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Anti-Diabetic Drugs
Published in Awanish Kumar, Ashwini Kumar, Diabetes, 2020
Oral anti-diabetic drugs are, in most cases, the mainstay of diabetes treatment until the physician diagnoses the need to start parenteral drugs (insulin, amylin and GLP-1 analogues). The initial anti-diabetic drugs were from a class of molecules known as sulphonylurea and biguanide. Sulphonylureas stimulate insulin secretion (insulin secretagogues), while biguanide increases insulin sensitivity in the insulin-responsive cells and also inhibits the extra hepatic gluconeogenesis. Sulphonylureas primarily bind to the SUR1 receptor on the β-cell membrane that follows the closure of ATP-K+ channels. This closure stimulates the opening of voltage-gates Ca2+ channels which results in the fusion of insulin granules with the membrane, and thus, their release into the blood. As this effect does not depend upon the plasma glucose concentration, sulphonylureas are, therefore, associated with an increased risk of hypoglycaemia. Another class of insulin secretagogues is from the meglitinide class (glinide class of drugs) which includes drugs such as repaglinide, mitiglinide and nateglinide. They bind to a separate receptor site compared to the conventional sulphonylureas, but they also stimulate insulin release in a similar manner that begins with closure of ATP-potassium channels [1,4,7]. Metformin, on the other hand, increases the peripheral insulin sensitivity in the skeletal muscles cells by stimulating the translocation of GLUT-1 receptors on the cell surface. Metformin was also reported to increase the endogenous secretion of GLP-1, thus improving further insulin responsiveness. Metformin, with minimum adverse effects as compared to all other anti-diabetic drugs, can be said to be the ‘safest’, and is considered to be the first-line therapy in diabetes. In terms of adverse effects, metformin is contraindicated in diabetic patients with severe renal damage as metformin can result in a life-threatening condition called lactic acidosis in such patients.
The role of sulfonylureas in the treatment of type 2 diabetes
Published in Expert Opinion on Pharmacotherapy, 2022
Brian Tomlinson, Nivritti Gajanan Patil, Manson Fok, Paul Chan, Christopher Wai Kei Lam
Meglitinide is the non-sulfonylurea carboxamido moiety of glibenclamide, which has hypoglycemia activity by binding to one receptor site and has overall lower binding affinity than glibenclamide [17]. Repaglinide, a benzoic acid derivative of meglitinide, was the first analogue to become available. Nateglinide, a derivative of d-phenylalanine, was subsequently developed and mitiglinide, a 3-phenylpropionic acid derivative, was developed in Japan [18]. These meglitinide or glinide derivatives have more rapid association/dissociation with the target receptor than conventional sulfonylureas and are very effective in promoting early-phase insulin secretion. Their pharmacokinetic properties also result in a short duration of action and their action is more dependent on glucose concentrations and therefore they are useful to attenuate postprandial hyperglycemia and have less risk of hypoglycemia than sulfonylureas but they have to be taken more frequently, usually with each meal [18].
How should rheumatologists manage glucocorticoid-induced hyperglycemia?
Published in Modern Rheumatology, 2021
Hiroyuki Nakamura, Yuichiro Fujieda, Akinobu Nakamura, Tatsuya Atsumi
Since glucocorticoids affect pancreatic β cells and suppress insulin secretion [4], insulin secretagogue may be reasonable for treating GIH as insulin injection is. Sulfonylureas promote insulin release from pancreatic β cells. Kasayama et al. [45] reported glimepiride improved mean fasting PG levels in 3 patients with GIH. But, sulfonylureas carry a risk of hypoglycemia overnight because of the longer duration of action than desired [46]. Glinides are fast- and short-acting stimulator for insulin secretion, targeting postprandial hyperglycemia [47]. Tanaka et al. [48] reported that glinides (mitiglinide/repaglinide) improved CGM findings, such as mean and postprandial PG levels, during methylprednisolone pulse therapy in five patients with thyroid ophthalmopathy. Ito et al. [49] showed by a medical record review that nateglinide improved postprandial hyperglycemia in patients with rheumatic diseases, if prednisolone was taken in a divided dose for each meal. Although these retrospective studies suggested the efficacy of glinides for GIH, there have been no designed prospective studies to confirm that.
Sulpiride gastro-retentive floating microsponges; analytical study, in vitro optimization and in vivo characterization
Published in Journal of Drug Targeting, 2020
Mahmoud A. Younis, Marwa R. El-Zahry, Mahmoud A. Tallat, Hesham M. Tawfeek
Oral route of drug administration is still the most convenient route for most of patients even though drugs facing many challenges to be delivered effectively. Dissolution limited absorption, drug complexation with GIT located materials, P-glycoprotein (P-gp) efflux and absorption window are mostly some of the obstacles facing effective drug absorption from oral route [1–3]. One of the important challenges facing researchers is the absorption of drugs from a specific site along the gastrointestinal tract, which refer to absorption window. Different approaches and solutions have been reported and investigated to address this point, leading to improvement of the absorption of these drugs [4,5]. Gastroretention is an approach to enhance the residence time of drugs in the stomach for relatively long period of time, which behaves like some sort of targeting in GIT for both systemic drug absorption and local effect [6,7]. Several techniques were performed to fulfil this approach like low and high density formulations [8,9], expandable systems which cannot escape from pyloric sphincter [10] and stomach bioadhesive formulations [11]. One of these techniques is the low-density systems which could be able to float into the contents of the stomach long time. These systems can be sorted as effervescent or non-effervescent based formulations [12]. Floating microsponges are categorised as a non-effervescent formulation which is typically sponge microparticles. These microparticles have numerous interconnecting channels and voids, in addition to a highly porous surface in a firm non-collapsible structure. This system when contacted with the stomach fluid showed a lower density structure which aid in buoyancy like hollow microspheres and microporous compartment formulations [13,14]. A recent study used mitiglinide calcium microsponge as an effective gastro-retentive tool for enhancement of drug release [15].