2. INTRODUCTION
• An oral antidiabetics agents commonly used in
the treatment of type 2 diabetes mellitus.
• An oral hypoglycemic agents cannot be used as
monotherapy in pt. With type 1 diabetes mellitus
since these pt. Lack sufficent insulin.
3.
4. COMBINATIONS
What are Antidiabetic combnations ?
Antidiabetic combinations are medicines with two
or more classes of antidiabetic agent in one pill or
dose .
just having one pill may improve glycemic control .
5. SULFONYLUREASE
• INTRODUCTION
• A Sulfonamide derivative used for its
antibacterial effects in typhoid patients
produced hypo -glycemia.
• This observation led to the development of
sulfonylureas.
6. MECHANISM OF ACTION
• Sulfonylurease reduce the blood glucose level by:
1) Stimulating the release of insulin from the
pancreatic B-cells.
2) Increasing the sensitivity of peripheral tissues
to insulin.
3) Increasing the no. Of insulin receptors.
4) Suppressing gluconeogenesis in the liver.
7.
8. Adverse reactions
• Hypoglycemia
• Weight gain[1-3]
• Nausea and vomiting
• Cholestatic jaundice, agranulocytosis, aplastic and
hemolytic anemias
• Generalized hypersensitivity reactions
• CONTRA INDICATIONS
▫ Pregnancy, lactation
▫ Renal and hepatic impairment
9. DRUG INTERACTIONS
1. Drugs that increase hypo-glycemic effects.
• NSAIDs, warfarin, sulfonamides- displace
sulfonylureas from protein bindingmsites.
• Alcohol, chloramphenicol,cimetidine- inhibit
metabolism of sulfonylureas.
2. Druges that decrease the action of
sulfonylureas
• Diuretics and corticosteroids increase blood
glucose level
10. FIRST – GENERATION SULFONYLUREAS
Tolbutamide
Its half- life is relatively short [6 hours]
Is the safest sulfoylureas for use in elderly
Chlorpropamide
• Has a long half- life [32hr]
• Contraindicated in elderly patients
Tolazamide
• Comparable to chlorpropamide in potency but shorter
acting [half life 7 hr.]
11. Second GENERATION SULFONYLUREAS
• Glyburide
▫ Has few adverse effects other than hypoglycemia.
▫ Contraindicated in the presence of hepatic and
renal insufficiency.
• Glipizide
Has the shortest half-life[3hr]
Taken 30 min. Before meals
• Glimepiride
Has the lowest dose of any sulfonylurea [a single
daily dose of 1 mg]
12. Meglitinide
• INTRODUCTION
• A class of agents includes repaglinide and
nateglinide. Although they are not sulfonylureas,
they have common action.
13. Mechanism of action;
• Their action is dependent on functioning
pancreatic B-cells.
• The meglitinides have a rapid onset and a
short duration of action.
15. Biguanides
• METFORMIN the only currently available
biguanide
• It increases glucose uptake and utilization by
target tissues, thereby decreasing insulin
resistance.
16. Mechanism of action
• Suppresses hepatic gluconeogenesis
• Inhibit glucose absorption from the intestines
• Stimulate peripheral uptake of glucose in tissues
in the presence of insulin.
17. Biguanides
• Adverse effects;
• These are largely gastrointestinal.
• LONG TERM use may interfere eith vita. B12
absorption.
• Nausea
• diarrhea
20. Mechanism of action
• Increase insulin sensetivity in liver and muscle
• Do not increase insulin secretion
• Reduce hepatic glucose output
• improve lipid profile
• May induce weight gain