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oral hypoglycemic agents. Oral hypoglycemic agents. Biguanides Sulfonylureas α - glucosidase inhibitors Thiazolidinediones Prandial glucose regulator. Biguanides . Biguanides are derivatives of the antimalarial agent Chloroguanide. Which is found to have hypoglycemic action.

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oral hypoglycemic agents
Oral hypoglycemic agents
  • Biguanides
  • Sulfonylureas
  • α- glucosidase inhibitors
  • Thiazolidinediones
  • Prandial glucose regulator
biguanides
Biguanides
  • Biguanides are derivatives of the antimalarial agent Chloroguanide. Which is found to have hypoglycemic action.
  • The most commonly used member of biguanides is Metformin.
biguanides1
Biguanides
  • Indication:
    • Type 2 diabetes failed on diet
    • Metformin can be given alone or in combination with sulfonylureas or Insulin
biguanides2
Biguanides
  • Mode of action

Biguanides [Metformin] is an Antihyperglycemic and not Hypoglycemic agent.

    • It does not stimulate pancreas to secrete insulin and does not cause hypoglycemia (as a side effect) even in large doses.
    • Also it has no effect on secretion of Glucagon or Somatostatin.
biguanides3
Biguanides
  • Mode of action:
    • Decreases the intestinal absorption of CHO
    • Increases glucose uptake (GLUT 4)
    • Increases glucose utilization (glycogensynthase)
    • Increases glycolysis via anaerobic pathway (lactic acidosis)
biguanides4
Biguanides

Pharmacokinetics:

  • Metformin is well absorbed from small intestine, stable, does not bind to plasma proteins, excreted unchanged in urine.
  • Half life of Metformin is 1.5 - 4.5 hours, taken in three doses with meals
biguanides5
Biguanides

Side effects:

  • occur in 20-25 % of patients.
  • include.. Diarrhea, abdominal discomfort, nausea, metallic taste and decreased absorption of vitamin B12.
biguanides6
Biguanides

Contraindications

  • Patients with renal or hepatic impairment.
  • Past history of lactic acidosis.
  • Heart failure, Chronic lung disease.

.. These conditions predispose to increased lactate production which causes lactic acidosis which is fatal.

sulfonylureas
SULFONYLUREAS
  • SUs., have been discovered during the 2nd. World war (sulfonamide).
  • SUs are drugs that used orally to control blood glucose levels of type 2 diabetes.
sulfonylureas1
SULFONYLUREAS
  • Types:
    • First generation,
      • Chlorpropamide
      • Tolbutamide
    • Second generation,
      • Gliclazide
      • Glibenclamide
      • Glipizide
    • Third generation,
      • Glimepiride
sulfonylureas2
SULFONYLUREAS
  • Mechanism of action:
    • Pancreatic effect
    • Extra-pancreatic effect
sulfonylureas3
SULFONYLUREAS

Pancreatic effect:

  • Increase insulin release from pancreas
  • Suppress secretions of Glucagon
sulfonylureas4
SULFONYLUREAS
  • Extra pancreatic effect:
    • Increases the number of insulin receptors
    • Increases post-receptor insulin sensitivity
    • Increases glucolysis
    • Increases glycogen storage in muscle and liver
    • Decreases the hepatic output of glucose
sulfonylureas5
SULFONYLUREAS
  • Pharmacokinetics:
    • They are effectively absorbed from gastrointestinal tract.
    • Food can reduce the absorption of sulfonylurea.
    • Sulfonylureas are more effective when given 30 minutes before eating.
    • Plasma protein binding is high 90 – 99 % .. mainly bind to albumen.
sulfonylureas6
SULFONYLUREAS
  • Pharmacokinetics:
    • 1st generation members have short half lives.
    • 2nd generation is administered once, twice or several times daily.
    • 3rd generation is administered once daily.
sulfonylureas7
SULFONYLUREAS
  • Pharmacokinetics:
    • All sulfonylurea are metabolized by liver and their metabolites are excreted in urine with about 20 % excreted unchanged.
    • Sulfonylurea should be administered with caution to patients with either renal or hepatic insufficiency.
sulfonylureas8
SULFONYLUREAS

Adverse Reactions :

  • Very few adverse reactions [4 %] in the first generation and rare in the 2nd and 3rd generation.
  • SUs may induce hypoglycemia especially in elderly patients with impaired hepatic or renal functions-These cases of hypoglycemia are treated by I/V glucose infusion.
slide19

SULFONYLUREAS

Adverse Reactions :

  • First generation may induce other side effects as …nausea and vomiting & dermatological reactions

…These side effects are fewer in the 2nd generation and rare in the 3rd generation.

sulfonylureas9
SULFONYLUREAS

Drug interactions:

  • Some drugs may enhance or suppress the actions of sulfonylureas Either by affecting:
    • Their metabolism and excretion
    • The concentration of free sulfonylureas in plasma through competing them on plasma proteins.
drug drug interaction
NSAIDs

Salicylates

Sulfonamide

ß-blockers

Chloramphenicol

Diazepam

MAOI

Barbiturates

Thiazide and loop diuretics

Sympathomimetics

Corticosteroids

Oestrogen / Progesterone combinations

Drug – Drug interaction
sulfonylureas10
SULFONYLUREAS
  • Contraindications :
    • Type 1 DM
    • Pregnancy and Lactation.
    • Significant hepatic or renal failure.
glucosidase inhibititor
α Glucosidase Inhibititor

Acarbose

  • Indicated for type 2 diabetes
    • In addition with diet
    • In addition with other anti-diabetic therapies
acarbose glucobay
Acarbose (Glucobay)
  • Mode of action:
    • Poorly absorbed 1% (act locally in G.I.T.)
    • Inhibits α glucosidase, so inhibits CHO degradation
  • Dose:
    • 50mg to 100mg 3 times daily before meals
acarbose glucobay1
Acarbose (Glucobay)
  • Side effects:
    • Flatulence (77%)
    • Diarrhea
    • Abdominal pain (21%)
    • Decreased iron absorption
thiazolidenedione
Thiazolidenedione

Rosiglitazone

Pioglitazone

thiazolidenedione1
Thiazolidenedione
  • Mode of action:
    • Insulin sensitizer (increase insulin sensitivity in muscle, adipose tissue & liver)
    • They are not insulin secretagogues (Not insulin releasers)
thiazolidenedione2
Thiazolidenedione
  • Drawbacks:
    • They are not effective alone in case of severe insulin deficiency and should be combined with sulfonylurea or metformin or both
  • Side effects:
    • Hepatotoxicity
    • weight gain
    • Dyslipidaemia (increases LDL)
prandial glucose regulators meglitinide
Prandial glucose regulators (Meglitinide)
  • Example:
    • Repaglinide
  • Rational:
    • Fast acting, short duration non-sulfonylurea
    • Designed to minimize mealtime blood glucose peaks
repaglinide
Repaglinide
  • Mechanism of action:
    • Stimulation of pancreatic insulin release by closing ß-cells KATP channels
    • Very rapid onset of action and short duration (TMAX = 1 hour, metabolized by liver T1/2 = 70 minutes)
    • No hypoglycemic metabolites
repaglinide1
Repaglinide
  • Clinical efficacy:
    • Improves postprandial glycemia
    • Less effective in decreasing fasting blood glucose levels and HbA1C
  • drawbacks:
    • Fails to provides a stable 24 hours blood glucose control
    • Complicated dosage style (3-8 tablets/daily)
    • How to adapt the dosage to the meal volume?