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Endocrine Disorders, Contraception, and Hormone Therapy during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Vildagliptin is a DPP-4 inhibitor used to treat type 2 diabetes mellitus. The frequency of birth defects was apparently not increased among 69 infants born after first trimester exposure to vildagliptin (Benhalima et al., 2018). Renal aplasia and patent ductus arteriosus were the two congenital anomalies observed (2/69).
Oral Agents and Insulin in Care of Older Adults with Diabetes
Published in Medha N. Munshi, Lewis A. Lipsitz, Geriatric Diabetes, 2007
Hermes Florez, Jennifer B. Marks
Dipeptidyl peptidase-IV (DPP-IV) inhibitors are in various stages of development (26). DPP-IV is the enzyme that degrades native GLP-1. Inhibition of this enzyme can increase GLP-1 levels and potentially improve postprandial glycemic control. In clinical trials, vildagliptin improves glycemic control both as monotherapy and in combination with metformin (27). Analyses of efficacy data for elderly patients in two phase 3 clinical studies (about 500 patients) and safety data from monotherapy studies including 2000 elderly patients revealed significant, consistent and sustained reductions in HbAlc and similar safety and tolerability to that found in younger patients [data presented by Baron MA et al. (28)]. Studies with sitagliptin demonstrated similar benefits in older patients as in younger ones receiving the drug. Further studies are now required to evaluate its long-term durability, effects, safety, and tolerability in comparison with other anti-diabetic agents and in different patient subgroups, including elderly patients with diabetes.
Green polymer altered in-situ gel oral liquid sustainable release preparation of vildagliptin suitable for dysphagic diabetic patients: assessment in-vitro & in-vivo
Published in Pharmaceutical Development and Technology, 2023
Soha M. El-masry, Heba M. ElBedaiwy, Mohammad M. Abd-Alhaseeb, Mohamed S. Abdel-Maksoud, Doaa A. Habib
Vildagliptin belongs to a new class of drugs known as DPP4 inhibitors (dipeptidyl peptidase IV) inhibitors. Vildagliptin increases the intestinal hormone GLP-1, which helps with glucose homeostasis and insulin secretion, by blocking DPP4 in the body. Vildagliptin significantly reduces fasting blood sugar, postprandial glucose, and glycosylated hemoglobin (HbA1c) levels. Beta-cell performance might also be enhanced. Following oral administration, vildagliptin is quickly absorbed achieving peak plasma concentrations after 1.7 h. The absolute bioavailability of vildagliptin is 85%. It has a terminal elimination half-life of 2–3 h. Vildagliptin is extensively eliminated in the urine; with 18–22% of the excreted amount in the unmetabolized form of the drug (Lauster et al. 2007). The drug’s primary problem is its fast excretion, which results in an extremely short half-life, Which may lead to frequent doses required and impaired patient compliance. Additionally, the quick action of vildagliptin can lead to a quick hypoglycemic effect, which needs to be handled with care to avoid needless risks. As a result, the characteristics of this drug can be improved by the development of a controlled release formulation because it will allow for appropriate adjustment of the onset and duration of action. This may increase patient compliance, lower the risk of hypoglycemic crisis, and stop blood glucose levels from fluctuating.
Cardiovascular safety and effectiveness of vildagliptin in patients with type 2 diabetes mellitus: a 3-year, large-scale post-marketing surveillance in Japan
Published in Expert Opinion on Drug Safety, 2020
Yosuke Ishida, Hiroki Murayama, Yohei Shinfuku, Tomoko Taniguchi, Takayoshi Sasajima, Naotsugu Oyama
In a meta-analysis of vildagliptin treatment in non-Japanese patients, it was shown that there was no increase in the incidence of major CV events (risk ratio 0.82, 95% CI 0.61–1.11) [17]. Murayama et al recently reported results of a 2-year post-marketing surveillance (PMS) study of vildagliptin in nearly 20,000 Japanese T2DM patients, in which the incidence of macrovascular disease (including MI and stroke) was 1.14% [18]. However, the entire CV risk was not directly evaluated and the study had a limited follow-up period [18]. Another PMS in a large Japanese T2DM population recently provided real-world efficacy and safety data of vildagliptin used concomitantly with oral antidiabetic drugs and insulin for a period of up to 52 weeks. However, CV outcomes were not specifically evaluated [19]. Thus, further study is necessary to clarify the incidence of CV events in Japanese patients receiving long-term vildagliptin treatment. This is relevant because the incidence and nature of CV events in Japanese and Caucasian patients are different: the incidence of stroke is higher in Japanese patients while the incidence of MI is lower [20]. Moreover, the long-term safety profile of vildagliptin in patients with different patient backgrounds, including renal impairment, hepatic impairment, and heart failure, has not been confirmed. Therefore, the present 3-year PMS was conducted to evaluate the real-world, long-term safety, focusing on the CV safety of vildagliptin in a large group of Japanese patients with diverse baseline characteristics.
Vildagliptin inhibits high free fatty acid (FFA)-induced NLRP3 inflammasome activation in endothelial cells
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2019
Yanyan Qi, Xianhui Du, Xiangyan Yao, Yuanyuan Zhao
The main limitation of the current study is that we only examined the protective effects of vildagliptin against FFA-induced NLRP3 inflammasome activation and the inflammatory response in an in vitro primary endothelial culture model. It should be noted that the pathological mechanisms of endothelial dysfunction are complicated and need to be further elucidated. Diverse risk factors, including genetics, aging, and obesity, are reported to be involved in cardiovascular disease [30]. Animal experimentation is an important method for exploring the pathogenesis and treatment of cardiovascular diseases. In addition, the pathogenesis of cardiovascular diseases is regulated through a complex network of signaling pathways. It is possible that vildagliptin plays a role in regulating the crosstalk of signaling pathways involved in FFA-induced endothelial dysfunction. Future investigations with animal models or clinical trials are necessary to verify the pharmacological function of vildagliptin in vivo. Vascular endothelial dysfunction is present in diabetes and its vascular complications. Now, cardiovascular diseases have emerged as a common complication of diabetes and improved strategies for the prevention and treatment of cardiovascular diseases are evolving rapidly. Dysfunction of vascular cells has been shown to contribute to the pathogenesis and clinical expression of atherosclerosis in diabetes. Elucidation of the molecular mechanism behind the protective effects of vildagliptin on vascular function will provide valuable data for its implication in the treatment of diabetes and its cardiovascular complications.