Comparative Bioavailability of Lornoxicam as Single Doses of Quick-Release Tablet, Standard Tablet and Intramuscular Injection

Radhofer-Welte, S; Dittrich, P.; Šimin, Marija; Branebjerg, Poul Erik

doi:10.2165/00044011-200828060-00002

Cited by 12 publications

(10 citation statements)

References 7 publications

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“…Milder histopathological changes were observed on evaluating the toxic effects of the other drugs. Lornoxicam seems to be one of the drugs that can be intramuscularly used for acute pain treatment, and there are no reports on sciatic nerve damage induced by an intramuscular injection of this drug in the gluteal region or its histopathological effects on the sciatic nerve [24, 25]. Lornoxicam injection in the sciatic nerve resulted in greater damage supported based on the histopathological evidence, and anti-S100 positivity was detected to be lower in the lornoxicam group with injection in the sciatic nerve than in the control group with serum physiological injection in the sciatic nerve.…”

Section: Discussionmentioning

confidence: 99%

A Histopathological Examination: The Sciatic Nerve Injury Following Analgesic Drug Injection In Rats

Bostan

Çabalar

Altınay

et al. 2017

North Clin Istanbul

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OBJECTIVE:Sciatic nerve neuropathy can be observed following intramuscular gluteal injections. The histopathological examination of sciatic nerve damage following intramuscular injection in the gluteal region for acute pain treatment is not feasible in humans due to the inability to dissect and examine the nerve tissue. To overcome this issue, we used a rat model for demonstrating damage to the sciatic nerve tissue after the application of commonly used drug injections.METHODS:We investigated possible damage following the intramuscular injection of diclofenac, lornoxicam, morphine, and pethidine in a rat model based on histopathological characteristics such as myelin degeneration, axon degeneration, epineurium degeneration, fibrosis, epineurium thickening, perineurium thickening, lymphocyte infiltration, vacuolization, and edema.RESULTS:All the analgesic drugs used in our study induced histopathological changes in the sciatic nerve. Anti-S100 positivity, showing nerve damage, was found to be the lowest in the group treated with diclofenac. Neurotoxic effects of diclofenac on the sciatic nerve were greater than those of the other drugs used in the study. Lornoxicam induced the least histopathological changes in the nerve.CONCLUSION:Diclofenac induced severe nerve damage not only after direct injection in the sciatic nerve but also after injection in the area around the nerve. Thus, we recommend restricting the use of intramuscular gluteal injections of diclofenac. Intramuscular use of morphine and pethidine should also be overviewed.

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Section: Discussionmentioning

confidence: 99%

A Histopathological Examination: The Sciatic Nerve Injury Following Analgesic Drug Injection In Rats

Bostan

Çabalar

Altınay

et al. 2017

North Clin Istanbul

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“…1 and 2 respectively. Furthermore, the fact that, LOR being water insoluble drug 15,16 has high affinity towards the fatty bases than PEGs base 14 . This result also agrees with Abou-Taleb et al, 2006 who found that the release of rofecoxib, selective cox-II inhibitor, from PEGs bases was higher than those of fatty bases e.g., witepsol E-75 and suppocire AM and CM 4 .…”

Section: Physical Characteristics Of Lor Suppositoriesmentioning

confidence: 99%

Untitled

2013

IJPSR

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ABSTRACT:The aim of the present study was to formulate lornoxicam into rectal suppositories as a new dosage form, to avoid its reported gastric irritation and to provide a rapid onset of action for children. Suppositories were prepared using fatty bases namely; witepsol H-15, suppocire AML, CM, witepsol E-75 and water soluble bases; mixtures of poly(ethylene glycol), PEGs, with different molecular weights. The prepared suppositories were investigated for their weight variation, drug content, melting point, fracture point, disintegration time and in-vitro release pattern. Moreover, aging study was performed both at room temperature and in refrigerator for 6 month. In-vivo study was also carried out in rabbits and the pharmacokinetic parameters were estimated. The prepared suppositories complied with the USP 34 pharmacopoeial requirements and PEGs-based suppositories released significantly higher amounts of lornoxicam compared with fatty bases (p<0.05, ANOVA/Dunnett). Furthermore, lornixocam in selected formulations was found to be stable in both fatty and PEGs bases after the aging study. Formulation No. 5 showed a higher C max of 1.832±0.35 µg/ml, short t max of 1 hr and absolute bioavailability of 80.1%. These findings suggest that lornoxicam was successfully formulated into rectal suppositories with a higher bioavailability.

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“…Гепатотоксичность при использовании НПВС проявляется нечасто. В 1-4% случаев может наблюдаться бессимптомное умеренное повышение уровня печеночных ферментов [2,9,15,17].…”

Section: в практику педиатраunclassified

“…Так, ЦОГ-1 постоянно присутствует в тканях, и с ее участием образуются простагландины, выполняющие протективные функции в слизистой оболочке желудка, эндотелии, регулирующие почечный кровоток. С ингибированием ЦОГ-1 и снижением регулирующих физиологических эффектов ПГ связаны побочные действия НПВС [6,8,9]. ЦОГ-2 в норме обнаруживается в незначительных количествах.…”

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Use of Topical Non-Steroid Antiinflammatory Drugs in Pediatric Practice

Шахтахтинская¹

2012

Pediatr. farmakol.

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В статье рассматривается одна из актуальных проблем практической педиатрии-применение нестероидных противовоспалительных препаратов у детей. Освещены вопросы эффективности и безопасности различных форм нестероидных противовоспалительных препаратов, в частности, топических форм. Ключевые слова: боль, нестероидные противовоспалительные средства, диклофенак.

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Comparative Bioavailability of Lornoxicam as Single Doses of Quick-Release Tablet, Standard Tablet and Intramuscular Injection

Abstract: Lornoxicam-QR and lornoxicam-IM did not differ with respect to AUCinfinity, Cmax and tmax, but both lornoxicam-QR and lornoxicam-IM showed significantly shorter tmax and significantly higher Cmax values than lornoxicam-ST.

Cited by 12 publications

References 7 publications

A Histopathological Examination: The Sciatic Nerve Injury Following Analgesic Drug Injection In Rats

A Histopathological Examination: The Sciatic Nerve Injury Following Analgesic Drug Injection In Rats

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Use of Topical Non-Steroid Antiinflammatory Drugs in Pediatric Practice

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