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Endocrine Diseases
Published in Miriam Orcutt, Clare Shortall, Sarah Walpole, Aula Abbara, Sylvia Garry, Rita Issa, Alimuddin Zumla, Ibrahim Abubakar, Handbook of Refugee Health, 2021
If glycaemic control is not achieved, a sulfonylurea is added. Gliclazide and glibenclamide are widely available sulfonylureas; gliclazide is associated with fewer hypoglycaemic episodes. Sulfonylureas should not be used in ketosis, lactation or porphyria.Start gliclazide at 40 mg daily; increase weekly up to 160 mg/day with breakfast or, if needed and tolerated, increase to a maximum of 160 mg twice daily with meals.Glibenclamide is initiated at 2.5 mg daily with breakfast and increased by 2.5 mg each week, as needed and tolerated, to a maximum of 15 mg daily.
Endocrine system
Published in Brian J Pollard, Gareth Kitchen, Handbook of Clinical Anaesthesia, 2017
Brian J Pollard, Gareth Kitchen
Sulphonylureas (e.g. gliclazide) increase pancreatic β-cell sensitivity to glucose thereby enhancing insulin release. Long-acting drugs (e.g. chlorpropamide) may exacerbate hypoglycaemia during fasting and are now rarely used.
Protecting Pancreatic β-cells from Metabolic Insults
Published in Christophe Wiart, Medicinal Plants in Asia for Metabolic Syndrome, 2017
Ethanol extract of leaves of Ipomoea batatas (L.) Lam. given as 3% part of diet given to KK-Ay mice for 5 weeks lowered glycemia from 418.3 to 339.3 mg/dL without changing plasma insulin.393 Body weight and food intake were not changed compared with untreated diabetic mice.393 The extract in vitro increased the secretion of glucagon-like peptide-1 from a murine enteroendocrine cell line.393 From this extract, 3,4,5 tricaffeoylquinic acid evoked an increased glucagon-like peptide-1 secretion from about 40 pM to 650 pM in vitro.393 The extract given at a single oral dose of 2 g/kg, 30 minutes before intraperitoneal glucose loading in Sprague–Dawley rats lowered 15 minutes peak glycemia by about 20%, increased 15 minutes insulin secretion and increased plasma glucagon-like peptide-1.393 In Sprague–Dawley rats, a single oral administration of gliclazide at a dose of 30 mg/kg provoked a quick and prolonged hypoglycemia and increased insulinemia whereby the extract given orally at a dose of 2 g/kg had no hypoglycemic effect nor insulinotropic effects.393 The insulinotropic gut hormone glucagon-like peptide-1 is released from small intestine endocrine L cells during digestion of mixed meals.394 This hormone bind to its G protein-coupled receptors on β-cells to promote glucose-induced secretion of insulin by activating adenylate cyclase and increasing cyclic adenosine monophosphate, activating cyclic adenosine monophosphate-regulated guanine nucleotide exchange factor II leading to altered ion channel activity, elevation of cytoplasmic calcium contents and exocytosis of insulin-containing vesicles.202 The insulinotropic gut hormone glucagon-like peptide-1 also suppresses glucagon secretion395 inhibits appetite and food intake,396 and ameliorates pancreatic β-cell dysfunction.397 glucagon-like peptide-1 secretion is lower in type 2 diabetic patients compared with healthy individuals.398 The insulinotropic gut hormone glucagon-like peptide-1 activity is decreased in type 2 diabetic patients398 and could be a strategy to prevent β-cell degeneration in metabolic syndrome. It should be noted that 3,4,5-tricaffeoylquinic acid inhibited rat intestinal maltase, rat intestinal sucrose and human saliva α-amylase with IC50 values of 24 µM (acarbose: 0.4 µM), 574 µM (acarbose: 1.2 µM) and 634 µM, respectively,399 contributing to the hypoglycemic activity of Ipomoea batatas (L.) Lam. in KK-Ay mice. Note that chlorogenic acid and 3,5-dicaffeoylquinic acid which are not uncommon in members of the family Solanaceae, Lamiaceae and Asteraceae stimulate glucagon-like peptide-1 secretion in rodents.400
All-cause and cardiovascular mortality associated with sulphonylurea and metformin therapy in type 2 diabetes
Published in Endocrine Research, 2018
Sorin Ioacara, Cristian Guja, Aura Reghina, Sorina Martin, Anca Sirbu, Simona Fica
Prescription time and dose was accounted for MET, gliclazide, glipizide, gliquidone, glimepiride, and glibenclamide, as time-dependent variables. Exposure during follow-up was calculated in a time-dependent manner separately for MET monotherapy, SU monotherapy, SU added to MET, and MET added to SU. SU added to MET as used in results means combined treatment with SU and MET in a patient with MET monotherapy at screening (and baseline), and likewise for MET added to SU. Combined therapy status was captured in a time-dependent manner, with daily updates of the system. SU replacing MET was used in results for designating patients on SU monotherapy with initial screening allocation to MET group. A sensitivity analysis was done including the above mentioned subclasses of SU. Defined daily dose expresses the average dose of a specific drug as used in the routine clinical practice.11 There was a high heterogeneity of dose exposure expressed in grams, as clearly 1 g of MET cannot be directly compared with 1 g of the available SU. Therefore, individual dose registrations were divided by the corresponding defined daily dose as recommended by the WHO.11 The defined daily dose for gliclazide was 60 mg, resulting in a value of 2 if the patient took a total daily dose of 120 mg. Cumulative dose should be interpreted as cumulative numbers of defined daily doses, throughout the study. Each SU subtype contributed to cumulative dose accretion only when SU were evaluated altogether; otherwise they contributed only to their respective subclass. Cumulative time and dose were used as risk factors for the primary end-point. Direct exposure measurement was not available after December 31, 2008, so last observation was carried forward until the end-point or censor. This was accepted as a tradeoff for some exposure misclassification against reduction in reverse causality.
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
In a systematic review and meta-analysis of randomized controlled trials comparing the safety and efficacy of gliclazide to other oral glucose-lowering agents, the proportion of non-severe hypoglycemic events in gliclazide users (2.2%) was similar to that in the comparator group (1.8%) and only one out of 2,387 gliclazide users had a severe hypoglycemic event, whilst also using insulin [77].
Evaluating gliclazide for the treatment of type 2 diabetes mellitus
Published in Expert Opinion on Pharmacotherapy, 2022
Brian Tomlinson, Yan-Hong Li, Paul Chan
This review is based on the published literature related to gliclazide, identified by searching PubMed for articles in English from the start of the database up to 30 April 2022. It focuses on the pharmacokinetics, clinical pharmacology and the role of the modified release (MR) formulation of gliclazide in the treatment of T2D.