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Euglucon

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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.

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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  • Presenter’s Notes Metformin is absorbed along the entire gastrointestinal mucosa and improves peripheral and hepatic sensitivity to insulin. This results in increased uptake of glucose by peripheral tissues and decreased hepatic glucose production. It is not stored in the liver and it is excreted in the urine. It does not stimulate insulin production or release from the pancreas and therefore does not cause hypoglycemia. It is the treatment of choice in patients who are overweight.
  • Presenter’s Notes Renal disease is the only absolute contra-indication to metformin and serum creatinine should be checked routinely. Gastrointestinal disturbances may include anorexia, nausea, diarrhea and a metallic taste. Lactic acidosis can be caused by excessive alcohol and symptoms include nausea, vomiting & diarrhea. Metformin is taken with meals to decrease gastrointestinal effects.
  • Presenter’s Notes Sulphonyureas stimulate insulin secretion by increasing pancreatic beta cell responsiveness to glucose. All people taking Sulphonylureas should receive information about the prevention and treatment of hypoglycemia. Glipizide is a potent but shorter acting OHA. Must be given before meals or it loses 40 % efficacy. Metabolism occurs mainly in the liver. It is contra-indicated in severe renal or hepatic failure. Gliclazide restores the diminished first phase of insulin secretion that is common in type 2 diabetes. It is absorbed along the gastrointestinal tract. The liver is the probable site of metabolism. Glibenclamide is a strong and long acting OHA. Should be used in caution in the elderly. Hypoglycemia may be severe, prolonged and fatal. Tolbutamide is the drug of choice in renal disease. It is relatively short acting in comparison to other Sulphonylureas. Contra-indicated in severe renal or hepatic impairment.
  • Presenter’s Notes Sulphonyureas can be used in conjunction with a biguanide. This is due to the different modes of action egg metformin and localized. There is no value in using two different types of Sulphonylureas as they do not complement each other egg localized and glipizide.
  • Presenter’s notes All Sulphonylureas can cause hypoglycemia and this risk increases with age and impaired renal function. Hypoglycemia is more common with longer acting sulphonylurea egg chloropropramide and glibenclamide. Weight gain can occur due to increased insulin production.
  • Presenter’s notes Used if other oral agents are ineffective. It can be used in conjunction with metformin and sulphonylurea. The action depends on inhibition of intestinal enzymes involved in the digestion of some carbohydrates and thereby reduces the post prandial rise in blood glucose levels. Precautions and side effects : gastrointestinal: flatulence, abdominal pain and distention does not produce hypoglycaemia when used alone need to treat hypoglycaemia, with quick acting glucose.
  • Presenter’s notes
  • Presenter’s Notes Use: Type 2 diabetes (as monotherapy or with metformin). Repaglinide is a novel short-acting oral hypoglycaemic agent structurally unrelated to the sulphonylurea drugs. It lowers blood glucose levels acutely by stimulating the release of insulin from the pancreas, an effect which is dependent upon functioning beta cells in the pancreas. Note: Meal related dosing means a person only needs to take this medication when eating a meal.
  • Presenter’s Notes Like other oral hypoglycaemic agents (sulphonylureas) repaginate is capable of causing hypoglycaemia. People with impaired renal or hepatic function may be exposed to higher concentrations of repaginate than would occur with the usual doses prescribed for people with normal function. Therefore, a more conservative dose titration with longer titration intervals should be considered. The safety of repaginate during pregnancy has not been established.
  • Presenter’s Notes Rezulin is currently only to be used as adjunct therapy with insulin. It is the first medication released from this class. It is absorbed within 2-3 hours of ingestion. It should be taken with food to increase absorption. Half life of 16-34 hours.
  • Presenter’s Notes Rare cases of idiosyncratic hepatocellular injury have been reported and so regular monitoring is essential.

Euglucon Euglucon Presentation Transcript

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