Brand Name : GLUCUT
Generic Name : Metformin Hydrochloride
Preparations : 500 mg / 850 mg / SR 500 mg / SR 850 mg / SR 1 G Tablets
Pharmacological Category : Antidiabetic (Biguanide)

Mechanism of Action (MOA)
GLUCUT (Metformin) decreases blood glucose levels by decreasing hepatic glucose production, decreasing intestinal absorption of glucose and improving insulin sensitivity by increasing peripheral glucose uptake and utilization. These effects are mediated by the initial activation of AMP-activated protein kinase (AMPK), a liver enzyme that plays an important role in insulin signaling, whole body energy balance, and the metabolism of glucose and fats.

Pharmacokinetics

  • Absorption : Slowly and incompletely absorbed from the gastrointestinal tract
  • Bioavailability : About 50 to 60%
  • Plasma Half-life : 2 to 6 hours
  • Protein Binding : Negligible
  • Metabolism : Does not undergo metabolism
  • Elimination Half-life : 4 to 9 hours
  • Excretion : Urine (unchanged drug)

Indications and Dosage

  • Type 2 Diabetes Mellitus : Initially one tablet of GLUCUT 500 mg twice or thrice daily or one tablet of GLUCUT 850 mg once or twice daily with or after meals then gradually increased to GLUCUT 2 to 3 gm daily if necessary at intervals of at least 1 week; doses of GLUCUT 3 gm daily are associated with an increased incidence of gastrointestinal adverse effects.
    Modified Release Preparations : Initially one tablet of GLUCUT SR 500 mg once daily, may be increased in increment of GLUCUT SR 500 mg at intervals of at least 1 week to a maximum dose of GLUCUT 2 gm once daily with the evening meal.
  • PCOS (unlicensed) : Initially one tablet of GLUCUT 500 mg with breakfast for 1 week, then one tablet of GLUCUT 500 mg with breakfast and evening meal for 1 week, then GLUCUT 1.5 to 1.7 gm daily in 2 to 3 divided doses

Side Effects
Anorexia, nausea, vomiting, diarrhoea, taste disturbance, weight loss, impaired vitamin B12 absorption
RARE : Skin rashes, hypoglycemia

Contraindications

  • Hypersensitivity to metformin
  • Renal disease or dysfunction (serum creatinine level 1.5 mg per dL or above in male, 1.4 mg per dL or above in female or abnormal creatinine clearance) which may result from cardiovascular collapse (shock), acute myocardial infarction and septicemia
  • Acute or chronic metabolic acidosis, including diabetic ketoacidosis with or without coma
  • Metformin should be temporarily discontinued in patients undergoing radiologic studies.

Warnings / Precautions

  • Metformin is inappropriate for patients with diabetic coma, ketoacidosis, severe infection, trauma, or other severe conditions.
  • Metformin should not be given to patients with even mild renal impairment as metformin may predispose patients to lactic acidosis and renal function should be monitored throughout the therapy. Conditions associated with hypoxia, such as acute heart failure, recent myocardial infarction, or shock may increase the risk of lactic acidosis. Other conditions that may also predispose to lactic acidosis in a patient taking a biguanide include excessive alcohol intake and hepatic impairment.
  • Metformin should be temporarily stopped for examinations using contrast media.
  • Annual monitoring of vitamin B12 concentration is advised during long term treatment.

Drug Interactions

  • Alcohol may increase the risk of lactic acidosis as well as of hypoglycemia.
  • Metformin diminishes phenprocaumon activity.
  • With didanosine, stavudine and tenofovir fatal lactic acidosis has been reported.
  • Cimetidine increases plasma metformin concentration.

Pregnancy Category : B

Presentations
GLUCUT 500 mg : A box of 20 blisters, each blister of 10 tablets
GLUCUT 850 mg : A box of 10 blisters, each blister of 10 tablets
GLUCUT SR 500 mg : A box of 10 blisters, each blister of 10 tablets
GLUCUT SR 850 mg : A box of 10 blisters, each blister of 10 tablets
GLUCUT SR 1 G : A box of 10 blisters, each blister of 10 tablets