Metamorphin

Metamorphin

1. Metformin

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.

3. Galega officinalis , a natural source of galegine

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 ! H istory

5. Glucophage Metformin Hydrochloride ER Glumetza Riomet Fortamet Glucophage XR Diamin Formin Met-500 Bigomet Popular Brands

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 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.

12. Metformin combination medications Glipizide/metformin (Metaglip) Linagliptin/metformin (Jentadueto) Pioglitazone/metformin (Actoplus Met) Repaglinide/metformin (Prandimet) Rosiglitazone/metformin (Avandamet) Saxagliptin/metformin (Kombiglyze XR) Sitagliptin/metformin (Janumet)

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

16. Therapeutic Perspective Gestational diabetes  Diabetes prevention   Regulation of circadian clock Metformin and pharmacogenetics

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.

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