Explore chapters and articles related to this topic
Driver Capabilities in the Resumption of Control
Published in Donald L. Fisher, William J. Horrey, John D. Lee, Michael A. Regan, Handbook of Human Factors for Automated, Connected, and Intelligent Vehicles, 2020
Sherrilene Classen, Liliana Alvarez
Zane is a 72-year old male who immigrated to Canada in his 20s. Zane lives alone in a retirement condominium, where he moved five years ago after his wife passed away. He has two daughters, one who lives close to him and another who lives across the country. Zane is an accountant who worked in an accounting firm until his retirement, i.e., when he turned 65 years old. He enjoys reading and taking walks with his dog. Zane has a history of high blood pressure and a diagnosis of open-angle glaucoma. He underwent a laser trabeculoplasty—a laser surgery used to lower intraocular pressure—two years ago. He takes Acetazolamide to manage his glaucoma. He is experiencing worsening of his peripheral field of view even after surgery, and the optometrists have noticed some loss of visual acuity. He has been a licensed driver for over 50 years, and currently drives approximately three times a week in familiar environments and routes. He avoids driving at nights and in inclement weather. Table 10.1 summarizes Zane’s strengths and challenges, which help guide the assessment process.
Cross-Linked Polymers for Drug Delivery Systems
Published in Munmaya K. Mishra, Applications of Encapsulation and Controlled Release, 2019
Yu et al. developed in situ polyethylene glycol (PEG) hydrogels for sustained release of avastin for the treatment of corneal neovascularization. In vitro cytotoxicity studies on L-929 cells over 7 days of incubation showed the absence of cytotoxic effect. The drug release was within a period of 14 days [19]. Morsi et al. loaded acetazolamide, an antiglaucoma drug, onto an ion-induced nanoemulsion-based in situ gel for ocular delivery. The nanoemulsion formulations were prepared from peanut oil, Tween, cremophor EL, gellan gum, xanthan gum, Carbopol, HPMC, and propylene glycol. The drug release profile from the gel was sustained, and the gel was stable at all studied temperatures. However, the formulation of gellan/Carbopol exhibited partial drug precipitation during storage. Formulations of gellan gum/xanthan gum and gellan gum/HPMC exhibited high therapeutic efficacy with extended intraocular pressure–lowering effect when compared with commercial eye drops and oral tablets. The formulation is a promising therapeutic for the treatment of glaucoma with reduced systemic side effects of acetazolamide due to the local inhibition of carbonic anhydrase. The formulation also exerted an extended therapeutic effect, which can improve patient compliance resulting from reduced frequency of administration [20].
Therapeutic Use of Carbonic Anhydrase Inhibitors and Their Multiple Drug Interactions
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Andrea Angeli, Claudiu T. Supuran
The systemic carbonic anhydrase inhibitor, acetazolamide (1), was initially discovered as a diuretic agent (Supuran, 2008; Neri and Supuran, 2011) and introduced in 1954 into ophthalmology as a treatment for glaucoma and, since then, has been widely used for this purpose. At first, its clinical use as diuretic drug is limited to development of metabolic acidosis (Kassamali and Sica, 2011). However, this feature can afford some potential clinical benefit for disease states such as metabolic alkalosis (Faisy et al., 2010; Mazur et al., 1999) nephrolithiasis (Sterrett et al., 2008), rhabdomyolysis (Subbaramaiah et al., 2010; Davidov et al., 2006), contrast-induced nephropathy (CIN) (Pakfetrat et al., 2009), sleep apnea (Nakayama et al., 2002; Angeli and Supuran, 2018), and high-altitude erythropoiesis (Leaf and Goldfarb, 2007; Richalet et al., 2008). In subsequent years the systemic side effects of acetazolamide led to the development of new CAIs such as brinzolamide 3 and dorzolamide 4 (Fig. 3.2) with their high water solubility are administered via the topical route directly into the eye, making them less prone to drug-drug interactions and systemic side effects (Carta et al., 2012; Masini et al., 2013).
A review on ‘sulfonamides’: their chemistry and pharmacological potentials for designing therapeutic drugs in medical science
Published in Journal of Coordination Chemistry, 2023
Wardha Zafar, Sajjad Hussain Sumrra, Abrar Ul Hassan, Zahid Hussain Chohan
A majority of well-known marketed drugs are aromatic/heterocyclic sulfonamides having SO2NH2 group in their chemical structure (Figure 2). Examples include celecoxib as nonsteroidal anti-inflammatory drug for selective inhibition of cyclo-oxygenase COX-2 [63], glipizide and glibenclamide as sulfonylureas [64], acetazolamide for inhibition of carbonic anhydrase [65], sulfamethoxazole for antimicrobial activity [66], darunavir as HIV protease inhibitor [67], clopamide as diuretic agent for antihypertensive activity [68], sulfasalazine for rheumatoid arthritis [69], sumatriptan for migraine [70], dorzolamide as inhibitor of human carbonic anhydrase II [71], mafenide as antibiotic [72], zonisamide as anticonvulsant agent [73], and probenecid for treating hyperuricemia and gout [74]. Derivatives of the amino group containing sulfonamides can be easily developed, resulting in a broad-spectrum of biomedical applications. Sulfonamides containing hydrazino or amino derivatives are also considered as effective inhibitors of CA isozymes [75].
Synthesis and characterization of the Co(II) and Ni(II) complexes of 1,3,4-thiadiazole-derived ketones and secondary alcohols: thermal and magnetic properties
Published in Journal of Coordination Chemistry, 2021
Melih Erdogan, Kubra Kiymaz, Hakan Tahtaci, Saban Uysal
The synthesis of 1,3,4-thiadiazole have wide variety of biological activities, including antimicrobial, antifungal, antibacterial, anticonvulsant, antituberculosis, antiproliferative, anti-inflammatory, and anti-HIV properties [17–33]. Due to the anticancer activities of 2-amino-1,3,4-thiadiazole and its derivatives, which are used as starting materials in the synthesis of various compounds, the synthesis of these compounds is particularly significant [34–37]. It has been reported in various studies conducted with 1,3,4-thiadiazole and its derivatives that these compounds are used in industrial fields such as polymer, dye, herbicide, and insecticide production [38–41]. Additionally, the 1,3,4-thiadiazole nucleus is used in various commercial drugs such as acetazolamide (I), methazolamide (II) (carbonic anhydrase inhibitors for glaucoma treatment), sulfamethizole (III), cefazedone (IV), cefazolin (V), and ceftezole (VI) (used as antibacterial drugs) (Figure 1) [42, 43].
Synthetic and anti-cancer activity aspects of 1, 3, 4-thiadiazole containing bioactive molecules: A concise review
Published in Journal of Sulfur Chemistry, 2021
Vincent A. Obakachi, Babita Kushwaha, Narva Deshwar Kushwaha, Sithabile Mokoena, Ab Majeed Ganai, Tabasum Khan Pathan, Werner E. van Zyl, Rajshekhar Karpoormath
The display of interesting pharmacological properties of 1,3,4-thiadiazole heterocyclic compounds is considered to be due to N2C2S moiety, its lack of toxicity, in vivo stability, and high aromaticity [19]. Furthermore, the ability of the ‘hydrogen binding domain’ and the ‘two-electron donor mechanism’ allows the use of 1,3,4-thiadiazole as one of the latent molecules in a variety of marketed products, such as Methazolamide (Carbonic anhydrase inhibitor), Acetazolamide (for glaucoma), Desaglybuzole (anti-diabetic) [20], Cephazolin, Filanesib, Litronesib etc. as presented in (Figure 2) with their respective frameworks and activities that have been approved. The synthesis and evaluation of the chemical properties and biological activities of the novel 1,3,4-thiadiazole embedded analogues have accelerated over the years. In addition, the number of research studies on this moiety has also increased significantly in recent years. This review aims to capture a recent synthetic approaches and anticancer activities published in the literature, based on the compound's value in medicinal chemistry.