The document discusses various classes of hypoglycemic agents (drugs used to treat diabetes) including their classification, structure, uses, formulations, and brand names. It covers insulin and its preparations, as well as common oral hypoglycemic drugs like metformin, glibenclamide, glimepiride, pioglitazone, repaglinide, gliflozins, and gliptins. Diabetes is defined as persistent hyperglycemia that is divided into type 1, type 2, and gestational diabetes based on etiology and treatment approach. The mechanisms of action, pharmacokinetics and formulations of different classes of antidiabetic drugs are summarized.
2. Index
1. Hypoglycemic agents : Definition,
2. Diabetes mellitus- definition, types
[Study of the following category of medicinal compounds with
respect classification, chemical name, chemical structure
(compounds with * mark), uses, stability and storage
conditions, different types of formulation & their popular brand
names]
a) Insulin and Its Preparations, structure & types
b) Metformin*,
c) Glibenclamide*,
d) Glimepiride,
e) Pioglitazone,
f) Repaglinide,
g) Gliflozins,
h) Gliptins
3. The drugs which are used to lower blood sugar
are called hypoglycemic agents.
OR
The drugs which are used to treat diabetes are
called hypoglycemic agents.
used to treat Diabetes Mellitus.
Diabetes mellitus – persistent hyperglycemia.
4. Diabetes mellitus divided in two parts.
A) Type –I (IDDM) Insulin Dependant Diabetes Mellitus/
Juvenile – generally
occurs in children and adolescents
pancreatic B-cells are destroyed through an autoimmune
mediated reaction so that, pancreas is unable to produce
sufficient insulin to control the blood glucose level.
So, type-1 diabetes is called as insulin-dependent diabetes
mellitus (IDDM) or juvenile onset diabetes.
Insulin is essential.
5. b) Type-2 diabetes (T2D)/ (NIDDM) Non Insulin
Dependant Diabetes Mellitus/ Adult
onset or maturity onset :
It occurs more commonly in adults.
It is characterized by insulin resistance and called
as non-insulin-dependent diabetes mellitus
(NIDDM) or adult onset diabetes.
People with type-2 diabetes usually have a family
history of this condition.
treated by dietary modification, or by use of
oral hypoglycemic agent.
6. c) Gestational diabetes:
It involves high blood glucose level during
pregnancy an complication is associated with
both mother and child.
7.
8. Insulin & its preparation:
In 1920s, Frederick Banting and Charles Best
discovered insulin and demonstrated the
hypoglycaemic effect of an extract of pancreas.
Human insulin and insulin analogs are available for
insulin replacement therapy.
Insulin is a hormone, secreted by the beta cells of
pancreatic islets.
There are two polypeptide chains present in insulin
such as chain A and chain B.
Chain A has 21 amino acids and chain B has 30 amino
acids.
Both chains are linked together by two disulfide
bridges
(-s-s- bonds of cysteine).
Insulin facilitates the uptake of glucose by skeletal
muscle and adipose tissue by increasing the number of
glucose transporters (GLUT 1 and GLUT 4).
9.
10. TYPES OF INSULIN
Insulin's are classified based on the duration
of their action in body which include
a) fast acting
b) short acting
c) intermediate acting
d) long acting insulin.
11. a) Fast acting insulin: It is also called as rapid
acting insulin analogs.
It is absorbed quickly from fat tissue
(subcutaneous) into the bloodstream.
It is used to control the blood sugar during
meals.
This insulin analog have onset of action of 5 to
15 minutes, peak effect in 1 to 2 hours and
duration of action that lasts 4-6 hours.
The examples of rapid acting insulin analogs are
i) insulin Aspart, (Novolog)
ii) insulin Lyspro (Humalog):
ii) insulin Glulisine
12. (b) Short acting insulin:
It is considered as regular human insulin
(Humulin or Novolin).
It begins to lower blood glucose levels within 30
minutes.
It has peak effect in 2 to 4 hours and duration of
action of 6 to 8 hours.
This insulin is only approved to be administered
via IV. route.
It is obtained from Pork (porcine), beef (bovine)
or Human pancreas or genetically engineered
using rDNA technology from certain
microorganisms (E. coli)
13. (c) Intermediate acting insulin:
It is absorbed more slowly and lasts longer.
It is used to control the blood sugar overnight
while fasting and between meals.
Intermediate-acting insulin includes
1. (0) NPH human insulin
2. (ii) Insulin Zinc Suspension (Lente)
14. (d) Long-acting insulin: It is absorbed slowly with
minimum peak effect that lasts most of the day.
It is used while fasting and between meals.
Long acting Insulin
i) Detemir,
iii) Extended Insulin Zinc suspension (Ultra lente)
Iii) Insulin detemir
Stability & storage:
a) It is sensitive to heat & light.
b) So it is stored in tightly closed container at
temp below 8°C.
c) Insulin injection is stored in multidose
container at temperature between 2-8°C &
should not be allowed to freeze
15. Pharmaceutical Formulations :
1. Insulin injection IP.
2. Neutral insulin injection IP.
3. Biphasic Insulin injection IP.
4.Insulin Zinc Suspension IP.
Brand name: Humulin R, Novolin R, and Humulin R
U-500, Levemir.
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 hyperkalaemia
4. To treat severe ketoacidosis or diabetic coma.
17. Classification
1. Hormones:- e.g. INSULIN & its
derivative.
2. Oral Hypoglycemic Agent:-
a) Sulphonylureas: Glibencliamide*,
Glimepiride
b) Biguanides:- Metformin*.
c) Thiazolidinediones:- Pioglitazone
d) Meglitinides:- Repaglinide
e) SGLT2 inhibitors (Sodium-glucose
Cotransporter-2):- gliflozins
f) DPP-4 inhibitors (Dipeptidyl peptidase-
4) :- gliptins
18. 1. Metformin :
Molecular Weight: 165.6
Structure:
Chemical Name : 1, 1-Dimethylbiguanide
hydrochloride
19. 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.
Pharmaceutical Formulations :
1) Metformin tablets IP.
2) Metformin hydrochloride prolong release
tablets IP.
3) Metformin oral solution IP.
22. Storage: It is stored in well-closed containers.
Uses: It is used
1. To treat non-insulin dependent diabetes mellitus,
either alone with control diet or in combination
with biguanides.
2. As a substitute for other hypoglycemic agents
which cause undesirable side effect.
3. As a substitute for insulin in non-insulin
dependent diabetes mellitus.
Pharmaceutical Formulation:
1. Glibenclamide tablet IP.
23. Brand Names: Daonil, Euglucon, Diabeta,
Aviglen.
2. Glimepiride:
Storage and stability: Store protected from
moisture, a temperature not exceeding 30°C.
Uses: It is used in type 2 DM along with other
antidiabetics, to control rise blood glucose.
Pharmaceutical Formulations: Glimepiride
Tablets I.P.
Brand Names: Avandaryl, Duetact, Amaryl,
Glypride and Glimer.
24. 3. Pioglitazone:
Storage: It is stored well-closed containers
protected light and moisture.
Uses
1) Pioglitazone indicated type 2 DM, but not in
type 1 DM.
2) It reduces blood glucose without increasing
circulating insulin.
3) Pioglitazone primarily to supplement
SUs/metformin in case of insulin resistance.
Pharmaceutical Formulations :
1) Pioglitazone Tablets. I.P.
2) Pioglitazone Hydrochloride Tablets I.P.
Brand Names: Actos, Actoplus Met and
Duetact, Pionorm, Piorest.
25. 4. Repaglinide
Storage: It is stored in well-closed containers
protected from light and moisture.
Uses:
1) It is used only in selected type 2 diabetics
who suffer pronounced post prandial
hyperglycemia.
2) As an adjunct to diet and exercise to improve
glycemic control in adults with type 2 DM.
Pharmaceutical Formulations : Repaglinide
Tablet I.P.
Brand Names: Prandimet, Eurepa, Raplin and
Regan Enyglid, Gluconorm and Prandin.
26. 5. Gliflozins:
Uses:
1) It used for the treatment of type 2 diabetes
mellitus
2) Some time it can be used along with insulin
to treat type-1 diabetes.
Stability and storage conditions: It should
stored in cool dry place. The container is kept
tightly closed & protected from light.
Formulations: Gliflozins film coated tablet IP
Brand Names: Farxiga, Invokana,
27. 6. Gliptins:
Uses: These are indicated as adjunct to diet and
exercise to improve glycemic control in adults
with type 2 diabetes mellitus.
Stability and storage conditions: These are
stored in tightly closed container
Formulations:
1) Vildagliptin Tablet IP.
2) Sitagliptin Tablet IP.
Brand names: Eucreas, Galvus