Hypoglycemic
agent
Definition: The drugs
which are used to lower the blood sugar are called as hypoglycemic agents.
Classifications
of Hypoglycemic agent:
1. Hormones: e.g. Insulin
and its preparations
2. Oral
hypoglycemic agents:
a. Sulphonylureas:
e.g. chlorpropamide, Tolbutamide, Glibenclamide
b. Biguanides:
e.g. Phenformine, Metformin
3. Plant products:
guar gum
Insulin
• It is hormone produced by beta cell of islets of langerhans of
pancreas.
• It is polypeptide containing 51 amino acid arranged in two chains
namely A and B having 21 and 30 amino acid respectively.
• The two chains are connected by two disulphide bridges (-s-s bond
of cysteine) (source: pancreas of pig or Ox)
Properties of Insulin:
• It is white powder.
• It is slightly soluble in water
• It dissolve in dilute solution of mineral and acid
• It is inactivated by photolytic enzymes
• It is soluble in alkali hydroxide.
Stability and storage: it is sensitive to heat and light,
hence it is stored in well closed containers at room temperature below 8 degree
Celsius.
• Insulin injection is stored in multidose containers at room
temperature between 20 and 8 degree Celsius and should not be allowed to freeze.
• The label
on the containers should be bear
1. Number of unit per ml.
2. The animal source of insulin
3. Expiry date
4. Storage condition with precaution
that
a) It should not be allowed to freeze.
b) The containers should be shaken
gently before withdrawal of dose.
Uses of Insulin:
• To control diabetes mellitus or to
treat insulin dependent diabetes mellitus.
• To regulate carbohydrate metabolism.
• To treat gyperkalaemia.
• To treat severe ketoacidosis or coma
Pharmaceutical formulations of Insulin:
• Insulin injection
• Neutral Insulin injection.
• Biphasic Insulin injection
• Globin zinc Insulin injection
• Isophane Insulin injection
• Protamine zinc Insulin injection
• Insulin zinc suspension
Chlorpropamide
Structure
of Chlorpropamide
Chemical
name: N – (p-chlorobenzene sulphonyl)
N, -propyl urea.
Properties of Chlorpropamide:
• It occurs as white crystalline powder
which is odorless and tasteless.
• It is practically insoluble in water
• But soluble in alcohol and solution of
alkali hydroxide.
Storage: it is stored in well closed containers
Uses
of Chlorpropamide:
• To treat non -insulin dependent
diabetes mellitus
• Mild to moderate diabetes insipidus
Pharmaceutical formulations: ChlorpropamideTablets
Brand names: Diabetol, Diabetin, Chloroformin
Tolbutamide
Properties of Tolbutamide:
• It occurs as white crystalline powder
• It is odorless
• It is practically insoluble in water.
• Soluble in alcohol, sodium hydroxide,
dilute mineral acids.
Storage: stored in
well closed containers
Uses of Tolbutamide:
• To control blood glucose in previously
untreated non-insulin dependent diabetes mellitus.
• In treatment of diabetes mellitus when
blood glucose is unsatisfactory despite with diet.
• In conjugation with Metformin, if the
drug alone fail to control blood glucose level.
Dosage form: Tolbutamide
tablets
Brand names: Tolbutab, Rastinon
Phenformine
Structure of Phenformine
Chemical
names: 1-(2-phenyl ethyl) biguanidine
Properties of Phenformine:
• It is official as a hydrochloride
salt.
• It is white crystalline powder.
• It is odorless
• It has bitter taste.
• It is freely soluble in water.
• It is soluble in alcohol.
Storage: stored in well closed
containers
Uses of Phenformine:
• To treat non –insulin dependent diabetes mellitus.
• To reduce the blood sugar level in cortisone induced hyperglycemia.
• To reduce the blood cholesterol in maturity onset diabetes
Dosage forms: Phenformine Tablets
Brand names: Sucronase,
Bislim
Metformin
Properties of Metformin:
• It is hydrochloride salt.
• It is white crystalline powder.
• It is odourless.
• It has bitter taste.
• It is hygroscopic in nature.
• It is freely soluble in water.
• Practically insoluble in chloroform.
Stability and storage: it is
hygroscopic and hence it is stored in tightly closed containers.
Uses of Metformin:
• To treat non –insulin dependent diabetes mellitus.
• Insulin dependent diabetes mellitus in combination with insulin.
• Diabetes associated with Hyperlipoproteinemia.
• Obesity
Dosage forms: Metformin
tablets
Brand names: Diabex, Diaformin
Glibenclamide / Glyburide
Properties of Glibenclamide:
• It is white crystalline powder.
• It is odourless.
• It is very slightly soluble in water.
• It is sparingly soluble in chloroform.
Storage: stored in well closed
containers
Uses of Glibenclamide:
• To treat the non-insulin dependent diabetes mellitus, either alone or
with combination with controlled diet or in combination with biguanidine.
• As a substitute for other hypoglycaemic agent which cause undesirable side
effects.
• As a possible substitute for insulin in non-insulin dependent diabetes mellitus.
Dosage forms: Tablets
Brand names: Daonil,
Euglucon