ANTIDIABETIC
DRUGS
Diabetes Mellitus
Metabolic disorder characterized
by hyperglycemia, glycosuria
Types: type I (IDDM)
type II (NIDDM)
Actions of insulin
Inhibits glycogenolysis
Inhibits gluconeogenesis
Promotes glycogen synthesis
Fat
+ glucose uptake
+ storage of TG
Inhibits lipolysis
Muscle
+ protein synthesis
+ glycogen synthesis
- Protein breakdown
1. Rapid acting
a. Lispro
b. Aspart
c. Glulisine
2. Short acting
a. Regular insulin
Insulin preparations
3. Intermediate acting
a. Insulin zinc suspension (lente)
b. Neutral Protamine Hagedorn (NPH)
4. Long acting
a. Glargine
b. Detemir
Insulin administration
All insulin
preparations are
administered
subcutaneously
Regular insulin can be
administered i.v & i.m also
1. Hypoglycemia
Treatment- oral glucose
50ml of 50% dextrose i.v
2. Local reactions
lipodystrophy, swelling, erythema
3. Allergy and resistance
Adverse effects of insulin
Oral Antidiabetic
Drugs
Classification
A. Stimulators of insulin release from pancreas
i) Sulfonylureas
Tolbutamide, chlorpropamide, glibenclamide,
glipizide, gliclazide, glimepiride
ii) Meglitinide analogue
Repaglinide
iii) D-phenylalanine derivative
Nateglinide
B. Inhibitors of hepatic neoglucogenesis
Biguanides - Phenformin, metformin
C. Drugs which reduces insulin resistance
Thiazolidinediones - Rosiglitazone
Pioglitazone
D. ∝ - Glucosidase inhibitors
Acarbose, Miglitol
Adverse effects of sulfonylureas
• Hypoglycemia
• Nausea, vomiting, diarrhoea, headache,
weight gain
• Hypersensitivity reactions
• Chlorpropamide - Cholestatic jaundice
Repaglinide & Nateglinide
• Rapid and short acting
• Low risk of severe hypoglycemia
Biguanides
Adverse effects
• Nausea, metallic taste, abdominal
pain, diarrhea
• Lactic acidosis
• Vitamin B12 deficiency
Thiazolidinediones
Adverse effects
Nausea, vomiting, anemia, weight gain,
fluid retention, hepatotoxicity (rare)
∝ Glucosidase inhibitors
Adverse effects
Flatulence, loose stools, abdominal
pain
Therapeutic uses
• Type II DM
• Alone or in combination with insulin
• Cannot be used for Type I DM

36.antidiabetic agents