Diabetes Insulin and its preparations Classification of Oral Hypoglycaemic agents

1. ORAL HYPOGLYCAEMIC AGENTS
PHARMACEUTICAL CHEMISTRY
D. Pharm 1st year
2023-2024
MISS NIKITA J. BHUTE
Assistant professor
Nagpur college of Pharmacy, Wanadogri,
Hingna road, Nagpur 441110.

2. INDEX
• Diabetes
• Insulin and its preparations
• Classification of Oral
Hypoglycaemic agents

3. Diabetes
• Diabetes is a disease state which impairs the body's ability to
maintain blood glucose level. It is characterized by
hyperglycemia that occurs due to the defects in the secretion and
action of the insulin.
Types of Diabetes
(a) Type-1 diabetes
It can develop at any age but
frequently occurs in children and
adolescents. In case of type-1
diabetes, 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.
(b) Type-2 diabetes
(T2D)
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.
(c) Gestational
diabetes
It involves high
blood glucose
level during
pregnancy and
the
complication is
associated with
both mother
and child.

4. Insulin
• 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 is a hormone produced in pancreas and permits the body to utilise
sugar (glucose) from carbohydrates in the food.
• Insulin restricts the blood sugar levels from getting too high
(hyperglycaemia) or too low (hypoglycaemia).

5. TYPES OF INSULIN
(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.
(a) Fast acting insulin
(i) Insulin Aspart
(Novolog)
It is similar to the
regular human insulin
except that proline is
replaced by aspartic
acid in position B28.
Its onset of action is
15 min, and the
duration of action is
2-4 hours.
(ii) Insulin Lispro
(Humalog)
It is human insulin analog
where the usual B28 Proline
and B29 Lysine is reversed
that means B28 and B29 are
Lys and Proline
respectively. Its onset of
action is 15 min. and the
duration of action is 2-4
hours.
(iii) Insulin glulisine
It is another insulin
analogue in which the
asparagine at position
B3 is replaced by lysine,
and the lysine at B29 is
replaced by glutamic
acid. Its onset of action
is 15 min. and the
duration of action is 2-4
hours.

6. (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 LV.
route.
• It is obtained from Pork (porcine), beef (bovine) or Human
pancreas or genetically engineered using rDNA technology
from certain microorganisms (E. coli).

7. (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.
(c) Intermediate acting insulin
(i) NPH human insulin:
It is called as isophane insulin suspension or neutral
protamine hagedorn (NPH) (Humulin N and Novolin N).
It is the sterile suspension of Zinc Insulin crystals and
Protamine sulfate. Protamine sulfate is a protein isolated
from the sperm of a fish (Onchorynchus Fam..
Salmonidae). It has an onset of insulin effect of 1 to 2
hours, a peak effect of 4 to 6 hours, and duration of
action is 10 to 16 hours. Very small doses will have an
earlier peak effect and shorter duration of action, while
higher doses will have a longer time to peak effect and
prolonged duration.
(ii) Insulin Zinc
Suspension (Lente):
It is the sterile
suspension of insulin
modified by the
addition of Zinc
chloride. Its onset of
action is 1 to 2 hours
and duration of
action is 10 to 16
hours.

8. (d) Long-acting insulin: It is absorbed slowly with a minimal peak
effect, and a stable plateau effect that lasts most of the day. It is used
to control the blood sugar overnight, while fasting and between
meals.
(d) Long-acting insulin
(i) Glargine (Lantus)
It differs from Human
insulin that asparagine at
position A21 is replaced
by Glycine and an
additional 30B-a-L-
ARGinine-30B-b-L-
arginine. It has onset of
insulin effect in 1 hour
30 minutes to 2 hours
and the duration of
action that lasts 24
hours.
(ii) Insulin detemir
It is another long-acting
insulin analogue that may
have some benefit over
isophane insulin. It is a neutral
soluble human insulin
analogue in which the
terminal amino acid at B30
has been replaced by myristic
acid, a 14-carbon fatty acid
chain. It has onset of insulin
effect in 2 hours and duration
of action lasts for 12-24 hours.
(iii) Extended
Insulin Zinc
suspension (Ultra
Lente)
It is a sterile
suspension of
insulin modified by
the addition of Zinc
chloride. Its onset
of action is 4 to 8
hours and duration
of tion is 36 hours.

9. • Insulin Combinations:
1) It is pre-mixed insulin in which NPH pre-mixed with either
regular human insulin or rapid acting insulin analog.
2) The insulin action profile is a combination of the short and
intermediate acting insulin.
3) The combination of either rapid or short acting insulin and
intermediate or long acting insulin is being used (except
Insulin Glargine which should not be used in combination
with any other types of insulin).

10. Insulin Preparations
Insulin Preparations Onset
of
Action
Peak
Time
Effective
Duration
of Action
Comments
Generic
Names
Trade
Names
Rapid-
Acting
Insulin
Aspart
NovoLog 5-10
minutes
1-3
hours
3-5 hours Eat within 5-10 minutes
of injecting.
Insulin
Lispro
Humalog <15
minutes
30-90
minutes
2-4 hours
Insulin
Glulisine
Apidra <15
minutes
30-90
minutes
60-150
minutes
Take from 15" before to
20" after starting a
meal. May only be
mixed with NPH.
Short-
Acting
Regular Humulin R
Novolin R
30-60
minutes
2-3
hours
3-6 hours Humulin R is also made
in U-500 strength. The
onset is slower than U-
100 and duration is up
to 24 hrs.
Intermed
iate-
Acting
NPH Humulin N
Novolin N
2-4
hours
4-10
hours
10-16
hours
Roll vigorously to mix.
Given once or twice
daily.

11. Insulin Preparations Onset of
Action
Peak Time Effective
Duration of
Action
Comments
Generic
Names
Trade
Names
Long-Acting Insulin
Glargine
Lantus 1 hour No peak 24 hours Do not put in the
same syringe with
any other insulin.
Usually given once
daily.
Detemir Levemir 1-2 hours No peak 6-23 hours,
depending on
dose
Combinations 70%
NPH+30%
Regular
Humulin
70/30
Novolin
70/30
30-60
minutes
There are 2
peaks: 2-3
hours and 4-
10 hours
10-16 hours
Roll vigorously to
mix. Do not put in
the same syringe
with any other
insulin.
70% Aspart
Protamine
+30% Aspart
Novolog
Mix
70/30
5-10
minutes
There are 2
peaks: 1-3
hours and 4-
10 hours
Eat within 5-10
minutes of injecting.
Roll vigorously to
mix. Do not put in
the same syringe
with any other
insulin.
50% Lispro
Protamine +
50% Lispro
Humalog
50/50
< 15
minutes
There are 2
peaks:30-90
minutes and
4-10 hours
75% Lispro
Protamine
+25% Lispro
Humalog
Mix
75/25

12. Classification of Oral Hypoglycaemic agents
Class Name of Drugs
Sulfonylureas 1st generation Acetohexamide, Chlorpropamide,
Tolazamide, Tolbutamide
2nd generation Glibenclamide/Gliburide, Glipizide
Gliclazide
3rd generation Glimepiride
Biguanides Metformin, Phenformin, Buformin
Meglitinides Repaglinide, Nateglinide, maglitinide
Thiazolidinediones Rosiglitazone, Pioglitazone, Ciglitazone
α-Glucosidase
inhibitors
Acarbose, Miglitol
Incretin agonists Exenatide, Liraglutide
SGLT2 inhibitors Canagliflozin, Dapagliflozin, Empagliflozin
DPP-4 inhibitors Sitagliptin, Vildagliptin, Saxagliptin
Miscellaneous Linogliride, Palmoxirate sodium
• Oral hypoglycemic agents are the medications that are administered
orally to reduce the blood glucose levels in diabetic patients.

13. THANK YOU