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Diabetes Mellitus Is Due To A Disorder Of Carbohydrate, protein And Lipid Metabolism As A Result Of An Absolute Or Deficiency In Metabolically Active Insulin.

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Euglucon

  1. 1. GLIBENCLAMIDE ANTI-DIABETIC DRUG
  2. 2. DIABETES MELLITUS <ul><li>Diabetes Mellitus Is Due To A Disorder Of Carbohydrate, protein And Lipid Metabolism As A Result Of An Absolute Or Deficiency In Metabolically Active Insulin. </li></ul><ul><li>IN OLDER DAYS </li></ul><ul><li>Diabetes = Over Abundant Urine </li></ul><ul><li>Or </li></ul><ul><li>Melting of flesh in urine </li></ul><ul><li>MELLITUS = Sweet As Honey </li></ul>
  3. 3. TYPES OF DIABETES MELLITUS <ul><li>Improper Working Of Pancreas Is Diabetes Mellitus. SO TYPES ARE </li></ul><ul><li>DIABETES MELLITUS TYPE-I = IDDM </li></ul><ul><li>DIABETES MELLITUS TYPE-II = NIDDM </li></ul><ul><li>DIABETES TYPE-II a = NORMAL WEIGHT OR THIN DIABETES </li></ul><ul><li>DIABETES TYPE-II b = OVER WEIGHT DIABETES </li></ul><ul><li>ABOUT 80% OF TYPE 2 DIABETES ARE OVERWEIGHT </li></ul>
  4. 4. <ul><li>60 g </li></ul><ul><li>18 cm </li></ul><ul><li>Below liver </li></ul><ul><li>Under stomach </li></ul><ul><li>Acinar cells </li></ul><ul><li>Islets of langerhans </li></ul>
  5. 5. <ul><li>Acinar cell makes bulk of pancreas and make digestive enzymes </li></ul><ul><li>Islets of langerhans are only 1-2%of pancreas </li></ul>
  6. 6. <ul><li>They are responsible for the release of insulin and somastatin and glucagon. </li></ul><ul><li>Beta cells are for insulin </li></ul>
  7. 7. INSULIN <ul><li>51 amino acids in chain </li></ul><ul><li>Orally rapidly destroyed </li></ul><ul><li>Half-life 7-10 minutes </li></ul>C-peptide s s A-chain
  8. 8. INSULIN SECRETION <ul><li>10 </li></ul><ul><li>5 </li></ul><ul><li>0 1 2 </li></ul>Insulin secretion FOOD INSULIN EFFECT 25-50 UNITS OR 1-2 mg OF INSULIN IS SECRETED EACH DAY
  9. 9. INSULIN EFFECTS <ul><li>SUGAR CONSUMING </li></ul><ul><li>GLUCOSE TRANSPORT FUNCTIONTHROUGH THE CELL MEMEBRANE TO THE MUSCLE AND FAT CELLS </li></ul><ul><li>GLYCOGEN FORMATION FROM GLUCOSE IN LIVER & MUSCLES </li></ul><ul><li>FORMATION OF FATS FROMGLUCOSE </li></ul><ul><li>INSULIN PREVENTS THE ACTION OF LIPOLYTIC HARMONES </li></ul>
  10. 10. <ul><li>SUGAR-PROVIDING </li></ul><ul><li>Absorption of carbohydrates in the intestine </li></ul><ul><li>Glycogenolysis = glucose molecules come from glycogen (|stored form of sugar in the body) </li></ul><ul><li>GLUCONEOGENSIS = FROM PROTEIN IN THE LIVER. OR Synthesis Of Glucose From Another Fundamental Unit(aminoacids) </li></ul>INSULIN EFFECTS
  11. 11. TYPE-I DIABETES <ul><li>ABSOLUTE INSULIN DEFICIENCY DUE TO INABILITY OF BETSA CELLS TO RELEASE INSULIN </li></ul>
  12. 12. TYPE-II DIABETES <ul><li>RELATIVE INSULIN DEFICIENCY </li></ul><ul><li>NUMBER OF INSULIN RECEPTORS COMPLEX IS TOO LOW </li></ul>
  13. 13. INSULIN RECEPTOR <ul><li>GLUCOSE </li></ul><ul><li>MEMBRANE </li></ul><ul><li>EFFECTS </li></ul><ul><li>RECEPTOR </li></ul><ul><li>SECOND MESSENGER </li></ul><ul><li>ENZYME EFFECTS </li></ul><ul><li>LYSOSOME </li></ul>INSULIN
  14. 14. DIAGNOSIS <ul><ul><li>FASTING BLOOD SUGAR </li></ul></ul><ul><ul><li>POST PRANDIAL GLUCOSE LEVEL </li></ul></ul><ul><ul><li>GLUCOSE TOLERANCE TEST </li></ul></ul><ul><ul><li>GLYCOSYLATED HEMOGLOBIN LEVELS </li></ul></ul><ul><ul><li>URINE GLUCOSE LEVELS </li></ul></ul>
  15. 15. REFERENCE VALUES CONDITION FBS RBS LEVEL AT 120 mg NORMAL BELOW 115 BELOW 200 BELOW 140 IMPAIRED 115-139 ABOVE 200 140-199 DM ABOVE 140 ABOVE 200 ABOVE 200
  16. 16. HbA1c <ul><li>The HbA1c is a blood test that measures your average blood sugar over two to three months. The term ‘HbA1c’ refers to changes in the haemoglobin molecule. </li></ul><ul><li>Glucose can attach itself to the haemoglobin molecule. The difference is that once the glucose is attached, it remains there until the red cell dies. Red cells live for about three months. As blood glucose levels rise, more and more glucose becomes attached to the haemoglobin molecule. The HbA1c test measures how much glucose has become attached and therefore provides an indication of your average blood glucose for the past 6 weeks or so </li></ul>
  17. 17. HbA1c
  18. 18. COMPLICATIONS DUE TO INCREASE BLOOD GLUCOSE LEVELS <ul><li>RETINOPATHY </li></ul><ul><li>NEUROPATHY </li></ul><ul><li>NEPHEROPATHY </li></ul><ul><li>MICRO ANGIOPATHY </li></ul><ul><li>MACROANGIOPATHY </li></ul>
  19. 19. PILLARS FOR THE DIABETIC TREATMENT DIABETIC THERAPY PHYSICAL ACTIVITY DIET EUGLUCON MEDICAL TREAMENT DIABETIC INSTRUCTION + SELF-MONITORING
  20. 20. <ul><li>Diabetes is on of the most common metabolic diseases </li></ul><ul><li>The prevalence of Diabetes is increasing all around the world especially in developing countries . </li></ul>
  21. 21. Management of Diabetes <ul><li>DIET </li></ul><ul><li>EXERCISE </li></ul><ul><li>OHA </li></ul><ul><li>INSULIN </li></ul>
  22. 22. Oral anti-hyperglycemic agents <ul><li>Sulfonylureas: FIRST GENERATION </li></ul><ul><li>Chlorpropamide-Glyburide-Acetohexamide-Tolbutamide-Tolazamide- </li></ul><ul><li>SECOND GENERATION </li></ul><ul><li>Glibenclamide-Glipizide-Glibornurid- Glimepride GLICLAZIDE </li></ul><ul><li>* Biguanides: Phenformin Metformin </li></ul><ul><li>* a-glycosidase inhibitors: </li></ul><ul><li>Acarbose - Miglitol </li></ul><ul><li>* Thiazolidendiones: </li></ul><ul><li>Troglitazone Ciglitazone </li></ul><ul><li>Pioglitazon englitazone </li></ul><ul><li>* Meglitinide: Repaglinide </li></ul>
  23. 23. Biguanides (Metformin) <ul><li>Trade names: Glucophage, NEOPHAGE, NEODIPAR. </li></ul><ul><li>Mode of action: </li></ul><ul><ul><li>reduces hepatic glucose production </li></ul></ul><ul><ul><li>decreased intestinal absorption of glucose </li></ul></ul><ul><ul><li>increases peripheral utilization of glucose in muscle & fat tissue </li></ul></ul><ul><ul><li>decreased insulin requirements for glucose disposal </li></ul></ul>
  24. 24. Biguanides (Metformin) <ul><li>Precautions: chronic renal or cardiac failure </li></ul><ul><li> hepatic impairment </li></ul><ul><li> elderly </li></ul><ul><li> excessive alcohol intake </li></ul><ul><li>Side effects: gastrointestinal disturbances </li></ul><ul><li>metallic taste </li></ul><ul><li>malabsorption of B12 </li></ul><ul><li>Administer: with or after meals </li></ul>
  25. 25. Sulphonylurea <ul><li>Generic : Trade : Administer : </li></ul><ul><li>Glipizide Minidiab before meals </li></ul><ul><li>Gliclazide Diamicron with meals </li></ul><ul><li>Glibenclamide Euglucon Before meals </li></ul><ul><li>Tolbutamide Rastinon with meals </li></ul>
  26. 26. Sulphonylureas <ul><li>Mode of action: </li></ul><ul><li>increase pancreatic insulin secretion </li></ul><ul><li>may improve insulin sensitivity in peripheral tissue and decrease hepatic glucose output </li></ul>
  27. 27. Sulphonylureas <ul><li>Contra-indications : </li></ul><ul><ul><li>pregnancy, surgery, severe renal failure, type 1, hypersensitivity </li></ul></ul><ul><li>Precautions: </li></ul><ul><ul><li>renal impairment, hepatic impairment, elderly </li></ul></ul><ul><li>Side effects: </li></ul><ul><ul><li>hypoglycemia </li></ul></ul><ul><ul><li>weight gain </li></ul></ul>
  28. 28. Alpha Glucosidase Inhibitor (Acarbose) <ul><li>Trade name: Glucobay </li></ul><ul><li>Mode of action: </li></ul><ul><ul><li>delays breakdown of CHO such as starch & sucrose </li></ul></ul><ul><li>Contra-indications: </li></ul><ul><ul><li>pregnancy </li></ul></ul><ul><ul><li>renal impairment </li></ul></ul><ul><ul><li>gastrointestinal disorders </li></ul></ul>
  29. 29. Alpha Glucosidase Inhibitor (Acarbose) <ul><li>Precautions: </li></ul><ul><ul><li>high sucrose diet </li></ul></ul><ul><li>Side effects: </li></ul><ul><ul><li>gastrointestinal </li></ul></ul><ul><ul><li>rash </li></ul></ul><ul><ul><li>erythema </li></ul></ul><ul><li>Important considerations: </li></ul><ul><ul><li>take directly before or with the first few spoons of the meal </li></ul></ul>
  30. 30. Repaglinide <ul><li>Trade Name: NovoNorm </li></ul><ul><li>Mode of action: </li></ul><ul><ul><li>short acting oral hypoglycaemic agent </li></ul></ul><ul><ul><li>stimulates pancreatic insulin release </li></ul></ul>
  31. 31. Repaglinide <ul><li>Contra-indications: </li></ul><ul><li>type 1 diabetes, pregnancy, lactation, children </li></ul><ul><li>< 12 years </li></ul><ul><li>Precautions: </li></ul><ul><li>impaired renal or hepatic function </li></ul><ul><li>Side effects: </li></ul><ul><li>hypoglycaemia, gastrointestinal upset, raised Left's, blurred vision </li></ul>
  32. 32. Thiazolidinedione (Rezulin) <ul><li>Trade name: Rosiglitazone, Poiglitizone </li></ul><ul><li>Mode of action: </li></ul><ul><li>improves sensitivity to insulin in skeletal muscle and adipose tissue </li></ul><ul><li>inhibits glucose release from the liver </li></ul>
  33. 33. Thiazolidinedione <ul><li>Contra-indications </li></ul><ul><li>heart failure, moderate to severe hepatic impairment. </li></ul><ul><li>Precautions </li></ul><ul><li>oedema or heart failure </li></ul><ul><li>anovulatory premenopausal women with insulin resistance as ovulation may resume (consider contraception. </li></ul>
  34. 34. Glucose Regulation <ul><li>Glucose Sources: Endogenous (liver) Diet </li></ul>GLUCOSE REGULATION IN BODY: LIVER PANCREAS KIDNEY ADIPOSE TISSUE GI TRACT
  35. 35. MODE OF ACTION OF EUGLUCON ATP dependent K+ channels VDCC Ca++ CHANNEL Ca++ ACTIVATED CHANNEL Ca++ RESTING CELL K+
  36. 36. MODE OF ACTION OF EUGLUCON ATP dependent K+ channels VDCC Ca++ CHANNEL Ca++ ACTIVATED CHANNEL Ca++ DEPOLARIZATION K+ INSULIN SECRETION CA++
  37. 37. MODE OF ACTION OF EUGLUCON ATP dependent K+ channels VDCC Ca++ CHANNEL Ca++ ACTIVATED CHANNEL Ca++ REPOLARIZATION K+ - +
  38. 38. EUGLUCON <ul><li>EUGLUCON IS AVAILBLE AS WHITE,OBLONG, SCORED, CONTAINING 5mg GLIBENCLAMIDE </li></ul>
  39. 39. EUGLUCON <ul><li>STIMULATE BETA-CELLS OF PANCREAS TO RELEASE INSULIN </li></ul><ul><li>INCREASE SENSITIVITY OF THE PERIPHERAL TISSUE TO INSULIN </li></ul><ul><li>MILD DIURESIS </li></ul>
  40. 40. EUGLUCON <ul><li>RAPIDLY ABSORBED </li></ul><ul><li>MAX.BLOOD LEVEL WITHIN 1-4 HOURS </li></ul><ul><li>BIOAVAILIBILITY 90-100 % </li></ul><ul><li>PROTEIN BINDING 90 % </li></ul><ul><li>VOLUME OF DISTRIBUTION 155ml/kg </li></ul><ul><li>ELIMINATION HALF-LIFE </li></ul><ul><ul><ul><ul><ul><li>BIPHASIC </li></ul></ul></ul></ul></ul><ul><ul><ul><ul><ul><li>2.1 HOURS & 10 HOURS </li></ul></ul></ul></ul></ul>
  41. 41. EUGLUCON <ul><li>EXECRETION </li></ul><ul><ul><ul><ul><li>50% KIDNEY </li></ul></ul></ul></ul><ul><ul><ul><ul><li>50% FECES </li></ul></ul></ul></ul><ul><li>HIGHEST TISSUE CONCENTRATION IN LIVER </li></ul><ul><li>NO TERTOGENEIC EFFECTS </li></ul><ul><li>CONTERA INDICATIONS </li></ul><ul><li>TYPE-1 DIABETES </li></ul><ul><li>DIABETIC COMA </li></ul><ul><li>KETO-ACIDOSIS </li></ul><ul><li>SDVERE RENAL IMSUFFICENCY </li></ul><ul><li>PREGANACY </li></ul><ul><li>HYPERSENSITIVITY TO GLIBENCLAMIDE </li></ul>
  42. 42. EUGLUCON <ul><li>GLIBECLAMIDE EXCRETION </li></ul><ul><li>THROUGH BILE RENAL FUNCTION </li></ul>53% 47% NORMAL FUNCTION 79% 21% MODERATE IMPAIRMENT 94% 6% SEVERE IMPAIRMENT DEPENDING UPON THE DEGREE OF RENAL EXCRETION DISORDER,AN INCREASE EXCRETION IN THE BILE AND FECES OCCURS AS COMPENSATORY EFFECT
  43. 43. EUGLUCON <ul><li>ADVERSE REACTION </li></ul><ul><li>NAUSEA AND EPIGASTRIC BLOATING </li></ul><ul><li>ALLERGY SKIN REACTION </li></ul><ul><li>ALLERGY CROSSS REACTION SULPHONAMIDES </li></ul><ul><li>EFFECTS HAEMATOPOIETIC SYSTEM </li></ul><ul><li>HAEMOLYTIC ANAMEIA </li></ul><ul><li>CHOLESATITIC JAUNDICE </li></ul><ul><li>HEPATITIS </li></ul><ul><li>INDICATIONS </li></ul><ul><ul><ul><li>NIDDM “(TYPE-II) MATURITY ONSET DIABETES, WNENEVER TREATMENT BY DIET ALONE PROVES INADIQUATE </li></ul></ul></ul>
  44. 44. EUGLUCON Dosage Administration Administration scheme Daily Dose To Be Taken ½ - 1 - 2 - 2 1
  45. 45. EUGLUCON <ul><li>INSULIN SECRETION IN RHYTHM WITH MEALS </li></ul><ul><li>NO RISK OF ACCUMLATION DUE TO DUAL ROUTE OF EXCRETION. </li></ul><ul><li>NORMALIZE TISSUE RESPONSE TO ENDDOGENOUS INSULIN. </li></ul><ul><li>IMPROVES DISTURBED LIPID PROFILE. </li></ul><ul><li>BETTER PATIENT COMPLIANCE. </li></ul><ul><li>LOW INCIDENCE OF ADVERSE RECATIONS. </li></ul><ul><li>RELIABLE LONG-THERAPY. </li></ul>
  46. 46. EUGLUCON <ul><li>POWERFUL MOBLIZATION OF THE DELAYED INSULIN SECRETION. </li></ul><ul><li>PARTICULARLY GREAT SYNERGISTIC WITH GLUCOSE. </li></ul><ul><li>RELEASE OF INSULIN WHEN NEEDED: AFTER EVERY MEAL. </li></ul><ul><li>SMOOTH DAILY BLOOD SUGAR PROFILE. </li></ul><ul><li>MOSTLY SINGLE DOSGE ADMINISTRATION. </li></ul><ul><li>BREAKING THROUGH OF PERIPHERAL INSULIN RESISTANCE. </li></ul><ul><li>REDUCTION OF PLATELET AGGREGATION. </li></ul><ul><li>BETTER STABILIZATION. </li></ul><ul><li>MORE DIABETICS CAN BE OPTIMALLY CONTROLLED. </li></ul><ul><li>EXCELLENT TOLERANCE. </li></ul>
  47. 47. THANK YOU

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