INSULIN, ORAL HYPOGLYCEMIC AGENTS.pdfb.pjarm pharmacology

Oral hypoglycemia agent

1. INSULIN, ORAL
HYPOGLYCEMIC
AGENTS

2. DIABETES MELLITUS
1.Diabetes mellitus (DM) : is
a chronic metabolic disorder characterized by a
high blood glucose concentration –hyperglycemia
2.Hyperglycemia occurs due to the uncontrolled
hepatic glucose output and reduced uptake of
glucose by skeletal muscle with reduced glycogen
synthesis

4. TYPES OF DIABETES
MELLITUS
There are main 2 types of diabetes mellitus
1. TYPE 1 DIABETES
2. TYPE 2 DIABETES
1.TYPE 1 DIABETES : a) Previously known as the INSULIN DEPENDENT
DIABETES mellitus or juvenile-onset diabetes
b) Generally it occurs to the patients below age of 20
c) 15 to 20% suffer from type 1 diabetes mellitus

5. Continue..
d) In type 1 diabetes there is an absolute
deficiency of insulin resulting from autoimmune
destruction of βcells. Without insulin treatment
the such patients will ultimately die with diabetic
ketoacidosis
e) TYPE 1 diabetic patients are
(usually young children or
adolescents)

6. TYPE 2 DIABETES
1.Perviously known as non insulin
dependent diabetes mellitus-NIDDM or
maturity onset diabetes
2.generally this occurs to the patients above
40 yrs.
3.80-85% suffer from this type 2 diabetes
mellitus
4.treatment is initially one third of patients
ultimately require insulin

7. ORAL HYPOGLYCEMIC
AGENTS
•The agents that are given orally
to reduce the blood glucose level
in diabetic patients
•it is also known as oral anti
diabetic drugs

8. CLASSIFICATION
1.ORAL HYPOGLYCEMIC /ANTI
HYPERGLYCEMIC:
a) Sulfonyl urea derivatives:
First generation-eg. Tolbutamide
second generation-eg. Glipizide
b) Bioguanide-eg. Phenformin,
metformin
c) Thiazolidine_ eg. Pioglitazone
d) α-Glucosidase Inhibitors-eg. acarbose

9. CLASSIFICATION
2. PARENTERAL ANTI-DIABETIC
DRUGS-
a) INSULIN.

10. SULFONYL UREA
DERIVATIVES
1.Numerous sulfonylurea are available. The
first therapeutically were tolbutamideand
chlorpropamide
2.The sulfonylurea are of 2 types
1. first generation
2. second generation

11. MOA OF SULFONYL UREA
1.The principle of action od sulfonylurea is on β
cells, stimulating insulin secretion and thus
reducing blood glucose
2.high affinity for sulfonylurea are present on
KATP channels in beta cells
3.These drugs reduce the permeability of k+
and blocks the sulfonylurea receptors on ATP
sensitive k+ channels
4.The inhibition of k+ channel cause open of
voltage gate ca2+ channel
5.Reduced blood glucose level

12. THERAPEUTIC USES
1.IN TYPE 2 DIABETES MELLITUS
2.SURGERY DURING DIASBETES
3.IN DIABETES COMA
ADR: (ADVERSE DRUG REACTION)
1.WEIGHT GAIN
2.FLATULENCE

13. BIOGUANIDE
MOA ( MECHANISM OF ACTION OF BIOGUANIDE)
1.They increase glucose uptake in skeletal muscle
2.reduce hepatic and renal glucose gluconeogenesis
which reduce hepatic glucose output
3.It also promote insulin binding the receptor
4.beside decrease in level of glucose it also decrease
low density lipoprotein
5.all above action leads to antidiabetic effects

14. THERAPEUTIC USES
1.IN TYPE 2 DIABETIC MELLITUS
2.IN OBSES DIABETIC MELLITUS
3.SURGERY DURING DIABETES
4.IN DIABETES COMA
ADR: ADVERSE DRUG REACTION)
1.NAUSEA
2.DIARRHOEA

15. THIAZOLIDINE
MOA( MECHANISM OF ACTION)
1.Thiazolidine binds to nuclear receptor called
peroxisome proliferator activated receptor
2.thiazolidinedione cause the PPAR-RXR
complex to bind to DNA promoting transcription
of several genes with products that are
important in insulin signaling
3.these includes lipoprotein, fatty acid
transporter protein
4.it also cause reset of the glucose fatty acid
cycle by reduction in circulating free fatty acid

17. THREAPEUTIC USES
1.IN TYPE 2 DIABETES MELLITUS
2.IN OBESE DIABETES MELLITUS
3.SURGERY DURING DIABETES
ADR: ( ADVERSE DRUG REACTION)
1.WEIGHT GAIN
2.EDEMA

18. α-GLUCOSIDEASE INHIBITOR
MOA:( MECHANISM OF ACTION)
a) Acarbose an inhibitor is used in type 2 diabetes
patients whose diabetes is inadequately controlled by diet
b) it delays carbohydrate absorption, reducing the
postprandial increase in blood glucose
1.Carbohydrate
↓
Inhibits monossachsaridesynthesis
↓
Slow down absorption of monossacharidefrom GIT
↓
Anti diabetic action

19. THERAPEUTIC USES
1.USED IN TYPE 2 DIABETES MELLITUS
ADR: (ADVERSE DRUG REACTION)
1.DIARRHEA
2.ABDOMINAL PAIN
3.FLATULENCE

20. PARENTERAL ANTI
DIABETIC DRUGS
INSULIN:
1.Insulin was the first protein for which an
amino acid sequence was determined by
(sangers group in Cambridge in 1955)
2. it consist of two peptide chains (A and B )

21. PHARMACOLOGICAL
ACTION
▪EFFECT OF INSULIN ON
CARBOHYDRATE METABOLISM:
▪IN LIVER: 1. It influence glucose
metabolism in most of tissue, especially in
liver where it inhibits glyconeogenesis
2. it also inhibits gluconeogenesis
3. it also increase glucose utilization but
overall effect is to increase hepatic glycogen
stores

22. EFFECT OF INSULIN ON
PROTEIN METABOLISM
▪IN LIVER: 1. IT INHIBITS OXIDATION OF AMINO
ACID IN THE LIVER
2. It inhibits lipolysis partly via
dephosphorylation
3. it also inhibits lipolytic actions of adrenaline
by opposing their action on adenylate cyclase
OTHER METABOLIC EFFECTS:
1. Insulin increase transport of K+ and phosphate

23. THERAPEUTIC USES
1.Patients with type 1 and type 2 diabetes
mellitus
2.for gestational diabetes mellitus
3.For emergency treatment of diabetic
ketoacidosis
ADR: (ADVERSE DRUG REACTION )
1. HYPOGLYCEMIA
2. BLURRED VISION
3. OBESITY