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Endocrine Disorders, Contraception, and Hormone Therapy during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Exenatide is a non-oral drug available to treat diabetes but it has not been studied during pregnancy. No adequate human studies have been published of exenatide use during pregnancy, although a registry was established. The old FDA category was C. Importantly, the manufacturer states the drug should not be used during pregnancy. At doses two to three times the usual human dose of exenatide during gestation in mice, the drug was associated with increased frequency of cleft palate, irregular skeletal ossification, and an increased number of neonatal deaths (Manufacturer’s data).
Regulation of Food Intake
Published in Nathalie Bergeron, Patty W. Siri-Tarino, George A. Bray, Ronald M. Krauss, Nutrition and Cardiometabolic Health, 2017
Surya Panicker Rajeev, Ian W. Seetho, John P.H. Wilding, Nathalie Bergeron, Patty W. Siri-Tarino, George A. Bray, Ronald M. Krauss
Exendin-4 (4-39) is a purified derivative from the saliva of Heloderma suspectum, the Gila monster lizard, and was discovered in 1992. Exendin-4 shares only 53% homology with human GLP-1 but is a potent analogue and is resistant to the action of DPP-IV. Subsequently, exenatide, a synthetic form of exendin-4, became the first approved GLP-1 analogue for the treatment of type 2 diabetes in 2005. It has a short half-life of 2.4 hours and is administered subcutaneously, twice daily. In addition to improving glycemic control, exenatide treatment reduces body weight in patients with type 2 diabetes [91].
Obesity
Published in Philip E. Harris, Pierre-Marc G. Bouloux, Endocrinology in Clinical Practice, 2014
Ahmed Yousseif, Efthimia Karra, Sofia Rahman, Rachel L. Batterham
Exenatide is a long-acting synthetic peptide that is a GLP-1 receptor agonist, and liraglutide is a long-acting GLP-1 analog administered subcutaneously twice and once daily, respectively. They are currently available for adjunctive therapy for patients with T2DM who are inadequately controlled on oral agents. Dose-dependent weight loss has been reported in trials of exenatide in T2DM not well controlled on oral agents (~4.8 kg over 18 months in the absence of any dietetic or exercise interventions). In diabetes trials, liraglutide was associated with a significant reduction in weight up to 2.5 kg compared with placebo or glimepiride, whereas weight loss has also been reported in patients without diabetes who received liraglutide. In a 20-week randomized trial comparing liraglutide (administered subcutaneously in one of four daily doses, 1.2–3 mg), placebo, and open-label orlistat (120 mg orally three times daily) in 564 patients (mean BMI, 35 kg/m2), weight loss increased with increasing doses of liraglutide, with mean weight loss ranging from 4.8 to 7.2 kg. Patients randomly assigned to any dose of liraglutide lost significantly more weight than those assigned to placebo (mean weight loss, 2.8 kg); whereas patients receiving the two highest doses of liraglutide (2.4 and 3.0 mg) lost significantly more weight than those assigned to orlistat (6.3, 7.2, and 4.1 kg, respectively). The two highest doses of liraglutide are higher than those currently prescribed for treatment of T2DM, and a greater proportion of patients taking these doses reported nausea (37%–47%) and vomiting (12%–14%).
Neuro-Ophthalmic Literature Review
Published in Neuro-Ophthalmology, 2023
David A. Bellows, John J. Chen, Hui-Chen Cheng, Michael S. Vaphiades, Xiaojun Zhang
In this trial 15 IIH patients were randomly assigned to either exenatide (n = 7) or placebo (n = 8) and followed with telemetric ICP monitoring for 12 weeks. At 2.5 hours, the exenatide group had a mean ICP reduction of −4.2 mmHg compared with placebo, which was sustained at 24 hours (−4.7 mmHg) and 12 weeks (−4.1 mmHg). Vision also significantly improved in the exenatide arm compared with placebo. There was a trend toward improved headaches in the exenatide group. Surprisingly, despite the improvement in the ICP and visual acuity, there was no significant difference in the perimetric mean deviation or RNFL between the two arms. There was also no significant change in body mss index (BMI) at 12 weeks. Exenatide was fairly well tolerated other than being associated with nausea in many of the patients.
Polymeric microparticle systems for modified release of glucagon-like-peptide-1 receptor agonists
Published in Journal of Microencapsulation, 2021
Luis Peña Icart, Fernando Gomes Souza, Luís Maurício T. R. Lima
Exenatide was also microencapsulated by the water in oil in oil (W/O/O) procedure to obtain PLGA microspheres with a low initial burst release and sustained pharmacological activity. In this procedure, the insolubility of the PLGA in silicon oil causes it to concentrate on the surface of the aqueous drops. Thus, the particle size of the resulting microspheres could be regulated by controlling the time at which the silicon oil is added (Xuan et al.2013, Wang et al.2016). The W/O/O procedure yields PLGA microspheres with a diameter of about 75 µm and an encapsulation efficiency of 83.8 ± 1.3%. The in vitro study showed a sustained release of 80% of the entrapped peptide after 42 days with a low initial burst release of 1.3 ± 0.13%. Pharmacokinetic and pharmacodynamic assays suggested that most of the incorporated exenatide into the microspheres was released up to 32 days after a single dose, with a cumulative bioavailability of 70.3%. The hypoglycaemic effect of the product in diabetic mice was sustained for the full three-week duration of the experiment.
Exenatide-loaded inside-porous poly(lactic-co-glycolic acid) microspheres as a long-acting drug delivery system with improved release characteristics
Published in Drug Delivery, 2020
Junqiu Zhai, Zhanlun Ou, Liuting Zhong, Yu-e Wang, Li-Ping Cao, Shixia Guan
Type 2 or noninsulin-dependent diabetes accounts for 90–95% of all patients with diabetes and is a chronic disease with substantial morbidity and mortality. Patients with type 2 diabetes have a life expectancy that is reduced by 10 years and the disease is estimated to affect about 550 million people worldwide by 2030 (Johnson et al., 2009; Chatterjee et al., 2017; Rowley et al., 2017). Exenatide (EXT), the synthetic exendin-4, is an outstanding incretin mimetic that is approved by the Food and Drug Administration and the European Medicines Agency as the drug for type 2 diabetes (Deacon, 2004; Davidson et al., 2005; Song et al., 2019). It has multiple glucose regulatory therapeutic effects, such as enhancement of insulin secretion, reduction of food intake, and deceleration of gastric emptying (Li et al., 2015; Song et al., 2019). However, EXT only has a short plasma half-life of 2.4 h and an action time of about 8 h, thus the long-acting EXT formulations are of prime importance (DeYoung et al., 2011; Cai et al., 2013).