Diclofenac Sodium Injection (Akis®, Dicloin®): A Review of Its Use in the Management of Pain

Blair, Hannah A.; Plosker, Greg L.

doi:10.1007/s40261-015-0294-6

Cited by 14 publications

(14 citation statements)

References 14 publications

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“…The choice of diclofenac sodium as an anti-inflammatory analgesic for relief of mildmoderate dental pain is supported by (a)extensive studies reported from the Cochrane database (Barden et al 2004;Moore 2007;Moore et al 2015b;Moore et al 2015c) showing this drug's effectiveness in dental pain with low AE incidence encountered with other NSAIDs and analgesics (Gan 2010;Moore et al 2015a); (b)rapid absorption from oral/parenteral preparations and other favourable pharmacokinetic properties (Sengupta et al 1985) as well as its ability to accumulate into the cerebrospinal fluid and pain inhibition in the central nervous system (Bjorkman and Elam 1993;Kokki et al 2008); and (c)its novel mechanism of analgesia involving selective effects on ion channels (Duan et al 2012;Gwanyanya et al 2012 All four drug dose levels produced significantly superior effects compared with placebo in preventing pain during the 6-hour post-surgical observation period in terms of pain intensity levels, time until pain onset and time to first RM intake. The results are consistent with findings from previous studies showing the efficacy of the parenterally administered sodium diclofenac HPβCD formulation (Blair and Plosker 2015;Chiarello et al 2015;Dietrich et al 2014).…”

Section: Discussionsupporting

confidence: 92%

“…The main reported ADRs were injection site reactions, i.e.pain or swelling, reported in 14.6% of active group patients, which concurs with previous evaluations (Blair and Plosker 2015;Dietrich et al 2014); although this was somewhat surprising given that the injection was given following LA. Previous studies have shown that there were no serious adverse reactions following SC administration of sodium diclofenac HPβCD at three dose levels of 25, 50 and 75mg/mL (Dietrich et al 2014;Zeitlinger et al 2012).…”

Section: Lasupporting

confidence: 86%

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Submucosal Diclofenac for Acute Postoperative Pain in Third Molar Surgery: A Randomized, Controlled Clinical Trial

et al. 2017

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Diclofenac sodium is a widely used nonsteroidal anti-inflammatory drug (NSAID) for relief of inflammatory pain. A recent formulation combines this drug with hydroxypropyl-β-cyclodextrin (HPβCD) to improve its solubility and to enable subcutaneous administration. Previous studies confirmed the efficacy of this combination. This study's aim was to evaluate the efficacy, safety, and local tolerability of diclofenac HPβCD administered as a local submucosal injection prior to lower third molar surgery. We conducted a prospective, randomized, double-blind, placebo-controlled, parallel-group phase II single-center study. Seventy-five patients requiring mandibular third molar surgery were randomized into 1 of 5 groups: 5 mg/1 mL diclofenac HPβCD, 12.5 mg/1 mL diclofenac HPβCD, 25 mg/1 mL diclofenac HPβCD, 50 mg/1 mL diclofenac HPβCD, or 1 mL placebo. The respective study drug was injected into the mucosal tissue surrounding the surgical site prior to surgery following achievement of local anesthesia. The primary outcome measure was the area under the curve (AUC) of cumulative pain scores from end of surgery to 6 h postsurgery. This demonstrated a global treatment effect between the active groups and placebo, hence confirming the study drug's efficacy ( P = 0.0126). Secondary outcome measures included the time until onset of pain and the time until patients required rescue medication, both showing statistical significance of the study drug compared to placebo ( P < 0.0161 and P < 0.0001, respectively). The time until rescue medication ranged between 7.8 h (for 25 mg/1 mL diclofenac HPβCD) and 16 h (for 50 mg/1 mL diclofenac HPβCD). Interestingly, the 5-mg/1-mL solution appeared superior to the 12.5-mg/1-mL and 25-mg/1-mL solutions (time until rescue medication = 12.44 h). A total of 14% of patients experienced minor adverse drug reactions (ADRs), of which 2 cases demonstrated flap necrosis. These resolved without further intervention. The study results overall indicate efficacy, safety, and relative tolerability of diclofenac HPβCD used locally as a submucosal injection prior to third molar surgery (ClinicalTrials.gov NCT01706588).

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Section: Discussionsupporting

confidence: 92%

Section: Lasupporting

confidence: 86%

Submucosal Diclofenac for Acute Postoperative Pain in Third Molar Surgery: A Randomized, Controlled Clinical Trial

et al. 2017

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“…However, consumption of high doses of these drugs (such as: ibuprofen, diclofenac [DIC], and naproxen) can lead to toxicity (2,3). DIC is the most common NSAID used to decrease inflammation and arthritis-associated pain (4,5). It is absorbed quickly and completely after consumption and attaches to albumin in plasma (6).…”

Section: Introductionmentioning

confidence: 99%

Nephroprotective effect of silymarin against diclofenac induced renal damage and oxidative stress in male rats

Nouri

Heidarian

2019

J Herbmed Pharmacol

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Introduction: Diclofenac (DIC), a phenylacetic acid compound which belongs to nonsteroidal anti-inflammatory drugs (NSAIDs), is generally used for the treatment of various diseases such as rheumatoid arthritis, ankylosing spondylitis, acute muscle pain conditions and osteoarthritis. Overdose of DIC can lead to renal injuries in both experimental animal and human. Our research was done to assess the protective role of silymarin on renal damage induced by DIC in rats. Methods: Thirty-two Wistar rats were assigned to four groups (n=8/group). Group 1 was control group; animals in group 2 were administrated DIC; Groups 3 and 4 administrated DIC plus silymarin with doses of 100 mg/kg and 200 mg/kg, orally (p.o), respectively. Various biochemical, molecular, and histological parameters were evaluated in serum and tissue homogenate. Results: In the second group, the levels of kidney catalase (CAT), vitamin C and superoxide dismutase (SOD) remarkably reduced (P < 0.05) relative to the control group. Also, urea, creatinine (Cr), malondialdehyde (MDA), serum tumor necrosis factor-α (TNF-α) and gene expression of TNF-α in this group were noticeably elevated (P < 0.05) relative to the control group. Treatment with silymarin caused a remarkable elevation (P < 0.05) in vitamin C, SOD, CAT and a remarkable reduction (P < 0.05) in the content of MDA, urea, Cr, TNF-α gene expression and serum TNF-α in comparison with second group. Histological injuries were also ameliorated by silymarin administration. Conclusion: The results confirm that silymarin has an ameliorative role against renal damage and oxidative stress induced by DIC in male rats.

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“…The complexing agent HP‐β‐CD had been used as a solubility enhancer to render DS more suitable for subcutaneous or intramuscular injection (Akis, Dicloin) in several European countries. Besides, it was reported that the addition of HP‐β‐CD could reduce the muscle stimulation of DS . In this study, HP‐β‐CD was used to increase the drug loading of DS by forming inclusion complex and decrease the drug irritation.…”

Section: Resultsmentioning

confidence: 95%

Rational Design of Rapidly Separating Dissolving Microneedles for Precise Drug Delivery by Balancing the Mechanical Performance and Disintegration Rate

Hou

Quan

Yang

et al. 2019

Adv Healthcare Materials

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The precise delivery of traditional dissolving microneedles (TDMNs) is often limited by the incomplete insertion due to the skin deformation, and the topical irritation is inevitable after long application, which ultimately results in compromised therapeutic efficacy. The aim of this study is to develop a rapidly separating dissolving microneedles (RSDMNs) system to achieve precise drug delivery. Therapeutic molecules are concentrated in the needle tip, while the blank separating part allows it to counteract skin indentation and rapidly separate from the base part. For rational design of an ideal separating part, and the molecular interactions between polymer and sugar are explored to make a good balance between mechanical performance and disintegration rate. The optimal RSDMNs can rapidly disintegrate in the mimic skin within 30 s, and the generated micropores in the skin reseal quickly. The ex vivo drug permeation of RSDMNs is significantly higher than that of TDMNs due to the complete needle imbed aided by the separating part. Furthermore, RSDMNs exhibit excellent in vivo anti‐inflammation effect by remarkably down regulating the expression of TNF‐α, IL‐1β, and IL‐6. In conclusion, the RSDMNs can reach precise drug delivery in a short time, which are more reliable for the self‐administration strategy in the future.

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Diclofenac Sodium Injection (Akis®, Dicloin®): A Review of Its Use in the Management of Pain

Cited by 14 publications

References 14 publications

Submucosal Diclofenac for Acute Postoperative Pain in Third Molar Surgery: A Randomized, Controlled Clinical Trial

Submucosal Diclofenac for Acute Postoperative Pain in Third Molar Surgery: A Randomized, Controlled Clinical Trial

Nephroprotective effect of silymarin against diclofenac induced renal damage and oxidative stress in male rats

Rational Design of Rapidly Separating Dissolving Microneedles for Precise Drug Delivery by Balancing the Mechanical Performance and Disintegration Rate

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