Ms. Gunjegaonkar M.B. lecturer at SJVPM'S Rasiklal M. Dhariwal College of Pharmacy, Chinchwad, Pune This presentation is as per ER 2020

1. Hypoglycemic Agents
Prepared by, Ms. Gunjegaonkar M.B.
Lecture, SJVPM’S Rasiklal M. Dhariwal College of Pharmacy, Chinchwad,
Pune.

2. Diabetes Mellitus
Diabetes: persistent hyperglycemia, with glucosuria.
Factors:
• Heredity
• Immunology
• Age
• Stress
Either endogenous insulin is reduce or action of insulin is opposed.
Hypoglycaemic agents:
The drugs which are used to lower blood sugar level are called hypoglycemic agents.
They are used to treat diabetes mellitus

3. Types of DM
Type1: IDDM(Juvenile onset) develops in youth
Type2: NIDDM (maturity onset) middle age
Type3: MRDM malnutrition related
Type4: Secondary diabetes (Pancreatic disease)

4. Classification
1. Hormones: Insulin & its Preparation
2.Oral Hypoglycemic agent
• (a) Sulphonylureas,.
(i) First generation. e.g. Chlorpropamide, Tolbutamide, Acetohexamide
(ii) Second generation: e.g. Glibenclamide, Glipizide, Glimepiride
• (b) Biguanides e.g. Phenformine, Metformin.
• (c) Meglitinides: Repaglinide, Nateglinide.
• (d) Thiazolidinediones: Rosiglitazone, Pioglitazone.
• (e) Alpha glucosidase inhibitors e.g. Acarbose, Miglitol.
• (f) Dipeptidyl peptidase (DPP4): Sitagliptin.
• (g) Glucagon like peptide (GLP-1) analogoue: Exenatide.

5. INSULIN
• It is a hormone produced by beta-cells of islets of langerhans of pancreases. It is a
polypeptide containing 51 amino acids arranged in two chains, namely A & B having 21
& 30 amino acids respectively. These two chains are connected by two disulphide
bridges (-S-S-bonds of cysteine).
Source: pancreases of pig or ox.
• Porcine insulin differs from human insulin in only one amino acid in 'B' chain.
• Bovine insulin differs from human insulin in two amino acids in 'A' chain and one
amino acid in chain B.
• Human insulin is produced either by enzymatic modification of porcine insulin or by
use of DNA recombinant technology in micro-organisms so that amino acid sequence is
identical to that of human insulin.

6. INSULIN
Stability & storage:
• it is sensitive to heat & light. Hence stored in well-closed containers at a
temperature below 8°C. insulin injection is stored in Multidose containers at a
temperature between 2°C & 8°C. should not be allowed to freeze. The label on
the container should bear:
i. Number of units per ml.
ii. The animal source of insulin.
iii. Expiry date.
iv. Storage condition with precautions that:
a. It should not be allowed to freeze.
b. The container should be shaken gently before
withdrawal of dose.

7. INSULIN
• Uses:
• it is used:
1. To control diabetes mellitus (which is uncontrollable by diet alone) or to treat insulin
dependent diabetes mellitus.
2. To regulate carbohydrate metabolism.
3. To treat hyperkaliemia.
4. To treat severe ketoacidosis or diabetic coma.
• Pharmaceutical formulations:
1. Insulin injection.
2. Neutral Insulin injection
3. Biphasic Insulin injection
4. Globin zinc Insulin injection
5. Isophane Insulin injection
6. Protamine zinc Insulin injection
7. Insulin zinc suspension (mixed or amorphous or crystalline).

8. Metformin
• Structure:
• Chemical Name :
1, 1-Dimethylbiguanide hydrochloride.
It is the only biguanides derivative available therapeutically as Phenformine and
buformin have been withdrawn because of their high risk of inducing lactic
acidosis.

9. Metformin
Stability and Storage :
• It is hygroscopic and hence it is stored in tightly-closed containers.
Uses:
• It is used to treat
• 1. Non-insulin dependent diabetes mellitus.
• 2. Insulin dependent diabetes mellitus in combination with insulin.
• 3. Diabetes associated with hyperlipoproteinaemia.
• 4. Obesity.

10. Metformin
• Pharmaceutical Formulations :
• Metformin tablets LP.
• Metformin hydrochloride prolong release tablets I.P.
• Metformin oral solution L.P.
Brand Names:
Diabex, Diaformin, Glycomet, Gylyciphage

11. Glibenclamide (Glyburide)
• It is a second generation most potent on weight basis.
Storage:
• It is stored in well-closed containers.
Uses:
• It is used
• 1. To treat non-insulin dependent diabetes mellitus, either alone with
controlled diet or in combination with biguanides.
• 2. As a substitute for other hypoglycemic agents which cause
undesirable side effects.
• 3. As a possible substitute for insulin in non-insulin dependent
diabetes mellitus.

12. Glibenclamide (Glyburide)
• Pharmaceutical Formulation :
• Glibenclamide tablet.
• Brand Names:
• Daonil, Euglucon.

13. Glimepiride
• It is very similar to glipizide with the exception of their heterocyclic rings. Instead of
the pyrazine ring found in glipizide, glimepiride contains a pyrrolidine system.
Glimepiride is sometimes classified as a third-generation molecule, but structurally,
there is no real basis for this distinction.
Uses:
It is used in type 2 DM along with other antidiabetics, to control rise in blood glucose.
Storage:
Store protected from moisture, at a temperature not exceeding 30°C.
Pharmaceutical Formulations :
• Glimepiride Tablets I.P.
Brand Names:
• Avandaryl, Duetact, Amaryl, Glypride and Glimer.

14. Pioglitazone Hydrochloride
Uses:
(i) Pioglitazone is indicated in type 2 DM, but not in type 1 DM.
(ii) It reduces blood glucose without increasing circulating insulin.
(iii) Pioglitazone is primarily used to supplement SUs/metformin and in case of insulin
resistance.
Storage:
It is stored in well-closed containers protected from light and moisture
Pharmaceutical Formulations :
• (i) Pioglitazone Tablets I.P.(ii) Pioglitazone Hydrochloride Tablets.
Brand Names:
• Actos, Actoplus Met and Duetact, Pionorm, Piorest.

15. Repaglinide
This meglitinide analogue oral hypoglycemic analogue, Repaglinide has a rapid onset and a
short duration of action. It is administered before each major meal to control postprandial
hyperglycemia; the dose should be omitted if a meal is missed.
Storage:
It is stored in well-closed containers protected from light and moisture.
Uses:
(i)It is used only in selected type 2 diabetics who suffer pronounced post prandial
hyperglycemia
(ii) As an adjunct to diet and exercise to improve glycemic control in adults with type 2
diabetes mellitus.

16. Repaglinide
Pharmaceutical Formulations :
• (i) Repaglinide Tablet I.P.
Brand Names:
• Prandimet, Eurepa, Raplin and Regan Enyglid, Gluconorm and Prandin.

17. Gliflozins
Dapagliflozin is a sodium-glucose cotransporter 2 inhibitor used in the management of
type 2 diabetes mellitus. Dapagliflozin is indicated to improve glycemic control in adult
patients with type 2 diabetes mellitus along with diet and exercise.
Storage:
It is stored in cool and dry place in tightly closed containers protected from light.
Uses:
(i) Used for glycemic control in adult patients with type 2 diabetes.
(ii) Some time used together with insulin to treat type 1diabetes.
(iii) It is also indicated to reduce the risk of cardiovascular death in adult patients with
both type 2 diabetes mellitus and established cardiovascular disease.
(iv) In combination with metformin for type 2 diabetes.

18. Gliflozins
Pharmaceutical Formulations :
Tablet, film coated.
Brand Names:
Glyxambi, Jardiance, Synjardy, Trijardy

19. Gliptine
Sitagliptin is an oral dipeptidyl peptidase-4 (DPP-4) inhibitor used for the managementof
type 2 diabetes mellitus, Sitagliptin is an anti-diabetic drug that works by increasing the
levels of natural substances called incretins.
Incretins help to control blood sugar by increasing insulin release, especially after a meal.
They also decrease the amount of sugar your liver makes.
Storage:
It is stored in tightly closed containers protected from light.
Uses: Used for glycemic control in adult patients with type 2 diabetes.
Pharmaceutical Formulations : Gliptine Tablet
Brand Names:
Janumet, Januvia, Ristaben, Steglujan, Tesavel, Velmetia, Xelevia.