2. • Metformin (1,1-dimethylbiguanide), a biguanide
derivate and its chemical structure is related to
guanidine.
• First line oral therapy in the recent guidelines of
the American Diabetes Association
• Most widely prescribed drug to treat
hyperglycemia, at least 120 million user
worldwide.
• Insulin sensitizer
• Monotherapy & in combination with all
antidiabetic.
4. • Metformin was first prepared in 1922 by the Dublin chemists
Emil A. Werner and James Bell.
• Jean Sterne was the first to try metformin on humans for the
treatment of diabetes.
• He coined the name "Glucophage" (glucose eater) for the drug
and published his results in 1957.
• Metformin was introduced to the United Kingdom in 1958,
France in 1957, and Canada in 1972.
• US FDA approval in 1994!
History
6. • Decrease hepatic glucose
production through a mild
inhibition of the mitochondrial
respiratory-chain complex 1.
• Decrease intestinal absorption
of glucose
• anti-oxidative properties of
metformin on endothelial cells.
Mechanism of action
7. Pharmacokinetics
• Oral Medication
• Supplied in a regular-release form, oral suspension, and extended-
release form
• Doses range from 500mg-2000mg
• Absorbed through the GI tissue
• Excreted through the kidneys
• Is NOT metabolized by the liver
• Only special consideration is in the elderly
• Due to decreased renal function as people age
• Half-life: 6 hours in plasma and 17 hours in the blood system
8. .
• Helps your body to use insulin more normally
o Insulin controls your blood sugar
• Lowers how much sugar your body takes from food
• Lowers how much sugar your liver makes
9. Anti-obesity effects:
• Decreased appetite
• Increased GLP-1 secretion
Anti-hyperglycemic effects:
• Decreased intestinal carbohydrate absorption
• Inhibition of hepatic gluconeogenesis
• Enhancement of insulin-stimulated glucose transport
in skeletal muscle: increased activity of GLUT-4
Actions of metformin
10. Anti-lipidemic effects:
• Inhibition of lipolysis in adipose tissue
Anti-diabetic protective effects:
• Protection of β-cells from glucose toxicity and lipotoxicity
Hepatoprotective effects:
• Decreased hepatic insulin resistance
Cardioprotective effects:
• Cumulative effects of decreased weight gain and better lipid
profile
11. Drug Binding Issues
• Does not bind to the hepatic or plasma proteins in the
patient’s body
• Competes with other positively charged ions to get excreted
by the kidneys
• If unable to eliminate through a pathway in the kidneys,
medication remains in circulation in the kidneys which is
where damage can occur.
13. PCOS is a common endocrinopathy, 5 to 15% women .
• high levels of insulin
• Menstrual disturbance , Hyperandrogenism , polycystic ovary
on ultrasound.
• Insulin resistance, obesity
• Insulin sensitizer e.g. Metformin by alleviation of insulin
excess acting upon ovary and through direct ovarian effects.
Polycystic Ovary syndrome
14. Indications
Obese patients with type II diabetes
Alone or in combination with sulfonylureas
Contraindications
Hepatic impairment
Renal impairment
Alcoholism
Heart failure
15. Side Effect
1. Metallic taste in the mouth
2.Gastrointestinal (anorexia, nausea, cough, vomiting, diarrhea, abdominal
discomfort)
3. Vitamin B 12 deficiency (prolonged use)
4. Lactic acidosis ( rare – 01/ 30,000-exclusive in renal & hepatic failure)
5. Reduce appetite
6. Fatigue
17. Metformin Top 5
1. Why I am I taking metformin?
Metformin helps to control your blood sugar.
2. How should I take metformin?
You should take with metformin with food.
3. What are some common side effects of metformin?
Upset stomach, diarrhea, stomach cramping, headache
4. What are the severe side effects of metformin?
Lactic acidosis
5.Who may not be able to take metformin safely?
People with kidney disease, liver disease, alcoholism, or
people over 80 years old.
