Oral Hypoglycemic Drugs
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Transcript Oral Hypoglycemic Drugs
Oral Hypoglycemic Drugs
Heider SH. AL-Qassam
MSc.PH. & TH.
Diabetes Mellitus
Chronic systemic disease characterized
by metabolic abnormalities
Disorder of carbohydrate metabolism
Results from inadequate production of
insulin
Diabetes Mellitus
Characterized by glucosuria and
hyperglycemia
Two forms—Type 1 and Type 2
Type 1—patient's βcells are destroyed
this willcause absolute insulin deficiency
Type 2 ــــpatient secretes insufficient
amounts of insulin and insulin receptors
are resistant to existent circulating
insulin
Oral Hypoglycemic Drugs
II. Insulin
Sensitizers
I. Insulin
Secretagogues
Sulfonylureas
Biguanides
Meglitinide
analogs
glitazones
III.α-Glucosidase
Inhibitors
IV.Dipeptidyl
Peptidase-IV
Inhibitors
V.Incretin Mimetics
I.Sulfonylureas
(mechanism of action) :
A. Increase release of insulin
B. Decrease production of glucose in the liver
C. Increase the number of insulin receptors
D. Effective only if have functioning beta cells
Primary side effect is hypoglycemia and weight
gain
These drugs include glibenclamide, glipizide,
and glimepiride .
II.Meglitinides
Nateglinide and repaglinide are nonsulfonylureas that
lower blood sugar by stimulating pancreatic secretion
of insulin
In contrast to the sulfonylureas, the meglitinides have
a rapid onset and a short duration of action
They are categorized as postprandial glucose
regulators
Monotherapy or in combination with metformin
Should be taken 1 to 30 minutes before a meal
Side effects hypoglycemia and weight gian
caution in patients with hepatic impairment
III.Biguanides
(mechanism of action): increases the use of glucose
by muscle and fat cells, decreases hepatic glucose
production, and decreases intestinal absorption of
glucose
Does not cause hypoglycemia
May be used alone or in combination
Side effects include GIT disturbance and lactic acidosis
Contraindicated in liver or renal impairment. Can
result in lactic acidosis.
This group include metformin
IV.Glitazones
(mechanism of action):Decrease insulin resistance.
Through binding with PPAR lead to regulation adipocyte
production and secretion of fatty acids as well as glucose
metabolism, resulting in increased insulin sensitivity in
adipose tissue, liver, and skeletal muscle
Side effects include weight gain, headache and anemia
Contraindicated in patients with liver disease and acute
MI
May be used as monotherapy or in combination with
insulin, metformin or a sulfonylurea
These drugs include Pioglitazone and rosiglitazone
Alpha glucosidase Inhibitors
Include acarbose and miglitol
(mechanism of action): inhibit alphaglucosidase enzymes (maltase, amylase,
sucrase) in GI tract. Delays absorption of
complex CHO and simple sugars
Can be combined therapy with sulfonylurea
Contraindicated in malabsorption, severe renal
impairment
Side effects include bloating and diarrhea
Incretin Mimetics
Exenatide is an incretin mimetic with a polypeptide
homologous to GLP-1
It is improves glucose-dependent insulin secretion
,slows gastric emptying time, decreases food intake,
decreases glucagon secretion, and promotes βcell
proliferation
It must be administered subcutaneously
Side effects include nausea, vomiting, and diarrhea
newOral Agents: Dipeptidyl
Peptidase-IV Inhibitors
Sitagliptin is an orally active dipeptidyl peptidase-IV
inhibitor used for the treatment of patients with
Type 2 diabetes
(Mechanism of action)
inhibits the enzyme DPP-IV, which is responsible for
the inactivation of incretin hormones, such as
glucagon-like peptide-1 (GLP-1).
Prolonging the activity of incretin hormones results
in increased insulin release in response to meals
Adverse effects include nasopharyngitis and
headache
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