DOCSLIB.ORG

Comparison of Gliclazide and Glibenclamide Treatment in Non-Insulin-Dependent Diabetes

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
Comparison of Gliclazide and Glibenclamide Treatment in Non-Insulin-Dependent Diabetes Tohoku J. exp. Med., 1983, 141, Suppl., 693-706 Comparison of Gliclazide and Glibenclamide Treatment in Non- Insulin-Dependent Diabetes SHIGEAKI BABA, SHOICHI NAKAGAWA,* KAZUO TAKEBE,•õ YOSHIO GOTO•ö, HIDENORI MAEZAWA•˜, RYOYU TAKEDA//, NOBUO SAKAMOTO•÷ and IWAO FUKUI// The Second Dept. of Internal Medicine, Kobe University, School of Medicine, Kobe 650, *The Second Dept. Of Internal Medicine, Hokkaido University, School of Medicine, Sapporo 060, •õ The Third Dept. of Internal Medicine, Hirosaki University, School of Medicine, Hirosaki 036, •öThe Third Dept. of Internal Medicine, Tohoku University, School of Medicine, Sendai 980, •˜The Third Dept. of Internal Medicine, Tokyo Medical and Dental University, School of Medicine, Tokyo 113, //The Second Dept. of Internal Medicine, Kanazawa University, School of Medicine, Kanazawa 920, •÷The Third Dept. of Internal Medicine, Nagoya University, School of Medicine, Nagoya 466, //Central Laboratory for Clinical Investigation, Kyoto Prefectural University of Medicine, Kyoto 602. BABA,S., NAKAGAWA,S., TAKEBE,K., GOTO,Y., MAEZAWA,H., TAKEBA,R., SAKAMOTO,N. and FUKUI, I. Comparison of Gliclazide and Glibenclamide Treatment in Non-Insulin-Dependent Diabetes. Tohoku J. exp. Med., 1983, 141, Suppl., 693-706 - Gliclazide has been reported to decrease platelet function and to inhibit the progression of diabetic retinopathy in addition to having a hypogly cemic effect. To confirm these effects we performed a double-blind randomized study using glibenclamide as a reference drug. Thirty-eight hospitals from eight university groups in Japan performed the study on type II diabetic subjects. Evaluation of blood glucose control, platelet adhesiveness, platelet aggregation and blood lipids over 24 weeks were assessed by the central committee. Two hundred and eighty-nine patients were enrolled in the study. Twelve were excluded and 277 were statistically analysed. Homogeneity between the two diabetic groups was demonstrated for background factors. Forty mg of gliclazide was comparable to 2.5mg of glibenclamide in the potency of hypoglycemic efficacy. Funduscopic aggravations were observed in a statistically smaller number of cases in the gliclazide group than in the glibenclamide group and in evaluation of serum lipids, the gliclazide group was also superior to the glibenclanide group. No significant differnce between the two groups was found in platelet adhesiveness and aggrega tion. Gliclazide is a useful drug in the therapy of diabetes mellitus. oral hypoglycemic drug ; glielazide ; glibenclamide ; diabetes mellitus ; randomized study 693 694 S. Baba et al. Gliclazide (SE-1702) is a new sulfonylurea hypoglycemic drug, developed by Laboratoires Servier in France. It shows a platelet adhesiveness and aggregation reducing activity in addition to hypoglycemic activity, in vivo and in vitro1-8). From these findings, we expect it to prevent the further advancement of diabetic retinopathy9-10). In order to assess the efficacy of gliclazide, a double-blind randomized study was conducted for the treatment of patients with type II diabetes mellitus, employing glibenclamide as an active control drug. This study was carried out in thirty-eight hospitals from 8 university groups in Japan. MATERIALS AND METHODS Test drugs. Gliclazide (S), 1-(3-azabicyclo •u3. 3.0•v oct-3-yl)-3-(p-tolylsulfonyl) urea was used as a test drug (Fig. 1). In order to assess the efficacy of the drug, we adopted glibenclamide (G) as an active control drug. Fig. 1. Bliclazide (SE-1702). Design of double-blind study. The subjects were type II diabetes mellitus patients with FBS over 130mg/100ml after diet therapy for one to two weeks, in the case of patients who had received no other medication before the trial, or in the case of patients transferred from other drugs, they were changed to the test drug on the first day of the study. The treatment lasted 24 weeks. We applied the variable dose schedule method in which dosage is adjusted according to the patient's response up to 4 tablets per day. Gliclazide and glibenclamide tablets contain 40mg and 2,5mg of active ingredient, respectively. Gliben clamide tablets bioequivalent to the commercial product were prepared. Body weight, blood glucose (FBS, blood glucose 2hours after meal), and platelet adhesiveness were examined 2 times before medication and 6 times in total each 4 week after medication. Serum lipids (total cholesterol, triglyceride, HDL-cholesterol) and platelet aggregation were examined 4 times before and after medication. Funduscopic examina tions were carried out before and after medication. Additionally, urine examination (sugar, protein, ketone body), hematological examination (WBC, RBC, Ht, Hb), liver and renal function test (GOT, GPT, Al-P, ƒÁ-GTP, total protein, BUN, creatinine), blood pressure, ECG, subjective symptoms, adverse effects, hypoglycemic symptoms, compliance with diet and exercise therapy, drinking and smoking were also observed. Criteria of blood glucose control by the committee. Blood glucose control evaluation at each observation time was made according to the classification ranging from excellent to poor shown in Table 1. Blood glucose control was judged the committee to be excellent in cases where 60% or more of the blood glucose evaluations were excellent after administra tion, good in cases where 60% or more of the blood glucose evaluations were good or excellent after administration, fair in cases where 60% or more of the blood glucose evaluations were fair, good or excellent after administration, and all other cases were considered as poor. Criteria for platelet adhesiveness control by the committee. Criteria for platelet adhesi veness at the time of observation are summarized. Cases where 80% or more of platelet adhesiveness evaluations were normal (platelet adhesiveness : 10.0-56.2%) after administra tion were considered good. Cases where 60% or more of platelet adhesiveness evaluations were normal after administration were considered fair, and cases where 59% or less of Comparison of Gliclazide and Glibenclamide 695 TABLE1. Criteria of blood glucosejudgement TABLE2. Criteria of serum lipid judegement (compared with the value before study) platelet adhesiveness evaluations were normal after administration were considered poor. Criteria of serum lipid evaluation by the committee. The average difference between the value for premedication and that for post-medication was calculated, and evaluated according to Table 2. RESULTS and DISCUSSION Diabetic patients taking part in the study Of 289 patients given the drugs, 3 subjects in the glibenclamide group were excluded due to a FBS of 78mg/dl on the first day of administration, a diagnosis of hepatoma 4 weeks after administration and death from heart disease 4days after administration, respectively. Two hundred and eightysix eligible cases, excluding the above 3 cases, were subjected to the safety assessment. Nine more cases were excluded due to difficulty in evaluating the efficacy- patients with a duration of administration of less than 8 weeks could not be considered equivalent to subjects of 24 weeks administration. But subjects who dropped out due to lack of effect, adverse effects or hypoglycemic symptoms were included. As a result, 277 eligible cases were subjected to the efficacyevaluation. Background of patients As shown in Table 3, there was a slight difference in the number of each sex between the groups. The gliclazide group had a higher percentage of males than 696 S. Baba et al. TABLE3. Background of patients Comparison of Gliclazide and Glibenclamide 697 U, Mann-Whitney U-test ; x2, x2 test. *** p <0.001 , ** p <0.01, * p <0.05, + p <0.10, NS, not significant. 698 S. Baba et al. the glibenclamide group (p <0.1). But, there were no significant differences in age, obesity index, duration of DM, premedication and control of DM before the study between the two groups. Hypertention as a complication was observed in more cases in the gliclazide group (p <0.05). But there were no significant differences in diabetic complications, hyperlipidemia or heart disease between the two groups. Patient's situation during the study Hospitalization, drinking, smoking, compliance with diet and exercise the- rapy, changes in body weight and number of tablets taken daily were examined (Table 4). Among them, only the number of tablets taken daily in the gliclazide group tended to be slightly higher than in the glibenclamide group (minimum and final p <0.01). Blood glucose Fasting and 2 hr blood glucose profiles during the study were markedly reduced in both groups. Two hour blood glucose is shown in Fig. 2. The results of the evaluation of blood glucose by the central committee are shown in Table 5. Eighteen percent of cases in the gliclazide group were judged as excellent, and 17% in the glibenclamide group. Forty-nine percent in the gliclazide group and 50% in the glibenclamide group were judged as good or excellent, and 71% in the gliclazide group and 76% in the glibenclamide group were judged as fair, good or excellent. Poor cases were 27% in the gliclazide group and 21% in the glibenclamide group. As a whole, there was no significant difference between the two groups. Platelet adhesivenessand aggregation Platelet adhesiveness levels decreased over 4-20 weeks after medication in both groups. There was no significant difference between the two groups. According to the evaluation of the central committee, 31% of cases in the gliclazide group were good, and 30% in the glibenclamide group. Forty-seven percent
Load more

Recommended publications
  • Environmental Risk Management for Pharmaceutical Compounds
    RISK MANAGEMENT AND REGULATORY ASPECTS Environmental risk managementfor pharmaceutical compounds Nick Voulvoulis1 imperial College London Introduction Pharmaceuticals are a highly variable group of organic compounds with the potential to cause harm to aquatic ecosystems and human health. Thousands of tones of pharmacologically active substances are used annually but surprisingly little is known about their ultimate fate in the environment (Jones et al., 2001). The data collected to date, rarely provide information on the processes that determine their environmental fate and although they receive considerable pharmacological and clinical testing during development, knowledge of their ecotoxicity is poor. One major concern is that antibiotics found in sewage effluent may cause increased resistance amongst natural bacterial populations (Willis, 2000). The debate over risks associated with chemicals in the environment represents more than just another disagreement in the scientific community. It has opened the door to a new way of thinking about the onset of uninherited diseases, the nature of scientific investigation, and the role of scientific knowledge in the policymaking process. Forexample, research evidence on endocrine disruption collected over the last few years has changed dramatically the way we think about chemical risks. In part, this change has also been attributed to the precautionary principle, as a new approach to environmental policy forged in Europe. The term "precautionary approach" declares an obligation to control the dangerous substances even before a definitive causal link had been established between the chemicals and health or environmental effects, and represents a radical departure from traditional approaches to risk assessment and particularly risk management, which includes an integration of the assessment, communication and mitigation of risks.
    [Show full text]
  • 19Th Expert Committee on the Selection and Use of Essential Medicines
    Expert Peer Review 2 19th Expert Committee on The Selection and Use of Essential Medicines April 8‐12 2013 Expert peer review on glibenclamide vs gliclazide, glipizide and glimepiride in the elderly. 1. Assessment of efficacy a. Have all relevant studies on efficacy been included No 1. Bollen S et al .Comparative efficacy and safety of oral diabetic medications for patients with Type 2 Diabetes AHRQ Publication No07 ‐ EHC010‐ EF July 2007 Comparative effectiveness review No. 8 A metanalysis done by these reviewers showed that there was no difference in the efficacy of Glibenclamide in reducing HbA1c as compared to Gliclazide, Glipizide and Glimepiride 2. Harrower AD. Comparison of diabetic control in type 2 (non‐insulin dependent) diabetic patients treated with different sulphonylureas. Curr Med Res Opin. 1985;9(10):676‐80. In this unblinded trial, Gliclazide was significantly better in reducing HbA1c than Glipizide 3. Schernthaner G, Grimaldi A, Di Mario U, Drzewoski J, Kempler P, Kvapil M, Novials A, Rottiers R, Rutten GE, Shaw KM.GUIDE study: double‐blind comparison of once‐daily gliclazide MR and glimepiride in type 2 diabetic patients. Eur J Clin Invest. 2004 Aug;34(8):535‐42. In this study once daily sustained release Gliclazide was shown to be as effective as Glimepiride in reducing HbA1c. b. Summarize the data on efficacy, in comparison to what is listed in EML where applicable (limit to 2 to 3 sentences) On metanalysis, Glibenclamide was not superior to Gliclazide, Glipizide and Glimepiride in reducing HbA1c. Gliclazide was significantly better in reducing HbA1c than Glipizide in 1 unblinded trial.
    [Show full text]
  • Marketing Authorisations Granted in December 2020
    Marketing authorisations granted in December 2020 PL Number Grant Date MA Holder Licensed Name(s) Active Ingredient Quantity Units Legal Status Territory PL 14251/0100 01/12/2020 MANX HEALTHCARE LIMITED COLCHICINE 500 MICROGRAMS TABLETS COLCHICINE 0.500 MILLIGRAMS POM UK PL 34424/0050 02/12/2020 KEY PHARMACEUTICALS LIMITED SPIRONOLACTONE 25MG FILM-COATED TABLETS SPIRONOLACTONE 25 MILLIGRAMS POM UK PL 34424/0051 02/12/2020 KEY PHARMACEUTICALS LIMITED SPIRONOLACTONE 50MG FILM-COATED TABLETS SPIRONOLACTONE 50 MILLIGRAMS POM UK PL 34424/0052 02/12/2020 KEY PHARMACEUTICALS LIMITED SPIRONOLACTONE 100MG FILM-COATED TABLETS SPIRONOLACTONE 100 MILLIGRAMS POM UK PL 36282/0021 03/12/2020 RIA GENERICS LIMITED COLCHICINE 500 MICROGRAM TABLETS COLCHICINE 500 MICROGRAMS POM UK PL 39352/0439 03/12/2020 KOSEI PHARMA UK LIMITED FROVATRIPTAN 2.5 MG FILM-COATED TABLETS FROVATRIPTAN SUCCINATE MONOHYDRATE 2.5 MILLIGRAMS POM UK PL 31750/0174 04/12/2020 SUN PHARMACEUTICAL INDUSTRIES EUROPE BV CETRORELIX SUN 0.25 MG SOLUTION FOR INJECTION IN PRE-FILLED SYRINGE CETRORELIX ACETATE 0.25 MILLIGRAMS PER MILLILITRE POM UK PL 34424/0054 04/12/2020 KEY PHARMACEUTICALS LIMITED ALIMEMAZINE TARTRATE 10MG FILM COATED TABLETS ALIMEMAZINE TARTRATE 10.00 MILLIGRAMS POM UK PL 17780/0858 07/12/2020 ZENTIVA PHARMA UK LIMITED FINGOLIMOD ZENTIVA 0.5 MG HARD CAPSULES FINGOLIMOD HYDROCHLORIDE 0.56 MILLIGRAMS POM UK PL 01502/0113 08/12/2020 HAMELN PHARMA LTD AMIODARONE HYDROCHLORIDE 20 MG/ML SOLUTION FOR INFUSION AMIODARONE HYDROCHLORIDE 20 MILLIGRAMS POM UK PL 16786/0006 08/12/2020
    [Show full text]
  • MRI Evidence That Glibenclamide Reduces Acute Lesion Expansion in a Rat Model of Spinal Cord Injury
    Spinal Cord (2013) 51, 823–827 OPEN & 2013 International Spinal Cord Society All rights reserved 1362-4393/13 www.nature.com/sc ORIGINAL ARTICLE MRI evidence that glibenclamide reduces acute lesion expansion in a rat model of spinal cord injury JM Simard1,2,3, PG Popovich4, O Tsymbalyuk1, J Caridi1, RP Gullapalli5, MJ Kilbourne6 and V Gerzanich1 Study design: Experimental, controlled, animal study. Objectives: To use non-invasive magnetic resonance imaging (MRI) to corroborate invasive studies showing progressive expansion of a hemorrhagic lesion during the early hours after spinal cord trauma and to assess the effect of glibenclamide, which blocks Sur1-Trpm4 channels implicated in post-traumatic capillary fragmentation, on lesion expansion. Setting: Baltimore. Methods: Adult female Long–Evans rats underwent unilateral impact trauma to the spinal cord at C7, which produced ipsilateral but not contralateral primary hemorrhage. In series 1 (six control rats and six administered glibenclamide), hemorrhagic lesion expansion was characterized using MRI at 1 and 24 h after trauma. In series 2, hemorrhagic lesion size was characterized on coronal tissue sections at 15 min (eight rats) and at 24 h after trauma (eight control rats and eight administered glibenclamide). Results: MRI (T2 hypodensity) showed that lesions expanded 2.3±0.33-fold (Po0.001) during the first 24 h in control rats, but only 1.2±0.07-fold (P40.05) in glibenclamide-treated rats. Measuring the areas of hemorrhagic contusion on tissue sections at the epicenter showed that lesions expanded 2.2±0.12-fold (Po0.001) during the first 24 h in control rats, but only 1.1±0.05-fold (P40.05) in glibenclamide-treated rats.
    [Show full text]
  • Gliclazide MR Versus Glyburide for Management of Type 2 Diabetes: a Review of the Clinical Effectiveness and Safety
    TITLE: Gliclazide MR versus Glyburide for Management of Type 2 Diabetes: A Review of the Clinical Effectiveness and Safety DATE: 03 March 2009 CONTEXT AND POLICY ISSUES: About 5% of the Canadian population has diabetes mellitus, an endocrine disorder that is characterized by hyperglycemia (high blood glucose) that results from defective insulin secretion, defective insulin action, or a combination of the two.1 Diabetes mellitus is further classified as type 1, type 2, or gestational diabetes. Type 2 diabetes accounts for the majority of diabetes cases and can be managed through lifestyle modification (e.g. diet and exercise), oral medications that lower blood glucose, and insulin.1 Canadian Diabetes Association Guidelines for the management of type 2 diabetes recommend the use of sulfonylureas (medications which increase the secretion of insulin from the pancreas to lower blood glucose) in individuals whose blood glucose is not adequately controlled with diet, exercise, and metformin, an oral medication that potentiates that the effects of insulin.1 There are a number of sulfonylureas available on the market in Canada, two of which are gliclazide and glyburide (also referred to as glibenclamide).1 Glyburide is administered orally at dosages of 5 mg to 20 mg daily.2 Depending on the dose, glyburide is administered once or twice daily.2 Gliclazide is available in a modified release (MR) preparation that allows the drug to be orally administered once daily at dosages of 30 mg to 120 mg.3 Gliclazide MR has a hydrophilic polymer matrix that
    [Show full text]
  • Prescribing Information 1. Generic Name Paracetamol and Mefenamic
    Not to be sold by retail without the prescription of a Registered Medical Practitioner Prescribing Information 1. Generic Name Paracetamol and Mefenamic Acid Suspension (Brand Name: MEFTAGESIC ®- P Suspension) Paracetamol: Box Warning About Its Liver Toxicity Taking more than daily dose may cause serious liver damage or allergic reactions (e.g., swelling of the face, mouth and throat, difficulty in breathing, itching or rash). The risk of liver injury primarily occurs when patient take multiple products containing paracetamol/acetaminophen at one time and exceed the current maximum dose of 4,000 mg within a 24-hour period. 2. Qualitative and Quantitative Composition Each 5 ml contains: Paracetamol IP ……………………………………..… 125 mg. Mefenamic Acid IP ………………………………..… 50 mg. Flavored Syrup Base…………………………………... q.s. Colour: Sunset Yellow FCF. 3. Dosage Form and Strength Dosage Form: Oral liquid (suspension). Dosage Strength: Paracetamol 125 mg with Mefenamic Acid 50 mg per 5 ml. 4. Clinical Particulars 4.1 Therapeutic Indication MEFTAGESIC-P Suspension is indicated in the treatment of fever. This medicine is also useful for the treatment of mild to moderate pain of varied etiologies. 4.2 Posology and Method of Administration For oral administration in children above 6 months of age. Recommended dosage of individual ingredients based on body weight. Paracetamol: 50-75 mg/kg daily in divided doses, or 10 to 15 mg/kg/dose every 4 to 6 hourly. Mefenamic Acid: 25 mg/kg daily in divided doses, or 4 to 6.5 mg/kg/dose every 8 hours. Recommended dosage of MEFTAGESIC-P Suspension based on age group. 6 months to 1 year: 5 ml to be administered three times daily.
    [Show full text]
  • Effects of Glibenclamide and Glimepiride Compared in Type II DM Patients in Accordance with Lipid Parameters, ESF and Glycated Haemoglobin
    British Journal of Applied Science & Technology 10(3): 1-10, 2015, Article no.BJAST.17537 ISSN: 2231-0843 SCIENCEDOMAIN international www.sciencedomain.org Effects of Glibenclamide and Glimepiride Compared in Type II DM Patients in Accordance with Lipid Parameters, ESF and Glycated Haemoglobin K. Chandra Mouli Krishna1, B. Sowmya2, Bandopadhyay Mamata3 and M. Prasad Naidu4* 1NRI Institute of Medical College, Sangivalasa, Visakhapatnam -531162, Andhra Pradesh, India. 2Kamala Nursing Home, Marripalem, Visakhapatnam - 530018, Andhra Pradesh, India. 3Department of Pharmacology, Maharaja Institute of Medical Sciences, Nellimarla, Vizinagaram - 535217, Andhra Pradesh, India. 4Department of Biochemistry, Narayana Medical College and Hospital, Nellore-524003, Andhra Pradesh, India. Authors’ contributions This work was carried out in collaboration between all authors. All authors read and approved the final manuscript. Article Information DOI: 10.9734/BJAST/2015/17537 Editor(s): (1) Gautam R. Ullal, Course Director Neuroscience and Foundations of Clinical Medicine, Medical University of Americas, West Indies. Reviewers: (1) Ayşenur Yeğin, Clinical Biochemistry, Antalya Research and Educational Hospital, Turkey. (2) Anonymous, The Third Hospital of Hebei Medical University, China. (3) Anonymous, MGM Medical College, Navi-Mumbai, India. Complete Peer review History: http://sciencedomain.org/review-history/9912 Received 17th March 2015 th Original Research Article Accepted 5 June 2015 Published 27th June 2015 ABSTRACT The population of Indian adults suffering from diabetes is expected to increase threefold, from 19.4 million in 1995 to 57.2 million in 2025. The objective of the study was to evaluate the efficacy and safety of antidiabetic drug and to find out their cardio protective action in patients with diabetes mellitus.
    [Show full text]
  • HPMC AS HG Amorphous Solid Dispersions: Dissolution Enhancement Using Hot Melt Extrusion Technology
    University of Mississippi eGrove Electronic Theses and Dissertations Graduate School 2019 Mefenamic Acid – HPMC AS HG Amorphous Solid Dispersions: Dissolution Enhancement Using Hot Melt Extrusion Technology Ashay Shukla University of Mississippi Follow this and additional works at: https://egrove.olemiss.edu/etd Part of the Statistics and Probability Commons Recommended Citation Shukla, Ashay, "Mefenamic Acid – HPMC AS HG Amorphous Solid Dispersions: Dissolution Enhancement Using Hot Melt Extrusion Technology" (2019). Electronic Theses and Dissertations. 1690. https://egrove.olemiss.edu/etd/1690 This Thesis is brought to you for free and open access by the Graduate School at eGrove. It has been accepted for inclusion in Electronic Theses and Dissertations by an authorized administrator of eGrove. For more information, please contact [email protected]. Mefenamic acid – HPMC AS HG amorphous solid dispersions: dissolution enhancement using Hot Melt Extrusion Technology A Thesis Presented for the Master of Science Degree The University of Mississippi ASHAY SHUKLA May 2019 Copyright © 2019 by Ashay Shukla All rights reserve ABSTRACT Mefenamic acid, a BCS class II drug, displays high permeability and low solubility, thereby exhibiting a poor dissolution profile. Hence to improve the solubility and dissolution rate of Mefenamic acid, Hot Melt Extrusion (HME) technique was employed. The amorphous solid dispersion matrix exhibited enhanced dissolution with desired release characteristics. Hydroxypropylmethylcellulose acetate succinate (AquaSolve™ HPMC-AS HG) was used as a carrier with the poloxamer (Kolliphor P407). The drug load was varied from 20% to 40% within the blend. Drug and polymers were blended using a twin shell V-blender for 10 minutes and extruded using an 11mm twin-screw co-rotating extruder (ThermoFisher Scientific, Waltham, MA, USA).
    [Show full text]
  • Indiscriminative Effects of Repaglinide and Other Specific Modulators of Transmembrane KATP-Channel Gating Properties Upon Ischa
    Journal of Clinical and Basic Cardiology An Independent International Scientific Journal Journal of Clinical and Basic Cardiology 2003; 6 (Issue 1-4), 81-85 Indiscriminative Effects of Repaglinide and Other Specific Modulators of Transmembrane KATP-Channel Gating Properties upon Ischaemic/Hypoxic Bovine Coronary Artery Smooth Muscle Relaxation Gasser R, Esche G, Gasser S, Holzmann S, Köppel H Moosbrugger B, Salzer M Homepage: www.kup.at/jcbc Online Data Base Search for Authors and Keywords Indexed in Chemical Abstracts EMBASE/Excerpta Medica Krause & Pachernegg GmbH · VERLAG für MEDIZIN und WIRTSCHAFT · A-3003 Gablitz/Austria ORIGINAL PAPERS, BASIC CARDIOLOGY Repaglinide and Coronary Dilation J Clin Basic Cardiol 2003; 6: 81 Indiscriminative Effects of Repaglinide and Other Specific Modulators of Transmembrane KATP-Channel Gating Properties upon Ischaemic/Hypoxic Bovine Coronary Artery Smooth Muscle Relaxation R. Gasser1, H. Köppel2, B. Moosbrugger1, G. Esche1, M. Salzer1, S. Gasser1, S. Holzmann3 The opening of KATP channels both in myocardium and vascular smooth muscle constitutes an important mechanism in the regulation of myocardial metabolism and perfusion, in particular, during hypoxia and ischaemia. In coronary smooth muscle, KATP channel opening invariably leads to vasodilation and hence to improved myocardial perfusion. Blockade of these chan- nels may disturb this pivotal response. We compare the effects of glibenclamide with two new sulfonylureas on coronary artery dilation secondary to hypoxia and simulated ischaemia. We use bovine coronary arteries in a modified Tyrode solution (equili- brated with 95 % O2 and 5 % CO2 at 37 °C at a constant pH of 7.4). The solution contained the following solutes (in mM): NaCl 112.8, KCl 26.8, CaCl2 1.36, MgSO4 1.16, NaHCO3 11.9, glucose 10.1.
    [Show full text]
  • [Nationally Completed Name] 500Mg/2.5Mg, Film-Coated Tablets [Nationally Completed Name] 500Mg/5Mg, Film-Coated Tablets Metformin Hydrochloride and Glibenclamide
    Sandoz Business use only Page 1 of 10 1.3.1 spc-label-pl - common-pl - 7,188 20160525 (NL/H/1545/001-002/IA/011) GLIBENCLAMIDE+METFORMIN HYDROCHLORIDE 2.5 MG + 721-8322.00 721-8323.00 500 MG; 5 MG + 500 MG FILM-COATED TABLET Package leaflet: Information for the patient [Nationally completed name] 500mg/2.5mg, film-coated tablets [Nationally completed name] 500mg/5mg, film-coated tablets metformin hydrochloride and glibenclamide Read all of this leaflet carefully before you start taking this medicine because it contains important information for you. Keep this leaflet. You may need to read it again. If you have any further questions, ask your doctor or pharmacist. This medicine has been prescribed for you only. Do not pass it on to others. It may harm them, even if their signs of illness are the same as yours. If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet. See section 4. What is in this leaflet: 1. What [Nationally completed name] is and what it is used for 2. What you need to know before you take [Nationally completed name] 3. How to take [Nationally completed name] 4. Possible side effects 5. How to store [Nationally completed name] 6. Contents of the pack and other information 1. What [Nationally completed name] is and what it is used for [Nationally completed name] contains two antidiabetic medicines, belonging to groups of medicines called biguanides (metformin hydrochloride) and sulphonylureas (glibenclamide). Insulin is a hormone that enables body tissues to take up glucose (sugar) from the blood and to use it for producing energy or to store it for future use.
    [Show full text]
  • Gliclazide Directly Inhibits Arginine-Induced Glucagon Release Kenan Cejvan,1 David H
    Gliclazide Directly Inhibits Arginine-Induced Glucagon Release Kenan Cejvan,1 David H. Coy,2 Jens Juul Holst,3 Erol Cerasi,4 and Suad Efendic1 Arginine-stimulated insulin and somatostatin release is abolished insulin and somatostatin responses. The insulin enhanced by the sulfonylurea gliclazide. In contrast, response was blunted by destruction of B cells with gliclazide inhibits the glucagon response. The aim of the alloxan (4) or streptozotocin (STZ) (3), whereas the soma- present study was to investigate whether this inhibition tostatin release was nearly abolished by perfusing pancre- of glucagon release was mediated by a direct suppres- ata with a medium containing a low calcium concentration sive effect of gliclazide or was secondary to the para- (4) or by treating the animals with cysteamine (3). crine effect of released somatostatin. To eliminate the The action of somatostatin on target cells is mediated by paracrine effects of somatostatin, we first perfused iso- five somatostatin receptor subtypes (SSTR 1–5) (5). In lated rat pancreata with a medium supplemented with rodents, somatostatin inhibits glucagon and insulin release 23% of the standard calcium content. Second, we peri- fused isolated rat islets with a novel and highly specific via SSTR2 and SSTR5, respectively (6,7). A novel highly antagonist of type 2 somatostatin receptor, DC-41-33 (2 specific SSTR2 antagonist, DC-41-33, has recently been ␮mol/l), which fully antagonizes the suppressive soma- synthesized (8). When applied in both perifused isolated tostatin effect on rat A cells. Gliclazide (30 ␮mol/l) rat islets and isolated perfused rat pancreas, this com- inhibited glucagon release by 54% in the perfusion ex- pound enhances arginine-stimulated glucagon release periments, whereas the somatostatin response was nearly nearly threefold, which implies that islet somatostatin abolished.
    [Show full text]
  • Effect of Nateglinide and Glibenclamide on Endothelial Cells and Smooth Muscle Cells from Human Coronary Arteries H
    KardiologieJournal für Austrian Journal of Cardiology Österreichische Zeitschrift für Herz-Kreislauferkrankungen Effect of Nateglinide and Homepage: Glibenclamide on Endothelial Cells www.kup.at/kardiologie and Smooth Muscle Cells from Human Online-Datenbank Coronary Arteries mit Autoren- und Stichwortsuche Seeger H, Abletshauser C, Mueck AO Journal für Kardiologie - Austrian Journal of Cardiology 2004; 11 (1-2), 35-37 Member of the ESC-Editor‘s Club Offizielles Organ des Österreichischen Herzfonds Indexed in EMBASE Krause & Pachernegg GmbH • Verlag für Medizin und Wirtschaft • A-3003 Gablitz P.b.b. 02Z031105M, Verlagsort: 3003 Gablitz, Linzerstraße 177A/21 Preis: EUR 10,– EINE FRÜHE DIAGNOSE VON ATTR-CM KANN LEBEN RETTEN. Erfahren Sie mehr über diese LEBENSBEDROHLICHE und UNTERDIAGNOSTIZIERTE ERKRANKUNG1 auf unserem AMYLOIDOSE FORTBILDUNGSPORTAL und tragen Sie dazu bei, Ihre Patient*innen frühzeitig zu diagnostizieren. HIER ENTLANG & DFP-PUNKTE SAMMELN Bleiben Sie auf dem Laufenden und sammeln Sie jetzt Ihre DFP-Punkte: NUKLEARMEDIZINISCHE 2 DFP- DER AMYLOIDOSE 2 DFP- ECHOKARDIOGRAPHIEKURS ZUR 1 DFP- PUNKTE AUF DER SPUR PUNKTE KARDIALEN AMYLOIDOSE – VON PUNKT BILDGEBUNG DER KARDIALEN DER KLINIK BIS ZUR DIAGNOSE ATTR-AMYLOIDOSE ATTR-CM, Transthyretin-Amylodiose mit Kardiomyopathie Pfizer Corporation Austria GmbH, Wien 1. Witteles RM et al, JACC Heart Fail. 2019 www.pfizer.at PP-VYN-AUT-0403/07.2021 Anzeige Nateglinide and Glibenclamide and Direct Vascular Effects Effect of Nateglinide and Glibenclamide on Endothelial Cells and Smooth Muscle Cells from Human Coronary Arteries H. Seeger, C. Abletshauser, A. O. Mueck Abstract: In the present work the effect of nateglinide These results indicate that both nateglinide and Endothelfunktion dienten Prostazyklin, Endothelin und and glibenclamide, two different substances used for glibenclamide may have potential in reducing negative Plasminogen-Aktivator-Inhibitor-1 (PAI-1).
    [Show full text]