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Anti Diabetic Anti Diabetic
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Dwi Indria AnggrainiDept. of Pharmacology-Medical Faculty UNILA
Antidiabetic Agents
Diabetes Mellitus
Syndrome characterized by • Blood glucose • Caused by a relative or
absolute deficiency of insulin
Disorders of carbohydrate, protein and lipid metabolisms
TYPE I DM
Defect: cells - destroyed, eliminates insulin prod.
Onset: Childhood/puberty
Nutritional status at onset:
Undernourished
TYPE II DM
Defect: + Inadequate prod.+ Insulin resistance
Onset: 0ver 35 year old
Nutritional status at onset:
Obese
Treatment Type I DM
Exogenous insulin
Good control of Blood Glucose
• Hb1C
less than 9%
2 types:
Treatment Type II DM
Good control of Blood Glucose
Delays long-term complications
Diet and exercise necessities
Treated by Oral Hypoglycemic Agents and/or insulin
Insulin in pregnancy or in severe illness
Insulin
Pork, Beef, Human Parenteral, per oral is preferable but not
yet established Preparation
Rapid action: Regular, lispro Intermediate action: NPH Prolonged action: Ultralente Combination: 30R 70N
ADR: Hypoglycemia
Tachycardi
aConfusion
Vertigo
Diaphoresis
Insulin concentration and binding in normal and overweight subjects
Development of maturity-onset diabetes
ORAL HYPOGLYCAEMICS
Sulphonylureas
Biguanides: Metformin
Thiazolidinediones:
• Rosiglitazone• pioglitazone
Action of oral antidiabetic drugs
Oral Hypoglycemic Agents Sulfonylureas
First Generation : Tolbutamide• Stimulates insulin release• Reduces glucagon release• Increases insulin Binding• Inhibits gluconeogenesis
Second Generation: Glyburide
Mechanisms:
Glipizide and Glyburide have high potency
Drugs Interaction:
• Protein binds• Salicylates, sulfonamides, clofibrate, phenylbutazone
• Metabolized by liver• Dicumarol, MAO inhibitors, phenylbutazone, chloramphenicol,
• Excreted by Kidney• Allopurinol, probenecid, phenylbutazone, salicylates, sulfonamides.
Drug interactions increase the risk of hypoglycemia.
Adverse reactions:
Hypoglycemia, GI dist. Pruritus,
Anemia
Chlorpropamide causes disulfiram
like effects
Chlorpropamide and Glyburide have long T1/2 , especially are likely to cause hypoglycemia
Biguanides
Metformine• insulin release & binding• glucagon release• Inhibits gluconeogenesis and starch & disaccharides absorption
Mechanism:
• - mild-moderate NIDDM diabetes who demonstrate insulin resistance
Reduces hyperlipidemia
Indication:
AR: - GI disturbances
- Lactic acidosis in RF patient
- Long-term used: Vit B12 malabsorption
-Glucosidase InhibitorAcarbose
Inhibits the absorption of strach and disaccharides. control glucose pp
Monotherapy or Combination
NIDDM and IDDM
AR: flatulence, diarrhea, abdominal cramping.
Thiazolidinediones
MOA:• periphe
ral insulin resist insulin act Plasma gluc
Indication: Uncontrolled NIDDM
CI: • Hepatic
impairment
• History of heart dis.
AR: • GI
disturb• Weight
gain• Potential
ly liver failure