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Oral Hypo-glycemic drugs
By Rinku meena
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.
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 .
SULFONYLUREASE
• INTRODUCTION
• A Sulfonamide derivative used for its
antibacterial effects in typhoid patients
produced hypo -glycemia.
• This observation led to the development of
sulfonylureas.
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.
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
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
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.]
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]
Meglitinide
• INTRODUCTION
• A class of agents includes repaglinide and
nateglinide. Although they are not sulfonylureas,
they have common action.
Mechanism of action;
• Their action is dependent on functioning
pancreatic B-cells.
• The meglitinides have a rapid onset and a
short duration of action.
Adverse Effects
• Hypo -glycemia
• hypersensitivity reactions
Biguanides
• METFORMIN the only currently available
biguanide
• It increases glucose uptake and utilization by
target tissues, thereby decreasing insulin
resistance.
Mechanism of action
• Suppresses hepatic gluconeogenesis
• Inhibit glucose absorption from the intestines
• Stimulate peripheral uptake of glucose in tissues
in the presence of insulin.
Biguanides
• Adverse effects;
• These are largely gastrointestinal.
• LONG TERM use may interfere eith vita. B12
absorption.
• Nausea
• diarrhea
Biguanides
• Pharmacokinetics;
• metformin is well absorbed orally, is not bound
to serum proteins
• it is not metabolized
• Excretion is via the urine.
Thiazlidenediones
• Also knows as;
• 1- PPRAs [ peroxisome prolifelator activated
receptores]
• 2- Glitazones
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
THANK YOU

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oral hypoglycemic drugs

  • 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.
  • 14. Adverse Effects • Hypo -glycemia • hypersensitivity reactions
  • 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
  • 18. Biguanides • Pharmacokinetics; • metformin is well absorbed orally, is not bound to serum proteins • it is not metabolized • Excretion is via the urine.
  • 19. Thiazlidenediones • Also knows as; • 1- PPRAs [ peroxisome prolifelator activated receptores] • 2- Glitazones
  • 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