Zaltoprofen, a noninferior alternative to diclofenac for the treatment of primary knee osteoarthritis – a comparative evaluation of efficacy and safety in a 4-week, multicentric, randomized, double-blind, double-dummy trial

Pareek, Anil; Gupta, Anil; Chandurkar, Nitin; Sirsikar, Ashish; Ambade, Ratnakar; Jesalpura, Bhavesh; Swamy, Amit

doi:10.1517/14656566.2011.566867

Cited by 6 publications

(3 citation statements)

References 13 publications

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“…Despite the gaps in knowledge of the mechanism of pain and pain relief that exist at present, our study points out that zaltoprofen can be utilized as an effective alternative to standard analgesic in treatment of painful conditions. In a randomized, comparative, multicentric, double blind, double-dummy, Phase III clinical study conducted in patients with primary knee osteoarthritis, comparing zaltoprofen with diclofenac, it was concluded that the efficacy and safety of zaltoprofen is clinically non-inferior to that of diclofenac 22. In another observational, prospective study, zaltoprofen in combination with topical anesthetic gel was found to be superior to anesthetic gel alone in controlling cystoscopy-related pain 23.…”

Section: Discussionmentioning

confidence: 99%

<p>A comparative experimental study of analgesic activity of a novel non-steroidal anti-inflammatory molecule – zaltoprofen, and a standard drug – piroxicam, using murine models</p>

Chenchula¹,

Kumar²,

Sadasivam³

et al. 2019

JEP

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Purpose Pain is an unpleasant sensation, but a protective mechanism of our body. It is the most common medical complaint requiring a visit to a physician. The new non-steroidal anti-inflammatory drug (NSAID) – zaltoprofen, is a preferential COX-2 inhibitor. It also inhibits bradykinin-induced nociceptive responses by blocking the B2 receptor-mediated pathway in the primary sensory neurons. The present study was conducted to evaluate and compare the anti-nociceptive activity of zaltoprofen with a conventional NSAID – piroxicam, in a mouse model of acute pain using hot plate and tail flick tests. Materials and methods Twenty-four adult Swiss albino mice (20–25 g) of either sex were used in this study. Oral zaltoprofen and piroxicam were used as test and standard drugs respectively. Anti-nociceptive activity was evaluated and compared using hot plate and tail flick tests. Results In comparison to the control group (vehicle), zaltoprofen showed a significant increase in reaction time at various time periods in the hot plate and tail flick tests. In the hot plate method, zaltoprofen groups (15 and 20 mg/kg) showed a significant elevation in pain threshold in comparison to control group (vehicle) ( p <0.001). In the tail flick model also, zaltoprofen groups (15 and 20 mg/kg) showed a significant increase in the reaction time in comparison to control group (vehicle). In both the analgesiometer assays, zaltoprofen was found to be non-inferior compared to a standard drug – piroxicam (positive control). Conclusion Our study concludes that zaltoprofen is an effective analgesic agent in various pain models. Our results support that zaltoprofen has therapeutic potential for treating pain disorders and is non-inferior to a standard drug – piroxicam.

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Section: Discussionmentioning

confidence: 99%

<p>A comparative experimental study of analgesic activity of a novel non-steroidal anti-inflammatory molecule – zaltoprofen, and a standard drug – piroxicam, using murine models</p>

Chenchula¹,

Kumar²,

Sadasivam³

et al. 2019

JEP

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“…The general dose of zaltoprofen is 80–160 mg at a time, and it can be orally administered up to 240 mg per day depending on symptom severity [ 1 , 9 ]. The main clinical side effects of zaltoprofen include gastrointestinal bleeding and ulceration, irritability, and psychosomatic disorders, such as headache and dizziness [ 9 , 10 ]. Gastrointestinal bleeding and ulceration caused by excessive COX suppression are the most significant side effects in the clinical application of zaltoprofen [ 10 , 11 ] and require drug monitoring.…”

Section: Introductionmentioning

confidence: 99%

Population Pharmacokinetic Modeling of Zaltoprofen in Healthy Adults: Exploring the Dosage Regimen

2023

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Zaltoprofen is a drug used for various pain and inflammatory diseases. Scientific and quantitative dosage regimen studies regarding its clinical application are scarce. This study aimed to discover effective covariates related to interindividual pharmacokinetic variability through population pharmacokinetic modeling for zaltoprofen and to explore dosage regimens. The bioequivalence results of healthy Korean males, biochemical analysis, and CYP2C9 genotyping information were utilized in modeling. The established model has been sufficiently verified through a bootstrap, goodness-of-fit, visual predictive check, and normalized prediction distribution error. External data sets derived from the literature were used for further model validation. The final model could be used to verify the dosage regimen through multiple exposure simulations according to the numerical change of the selected covariates. Zaltoprofen pharmacokinetics could be explained by a two-compartment with a first-order absorption model. Creatinine clearance (CrCL) and albumin were identified as effective covariates related to interindividual zaltoprofen pharmacokinetic variability, and they had positive and negative correlations with clearance (CL/F), respectively. The differences in pharmacokinetics between individuals according to CYP2C9 genetic polymorphisms (*1/*1 and *1/*3) were not significant or valid covariates. The model simulation confirmed that zaltoprofen pharmacokinetics could significantly differ as the CrCL and albumin levels changed within the normal range. Steady-state plasma exposure to zaltoprofen was significantly reduced in the group with CrCL and albumin levels of 130 mL/min and 3.5 g/dL, respectively, suggesting that dose adjustment may be necessary. This study is useful to guide precision medicine of zaltoprofen and provides scientific quantitative judgment data for its clinical applications.

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“…It is used for the treatment of osteoarthritis, rheumatoid arthritis and other acute and chronic inflammatory pain. Compared to other NSAIDs, ZAL selectively inhibits the production of PGE 2 at inflammatory sites, presenting an anti-inflammatory effect with a good safety margin (Pareek et al, 2011). In addition, ZAL exhibits a unique inhibition effect on bradykinin-induced nociception, while other NSAIDs (e.g.…”

Section: Introductionmentioning

confidence: 99%

Development of a drug-in-adhesive patch combining ion pair and chemical enhancer strategy for transdermal delivery of zaltoprofen: pharmacokinetic, pharmacodynamic and in vitro/in vivo correlation evaluation

et al. 2016

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The aim of the study was to develop a drug-in-adhesive patch system for transdermal delivery of zaltoprofen (ZAL). The formulation was designed in combination with the ion pair and chemical enhancer strategy. Seven organic amines were chosen as counter ions, and the prepared ion pairs were characterized by Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). The in vivo pharmacokinetic performance of ZAL was studied on rabbits following transdermal and intravenous administration. A deconvolution method was applied to determine the correlation between the in vitro permeation and the in vivo absorption. Acetic acid-induced writhing response was conducted on mice to evaluate the analgesic effect. In vitro permeation results showed that both ion pairs and chemical enhancers were effective in modulating ZAL skin permeation from patches. The enhancement ratio was negatively correlated to the polar surface area (PSA) of counter ions, and was positively correlated to the octanol-water partition coefficient (log K o/w ) of chemical enhancers, respectively. The optimized formulation contained 10% (w/w) ZAL-triethylamine and 10% (w/w) isopropyl myristate, with DURO-TAK Õ 87-4098 as the pressure sensitive adhesive matrix. Furthermore, the in vitro permeation data were well correlated with the in vivo absorption data. The analgesic effect of the optimized patch was comparable to the commercial indometacin plasters. In conclusion, it was feasible for transdermal delivery of ZAL by the synergistic action of ion pair and chemical enhancer, and the in vitro permeation data were indicative of the in vivo performance for the developed patches. KeywordsIon pair, in vitro/in vivo correlation, pharmacokinetic, transdermal, zaltoprofen History

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Zaltoprofen, a noninferior alternative to diclofenac for the treatment of primary knee osteoarthritis – a comparative evaluation of efficacy and safety in a 4-week, multicentric, randomized, double-blind, double-dummy trial

Abstract: This study demonstrated that efficacy and safety of zaltoprofen is clinically noninferior to that of diclofenac.

Cited by 6 publications

References 13 publications

<p>A comparative experimental study of analgesic activity of a novel non-steroidal anti-inflammatory molecule – zaltoprofen, and a standard drug – piroxicam, using murine models</p>

<p>A comparative experimental study of analgesic activity of a novel non-steroidal anti-inflammatory molecule – zaltoprofen, and a standard drug – piroxicam, using murine models</p>

Population Pharmacokinetic Modeling of Zaltoprofen in Healthy Adults: Exploring the Dosage Regimen

Development of a drug-in-adhesive patch combining ion pair and chemical enhancer strategy for transdermal delivery of zaltoprofen: pharmacokinetic, pharmacodynamic and in vitro/in vivo correlation evaluation

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