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TRULY SITORUS
Depart. of Pharmacology & Therapy Faculty Of Medicine Padjadjaran University
It is a heterogeneous group of syndromes all characterized by an elevation of blood glucose caused by a relative or absolute deficiency of insulin. Symptom:
DM
A. TYPE I (INSULIN DEPENDENT DIABETES MELLITUS, IDDM)
Absolute deficiency of insulin Caused by massive -cell lesions or necrosis Treatment: exogenous insulin
INSULIN
Insulin exogen
Beef Pork Human (by. E.colli, OOA <<, DOA <<)
Effect
Hyperglycemia Normal
MECHANISM OF ACTION
PHARMACOKINETICS
Insulin p.o degradation subcutaneous IV: in hyperglycemic emergency
Lipodystrophy Hypersensitivity
INDICATION
1. All patients with type I DM regardless of age 2. Patient who have ketoacidosis or hyperosmolar coma 3. Patient with type II DM when diet restriction, exercise and oral hypoglycemic agent have failed to maintain satisfactory blood glucose concentration 4. Patient with type II DM in presence of surgery fever, infections, serious renal or hepatic dysfunction, and other metabolic disturbances 5. Pregnant diabetic women
CONTRAINDICATION
There are no contraindications if the proper indication exists. Patients must be well educated regarding the role of diet, exercise and illness in modifying their insulin requirements.
INSULIN PREPARATIONS
A. RAPID ACTION INSULIN PREPARATION
Zinc insulin: sc
iv (in emergencies)
SULFONILUREAS
First generation Tolbutamide, Chlorpropamide, Tolazamide Second generation Glipizide, Glyburide
II. III.
BIGUANIDES
Metformin
GLUCOSIDASE INHIBITORS
Acarbose
V.
THIAZOLIDINEDIONES
Troglitazone
SULFONILUREAS
Mechanism of action 1. Stimulation of insulin release from the cells 2. Reduction of serum glucagon levels 3. Increased binding of insulin to target tissues Pharmacokinetics Oral, bind to serum proteins Metabolized by liver
1st G : inactive, less active, active 2nd G: inert
Side effect Hypoglycemia (especially: chlorpropamide, Glyburide) Contraindication: Renal or hepatic insufficiency Pregnancy Elderly
INTERACTION
METFORMIN
Used alone or in combination with sulfonilurea, others Drugs of choice in newly diagnosed type II DM Decreasing hepatic glucose output Reduced hyperlipidemia (LDL, VDL, cholesterol, HDL) Oral, unbound to serum protein Not metabolized Side effect: GI disturbance, hypoglycemic <<
ACARBOSE
Inhibits glucosidase in intestinal decreased the absorption of starch and disaccharides Taken with meals Not cause hypoglycemia Side effects: flatulence diarrhea abdominal cramping
REPAGLINIDE
Binds to the ATP- sensitive potassium channels of cells release of insulin Metabolized inactive
TROGLITAZONE
Decreases insulin resistance
BIGUANIDES
METFORMIN Inhibiting gluconeogenesis Reduce hyperlipidemia (LDL, VDL, cholesterol, HDL) Not bound to serum protein Is not metabolized SE: hypoglycemic <<