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Monographs of Topical Drugs that Have Caused Contact Allergy/Allergic Contact Dermatitis
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Oxyphenbutazone is a pyrazolidine nonsteroidal anti-inflammatory drug (NSAID) and a hydroxylated and active metabolite of phenylbutazone. Oxyphenbutazone eye drops have been used in the management of postoperative ocular inflammation, superficial eye injuries, and episcleritis. This NSAID was formerly used by mouth in rheumatic disorders such as ankylosing spondylitis, osteoarthritis, and rheumatoid arthritis but such use is no longer considered justified owing to the risk of severe hematological adverse effects and Stevens-Johnson syndrome. It was withdrawn in the mid-1980s in most countries but is apparently still available in China (www.drugs.com). The name oxyphenbutazone is also used for oxyphenbutazone monohydrate (CAS 7081-38-1, EC number not available, molecular formula C19H22N2O4), which is (or was) the usual form in drugs (1).
Species differences in plasma protein binding of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease inhibitor nirmatrelvir
Published in Xenobiotica, 2023
Siennah R. Greenfield, Heather Eng, Qingyi Yang, Chunyang Guo, Laura Byrnes, Alyssa Dantonio, Graham West, Li Di, Amit S. Kalgutkar
Human SA structures, as listed by protein data bank (PDB) reference numbers, were aligned and superimposed based on the alpha-carbon atoms of all amino acids (AAs). Site I, site II and site III are consistent with the naming described previously (Ghuman et al. 2005). Binding site AAs were counted as those with heavy atoms within 4 Å of known bound ligands. Oxyphenbutazone (2BXO) and iodipamide (2BXN) were used as reference ligands for the site I pocket AA comparison (Ghuman et al. 2005). Indomethacin (2BXM), diazepam (2BXF) and ibuprofen (2BXG) were used as reference ligands for the site II pocket comparison (Ghuman et al. 2005). The ligand teniposide (4L9Q) was used as ligand reference to define the site III AAs for sequence comparison across different species (Wang et al. 2013). The selection of above reference ligands resulted in 33 AAs at site I, 16 amino acids at site II, and 15 AAs at site III. Since the loop at site III of the dog SA structure (5GHK) was not resolved (Yamada et al. 2016), a full-length homology model of the dog SA structure was re-built based on the apo structure. The corresponding site II and III pockets were used in the docking study. Albumin AA sequences with the following accession numbers were used for sequence comparisons: human: P02768; monkey: Q28522; dog: P49822; rabbit: P49065; rat: P02770; mouse: P07724. In Figure 6, the HSA site I AA shown are R281, H312, A315, E316, P471, C472, D475, Y476, and V479. In Figure 7, site III AAs 134–180 are shown for all species except monkey where AAs 126–172 are shown.
The pharmacotherapeutics of sarcoidosis
Published in Expert Review of Clinical Pharmacology, 2022
Patrick Mangialardi, Richart Harper, Timothy E Albertson
GCs are considered the first-line therapy for pulmonary and extra-pulmonary sarcoidosis. Evidence for use in sarcoidosis comprises several randomized controlled trials, several prospective observational studies, retrospective cohort studies, and numerous case reports and case series. The earliest randomized controlled trial (RCT) came in 1967 when James performed a double-blind, randomized, placebo-controlled trial analyzing 75 patients and comparing 20 mg/day oral prednisolone for 6 months to placebo [8]. A third arm of this study included treatment with the anti-inflammatory agent oxyphenbutazone [8]. There was significant improvement in clinical and radiographic outcomes in patients treated with GCs compared to placebo, though there was no specific data reported for symptomatic improvement. Israel et al. performed a prospective randomized double-blind placebo-controlled trial of 83 patients comparing prednisone 60 mg/day for 3 months to placebo [9]. The primary endpoint was a grouped outcome of radiographic changes, lung function, and symptoms. There was a significant improvement in this grouped outcome for patients with radiographic stage II or III disease at the conclusion of the 3-month treatment period (see Table 1 for radiographic stages of sarcoidosis). This difference was lost in longer-term follow-up at 5 years.
Characterization of metabolites of larotaxel in rat by liquid chromatography coupled with Q exactive high-resolution benchtop quadrupole orbitrap mass spectrometer
Published in Xenobiotica, 2018
Zhenzhen Liu, Pengyi Hou, Lian Liu, Feng Qian
The identification of the metabolites of new drugs provides essential information for toxicological profile, and also provides information that may result in the generation of new, improved drug structures. Active metabolites may have superior pharmacological, pharmacokinetic, and safety profiles compared to their respective parent molecules. As a result, a number of active metabolites have been developed and marketed as drugs with improved profiles relative to their parent molecules. Examples of active metabolites of marketed drugs that have been developed as drugs include oxazepam, cetirizine, fexofenadine, oxyphenbutazone, desloratadine and so on (Clissold, 1986; Fura et al., 2004; Meeves & Appajosyula, 2003; Murdoch et al., 2003).