Metformin FAQ
Its Use, Metformin Dosage, Metformin Side Effects, Metformin Contraindications, Metformin Pregnancy, Metformin Weight Loss, Metformin PCOS and other
What is Metformin?
It is the first-line drug for the treatment Type 2 Diabetes Mellitus because of its excellent safety profile, high efficacy to control blood sugar level and low cost.
Metformin belongs to which class?
Metformin belongs to ‘Biguanide Class’ of Antidiabetic or Antihyperglyceamic drugs.
What is the use of Metformin?
Metformin as an Antidiabetic agent:
Metformin reduces of blood glucose concentrations without causing overt hypoglycemia. It increases glucose uptake and use by target tissues, thereby decreasing insulin resistance. Unlike Sulfonylurea’s, Metformin does not promote insulin secretion.
Metformin in PCOS:
It is also used in women with polycystic ovarian syndrome. PCOS is an endocrine and metabolic disorder found among women of reproductive age, which is characterized by hyperandrogenism, ovulatory dysfunction. Metformin may make menstrual cycles more regular and increase fertility.
Metformin in Weight Loss:
It is also considered as weight management agent; however evidences are insufficient to indicate the use of Metformin for the treatment of overweight or obesity.
Metformin in Cancer:
Metformin is also proven to have anticancer activity.
Metformin as Cardioprotective agent:
Large number of diabetic patients dies because of cardiovascular complications. A number of clinical studies have shown that Metformin has cardioprotective effects. It also improves the cardiovascular disease risk in overweight diabetic patients.
How Metformin Works?
Metformin act on the liver to improve blood glucose levels. Given that gluconeogenesis is an energy intensive process (consuming six ATP equivalents per molecule of glucose synthesized). Hepatocytes need to balance the demand for ATP with supply.
Metformin accumulates within mitochondria of cells. In mitochondria it causes inhibition of the Complex I of the respiratory chain (conversion of ADP to ATP), and further suppresses ATP production.
Metformin also slows intestinal absorption of sugars and improves peripheral glucose uptake and utilization. Weight loss may occur because Metformin causes loss of appetite.
What is the Dosage of Metformin?
How much Metformin can be taken in a day?
| Sr. No. | Category | Type of Dosage | Initial Dose | Dose Titration | Maintenance Dose | Maximum Dose |
| 1. | Usual Adult Dose for Diabetes Type 2 | Immediate Release | 500 mg orally twice a day or 850 mg orally once a day | Increase in 500 mg increments weekly or 850 mg every 2 weeks as tolerated | 2000 mg/day in divided doses | 2550 mg/day |
| Extended Release | 500 to 1000 mg orally once a day | Increase in 500 mg increments weekly as tolerated | — | 2000 mg/day |
| Sr. No. | Category | Type of Dosage | Initial Dose | Dose Titration | Maintenance Dose | Maximum Dose |
| 2 | Usual Paediatric Dose for Diabetes Type 2 (10 Yrs & Older) | Immediate Release | 500 mg orally twice a day | Increase in 500 mg increments weekly as tolerated; daily dose should be taken in divided doses 2 to 3 times a day with meals | 2000 mg/day | |
| Extended Release | 500 mg orally once a day with evening meal | Increase in 500 mg increments weekly based on glycemic control and tolerability | 2000 mg/day |
What are the side effects of Metformin?
These are largely gastrointestinal, including diarrhoea, nausea, and vomiting. These effects can be alleviated by titrating the dose of Metformin slowly and administering doses with meals.
What is Metformin Lactic Acidosis?
Lactic acidosis occurs due to an increase in lactic acid can due to either an overproduction of lactate in the serum or an underutilization of lactate by the liver. Lactate is formed during gluconeogenesis as a product of pyruvate metabolism.
This formation requires the presence of the catalytic enzyme lactate dehydrogenase to convert nicotinamide adenine dinucleotide hydrate into nicotinamide adenine dinucleotide. Lactic acid in the serum is buffered by bicarbonate to lactate, which in turn is converted back to pyruvate in the liver and kidney.
Metformin-associated lactic acidosis can occur acutely in an overdose but typically has a more gradual onset in patients with hepatic or renal dysfunction due to decreased excretion. It often presents with nausea, abdominal pain, tachycardia, hypotension, and tachypnea.
When Metformin is contraindicated?
Metformin is contraindicated in renal dysfunction due to the risk of lactic acidosis. It should be discontinued in cases of acute myocardial infarction, exacerbation of heart failure, sepsis, or other disorders that can cause acute renal failure.
Metformin should be used with caution in patients older than 80 years and in those with heart failure or alcohol abuse.
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Is Metformin safe during Pregnancy?
Metformin is known to cross the placenta and concerns regarding potential adverse effects on both the mother and the fetus have limited its use in pregnancy. The use of Metformin during pregnancy is still a matter of controversy.
Is Metformin safe during Gestational Diabetes?
Several studies have suggested that Metformin is as safe and effective as insulin for the treatment of gestational diabetes. It has been suggested that the mothers who have used Metformin instead of insulin might be healthier in the neonatal period. However, evidence is still lacking on the long term safety of Metformin for both children and mothers.
How often to take Metformin for weight loss?
FDA has not yet approved Metformin as a weight loss agent. Weight loss from Metformin tends to occur gradually over one to two years. The amount of weight lost also varies from person to person.
Rather than taking such medicines, you must follow a sensible weight loss plan with healthy eating and physical activity to see any significant change in weight.
How Metformin is useful in Polycystic Ovary Syndrome (PCOS)?
Many PCOS patients suffer from insulin resistance and resulting hyperinsulinemia. Patients with PCOS are predisposed to many complications such as cardiovascular and cerebrovascular diseases, hypertension, metabolic syndrome, and also Type 2 Diabetes Mellitus.
Metformin has been used for PCOS treatment by which most of the metabolic abnormalities of PCOS can be reversed.
What are different Metformin Combinations?
Metformin & Glipizide
Rosiglitazone & Glimepiride
Pioglitazone & Metformin
Metformin & Glyburide
Rosiglitazone & Metformin
Pioglitazone & Glimepiride
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- Metformin FAQ : Use, Dosage, Side Effects, Contraindications, Pregnancy, Weight Loss, PCOS
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