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TRULY SITORUS
Depart. of Pharmacology & Therapy
Faculty Of Medicine Padjadjaran University
INSULIN & ORAL
HYPOGLYCEMIC
DRUGS
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It is a heterogeneous group of syndromes
all characterized by an elevation of blood
glucosecaused by a relative or absolute
deficiency of insulin.
Symptom:
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DMA. TYPE I (INSULIN DEPENDENT
DIABETES MELLITUS, IDDM) Absolute deficiency of insulin
Caused by massive -cell lesions or necrosis
Treatment: exogenous insulin
B. TYPE II (NON INSULIN DEPENDENTDIABETES MELLITUS, NIDDM)
Inability of -cell to produce appropriate
quantities of insulin Insulin resistance
Other unknown defects
Treatment: Hypoglycemic oral drugs insulin
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Insulin exogen
Beef
Pork
Human (by. E.colli, OOA
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MECHANISM OF ACTION
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PHARMACOKINETICS
Insulin p.o degradation
subcutaneous
IV: in hyperglycemicemergency
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ADVERSE EFFECT &
OVERDOSE TOXICITY
Hypoglycemia
Hypoglycemia brain damage !
Symptom of hypoglycemiaTachycardia
Confusion
Vertigo
Diaphoresis
Lipodystrophy
Hypersensitivity
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INDICATION
1. All patients with type I DMregardless of age
2. Patient who have ketoacidosis or hyperosmolar
coma
3. Patient with type II DM when diet restriction,
exercise and oral hypoglycemic agent havefailedto maintain satisfactory blood glucose
concentration
4. Patient with type II DMin presence of surgeryfever, infections, serious renal or hepatic
dysfunction, and other metabolic disturbances
5. Pregnantdiabetic women
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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.
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INSULIN PREPARATIONS
A. RAPID ACTION INSULIN
PREPARATION
Zinc insulin: sc
iv (in emergencies)
B. INTERMEDIATE ACTION INSULINPREPARATION
1. Semilente insulin suspension
2. Isophane insulin suspension
3. Lente insulin4. Insulin incombination
C. PROLONGED ACTION INSULINPREPARATION
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I. SULFONILUREAS
First generation
Tolbutamide, Chlorpropamide, Tolazamide
Second generation
Glipizide, Glyburide
II. BIGUANIDES
Metformin
III. GLUCOSIDASE INHIBITORS
AcarboseIV. REPAGLINIDE (?)
Repaglinide
V. THIAZOLIDINEDIONES
Troglitazone
ORAL HYPOGLYCEMIC AGENTS
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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
1stG : inactive, less active, active 2ndG: inert
Excreted by kidney or liver
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Side effect
Hypoglycemia (especially: chlorpropamide,
Glyburide)
Contraindication:
Renal or hepatic insufficiency
Pregnancy
Elderly
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INTERACTION
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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 proteinNot metabolized
Side effect: GI disturbance, hypoglycemic
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ACARBOSE
Inhibits glucosidase in intestinal
decreased the absorption of starch and
disaccharidesTaken with meals
Not cause hypoglycemia
Side effects: flatulencediarrhea
abdominal cramping
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REPAGLINIDE
Binds to the ATP- sensitive potassium
channels of cells release of insulin
Metabolized inactive
TROGLITAZONE
Decreases insulin resistance
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BIGUANIDES
METFORMINInhibiting gluconeogenesis
Reduce hyperlipidemia (LDL, VDL,
cholesterol, HDL)Not bound to serum protein
Is not metabolized
SE: hypoglycemic