OBJECTIVE: In view of both the economic importance of ethylenebisdithiocarbamate (EBDC) fungicides in the current agricultural practice and the potential health hazards associated with ethylenethiourea (ETU) exposure, this study aimed to develop and validate a high-pressure liquid chromatography (HPLC) method to determine ETU in biological and environmental samples.

METHODS: The samples were pre-treated according to sample types and were analyzed for ETU using a reversed-phase HPLC system (JASCO?) equipped with UV detector set at 230 nm using C18 bonded silica column and a mobile phase of 0.05M ammonium acetate in methanol (95:5).

RESULTS: The method showed a limit of detection of 0.2 ug/L, with a precision of 3.33 to 12.86 %CV and an accuracy of >90% at 1, 10 and 100 ug/L of ETU in all sample types. The calibration curve was linear from 1 to 200 ug/L for blood, air and water samples and 1 to 2000 ug/L for urine.

CONCLUSION: This method showed an acceptable accuracy, precision, sensitivity and specificity and was used subsequently to determine ETU levels in blood, urine, air, soil and water samples among banana plantation workers.

Ethylenethiourea

The chlorpropamid (1) is an antidiabetic drug synthetized from chlorobenzene (2) in five steps through intermediates p-clorobenzenesulfonyl chloride (3), calcium p-chlorobenzene sulfonyl cyanamide (6), p-clorobenzenesulfonyl cyanamide (7), p-clorobenzenesulfonyl urea (8) and then the compound 8 was condensated with n-propylamine. The product have melting point, Rf, IR spectral data that suitable with to the chlopropamid extracted from Novopropamid tablet of Canada.
Chlorpropamide ; Methods

OBJECTIVETo compare the influence of different sulfonylureas on the myocardial protection effect of ischemic preconditioning (IPC) in isolated rat hearts, and ATP-sensitive potassium channel current (IK(ATP)) of rat ventricular myocytes.

METHODSIsolated Langendorff perfused rat hearts were randomly assigned to five groups: (1) control group, (2) IPC group, (3) IPC + glibenclamide (GLB, 10 micromol/L) group, (4) IPC + glimepiride (GLM, 10 micromol/L) group, (5) IPC + gliclazide (GLC, 50 micromol/L) group. IPC was defined as 3 cycles of 5-minute zero-flow global ischemia followed by 5-minute reperfusion. The haemodynamic parameters and the infarct size of each isolated heart were recorded. And the sarcolemmal IK(ATP) of dissociated ventricular myocytes reperfused with 10 micromol/L GLB, 1 micromol/L GLM, and 1 micromol/L GLC was recorded with single-pipette whole-cell voltage clamp under simulated ischemic condition.

RESULTSThe infarct sizes of rat hearts in IPC (23.7% +/- 1.3%), IPC + GLM (24.6% +/- 1.0%), and IPC + GLC (33.1% +/- 1.3%) groups were all significantly smaller than that in control group (43.3% +/- 1.8%; P < 0.01, n = 6). The infarct size of rat hearts in IPC + GLB group (40.4% +/- 1.4%) was significantly larger than that in IPC group (P < 0.01, n=6). Under simulated ischemic condition, GLB (10 micromol/L) decreased IK(ATP) from 20.65 +/- 7.80 to 9.09 +/- 0.10 pA/pF (P < 0.01, n=6), GLM (1 micromol/L) did not significantly inhibit IK(ATP) (n=6), and GLC (1 micromol/L) decreased IK(ATP) from 16.73 +/- 0.97 to 11. 18 +/- 3.56 pA/pF (P < 0.05, n=6).

CONCLUSIONSGLM has less effect on myocardial protection of IPC than GLB and GLC. Blockage of sarcolemmal ATP-sensitive potassium channels in myocardium might play an important role in diminishing IPC-induced protection of GLM, GLB, and GLC.

Animals ; Gliclazide ; pharmacology ; Glyburide ; pharmacology ; Heart ; drug effects ; Ischemic Preconditioning ; Male ; Rats ; Rats, Sprague-Dawley ; Sulfonylurea Compounds ; pharmacology

Developmental delay, Epilepsy and Neonatal Diabetes (DEND) syndrome is the most severe form of Permanent Neonatal Diabetes with KCNJ11 gene mutation which accounts for most of the cases. We report the first DEND syndrome in Malaysia with heterozygous missense mutation Q52R at KCNJ11 (Kir6.2) gene with delayed presentation beyond 6 months of age and failure to transition to glibenclamide. This report signifies the phenotypical variability among patients with the same genetic mutation and the different response to treatment.
Glyburide

We report a case that a 68-year-old man taking hydroxyurea for essential thrombocythemia produced milky urine during propofol infusion. Under microscopic analysis, the cloudy urine sample was revealed to comprise uric acid crystals. Postoperatively, kidney function such as urine output and blood urea nitrogen to creatinine ratio showed no abnormality. We suggest that the cloudy urine may be due to the increased excretion of uric acid after administration of propofol. Although this rare case of cloudy milky urine is resolved on its own, we need to consider the possibility of such urine color changes. It is particularly important to understand that medication, preoperative serum uric acid level, urine pH, and the hypothermal operating room can change the color of urine through the presence of uric acid crystals.
Aged ; Anesthesia, Intravenous* ; Blood Urea Nitrogen ; Creatinine ; Humans ; Hydrogen-Ion Concentration ; Hydroxyurea* ; Kidney ; Operating Rooms ; Propofol* ; Thrombocythemia, Essential ; Uric Acid

BACKGROUND: Sulfonylurea drugs have been used for many decades as one of the main families of drugs for the treatment of type 2 diabetes mellitus. Even though there are many opportunities to medicate sulfonylurea drugs concomitantly with many other drugs, and furthermore there have been several case reports on drug interactions with sulfonylurea drugs, there has been no clear demonstration revealing the mechanisms that cause these interactions. We therefore evaluated inhibitory potential of sulfonylurea drugs, including glibenclamide, glipizide and gliclazide, on the cytochrome P450 (CYP)-catalyzing enzymes using human liver microsomes. METHODS: The inhibitory effects of glibenclamide, glipizide and gliclazide, on the CYP-catalyzing reaction, were evaluated for CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4 using human liver microsomes, and probe drugs for each. RESULTS: Glibenclamide showed relative potent inhibitory effects on the CYP2C9- and CYP3A4-catallyzed reaction (IC50; 11.3 ( microM and 59.0 ( microM). The other CYP isoforms tested showed only weak inhibitory effects by due to glibenclamide (IC50 > 112 ( microM). Glipizide showed potent inhibitory effect on CYP3A4-catalyzed reaction only (IC50; 11.2 ( microM), and weak, or no, inhibitory effects on each on the other CYP isoforms tested (IC50 > 276 ( microM). CONCLUSION: The sulfonylurea drugs showed inhibitory potential on the CYP-catalyzing reaction in human liver microsomes. The results obtained in the present study provide insights into the potential of the drug interaction to ward drugs co-administered with sulfonylureas. It will be necessary to take into consideration the control of blood glucose, as well as therapeutic drug monitoring, to reduced toxicities when sulfonylurea drugs are co-administered with drugs of a narrow therapeutic range, or with severe dose-dependent toxicities.
Blood Glucose ; Cytochrome P-450 CYP1A2 ; Cytochrome P-450 CYP2D6 ; Cytochrome P-450 Enzyme System ; Cytochromes* ; Diabetes Mellitus, Type 2 ; Drug Interactions ; Drug Monitoring ; Gliclazide ; Glipizide ; Glyburide ; Humans* ; Liver* ; Microsomes, Liver* ; Protein Isoforms

BACKGROUND: Previous studies have noted that the simultaneous use of sulfonylureas and antimicrobials, which is common, could increase the risk of hypoglycemia. In particular, an age of 65 years or older is a known risk factor for sulfonylurea-related hypoglycemia in hospitalized patients. Therefore, we performed this study to determine the potential risk of hypoglycemia from the concurrent use of antimicrobials and sulfonylureas. METHODS: We performed a cross-sectional study on the National Health Insurance Service-National Sample Cohort from 2013. The eligibility criteria included patients of 65 years of age or older taking a sulfonylurea with 25 different antimicrobials. Different risk ratings of severity in drug-drug interactions (potential DDIs), level X, D, or C in Lexi-Interact™online, and contraindicated, major, or moderate severity level in Micromedex® were included. SAS version 9.4 was used for data analysis. RESULTS: A total of 6,006 elderly patients with 25,613 prescriptions were included. The largest age group was 70 to 74 (32.7%), and 39.7% of patients were men. The mean number of prescriptions was 4.3 per patient. The most frequently used antimicrobials were levofloxacin (6,583, 25.7%), ofloxacin (6,549, 25.6%), fluconazole (4,678, 18.0%), and ciprofloxacin (2,551, 9.8%). Among sulfonylureas, glimepiride was prescribed most frequently, followed by gliclazide, glibenclamide, and glipizide. CONCLUSION: Of the antimicrobials with a high potential of hypoglycemia, levofloxacin, ofloxacin, fluconazole, and ciprofloxacin were used frequently. Thus, the monitoring of clinically relevant interactions is required for patients concurrently administered sulfonylureas and antimicrobials.
Aged* ; Anti-Infective Agents ; Ciprofloxacin ; Cohort Studies ; Cross-Sectional Studies ; Drug Interactions ; Fluconazole ; Gliclazide ; Glipizide ; Glyburide ; Humans ; Hypoglycemia* ; Korea* ; Levofloxacin ; Male ; National Health Programs ; Ofloxacin ; Prescriptions ; Risk Factors ; Statistics as Topic ; Sulfonylurea Compounds

We report three cases of Diabetes insipidus which charactrized by the polyuria and polydipsia. All of the three cases well controlled with oral addministration of chlorpropamide. Two cases were idiopathic and the other was suspected pituitary tumor. A briet review of literature was made.
Chlorpropamide ; Diabetes Insipidus* ; Pituitary Neoplasms ; Polydipsia ; Polyuria

No abstract available.
Onychomycosis* ; Urea*

Method of improved pp biuret with high sensitivity and accuracy is frequently used in the biochemical techniques to determine the protein in the preparations. The sensitivity of this method was as same as this of method Anson and error of pp biuret was smaller than this of Anson. The pp biuret has been applied in Vietnam to determine the proteolytic activity of pharmaceutical pepsin.
Biuret Reaction ; Pepsin A