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Cyclodextrins and Skin Disorders: Therapeutic and Cosmetic Applications
Published in Andreia Ascenso, Sandra Simões, Helena Ribeiro, Carrier-Mediated Dermal Delivery, 2017
Oluwatomide Adeoye, Ana Figueiredo, Helena Cabral Marques
CyDs mediate skin delivery and have been used to optimize the efficacy of numerous anti-inflammatory drugs applied topically to the skin for various forms of dermatitis. Some of these drugs are non-steroidal anti-inflammatory drugs (NSAIDs) whose anti- skin cancer activities have also been demonstrated in cell culture and animal studies [92]. Skin accumulation of these drugs from topical therapy can cause localized cyclooxygenase inhibition and subsequent anti-inflammatory response to radiation-induced skin damage [93]. Thus, the objective of CyD carrier-mediated delivery is to optimize skin accumulation and prevent system absorption from the transdermal route. Topical formulations of ibuprofen at the maximum amount soluble in 10% HP-b-CyD resulted in a higher degree of skin accumulation and photo- protection, with huge potentials in the management of skin cancers [93]. Also, liquid crystalline gels containing lornoxicam-b-CyD showed a higher reduction in the degree of pain and inflammation ex vivo due to higher skin accumulation and avoidance of systemic absorption [94]. In another study, the coating of topical flurbiprofen PLGA and PLGA-PEG nanospheres with HP-b-CyD resulted in higher in vivo topical anti-inflammatory efficiency despite similar ex vivo skin accumulation data with uncoated nanospheres [95]. It is possible that CyDs can modulate enhanced anti-inflammatory activity by other means apart from skin accumulation.
Routes of administration
Published in Pamela E Macintyre, Suellen M Walker, David J Rowbotham, Clinical Pain Management, 2008
As few NSAIDs can be given intramuscularly, there are limited data comparing intramuscularly administered NSAIDs with NSAIDs given by other routes. Oral ketorolac 10 mg is at least as effective as intramuscular ketorolac 30 mg.47[I] Furthermore, intramuscular ketorolac 60 mg is comparable with parecoxib 40 mg which is equally effective whether administered intramuscularly or intravenously.48[II] Preoperative intramuscular lornoxicam is more effective than intramuscular ketoprofen in reducing postoperative pain.49[II]
Introduction to Human Cytochrome P450 Superfamily
Published in Shufeng Zhou, Cytochrome P450 2D6, 2018
S-Flurbiprofen (4′-hydroxylation) (Yamazaki et al. 1998a), S-warfarin (7-hydroxylation) (Yamazaki et al. 1998a), tolbutamide (methylhydroxylation), phenytoin (4′-hydroxylation) (Giancarlo et al. 2001), losartan (oxidation) (C.R. Lee et al. 2003), and diclofenac (4′-hydroxylation) (Yamazaki et al. 1998a) have been commonly used as probe substrates for CYP2C9 (Kumar et al. 2006). The substrates of CYP2C9 include oral sulfonylurea hypoglycemics (e.g., tolbutamide, glyburide, glimepiride, gliclazide, and glipizide), NSAIDs (e.g., diclofenac, ibuprofen, ketoprofen, suprofen, naproxen, flurbiprofen, indomethacin, meloxicam, piroxicam, tenoxicam, and lornoxicam), selective cyclooxygenase 2 inhibitors (e.g., celecoxib, lumiracoxib, etoricoxib, and valdecoxib), diuretics (e.g., torasemide and sulfinpyrazone), antiepileptics (e.g., phenytoin and phenobarbital), angiotensin II receptor inhibitors (e.g., losartan, irbesartan, and candesartan), anticancer drugs (e.g., cyclophosphamide and tamoxifen), and anticoagulants (e.g., S-acenocoumarol, phenprocoumon, and S-warfarin) (He et al. 2011; Miners and Birkett 1998; Rettie and Jones 2005). Vicriviroc (SCH 417690), a CCR5 receptor antagonist, is metabolized by CYP3A4/5 and 2C9 (Ghosal et al. 2007). CYP2C9 is also involved in the metabolism of the procarcinogen BaP, although CYP1A1/1A2 are the major enzymes responsible for its bioactivation (Ma and Lu 2007). Typical substrates of CYP2C9 such as celecoxib, ibuprofen, flurbiprofen, and diclofenac are relatively small, are lipophilic, and contain acidic groupings with pKa values in the range 3.8–8.1, which will be ionized at physiological pH, forming anions in vivo (He et al. 2011). The carboxylate groups of tienilic acid and diclofenac have been shown to be responsible for substrate preference and orientation in the active site of CYP2C9. Therefore, a typical CYP2C9 substrate should contain an anionic site and a hydrophobic site. However, neutral or positively charged compounds may also be substrates of CYP2C9.
Amelioration of physicochemical, pharmaceutical, and pharmacokinetic properties of lornoxicam by cocrystallization with a novel coformer
Published in Drug Development and Industrial Pharmacy, 2021
Kanwal Fatima, Nadeem Irfan Bukhari, Sumera Latif, Hafsa Afzal, Amjad Hussain, Rahat Shamim, Nasir Abbas
DSC has been one of the principal techniques to delineate cocrystals and has been routinely employed for fast screening of cocrystals [30]. Figure 2 represented the DSC thermograms of LORX, DMU, and cocrystals SGA & SEB. DSC data supported the findings of PXRD. LORX exhibited a single exothermic peak at 230.1 °C which depicted direct decomposition. Results for pure lornoxicam were in complete agreement with the previously published reports [31–34]. In previous studies, melting and thermal decomposition occurred simultaneously which was evident from an exothermic peak appearing at approximately 230 °C and the DSC thermogram of pure lornoxicam was typical of a crystalline substance [35,36]. DSC thermogram of DMU was also in agreement with the reported melting point and displayed a single endotherm at 108 °C. DSC curves of cocrystals SGA and SEB manifested melting endotherm between 135–140 °C followed by decomposition between 197–200 °C [14].
Dexmedetomidine vs hyaluronidase addition to fluoroscopy-guided caudal analgesia with steroid in lumbosacral spine surgery. A comparative double blinded study
Published in Egyptian Journal of Anaesthesia, 2021
Sanaa F. Wasfy, Waleed H. Nofal, Mona A. Ammar
Patients received 1 gm acetaminophen and 8 mg lornoxicam intravenously during the surgery. Acetaminophen was continued every 8 hours and lornoxicam was given every 12 hours postoperatively. Rescue analgesia was in the form of intravenous pethidine 0.5 mg/kg given if VAS was >3.
Effects of dexmedetomidine infusion during spinal anesthesia on hemodynamics and sedation
Published in Libyan Journal of Medicine, 2018
Ebru Tarıkçı Kılıç, Gaye Aydın
In subjects with postoperative pain scores equal to and higher than 4, 8 mg of lornoxicam (Xefo vial 8 mg, Abdi İbrahim Pharmaceutical Ind. and Trade Inc., İstanbul) was administered intravenously. Additional doses of analgesics were recorded.