Metformin, sold under the brand name Glucophage among others, is a diabetes medication used alone or with other medications, including insulin, to treat type 2 diabetes (condition in which the body does not use insulin normally and, therefore, cannot control the amount of sugar in the blood). Metformin is not used to treat type 1 diabetes (condition in which the body does not produce insulin and therefore cannot control the amount of sugar in the blood).
Over time, people who have diabetes and high blood sugar can develop serious or life-threatening complications, including heart disease, stroke, kidney problems, nerve damage, and eye problems. Taking medication(s), making lifestyle changes (e.g., diet, exercise, quitting smoking), and regularly checking your blood sugar may help to manage your diabetes and improve your health. This therapy may also decrease your chances of having a heart attack, stroke, or other diabetes-related complications such as kidney failure, nerve damage (numb, cold legs or feet; decreased sexual ability in men and women), eye problems, including changes or loss of vision, or gum disease. Your doctor and other healthcare providers will talk to you about the best way to manage your diabetes.
How Metformin works
Metformin is in a class of drugs called biguanides. Metformin helps to control the amount of glucose (sugar) in your blood. It decreases the amount of glucose you absorb from your food and the amount of glucose made by your liver. Metformin also increases your body’s response to insulin, a natural substance that controls the amount of glucose in the blood. The molecular mechanism of metformin is not completely understood. Multiple potential mechanisms of action have been proposed:
Inhibition of the mitochondrial respiratory chain (complex I), activation of AMP-activated protein kinase (AMPK), inhibition of glucagon-induced elevation of cyclic adenosine monophosphate (cAMP) with reduced activation of protein kinase A (PKA), inhibition of mitochondrial glycerophosphate dehydrogenase, and an effect on gut microbiota.
Metformin also exerts an anorexiant effect in most people, decreasing caloric intake. Metformin decreases gluconeogenesis (glucose production) in the liver. Metformin inhibits basal secretion from the pituitary gland of growth hormone, adrenocorticotropic hormone, follicle stimulating hormone, and expression of proopiomelanocortin, which in part accounts for its insulin-sensitizing effect with multiple actions on tissues including the liver, skeletal muscle, endothelium, adipose tissue, and the ovaries. The average patient with type 2 diabetes has three times the normal rate of gluconeogenesis; metformin treatment reduces this by over one-third.
How Metformin is used
Metformin comes as a liquid, a tablet, and an extended-release (long-acting) tablet to take by mouth. The liquid is usually taken with meals one or two times a day. The regular tablet is usually taken with meals two or three times a day. The extended-release tablet is usually taken once daily with the evening meal. To help you remember to take metformin, take it around the same time(s) every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take metformin exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.
Swallow metformin extended-release tablets whole; do not split, chew, or crush them.
Your doctor may start you on a low dose of metformin and gradually increase your dose not more often than once every 1–2 weeks. You will need to monitor your blood sugar carefully so your doctor will be able to tell how well metformin is working.
Metformin controls diabetes but does not cure it. Continue to take metformin even if you feel well. Do not stop taking metformin without talking to your doctor.
Ask your pharmacist or doctor for a copy of the manufacturer’s information for the patient.
What side effects can this medication cause?
This medication may cause changes in your blood sugar. You should know the symptoms of low and high blood sugar and what to do if you have these symptoms.
Metformin may cause side effects. Tell your doctor if any of these symptoms are severe, do not go away, go away and come back, or do not begin for some time after you begin taking metformin:
• diarrhea
• bloating
• stomach pain
• gas
• indigestion
• constipation
• unpleasant metallic taste in mouth
• heartburn
• headache
• flushing of the skin
• nail changes
• muscle pain
Some side effects can be serious. If you experience any of these symptoms, call your doctor immediately or get emergency treatment:
• chest pain
• rash.
Metformin may cause other side effects. Call your doctor if you have any unusual problems while taking this medication.
If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration’s (FDA) MedWatch Adverse Event Reporting program online (http://www.fda.gov/Safety/MedWatch) or by phone (1-800-332-1088).
