COMPOSITION AND PRESENTATION: EFFIMET 500 TABLETS Composition: Each tablet contains Metformin HCl 500 mg Presentation: 10 Tablets x 20 Blisters EFFIMET 850 TABLETS Composition: Each tablet contains: Metformin HCl 850mg Presentation: 10 Tablets x 10 Blisters MECHANISM OF ACTION:
Metformin acts by increasing the sensitivity of liver, muscle, fat, and other tissues to the
uptake and effects of insulin. These actions lower the level of sugar in the blood. Unlike glucose-lowering drugs of the sulfonylurea class, e.g. glyburide, metformin does not increase the concentration of insulin in the blood and, therefore, does not cause excessively low blood glucose levels (hypoglycemia) when used alone.
It directly stimulates peripheral anaerobic glycolysis in tissues and increases glucose
removal from blood, Reduces hepatic gluconeogenesis, Slows glucose absorption from GIT and Reduces plasma glucagon levels.
INDICATION:
1. NIDDM (Non Insulin Dependent Diabetes Mellitus): When diet alone has failed,
2. MODY (Maturity Onset Diabetes of the Young) (Unstable cases): Combination with
insulin to give better and smooth blood glucose levels.
DOSAGE: 500 mg BD. Increase gradually at 1week intervals (depending on blood glucose levels and GIT discomfort) 850 mg twice to thrice times daily (depending on blood glucose levels).
Should be taken by mouth with meals. [Max: 3 gm/day] PHARMACOKINETICS:
Excreted by the kidneys as active compound.
ADVERSE EFFECTS: The most serious side effect is lactic acidosis. The symptoms of lactic acidosis are weakness, trouble breathing, abnormal heartbeats, unusual muscle pain, stomach discomfort, light- headedness and feeling cold. Patients at risk for lactic acidosis include those with reduced function of the kidneys or liver, congestive heart failure, severe acute illnesses, and dehydration. The most common side effect of metformin is gastrointestinal upset. This includes diarrhea, cramps, nausea and vomiting, anorexia, abdominal discomfort. Others include dizziness, confusion, sweating, rash, weakness, and Vitamin B12 malabsorption. Therefore, it is recommended to take with meals. CONTRAINDICATION:
1. Diabetic Coma 2. Renal or Hepatic disease
3. Alcoholism 4. CCF (Congestive Cardiac Failure)
DRUG INTERACTIONS:
Cimetidine, by decreasing the elimination of metformin from the body, can increase the
amount of metformin in the blood by 40 %. This may increase the frequency of side effects from metformin.
The other drugs are corticosteroids and oestrogens.
The diuretics reduce the Metformin effects.
The monoamine oxidase inhibitors and beta blockers increase the effects of Metformin.
ADVANTAGES:
Since, it is an insulin sparing agent; it does not increase weight or provoke
Has an advantage over insulin and sulfonylureas in treating hyperglycemia.
Can be used in combination with sulfonylureas in Type2 diabetes in which sulfonylureas
Metformin is the only anti-diabetic drug that has been proven to reduce the
complications of diabetes, as evidenced in a large study of overweight patients with diabetes (UKPDS 1998).
These drugs lower blood sugar primarily by causing more of the body's own insulin to be
released. It lowers the amount of sugar in your blood by helping your body respond better to its own insulin. It does not cause your body to produce more insulin. Therefore, it rarely causes hypoglycemia (low blood sugar) and it doesn't usually cause weight gain.
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Metformin is the only anti-diabetic drug that has been proven to reduce the
complications of diabetes, as evidenced in a large study of overweight patients with diabetes (UKPDS 1998).
These drugs lower blood sugar primarily by causing more of the body's own insulin to be
released. It lowers the amount of sugar in your blood by helping your body respond better to its own insulin. It does not cause your body to produce more insulin. Therefore, it rarely causes hypoglycemia (low blood sugar) and it doesn't usually cause weight gain.