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Drugs Affecting the Musculoskeletal System
Published in Radhwan Nidal Al-Zidan, Drugs in Pregnancy, 2020
Risk Summary: It is better to be avoided during the 1st and 3rd Trimesters because the pregnancy experience in humans suggests a risk of pulmonary hypertension of the newborn, SABs, and congenital malformations linked to the use of Oxaprozin. Furthermore, Oxaprozin has been found to inhibit labor and to prolong the length of pregnancy.
Nonopiate Analgesics and Adjuvants
Published in Gary W. Jay, Clinician’s Guide to Chronic Headache and Facial Pain, 2016
Some prescribing information: Ibuprofen (Motrin): Its half-life is 2 to 2.5 hours after multiple dosing. Typical adult dose is 1200 to 2400 mg/day.Naproxen: It is highly protein bound with a half-life of 12 to 15 hours. May use naproxen sodium 275- and 550-mg tablets twice a day.Ketoprofen (Orudis): It is 99% protein bound; its half-life is between 1.4 and 3.3 hours. It is available in 25, 50, and 75 mg and an extended-release 200-mg capsule. It can be taken three times a day.Oxaprozin (Daypro): Elimination half-life is between 50 and 60 hours after repeated doses—adult dose is 600 to 1200 mg/day. Patients can begin with a loading dose of 1800 mg.Etodolac (Lodine): The elimination half-life is six to seven hours. Maximum analgesia in one hour after oral dose. Doses range, in the adult, from 400 to 1200 mg/day.Indomethacin (Indocin): Elimination half-life is 2 to 11 hours. Adult dose is 75 to 150Diclofenac [Cataflam (potassium salt), Voltaren (enteric coated)]: It has a 75-minute half-life. The adult dose is 75 to 225 mg/day.Nabumetone (Relafen): A prodrug, metabolized to active metabolite with half-life of 24 hours. Adult dose is 1000 to 2000 mg/day.Ketorolac (Toradol): It is the only NSAID with parenteral usage; its half-life is four to six hours. Oral dosing is 10 mg three or four times a day. If given via IM or IV route, typically oral dosing is limited to four to five days.When using NSAIDs in the elderly, dosages should be decreased, in many cases, 50%.Celecoxib (Celebrex): It has a half-life of 11 hours; adult dose is 100 to 400 mg a day.
Nonopiate Analgesics and Adjuvants
Published in Gary W. Jay, Practical Guide to Chronic Pain Syndromes, 2016
Some prescribing information: Ibuprofen (Motrin): Its half-life is 2 to 2.5 hours after multiple dosing. Typical adult dose is 1200 to 2400 mg/day.• Naproxen: It is highly protein bound with a half-life of 12 to 15 hours. May use naproxen sodium 275- and 550-mg tablets twice a day.Ketoprofen (Orudis): It is 99% protein bound; its half-life is between 1.4 and 3.3 hours. It is available in 25, 50, and 75 mg and an extended-release 200-mg capsule. It can be taken three times a day.Oxaprozin (Daypro): Elimination half-life is between 50 and 60 hours after repeated doses—adult dose is 600 to 1200 mg/day. Patients can begin with a loading dose of 1800 mg.Etodolac (Lodine): The elimination half-life is six to seven hours. Maximum analgesia in one hour after oral dose. Doses range, in the adult, from 400 to 1200 mg/day.Indomethacin (Indocin): Elimination half-life is 2 to 11 hours. Adult dose is 75 to 150 mg/day.Diclofenac [Cataflam (potassium salt), Voltaren (enteric coated)]: It has a 75-minute half-life. The adult dose is 75 to 225 mg/day.Nabumetone (Relafen): A prodrug, metabolized to active metabolite with half-life of 24 hours. Adult dose is 1000 to 2000 mg/day.Ketorolac (Toradol): It is the only NSAID with parenteral usage; its half-life is four to six hours. Oral dosing is 10 mg three or four times a day. If given via IM or IV route, typically oral dosing is limited to four to five days.When using NSAIDs in the elderly, dosages should be decreased, in many cases, by 50%.Celecoxib (Celebrex): It has a half-life of 11 hours; adult dose is 100 to 400 mg a day.
Review on Chemistry of Oxazole derivatives: Current to Future Therapeutic Prospective
Published in Egyptian Journal of Basic and Applied Sciences, 2023
Sweta Joshi, Meenakshi Mehra, Ramandeep Singh, Satinder Kakar
Heterocyclic compounds are extensively used for therapeutic purpose, research areas and industries. Heterocycle containing nitrogen and oxygen atoms are a vital class of compounds in the medicinal chemistry. There has been interest in the biology and chemistry of heterocyclic molecules for researchers from decades, and oxazole moiety has become popular in the last few years considering its increasing relevance in the area of medicinal chemistry [1]. Oxazole contains two unsaturation in a five-membered ring including A carbon atom supports a nitrogen atom at position 3 and an oxygen atom at position 1, respectively [2]. The structure of oxazole derivatives exerts divergent weak interactions like hydrophobic effect, Vanderwaals force, hydrogen bonds, coordination bonds, ion-dipole and pi-pi bond; hence the derivatives exhibit potential application in agricultural, biotechnology, medicinal, chemical and material sciences [3]. From past, an immense number of oxazole derived medicinal agents have been used clinically shown on compounds (1–6) (Figure 1), such as Linezolid, Furazolidone, Toloxatone, Oxaprozin, Ditazole, and Aleglitazar [4].
Erlotinib complexation with randomly methylated β-cyclodextrin improves drug solubility, intestinal permeability, and therapeutic efficacy in non-small cell lung cancer
Published in Pharmaceutical Development and Technology, 2021
Nazlı Erdoğar, Safiye Akkın, Gamze Varan, Erem Bilensoy
In the literature, studies are reporting that the increase in dissolution with the complexation using RAMEB CD (Zhang et al. 2005; Maestrelli et al. 2009; Sangpheak et al. 2015). This situation is thought to be related to the higher complexing and solubilizing property of RAMEB CD. The enhanced dissolution rate observed might be due to the increase in solubility, as well as a decrease in the crystallinity of guest molecules, brought about by complexation with RAMEB CD. In addition, over-saturation levels were not reached according to solubility values found in the phase-solubility study, and thus high stability of solutions is expected. Maestrelli et al. reported on comparative dissolution profiles of oxaprozin (OXA) complex prepared with different CD derivatives including β-CD, DIMEB, and RAMEB CD (Maestrelli et al. 2009). At the end of the study, it has been found that the OXA-RAMEB CD inclusion complex exhibits the highest dissolution due to the highest solubilizing and complexation ability of RAMEB CD, supporting our interpretation.
Dotinurad: a novel selective urate reabsorption inhibitor for the treatment of hyperuricemia and gout
Published in Expert Opinion on Pharmacotherapy, 2021
Tomohiko Ishikawa, Toshinari Takahashi, Tetsuya Taniguchi, Tatsuo Hosoya
Glucuronide and sulfate conjugates are the major metabolites of dotinurad that are excreted in urine [24–26]. Because nonclinical studies suggested potential effects of oxaprozin, a non-steroidal anti-inflammatory drug, on the plasma protein binding and glucuronidation of dotinurad, the PK and safety of a single dose of 4 mg dotinurad were evaluated in 12 healthy adult males with and without 600 mg oxaprozin in an open-label, two-period, add-on study [33]. Compared with dotinurad alone, coadministration with oxaprozin was associated with a 34.3% decrease in the urinary excretion rate of the glucuronide conjugates and a 16.5% increase in the AUC0–inf of dotinurad; however, these effects were within the standard range specified in the guidelines for drug–drug interactions [32]. No safety concerns were raised after coadministration with oxaprozin.