3. WHO defined diabetes mellitus as “a state of
absolute or relative insulin deficiency,
characterized by hyperglycemia and the risk of
microvascular and macrovascular complications.”
4. Types of Diabetes
There are three main types of diabetes:
Type 1 diabetes: results from the body's failure to
produce insulin, and presently requires the
person to inject insulin.
Type 2 diabetes: results from insulin
resistance, a condition in which cells fail to use
insulin properly, sometimes combined with an
absolute insulin deficiency.
Gestational diabetes: is when pregnant
women, who have never had diabetes
before, have a high blood glucose level during
pregnancy.
6. Insulin ＆Synthesis
Fauci AS, Kasper DL, Braunwald E, Hauser SL, Longo DL, Jameson JL, Loscalzo J: Harrison’s
Principles of Internal Medicine, 17th Edition: http://www.accessmedicine.com
7. Insulin Receptor and Drugs
· The insulin receptor is a transmembrane receptor that
is activated by insulin.
· The main activity of activation of the insulin receptor
is inducing glucose uptake.
Metformin, sulfonylureas, nonsulfonylurea secretagogues,
alpha glucosidase inhibitors, and thiazolidinediones.
8. common medicines
SUs Metformin
t1/2: 5h t1/2: 6.2h
Side-effect: Hypoglycemia Side-effect: GI system
Weight gain Lactic acidosis
Metallic taste
Acarbose
TZDs
t1/2: 2h t1/2: 3-7h
Side-effect: Hypoglycemia Side-effect: GI symptoms
11. Victoza®
· Helps lower A1C level and lower blood sugar
· Helps keep beta cells in pancreas working
· Helps lose weight
· Easy to use
NovoTwist® NovoFine®
12. In Vitro Assays
• Liraglutide was tested for its receptor selectivity
in binding and functional assays comprising
more than 75 different receptors, ion-channels
and drug transporters.
• Enhancement of glucose-dependent insulin
secretion
• Sulfonylureas uncouple the glucose-dependency
of GLP-1 induced insulin secretion.
13. In Vivo Assays
• Liraglutide is a potent agonist on cloned
GLP-1 receptors from human as well as
mouse, rat, rabbit, pig and monkey.
• Liraglutide treatment of all animal models
of diabetes was characterized by a
consistent, acute, and dose-dependent
reduction in plasma glucose.
14. Clinical Data
• The efficacy and safety of liraglutide were assessed in
five double-blind, randomized, controlled clinical trials
involving a total of 3,978 patients with type 2 diabetes.
• PhaseⅠ: Liraglutide is reported to produce weight loss
and reduce food intake.
• Phase Ⅱ: The program was supported by evidence
from five phase Ⅱ trials.
• Phase Ⅲ: A population pharmacokinetic analysis from
the long-term phase 3 Trial 1573 (52-week
monotherapy trial).
16. Conclusion
• Diabetes Mellitus is a disease of
hyperglycemia
• Liraglutide: high effciency, low risk drug
• Diet, regular exercises, proper eating
habits can reduce diabetes
