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Exploring the mechanism of endothelial involvement in acidosis-induced vasodilatation of aortic tissues from normal and diabetic rats

Yeo JL, Tan BT, Achike FI

Eur J Pharmacol, 2010 Sep 10;642(1-3):99-106.
PMID: 20553918 DOI: 10.1016/j.ejphar.2010.05.040

Acidosis modulates physiologic and pathophysiologic processes but the mechanism of acidotic vasodilatation remains unclear. We therefore explored this in aortic rings from normal and streptozotocin-induced diabetic Sprague-Dawley rats. Phenylephrine (PE)-induced contraction in endothelium-intact and -denuded rings were recorded under normal and acidotic pH with or without drug probes. Acidosis exerted a relaxant effect in endothelium-intact and -denuded euglycaemic and diabetic tissues. l-NAME or methylene blue partially inhibited acidotic relaxation in these endothelium-intact but not the -denuded tissues, with greater inhibition in the diabetic tissues, indicating that acidosis induces relaxation by endothelium-dependent and -independent mechanisms, the former being EDNO-cGMP mediated. Indomethacin had no effect on the tissues, indicating that cyclooxygenase products are neither involved in acidosis-induced vasodilatation nor in the modulation of phenylephrine-contraction. In euglycaemic tissues under normal pH, no K(+) channel blocker altered phenylephrine-contraction, but all (except glibenclamide) enhanced diabetic tissue contraction, indicating that normally, these channels (K(ir), K(V), BK(Ca), K(ATP)) do not modulate phenylephrine-contraction, but they (except K(ATP)) are expressed in diabetes where they attenuate phenylephine-induced contraction and modulate acidosis. Only the K(ir) channel modulates acidotic relaxation in euglycaemic tissues. Only tetraethylammonium and iberiotoxin enhanced phenylephrine-induced contraction in endothelium-denuded diabetic tissues indicating that BK(Ca) attenuates phenylephrine-contraction and that acidotic relaxation in this condition is modulated by a tetraethylammonium-sensitive mechanism. In conclusion, acidosis causes vasodilatation in normal and diabetic tissues via endothelium-dependent and -independent mechanisms differentially modulated by a combination of a NO-cGMP process and K(+) channels, some of which are dormant in the normal state but activated in diabetes mellitus.

Matched MeSH terms: Glyburide/pharmacology
Insulinotropic Activity of Standardized Methanolic Extracts of Ficus deltoidea from Seven Varieties

Yahaya N, Mohd Dom NS, Adam Z, Hamid M

Evid Based Complement Alternat Med, 2018;2018:3769874.
PMID: 30046337 DOI: 10.1155/2018/3769874

Ficus deltoidea is a traditional medicinal plant that has been proven to show antidiabetic effects. This study focus is to assess the insulin secretion activity of Ficus deltoidea standardized methanolic extracts from seven independent varieties and mechanisms that underlie the insulin secretion action of the extracts. The cytotoxicity of Ficus deltoidea extracts was tested using viability assay. The insulin secretion assay was carried out by treating clonal BRIN BD11 cell line with standardized methanolic Ficus deltoidea extracts or glybenclamide. The clonal BRIN BD11 cell was also treated with insulin agonist and antagonist to elucidate the insulin secretion mechanism. Only the viability percentage for Ficus deltoidea var. kunstleri and intermedia was identified to be toxic at 500 and 1000 μg/ml (P<0.001). The insulin secretion for Ficus deltoidea var. deltoidea, angustifolia, and motleyana was dose-dependent; further evaluation suggested that Ficus deltoidea var. trengganuensis was involved in KATP-independent pathway. This study suggests that standardized methanolic extracts of Ficus deltoidea varieties have an insulinotropic effect on clonal BRIN BD11 cell line and can be utilized as a modern candidate of antidiabetic agents targeting the escalation for insulin secretion from pancreatic beta cells.

Matched MeSH terms: Glyburide
Efficacy and safety of single versus multiple daily doses of glibenclamide in type 2 diabetes mellitus

Wan Mohamad WB, Tun Fizi A, Ismail RB, Mafauzy M

Diabetes Res Clin Pract, 2000 Aug;49(2-3):93-9.
PMID: 10963819 DOI: 10.1016/s0168-8227(00)00138-8

Although long acting, glibenclamide is frequently given in split doses for type 2 diabetes mellitus. This may discourage compliance. It is thus appropriate to consider dosing it less frequently. We therefore studied glibenclamide effects when used once daily and when used in split doses. Our objective was to assess the feasibility of using once daily dosing as a regimen of choice. We measured plasma glucose, insulin, glibenclamide, lipids, HbAl and body mass index associated with the regimens. We also compared the number of hypoglycemic episodes occurring with them. Thirty type 2 diabetics on multiple daily glibenclamide were enrolled. Their regimens were changed over to once daily. Blood for glucose, insulin, lipids, HbAl and glibenclamide and body weight measurements were determined before and after the crossover period. We found no major difference in the sugar and insulin profiles with the two regimens. Fasting total cholesterol and triglyceride were also similar and so were plasma glibenclamide. The HbAl levels and body mass index and number of minor and major hypoglycemic episodes and hospital admissions for hypoglycemia also did not differ. We conclude that single daily dosing of glibenclamide was equivalent to multiple daily dose regimens. It can be used to an advantage to improve patient's compliance.

Matched MeSH terms: Glyburide/adverse effects; Glyburide/blood; Glyburide/therapeutic use*
Fulltext Rhinacanthus nasutus Improves the Levels of Liver Carbohydrate, Protein, Glycogen, and Liver Markers in Streptozotocin-Induced Diabetic Rats

Visweswara Rao P, Madhavi K, Dhananjaya Naidu M, Gan SH

Evid Based Complement Alternat Med, 2013;2013:102901.
PMID: 24204387 DOI: 10.1155/2013/102901

The present study was designed to investigate the total carbohydrate, total protein, and glycogen levels in the liver and to measure functional liver markers such as aspartate aminotransferase (AST) and alanine aminotransferase (ALT) in streptozotocin-(STZ-) induced diabetic rats after treatment with methanolic extract of Rhinacanthus nasutus (R. nasutus). The methanolic extract of R. nasutus was orally administered at 200 mg/kg/day while glibenclamide was administered at 50 mg/kg/day. All animals were treated for 30 days before being sacrificed. The amounts of carbohydrate, glycogen, proteins, and liver markers (AST and ALT) were measured in the liver tissue of the experimental animals. The levels of carbohydrate, glycogen, and proteins were significantly reduced in the diabetic rats but were augmented considerably after 30 days of R. nasutus treatment. The elevated AST and ALT levels in diabetic rats showed a significant decline after treatment with R. nasutus for 30 days. These results show that the administration of R. nasutus ameliorates the altered levels of carbohydrate, glycogen, proteins, and AST and ALT observed in diabetic rats and indicate that R. nasutus restores overall metabolism and liver function in experimental diabetic rats. In conclusion, the outcomes of the present study support the traditional belief that R. nasutus could ameliorate the diabetic state.

Matched MeSH terms: Glyburide
Fulltext Rhinacanthus nasutus Ameliorates Cytosolic and Mitochondrial Enzyme Levels in Streptozotocin-Induced Diabetic Rats

Visweswara Rao P, Madhavi K, Dhananjaya Naidu M, Gan SH

Evid Based Complement Alternat Med, 2013;2013:486047.
PMID: 23662138 DOI: 10.1155/2013/486047

The present study was conducted to evaluate the therapeutic efficacy of Rhinacanthus nasutus (R. nasutus) on mitochondrial and cytosolic enzymes in streptozotocin-induced diabetic rats. The rats were divided into five groups with 6 rats in each group. The methanolic extract of R. nasutus was orally administered at a dose of 200 mg/kg/day, and glibenclamide was administered at a dose of 50 mg/kg/day. All animals were treated for 30 days and were sacrificed. The activities of both intra- and extramitochondrial enzymes including glucose-6-phosphate dehydrogenase (G6PDH), succinate dehydrogenase (SDH), glutamate dehydrogenase (GDH), and lactate dehydrogenase (LDH) were measured in the livers of the animals. The levels of G6PDH, SDH, and GDH were significantly reduced in the diabetic rats but were significantly increased after 30 days of R. nasutus treatment. The increased LDH level in diabetic rats exhibited a significant reduction after treatment with R. nasutus. These results indicate that the administration of R. nasutus altered the activities of oxidative enzymes in a positive manner, indicating that R. nasutus improves mitochondrial energy production. Our data suggest that R. nasutus should be further explored for its role in the treatment of diabetes mellitus.

Matched MeSH terms: Glyburide
Effect of acidosis on the mechanism(s) of insulin-induced vasorelaxation in normal Wistar-Kyoto (WKY) rat aorta

Subramaniam G, Achike FI, Mustafa MR

Regul. Pept., 2009 Jun 5;155(1-3):70-5.
PMID: 19362578 DOI: 10.1016/j.regpep.2009.04.008

The effect of acidosis on insulin-induced relaxation was studied in thoracic aortic rings (from Wistar-Kyoto (WKY) rats) with (+ED) or without (-ED) endothelium. The rings were mounted in normal (pH 7.4) or acidotic (pH 7.2) Krebs solution for isometric tension recording. Phenylephrine (PE, 3.0 microM)-contracted tissues were exposed to insulin in the presence or absence of various inhibitors. Insulin exerted similar concentration-dependent relaxation of +ED tissues in normal and acidotic pH. Endothelium denudation, significantly (p<0.05) reduced insulin effect in normal, but not acidotic pH. Under normal pH, treatment with L-NAME or methylene blue significantly (p<0.05) reduced insulin responses in the +ED (but not the -ED) tissues. The insulin effect was also significantly (p<0.05) inhibited by tetraethylammonium (TEA; BK(Ca) blocker), 4-Aminopyridine (4-AP; K(V) channel blocker), combined treatments (L-NAME+4-AP+TEA, in +ED tissues) or (4-AP+TEA, in -ED tissues). In either +ED or -ED tissues, indomethacin (cyclo-oxygenase inhibitor), glibenclamide (K(ATP) channel blocker), barium chloride (K(ir) channel blocker) or Ouabain (a Na(+)/K(+)-ATPase inhibitor) had no effect. Except for methylene blue (effect on +ED tissues), none of the drug treatments inhibited insulin vasodilator effect in acidosis (+ED or -ED tissues). These data indicate that insulin exerts an endothelium-dependent and -independent vasodilatation in rat aorta which in normal pH is mediated via BK(Ca) and K(v) channels, including the EDNO-cGMP cascade. Acidosis abolishes the endothelium-dependent relaxation mechanism unraveling a novel mechanism that is as efficacious and is cGMP-, but not EDNO-, BK(Ca)- or K(v)-mediated.

Matched MeSH terms: Glyburide/pharmacology
Fulltext Polymethoxyflavones fromNicotiana plumbaginifolia(Solanaceae) Exert Antinociceptive and Neuropharmacological Effects in Mice

Shajib MS, Rashid RB, Ming LC, Islam S, Sarker MMR, Nahar L, et al.

Front Pharmacol, 2018;9:85.
PMID: 29515437 DOI: 10.3389/fphar.2018.00085

Polymethoxylavones (PMFs) are known to exhibit significant anti-inflammatory and neuroprotective properties.Nicotiana plumbaginifolia, an annual Bangladeshi herb, is rich in polymethoxyflavones that possess significant analgesic and anxiolytic activities. The present study aimed to determine the antinociceptive and neuropharmacological activities of polyoxygenated flavonoids namely- 3,3',5,6,7,8-hexamethoxy-4',5'-methylenedioxyflavone (1), 3,3',4',5',5,6,7,8-octamethoxyflavone (exoticin) (2), 6,7,4',5'-dimethylenedioxy-3,5,3'-trimethoxyflavone (3), and 3,3',4',5,5',8-hexamethoxy-6,7-methylenedioxyflavone (4), isolated and identified fromN. plumbaginifolia. Antinociceptive activity was assessed using the acetic-acid induced writhing, hot plate, tail immersion, formalin and carrageenan-induced paw edema tests, whereas neuropharmacological effects were evaluated in the hole cross, open field and elevated plus maze test. Oral treatment of compounds1,3, and4(12.5-25 mg/kg b.w.) exhibited dose-dependent and significant (p< 0.01) antinociceptive activity in the acetic-acid, formalin, carrageenan, and thermal (hot plate)-induced pain models. The association of ATP-sensitive K+channel and opioid systems in their antinociceptive effect was obvious from the antagonist effect of glibenclamide and naloxone, respectively. These findings suggested central and peripheral antinociceptive activities of the compounds. Compound1,3, and4(12.5 mg/kg b.w.) demonstrated significant (p< 0.05) anxiolytic-like activity in the elevated plus-maze test, while the involvement of GABAAreceptor in the action of compound3and4was evident from the reversal effects of flumazenil. In addition, compounds1and4(12.5-25 mg/kg b.w) exhibited anxiolytic activity without altering the locomotor responses. The present study suggested that the polymethoxyflavones (1-4) fromN. Plumbaginifoliacould be considered as suitable candidates for the development of analgesic and anxiolytic agents.

Matched MeSH terms: Glyburide
Fulltext Glibenclamide induced chronic cholestasis simulating primary biliary cirrhosis: a case report

Ramanathan M, Wahinuddin S, Kew ST

Med J Malaysia, 1996 Mar;51(1):140-3.
PMID: 10967995

A 43-year-old lady with long standing non-insulin dependent diabetes mellitus on glibenclamide presented with cholestatic liver disease. Initially she was thought to have developed primary biliary cirrhosis (PBC). When she made a spontaneous recovery following the withdrawal of glibenclamide, it became obvious that the patient had been suffering from drug-induced chronic cholestasis (DICC). The subtle differences between PBC and DICC are highlighted.

Matched MeSH terms: Glyburide/adverse effects*
Fulltext Possible Participation of Ionotropic Glutamate Receptors and l-Arginine-Nitric Oxide-Cyclic Guanosine Monophosphate-ATP-Sensitive K+ Channel Pathway in the Antinociceptive Activity of Cardamonin in Acute Pain Animal Models

Pui Ping C, Akhtar MN, Israf DA, Perimal EK, Sulaiman MR

Molecules, 2020 Nov 18;25(22).
PMID: 33217904 DOI: 10.3390/molecules25225385

The perception of pain caused by inflammation serves as a warning sign to avoid further injury. The generation and transmission of pain impulses involves various pathways and receptors. Cardamonin isolated from Boesenbergia rotunda (L.) Mansf. has been reported to exert antinociceptive effects in thermal and mechanical pain models; however, the precise mechanism has yet to be examined. The present study investigated the possible mechanisms involved in the antinociceptive activity of cardamonin on protein kinase C, N-methyl-d-aspartate (NMDA) and non-NMDA glutamate receptors, l-arginine/cyclic guanosine monophosphate (cGMP) mechanism, as well as the ATP-sensitive potassium (K+) channel. Cardamonin was administered to the animals intra-peritoneally. Present findings showed that cardamonin significantly inhibited pain elicited by intraplantar injection of phorbol 12-myristate 13-acetate (PMA, a protein kinase C activator) with calculated mean ED50 of 2.0 mg/kg (0.9-4.5 mg/kg). The study presented that pre-treatment with MK-801 (NMDA receptor antagonist) and NBQX (non-NMDA receptor antagonist) significantly modulates the antinociceptive activity of cardamonin at 3 mg/kg when tested with glutamate-induced paw licking test. Pre-treatment with l-arginine (a nitric oxide precursor), ODQ (selective inhibitor of soluble guanylyl cyclase) and glibenclamide (ATP-sensitive K+ channel inhibitor) significantly enhanced the antinociception produced by cardamonin. In conclusion, the present findings showed that the antinociceptive activity of cardamonin might involve the modulation of PKC activity, NMDA and non-NMDA glutamate receptors, l-arginine/nitric oxide/cGMP pathway and ATP-sensitive K+ channel.

Matched MeSH terms: Glyburide
Momordica charantia for type 2 diabetes mellitus

Ooi CP, Yassin Z, Hamid TA

Cochrane Database Syst Rev, 2010.
PMID: 20166099 DOI: 10.1002/14651858.CD007845.pub2

Background: Momordica charantia is not only a nutritious vegetable, but is also used in traditional medical practices to treat type 2 diabetes mellitus. Experimental studies with animals and humans suggested that the vegetable has a possible role in glycaemic control.

Objectives: To assess the effects of mormodica charantia for type 2 diabetes mellitus.

Search strategy: Several electronic databases were searched, among these The Cochrane Library (issue 4, 2009), MEDLINE, EMBASE, CINAHL, SIGLE and LILACS (all up to November 2009), combined with handsearches. No language restriction was used.

Selection criteria: Randomized controlled trials that compared momordica charantia with a placebo or a control intervention with or without pharmacological or non-pharmacological interventions were included.

Data collection and analysis: Two authors independently extracted the data. Risk of bias of trials was evaluated using the parameters of randomization, allocation concealment, blinding, completeness of outcome data, selective reporting and other potential sources of bias. A meta-analysis was not performed given the quality of data and the variability of preparations of momordica charantia used in interventions (no similar preparation was tested twice).

Main results: Three randomised controlled trials with up to three months duration and investigating 350 participants met the inclusion criteria. Risk of bias of these trials (only one study was published as a full peer-reviewed publication) was generally high. Two RCTs compared the effect of preparations from different parts of the momordica charantia plants and placebo on the glycemic control in type 2 diabetes mellitus. There was no statistically significant difference compared to placebo. The effects of preparation from the leaves of the plant and glibenclamide were comparable in the third trial. No serious adverse effects were reported in all the trials. There were no documentations of death from any cause, morbidity, (health-related) quality of life and costs.

Authors' conclusions: There is insufficient evidence to recommend momordica charantia for type 2 diabetes mellitus. Further studies are therefore required to address the issues of standardization and the quality control of preparations. For medical nutritional therapy, further observational trials evaluating the effects of momordica charantia are needed before RCTs are established to guide any recommendations in clinical practice.

Matched MeSH terms: Glyburide/therapeutic use
Momordica charantia for type 2 diabetes mellitus

Ooi CP, Yassin Z, Hamid TA

Cochrane Database Syst Rev, 2012 Aug 15.
PMID: 22895968 DOI: 10.1002/14651858.CD007845.pub3

BACKGROUND: Momordica charantia (bitter gourd) is not only a nutritious vegetable but it is also used in traditional medical practices to treat type 2 diabetes mellitus. Experimental studies with animals and humans suggested that the vegetable has a possible role in glycaemic control.
OBJECTIVES: To assess the effects of mormodica charantia for type 2 diabetes mellitus.
SEARCH METHODS: Several electronic databases were searched, among these were The Cochrane Library (Issue 1, 2012), MEDLINE, EMBASE, CINAHL, SIGLE and LILACS (all up to February 2012), combined with handsearches. No language restriction was used.
SELECTION CRITERIA: We included randomised controlled trials (RCTs) that compared momordica charantia with placebo or a control intervention, with or without pharmacological or non-pharmacological interventions.
DATA COLLECTION AND ANALYSIS: Two authors independently extracted data. Risk of bias of the trials was evaluated using the parameters of randomisation, allocation concealment, blinding, completeness of outcome data, selective reporting and other potential sources of bias. A meta-analysis was not performed given the quality of data and the variability of preparations of momordica charantia used in the interventions (no similar preparation was tested twice).
MAIN RESULTS: Four randomised controlled trials with up to three months duration and investigating 479 participants met the inclusion criteria. Risk of bias of these trials (only two studies were published as a full peer-reviewed publication) was generally high. Two RCTs compared the effects of preparations from different parts of the momordica charantia plant with placebo on glycaemic control in type 2 diabetes mellitus. There was no statistically significant difference in the glycaemic control with momordica charantia preparations compared to placebo. When momordica charantia was compared to metformin or glibenclamide, there was also no significant change in reliable parameters of glycaemic control. No serious adverse effects were reported in any trial. No trial investigated death from any cause, morbidity, health-related quality of life or costs.
AUTHORS' CONCLUSIONS: There is insufficient evidence on the effects of momordica charantia for type 2 diabetes mellitus. Further studies are therefore required to address the issues of standardization and the quality control of preparations. For medical nutritional therapy, further observational trials evaluating the effects of momordica charantia are needed before RCTs are established to guide any recommendations in clinical practice.

Matched MeSH terms: Glyburide/therapeutic use
The effect of nitrazepam on depression and curiosity in behavioral tests in mice: The role of potassium channels

Nikoui V, Ostadhadi S, Azhand P, Zolfaghari S, Amiri S, Foroohandeh M, et al.

Eur J Pharmacol, 2016 Nov 15;791:369-376.
PMID: 27615446 DOI: 10.1016/j.ejphar.2016.09.017

Evidence show that gamma-aminobutyric acid (GABA) receptors are involved in depression, so the aim of this study was to investigate the effect of nitrazepam as agonist of GABAA receptors on depression and curiosity in male mice and the role of potassium channel in antidepressant-like response. For this purpose, we studied the antidepressant-like properties of fluoxetine, nitrazepam, glibenclamide, and cromakalim by both forced swimming test (FST) and tail suspension test (TST). Animals were injected by various doses of nitrazepam (0.05, 0.1, and 0.5mg/kg). Nitrazepam at dose of 0.5mg/kg significantly decreased the immobility time compared to control group in both FST and TST. Fluoxetine also showed such a response. Co-administration of nitrazepam (0.05mg/kg) with glibenclamide in TST (1mg/kg) and in FST (0.3, 1mg/kg) also showed antidepressant-like response. Beside, cromakalim (0.1mg/kg) could reverse the antidepressant-like effect of nitrazepam (0.5mg/kg) in both FST and TST, while cromakalim and glibenclamide alone could not change the immobility time compared to control group (P>0.05). The hole-board test revealed that nitrazepam at doses of 0.5 and 0.1mg/kg could increase the activity of the animal's head-dipping and boost the curiosity and exploration behavior of mice. The results of this study revealed that nitrazepam may possess antidepressant-like properties and this effect is dependent to potassium channels in both FST and TST.

Matched MeSH terms: Glyburide/pharmacology
Fulltext Edible Bird's Nest Protects Against Hyperglycemia-Induced Oxidative Stress and Endothelial Dysfunction

Murugan DD, Md Zain Z, Choy KW, Zamakshshari NH, Choong MJ, Lim YM, et al.

Front Pharmacol, 2019;10:1624.
PMID: 32116666 DOI: 10.3389/fphar.2019.01624

Increased oxidative stress by hyperglycemia is a major cause of vascular complications in diabetes. Bird's nest, which is made from the saliva of swiftlets has both medicinal and nutritional values dated back to ancient China. However, its role in improving endothelial dysfunction due to diabetes is yet to be elucidated. The present study examined the protective effect and mechanism of action of the aqueous extract of hydrolyzed edible bird nest (HBN) on endothelium in models of diabetes, in vitro and in vivo. Male db/m+ and db/db mice were orally administered with or without HBN and glibenclamide for 28 days, followed by vascular reactivity studies in mouse aortas. Human umbilical vein endothelial cells (HUVECs) and isolated mouse aorta from C57BL/6J were treated with high glucose (HG), HBN, sialic acid (SA), glibenclamide, and apocynin, respectively. The effects of HBN on reactive oxygen species (ROS) production and nitric oxide (NO) bioavailability were assessed by Western blot, 2',7'-dichlorofluorescin-diacetate (DCF-DA), and 4-amino-5-methylamino-2',7' difluorofluorescein (DAF-FM DA) in HUVECs, isolated mouse aorta, and db/db diabetic mice. HBN significantly reversed the endothelial dysfunction in diabetic mice and isolated mouse aorta. HBN normalized ROS over-production of NOX2 and nitrotyrosine, reversed the reduction of anti-oxidant marker, SOD-1 as well as restored NO bioavailability in both HUVECs challenged with HG and in db/db diabetic mice. Similarly, HG-induced elevation of oxidative stress in HUVECs were reversed by SA, glibenclamide, and apocynin. This attests that HBN restores endothelial function and protects endothelial cells against oxidative damage induced by HG in HUVECs, isolated mouse aorta, and db/db diabetic mice via modulating ROS mechanism, which subsequently increases NO bioavailability. This result demonstrates the potential role of HBN in preserving endothelial function and management of micro- or macrovascular complications in diabetes.

Matched MeSH terms: Glyburide
Fulltext Possible participation of nitric oxide/cyclic guanosine monophosphate/protein kinase C/ATP-sensitive K(+) channels pathway in the systemic antinociception of flavokawin B

Mohamad AS, Akhtar MN, Khalivulla SI, Perimal EK, Khalid MH, Ong HM, et al.

Basic Clin Pharmacol Toxicol, 2011 Jun;108(6):400-5.
PMID: 21214864 DOI: 10.1111/j.1742-7843.2010.00670.x

The possible mechanisms of action in the antinociceptive activity induced by systemic administration (intraperitoneal, i.p.) of flavokawin B (FKB) were analysed using chemical models of nociception in mice. It was demonstrated that i.p. administration of FKB to the mice at 0.3, 1.0, 3.0 and 10 mg/kg produced significant dose-related reduction in the number of abdominal constrictions. The antinociception induced by FKB in the acetic acid test was significantly attenuated by i.p. pre-treatment of mice with L-arginine, the substrate for nitric oxide synthase or glibenclamide, the ATP-sensitive K(+) channel inhibitor, but was enhanced by methylene blue, the non-specific guanylyl cyclase inhibitor. FKB also produced dose-dependent inhibition of licking response caused by intraplantar injection of phorbol 12-myristate 13-acetate, a protein kinase C activator (PKC). Together, these data indicate that the NO/cyclic guanosine monophosphate/PKC/ATP-sensitive K(+) channel pathway possibly participated in the antinociceptive action induced by FKB.

Matched MeSH terms: Glyburide/pharmacology
Fulltext Metabolic and immunologic alterations of ginger rhizome among streptozotocin-nicotinamide induced diabetic rats

Mansooreh, Sadat Mojani, Asmah Rahmat, Rajesh, Ramasamy, Vahid, Hosseinpour Sarmadi, Pratheep, Sandrasaigaran, Shalini, Vellasamy, et al.

Malays J Nutr, 2016;22(3):421-432.
MyJurnal

Introduction: This study was conducted to determine immunological and metabolic effects of different concentrations of ginger rhizome (Zingiber officinale Roscoe) in streptozotocin (STZ)-nicotinamide (NA) induced diabetic rats.

Methods: Forty-eight fasted male Sprague-Dawley rats were induced diabetes using a single intraperitoneal injection of NA(110 mg/kg b.w.) and STZ (65 mg/kg b.w, 15 min after NA). Diabetic rats orally received either different concentrations (250, 500 and 750 mg/kg body weight) of ginger rhizome suspension or glibenclamide (10 mg/kg body weight) for 6 weeks. Two control diabetic and normal groups were gavaged with only distilled water as a vehicle.

Results: The results indicated that the lower concentrations of ginger modulated body weight, fasting blood glucose, level of triglyceride and tumor necrosis factor-a (TNF-a) (p

Matched MeSH terms: Glyburide
Repaglinide versus glibenclamide treatment of Type 2 diabetes during Ramadan fasting

Mafauzy M

Diabetes Res Clin Pract, 2002 Oct;58(1):45-53.
PMID: 12161056 DOI: 10.1016/s0168-8227(02)00104-3

This study compared treatment with a prandial glucose regulator (repaglinide) and a sulphonylurea (glibenclamide) in Muslim Type 2 diabetic patients who practice Ramadan fasting. Two hundred and thirty-five patients, previously treated with a sulphonylurea, were randomised to receive either repaglinide (n=116, preprandially three-times daily) or glibenclamide (n=119, preprandially once- or twice-daily) 6 weeks before Ramadan. During Ramadan, patients changed their eating pattern to two meals daily, and the daily dose of repaglinide was redistributed to two preprandial doses. After Ramadan, patients resumed their regular meal pattern and treatment dosage for 4 weeks. During Ramadan, a statistically significant reduction in mean serum fructosamine concentration from baseline was observed in the repaglinide group (-16.9+/-4.9 micromol/l, -3.8%, P<0.05) but not the glibenclamide group (-6.9+/-4.8 micromol/l, -0.8%). Difference in change in HbA(1c) from baseline was not statistically significant between groups. The number of hypoglycaemic events with midday blood glucose <4.5 mmol/l was significantly lower in the repaglinide group (2.8%) than the glibenclamide group (7.9%) (P=0.001). Apart from hypoglycaemia, both treatments were equally well tolerated. Type 2 diabetic Muslims using prandial repaglinide showed a trend towards better glycaemic control and had a lower frequency of hypoglycaemia than patients using glibenclamide during Ramadan.

Matched MeSH terms: Glyburide/adverse effects; Glyburide/therapeutic use*
Treatment Options for Patients with Type 2 Diabetes Mellitus during the Fasting Month of Ramadan

Loh HH, Kamaruddin NA

Ann Acad Med Singap, 2020 Jul;49(7):468-476.
PMID: 33000110

During Ramadan, Muslims fast from sunrise (Sahur) to sunset (Iftar) and are required to abstain from food and fluids, including oral and injectable medications. Patients with diabetes who fast during Ramadan are at risk of developing hyperglycemia with increased risk of ketoacidosis, hypoglycemia, dehydration and thrombosis. Pre-Ramadan education and preparation of a fasting patient are essential to reduce severe complications. This review paper summarizes studies to date on oral and injectable medications available for patients with type 2 diabetes during Ramadan fasting, as well as recommendations on management of these patients during Ramadan. Although there is limited data on the use of Metformin, Acarbose and Thiazolidinedione in Ramadan, they appear to be safe. Sulphonylurea, especially Glibenclamide, is associated with higher risk of hypoglycemia during Ramadan fasting, hence may need adjustment in dosing and timing. The incretin group and SGLT2 inhibitor use during Ramadan fasting is associated with low risk of hypoglycemia with no increased adverse events. Insulin regimes need to be individualized for patients who fast during Ramadan.

Matched MeSH terms: Glyburide
In vitro vascular effects produced by crude aqueous extract of green marine algae, Cladophora patentiramea (Mont.) Kützing, in aorta from normotensive rats

Lim YL, Mok SL

Med Princ Pract, 2010;19(4):260-8.
PMID: 20516701 DOI: 10.1159/000312711

To investigate the antihypertensive activity of aqueous extracts obtained from Malaysian coastal seaweeds and to determine the pharmacological mechanisms of the extracts on rat aorta in vitro.

Matched MeSH terms: Glyburide/pharmacology
Fulltext Glycaemic control and cost analysis when changing from gliclazide co-administered with metformin to pre-combined glibenclamide-metformin tablets in type 2 diabetes mellitus

Lim PC, Lim SL, Oiyammaal C

Med J Malaysia, 2012 Feb;67(1):21-4.
PMID: 22582544

Type-2 diabetes mellitus (T2DM) patients who were on gliclazide co-administered with metformin were changed to pre-combined glibenclamide-metformin tablets in the Endocrine Clinic, Penang Hospital. We conducted a retrospective study to evaluate the differences in glycaemic control and treatment cost following the change. Eighty patients (60% females) with a mean age of 55 years old were studied. Mean glycosylated haemoglobin (HbAlc) reduction was -0.92% (p<0.01) and -0.83% (p<0.01) after three and six months respectively. Patients with baseline HbA1c > or =8% had greater reduction in mean HbA1c (-1.36%) after six months. The treatment cost per month was reduced by 45% at 3 months (p<0.01)) and 44% at 6 months (p<0.01). The change to pre-combined glibenclamide-metformin tablets resulted in significant improvement in glycaemia and reduction in treatment cost.

Matched MeSH terms: Glyburide/administration & dosage*
Fulltext A comparison between the pregnancy outcome of women with gestation diabetes treated with glibenclamide and those treated with insulin

Lim JMH, Tayob Y, O'Brien PM, Shaw RW

Med J Malaysia, 1997 Dec;52(4):377-81.
PMID: 10968114

The pregnancy outcome of 33 women with gestational diabetes who were treated with glibenclamide and changed to insulin if glibenclamide failed, were compared with the pregnancy outcome of 21 women with gestational diabetes treated conventionally with insulin. The pregnancy outcome, with regard to the overall glycaemic control, rates of preterm labour, neonatal hypoglycaemia, fetal macrosomia, perinatal morbidity and mortality, were not statistically different between the two treatment groups. The limited number of women studied, and the non-random allocation of these women to each treatment group however, could have influenced these results. There were a few observed differences in the pregnancy outcome between the two treatment groups, which although were not statistically significant, caused some concern. In particular we noted an increased rate of fetal macrosomia in the glibenclamide treated group, which in theory could have been drug mediated.

Matched MeSH terms: Glyburide/therapeutic use*

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