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Allopathic Medicines
Published in Varma H. Rambaran, Nalini K. Singh, Alternative Medicines for Diabetes Management, 2023
Varma H. Rambaran, Nalini K. Singh
Several specific and potent SGLTi drugs have undergone preclinical testing, most of which are glucosides that are structurally related to the lead drug: phlorizin. O-glucosides, such as sergliflozin etabonate (Figure 2.17a) and remogliflozin etabonate (Figure 2.17b), are strategically administered in the prodrug form of the biologically active sergliflozin A and remogliflozin to avoid degradation by β-glucosidase in the small intestine (Nair and Wilding 2010).Structural formulae of O-glucosides: (a) sergliflozin etabonate and (b) remogliflozin etabonate.
Development of lipid nanoparticles for transdermal loteprednol etabonate delivery
Published in Journal of Microencapsulation, 2022
Burcu Üner, Samet Özdemir, Çetin Taş, Yıldız Özsoy, Melike Üner
Treatment of skin diseases includes various medications. Topical corticosteroids have been used and provided an effective therapy. Moreover, they are employed to provide anti-inflammatory, antimitotic, and immunosuppressive actions (Goldstein et al.2021). These pharmacological actions depend on various mechanisms. The utilisation of topical corticosteroids for specific skin diseases are discussed in detail in the relevant review studies (Rathi and D’Souza 2012, Das and Panda 2017). The use and adverse effects of intralesional and systemic corticosteroids are discussed separately. Loteprednol etabonate (LE) is a topical corticosteroid that was synthesised via modification of prednisolone to achieve the desired anti-inflammatory action followed by rapid conversion to inactive metabolites (Comstock and Sheppard 2018, Fong et al.2019). Data from pharmacokinetic studies of LE indicate that it undergoes a high first-pass effect in the liver, and is rapidly eliminated from the systemic circulation. Its plasma half-life is 2.8 h and is highly bound to plasma proteins (Noble and Goa 1998). In addition, studies are showing that LE is more lipophilic (log k = 3.04) and has a low water solubility (0.5 µg/mL) compared to commonly used corticosteroids such as hydrocortisone and dexamethasone (Alberth et al.1991).
Pharmacotherapeutic management of atopic keratoconjunctivitis
Published in Expert Opinion on Pharmacotherapy, 2020
Ibtesham T Hossain, Priyanka Sanghi, Bita Manzouri
While effective anti-inflammatory agents, long-term use of topical corticosteroids can potentially result in a range of adverse effects. These include raised intraocular pressure, posterior subcapsular cataract formation, and increased susceptibility to infection (commonly herpetic keratitis). They are usually given as short, intensive courses with the aim to rapidly taper. Loteprednol etabonate is a topical corticosteroid that was engineered through retrometabolic drug design with the goal of maintaining robust and effective anti-inflammatory properties but also reducing the typical risks associated with this class of medication. A recent review by Comstock et al. of 20 years of clinical data on loteprednol demonstrated a lower risk profile for the treatment of allergic eye disease [37].
Pediatric Ocular Acne Rosacea: Clinical Features and Long Term Follow-Up of Sixteen Cases
Published in Ocular Immunology and Inflammation, 2021
Case 2 is a 3-year-old boy presented with redness, ocular irritation, photophobia since the age of 8 months. The patient had a history of recurrent chalazia and conjunctival hyperemia. Ophthalmological examination revealed bilateral conjunctival hyperemia, blepharitis, meibomitis, lid margin telangiectasia, limbal vascularisation, punctate keratopathy. Corneal haze located inferiorly was present in the left eye. He had no cutaneous involvement. His parents noticed spicy foods, heat, and sunlight were precipitating factors for his ocular signs and symptoms. He had also been examined by different ophthalmologists and was treated with topical antibiotics, preservative-free artificial tears, steroids and antiallergic drops with minimal relief.. Oral erythromycin suspension for 1 year, erythromycin ointment for 8 months, loteprednol etabonate 0.5% four times a day, topical azithromycin for 3 months and preservative-free artificial tears four times a day were prescribed with the diagnosis of ocular acne rosacea. Warm compresses and lid hygiene were recommended at least twice a day. The topical loteprednol etabonate 0.05% were tapered biweekly and the maintenance dose every 4 days were given. Topical cyclosporine 0.05% three times a day was given in order to control inflammation for 16 months. His symptoms improved significantly following 2 months of therapy. During seven-year follow-up, mild flare-ups were seen in the form of meibomitis with conjunctival hyperemia and were successfully treated with daily warm compresses, eyelid scrubbing, low dose of topical loteprednol etabonate 0.5% drop and topical azithromycin reinstitution.