analysis demonstrated that the amelioration of the neurological deficit was accompanied by changes in the gut microbiota. The effect of MT in rectal suppositories on neurological status and the gut microbiota is attributed to its neuroprotective and bacteriostatic properties.

PMID 42509431
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PubMedImmunopharmacology and immunotoxicology2026-07-22

Preclinical evaluation of 3,4-dimethoxybenzoic acid alone and in combination for adjuvant-induced arthritis in Wistar rats.

Saleem Ammara A, Afnan Afnan A, Irfan Muhammad M, Mobashar Aisha A et al.

Rheumatoid arthritis is a systemic autoimmune disorders of joints. Its available therapies having serious adverse effects, high cost and poor patient compliance. The present study aimed to evaluate the anti-inflammatory and anti-arthritic potential of 3, 4-dimethoxybenzoic acid or Veratric acid (VA) by in-vitro and in-vivo assays. Additionally, acute toxicity of VA was performed. The anti-inflammatory activity was assessed by Xylene-induced ear edema, and Carrageenan-induced paw edema models in Wistar rats. The VA was given at doses of 20, 40, and 80 mg/kg, with Piroxicam (10mg/kg) as standard drug. For anti-arthritic action, 0.1 ml of Complete Freund's adjuvant was intradermally inoculated in left posterior paw on first day while treatment with VA at 20, 40, 80, and VA 80 mg/kg + methotrexate and methotrexate (1 mg/kg) as standard drug were given orally on the 8th day for 21 days. Treatment with VA exhibited a substantial reinstatement of body weight, paw edema, arthritic scores, and oxidative stress in difference to disease control. All treatment groups exhibited notable down-regulation (p < .0001) of IL-6, TNF-α, IL-β, COX-2, and NF-κB and up-regulation of IL-10, 1-κβ, IL-4 in contrast to disease control. The combination group had exhibited noticeable anti-arthritic potential in comparison to individual treatment groups. In acute toxicity study, LD50 of VA was greater than 2000 mg/kg. It can be inferenced from data that VA can be safely used to treat arthritis especially in combination with MTX but it should be further evaluated in combination for long term use.

PMID 42482312
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PubMedJournal of cutaneous medicine and surgery2026-07-20

Vulvovaginal Lichen Planus Treatment Outcomes: A Systematic Review of Novel and Established Therapies.

Lee Andy D AD, Slade Alison A, Hong Joony J, Pollanen Sara S et al.

Vulvovaginal lichen planus (VVLP) is a chronic inflammatory mucocutaneous disease causing significant morbidity. Despite various available treatments, evidence regarding their effectiveness remains fragmented. To systematically evaluate the efficacy and safety of therapeutic interventions for VVLP with or without concomitant gingival involvement. We searched MEDLINE, Embase, CINAHL, and Scopus databases without date restrictions. We included randomized and non-randomized studies reporting treatment outcomes in adults with VVLP. Two reviewers independently screened studies and extracted data. Risk of bias was assessed. We analyzed 1417 patients across 66 studies. Monotherapy was used in 25.2% (357/1417), dual-component therapy in 12.0% (170/1417), triple-component therapy in 51.2% (726/1417), and complex therapy in 11.6% (164/1417) of cases. Among monotherapies, systemic corticosteroids demonstrated the highest complete resolution (CR) rate at 88.9% (24 of 27 patients), followed by biologics with tildrakizumab achieving 88.0% CR (22 of 25 patients), and JAK inhibitors with tofacitinib showing 75.0% CR (6 of 8 patients), and intravaginal corticosteroid suppositories at 55.7% (54 of 97 patients). Triple-component therapy combining systemic corticosteroids, topical calcineurin inhibitors, and antimetabolites (methotrexate or mycophenolate mofetil) was most commonly used (66.8%, 485/726), with 41.6% achieving CR. Adverse events were generally mild, including burning sensations with topical agents and gastrointestinal symptoms with systemic immunosuppressants. Recurrence rates varied widely: 84% for topical corticosteroids alone, 11.9% for methotrexate, and 3.2% for tildrakizumab. While corticosteroids remain the mainstay of VVLP treatment, newer therapies, including JAK inhibitors (75.0% CR, 6 of 8 patients) and biologics, show promising efficacy. Among biologic monotherapies, tildrakizumab achieved 88.0% CR (22 of 25 patients), while the overall CR rate across all 31 biologic-treated patients was 71.0% (22 of 31 patients). These findings are based on small patient numbers and require validation in larger controlled trials. Triple-combination therapy is frequently employed for resistant cases. High recurrence rates with monotherapy suggest combination approaches may be necessary for the long term.PROSPERO Registration: CRD42025101229.

PMID 42473437
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