MEGAMET

Each uncoated sustained release tablets contains:

(Metformin Hydrochloride IP 500 mg/ 850 mg / 1000mg)

Tablet for Oral Use

Metformin decreases blood glucose levels by decreasing hepatic glucose production (also called gluconeogenesis), decreasing the intestinal absorption of glucose, and increasing insulin sensitivity by increasing peripheral glucose uptake and utilization. It is well established that metformin inhibits mitochondrial complex I activity, and it has since been generally postulated that its potent antidiabetic effects occur through this mechanism. The above processes lead to a decrease in blood glucose, managing type II diabetes and exerting positive effects on glycemic control.

Absorption: Absorption is complete within 6 hours. The absolute oral bioavailability of the drug under fasting conditions is reported to be approximately 50–60% with metformin hydrochloride doses of 0.5–1.5 g. Food decreases and slightly delays the absorption of metformin conventional tablets.

Distribution: The apparent volume of distribution (V/F) of Metformin after one oral dose of Metformin 850 mg averaged at 654 ± 358 L

Plasma Binding: Negligible

Metabolism: Metformin is excreted as unchanged drug in the urine and does not undergo hepatic metabolism. After oral administration, about 90% of absorbed Metformin is eliminated by the kidneys within the first 24 hours post-ingestion.

Half Life: The plasma elimination half-life of Metformin is 6.2 hours in the plasma. The elimination half-life in the blood is approximately 17.6 hours, suggesting that the erythrocyte mass may be a compartment of distribution

• Along with diet &exercise, for the management &treatment of Type 2 Diabetes.
• Gestational diabetes
• Management of antipsychotic-induced weight gain
• The treatment and prevention of polycystic ovary syndrome (PCOS)

ADVERSE REACTION

Gastrointestinal side effects, including diarrhea, nausea, and vomiting, are very common and typically occur in up to 30% of patients taking Metformin. Occurring less frequently, some patients experience chest discomfort, headache, diaphoresis, hypoglycemia, weakness, and rhinitis. Decreased vitamin B12

levels are associated with long-term Metformin. Metformin has a black box warning for lactic acidosis.

DOSAGE AND ADMINISTRATION:

Treatment of Diabetes Mellitus type 2: The initial dose of 500 mg once or twice a day or 850 mg once a day. The daily dose is often titrated weekly in increments of 500 mg or 850 mg to reduce GI adverse effects. The typical maintenance dose is 850mg or 1000 mg twice a day.

Treatment of Antipsychotic-induced Weight Gain: The initial dose of 750 mg up to 2000 mg is recommended in two to three divided doses.

Treatment of Gestational Diabetes Mellitus: The initial dose of 500 mg once or twice a day is recommended. Then, it may increase up to 2000 mg – 2500 mg in two to three divided doses to achieve the glycemic targets.

Treatment of Oligomenorrhea due to PCOS: The initial dose of 500 mg once or twice a day. The daily dose is often titrated weekly in increments of 500 mg to minimize GI adverse effects.

CONTRAINDICATIONS: Hypersensitivity to Metformin, in patients with Chronic Kidney Disease, Heart Failure, Respiratory insufficiency, Hepatic cirrhosis.

WARNINGS AND PRECAUTIONS:

• Monitoring renal function is needed to aid in the prevention of lactic acidosis, especially in the elderly
• Metformin is present in breast milk. Breastfeeding is generally acceptable till the relative infant dose is below 10 mg per kg per day.

Pregnancy Category: B

Drug Interaction: Increased hypoglycemic effect with androgens, alpha-lipoic acid, salicylates, selective serotonin reuptake inhibitors, quinolones, prothionamide, pegvisomant, and other antidiabetic agents.

Increase the risk of developing lactic acidosis with bupropion, carbonic anhydrase inhibitors, cephalexin, cimetidine, dolutegravir, ethanol, glycopyrrolate, iodinated contrast agents, lamotrigine, ranolazine, and topiramate.