Glucophage

Tablet Glucophage (Metformin) is an oral hypoglycemic agent (OHA) also called as Anti-diabetic drug (ADA)
Belongs to the class Biguanide. The only drug to be available in the market in this class is Metformin, the other drugs were with drawn due to its adverse effects in the patiets.
The IUPAC name of Metformin is N,N-dimethylimidodicarbonimidic diamide
The brand Glucophage is manufactured by the license of Bristol-Meyers Squibb  Pharma Co.
The other brands available or Metformin are Obimet, Diaformin, Diabex, Glumetza, Cetapin and fortamet etc etc…
This is an Insulin sensitizer.

Pharmacology

The formula of Metformin is C4 H11 N5
White crystalline compound
Soluble in water and not soluble in alcohol
50-60% bio-availability
The drug is heavily bound to the protein almost 99%
Metabolizes in Liver and is excreted through urine.
T ½ is 6 hrs.

Usage/ Indication and Dosage

Glucophage (Metformin) is the first medicine to be used in Diabetes Mellitus along with diet and life style modification
Glucophage is available in the following strengths
Glucophage 500 mg, Glucophage 850 mg, Glucophage 1000 mg
Also supplied as extende release form, Glucophage XR 500mg
The appropriate Dosage will be calculated by your physician
Can be used as mono therapy or in combination with Glitazones and sulfanylureas and DPPIV inhibitors (januvia) available as Janumet
As mono therapy Glucophage 500 mg  is started as once daily dosage, and up titrated to twice daily, in case of inadequate control Glucophage 850- 1000 mg can be used as once or twice daily regimen
Glucophage can also be used along with other OHAs and insulin
The maximum dose of Glucophage available now is 1gm

Metformin is also used in pre-diabetes condition to prolong the onset of full blown diabetes.

The other condition where metformin is widely used is Poly cystic ovarian disease PCOD/ PCOS, here the insulin resistance is higher, through some yet to be established mechanism, metformin rectifies PCOD.

There have been evidences that metformin improved No-alcoholic liver diseases.

There are studies on the use of metformin in pregnancy proving to be safe, so can be used in GDM

Mechanism Of Action

This is an insulin sensitizer, this decreases the hepatic glucose production, and breakdown of glucose, decreases the absorption of glucose in the GI tract, then sensitizes the insulin in the peripheral tissue, aiding the optimum utilization of glucose. There are reports showing improvement in cholesterol levels, the exact mechanism is not known.

Side/ Adverse effects of Glucophage, Glucophage XR / Metformin

Weight loss, Hypoglycemia, in a lesser extend compare to the SU, allergic reaction, headache, nausea GI disturbances like flatulence, abdominal bloatedness, indigestion and diarrhea. Least common is lactic acidosis.

Precaution and contra indication

To be used cautiously in patients with the following
-Patient with history of lactic acidosis
-Renal and Hepatic disorders
-Hospitalized patients, in chronic illnesses
-Fluctuating sugar levels
-?In pregnancy and lactation
-with contrast material injections

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