Chandan Hypoglycemic Agent

hypoglycemic agents mainly the sulfonylureas which the most prescribed drug for combating the type II diabetes.

1. Hypoglycemic Agents
Chandan Kumar
Luqman College of Pharmacy.

2. Elementary Approach
Normal blood glucose Levels in human beings
ranges from 70-90 mg/ml.
Hyperglycemia is the condition in which the blood
glucose levels will be higher than the normal levels.
Hypoglycemia is the condition in which the blood
glucose levels fall below the normal range.
So Hypoglycemic agents are employed to treat
Hyperglycemia.

3. Hyperglycemia occurs due to high glucose levels and
this is due to chronic disorder characterized by Insulin
deficiency.
The deficiency of insulin is known as Diabetes.
Diabetes is a condition in which the body does not
produce or respond to insulin, which regulates the
sugar level in blood.

4. Overview of Diabetes
According to recent survey done by South Asian Cochrane
Network & I.C.M.R. states that 1/3 population of India will suffer
from Diabetes by year 2020.
Diabetes are broadly classified over 3 types:
Insulin dependent Diabetes/ Type I Diabetes.
Non Insulin dependent Diabetes/ Type II Diabetes.
Gestational Diabetes.

5. Non Insulin dependent / Type II Diabetes.
Type II Diabetes mostly occurs after the age of 40 yrs but people
can develop it at any age.
In type II at first pancreas keeps up the added body demand by
producing more insulin but with time it loses the ability to secrete
enough insulin in response to meals.
As it is non insulin dependent hence insulin exogenous
administration therapy does not effective. So Oral Hypoglycemic
Therapy is preferred.

6. Background of Hypoglycemic
Agents
Hypoglycemic Agents are better known as Oral Hypoglycemic
Agents.
These compound are referred as Sulfonylureas, a class of
compound.
Sulfonylureas are among the most widely prescribed
medication in the world.
Sulfonylureas are used to treat patients with Type II Diabetes.
These drugs are well absorbed orally in responsive Diabetic
Patient.

7. Generations of Sulfonylureas
First Generation:
First Generation Sulfonylureas compound became widely
available in year 1955.
First Generation Agents have longer half lives.
Examples: Acetohexamide, chlorpropamide,
tolazamide,tolbutamide.
Second Generation:
Second Generation Sulfonylureas were introduced in 1985.
Second Generation Agents have shorter half lives &are more
potent compared to First Generation
Examples: Glipizide, glyburide, & glimepiride.

8. Mechanism of Action of
Sulfonylureas
Sulfonylureas are likely to bind to ATP sensitive
Potassium channel receptors on the pancreatic cell
surface, reducing Potassium conductance & causing
depolarization of the membrane.
Depolarization stimulates calcium ion influx through
voltage sensitive calcium channels raising intracellular
concentration of calcium ions, which induces the
secretion of insulin.

9. Glipizide
Trade Names: Glucotrol {Tablets 5mg & 10mg}
Properties: It is an off white, odourless powder, insoluble in water
& alcohol but soluble in 0.1N NaOH.
Uses: It is used in the treatment of Type II Diabetes.
Dosage: 5mg/day to 15mg/day single dose should be taken
before breakfast.

10. Acetohexamide
Trade Names: Dimelor, Dymelor.
Properties: It is white, crystalline powder, insoluble in water &
slightly soluble in chloroform but soluble in alcohol.
Uses: Used in treatment of of Type II Diabetes.
Dosage: 5mg to 10mg per day.

11. Acetohexamide & Pregnancy
USFDA has given pregnancy category “C” to
Acetohexamide as its harmful effect is not known
clearly.
Hence it should not be given to pregnant and breast
nursing women without consulting to Doctor.

12. Chlorpropamide
Trade Names: Diabines {Tablets 100mg & 250mg}.
Properties: It is white, crystalline powder, insoluble in water &
slightly soluble in chloroform but soluble in alcohol.
Uses: It is employed for the management of Type II Diabetes
either alone or with combination of other Hypoglycemic Agents.
Dosage: Maintenance dose is usually 250mg once a day. Dose
should be adjusted in elderly persons as prolonged hypoglycemic
effect is been reported.

13. Chlorpropamide & Pregnancy
Chlorpropamide is not usually prescribed for pregnant women as
it may decrease Blood Glucose Level in foetus & cause birth
defects.
Insulin is generally used in pregnancy as it give better control.
Chlorpropamide passes into breast milk hence not recommended
to breast nursing mothers as it may cause low Blood Sugar Level
in baby.

14. References
Textbook of organic medicinal and pharmaceutical
chemistry by Wilson, O Gisvold.
Textbook of medicinal chemistry by O.V.K. Reddy.
Textbook of medicinal chemistry by Ashutosh Kar.
www.drug.com/sulfonylureas.
www.medicine.net/chlorpropamaide/article.

15. Thank You
Questions &
queries are
welcomed.