Glucophage is a widespread medication containing glimepiride and metformin. Showing good results in diabetes 2 mellitus treatment, this drug has also a number of specifications you will want to know before using it.

What Is Glucophage (Metformin)

Metformin is prescribed to patients who are treating diabetes II mellitus. The drug is not supposed to be treating diabetes but still can help you keep the blood sugar level down. Its effect is based on helping the body handle insulin, and, unlike other similar medications, metformin does not damage a patient’s kidneys and keeps the risks of diabetes complications relatively low. As a rule, Glucophage tablets are recommended in dosage as much as 500 mg (contained in one tablet) and have to go together with keeping the dietary recommendations and exercise.

Metformin 500mg tablets

What Is Metformin Used For

Glucophage belongs to the group of diabetes treating drugs and, basically, is used to increase the sensitivity to insulin. In a wider view, the substance hinders hepatic glucose production in the liver, keeps down its absorption, and makes the body more responsive to peripheral glucose uptake and use. The medicine is also often prescribed to women who suffer from the hormonal condition known in the medical world as Polycystic Ovarian Syndrome.

This medicine has to be prescribed by the doctor. Patients are also advised to measure their blood sugar level regularly without changing the dosage out of their own initiative.

Metformin Dosage

Doctors might define a different dosage of Glucophage, depending on a few factors. They include the medical history, the age, and the health condition of the patient. The common dose for an adult is 500 mg taken twice a day or 850 mg taken once a day during mealtime. Besides the common dose, there is a maximum metformin dosage allowed for patients with severe health conditions – 2550 mg once per day. The dosage must be discussed with the doctor. Many doctors start with instructing their patients to take the regular dose of 500 mg once per day but increase the metformin dosage till it reaches 2000 mg a day for maximum effect.

In case of an overdose, it is generally recommended to contact the doctor as soon as possible, not waiting for metformin side effects to show up. Missed doses, although, are simpler to tackle. A patient just has to take the dose as soon as he remembers to do it, except if it is already the time to take the next scheduled tablet. In the latter case, the patient is allowed to skip the missed dose. Caution: a patient should never attempt to compensate for the missed tablet by taking an extra dose. The medicine should never be taken before reading the leaflet with information for patients from a pharmacist.

Adult Dosage Forms & Strengths for Diabetes

In the therapy for controlling type 2 diabetes mellitus in adults, the initial metmorfin dosage makes 500 mg a day that, under the careful supervision of a doctor, can be increased to 2000 or 2550 g per day (taken in separate doses). Recommendations for extended release clarify that a dose should be increased no more than 500 mg per week with a maximum dose reaching 2000 mg a day.

The doctor prescribes the maximum metformin dosage of 2550 mg in case 2000 mg does not show results and adequate glycemic control is not achieved. The switch to immediate-release is also suitable in such cases. If the patient’s condition does not improve in 3 or 4 months, it is logical to intensify treatment.

Pediatric Dosage Forms & Strengths for Diabetes

Answering the common question about, ‘What is metformin dose for children?’ we advise you to consult the doctor first and read the patient information leaflet. However, there are general recommendations of metformin intake by children. Metformin is usually not prescribed to children under 10. The kids who are 10 years old or older can take Glucophage with the same goal as adults but in different doses. The medication will help them relieve insulin resistance that goes along with type 2 diabetes mellitus.

The strength of 500 mg is usually enough to take for children twice per day (with meals). The doctor should observe how the body tolerates metformin at the initial dose. Only after the doctor is sure that the medicine tolerability is good, the dose can be gradually titrated and reach no more than 2000 mg a day.

Immediate-release (10-16 years):

  • Initial dose: 500 mg every 12 hours.
  • Maintenance: increase by 500 mg every week (not more than 2000 mg in separate doses).

Immediate-release (17 and older):

  • Initial dose: 500 mg every 12 hours or 850 mg once a day with meals. Increase every 2 weeks.
  • Maintenance: 1500-2550 mg a day once a day with food.

Extended-release for children aged 10-16 is not established, and safety is not guaranteed.

Other Dosage Considerations

Glucophage must be used only as directed by your pharmacist or doctor. So before taking it, ask the doctor, ‘What is metformin used for, and what is the dose in my case?’

Every time a tablet is taken, you should drink a lot of liquid. Never crush or chew tablets, and don’t try to split them before swallowing (unless it was directed by the doctor). Regular Glucophage intake at the same time every day (along with the diet) can help you reach the best effect from the medication. Measure your blood sugar level before increasing or lowering the prescribed metformin dosage.

What Special Precautions Should You Follow?

There are certain conditions when metformin warnings are needed. The contraindications include the following.

  1. Being hypersensitive or allergic to one of the components present in the tablets.
  2. Suffering from anemia or other blood-related illnesses (consulting a doctor is recommended) since the medication might strongly change hematologic parameters or cause the red blood cells deficiency.
  3. Suffering from ailments of liver or kidneys (the medicine builds up lactic acid, which is undesirable for such patients).
  4. Chronic heart failure.
  5. Myocardial infarction.
  6. Pregnancy.
  7. Lactation (metformin changes the chemical composition of breast milk).
  8. Diabetic ketoacidosis (DKA).
  9. Renal disease.
    *In the case of different stages of renal disease, doses can be modified.

    Proposed use of metformin in renal disease

    eGFR* level
    >60 Maximum daily dose of 2,550 mg Monitor renal function annually
    45-60 Maximum daily dose of 2,000 mg Monitor renal function every 3-6 months Avoid in patients with rapidly decreasing renal function
    30-44 Maximum daily dose of 1,000 mg Check renal function every 3 months Do not initiate therapy (can continue patients who are on it)
    <30 Do not use

    *estimated glomerular filtration rate
    Note: Adapted from JAMA 2014;312:2668-75 and Diabetes Care 2011 ;34:1431-7.

  10. Metabolic acidosis.
    For more information about the possible risks of lactic acidosis, see the infographic below.
    Metformin mechanism of action

Before Taking Metformin

Since the details of taking the medication and the dosage heavily rely on what other drugs you are currently taking and other medical conditions that you have been dealing with, make sure your doctor knows it all. Tell them about all the drugs you use, including herbal products, prescription, and non-prescription medications, as well as reactions to them. Besides, ask your doctor about diet and exercise tips for you to maintain a good result.

If you are taking another anti-diabetes drug, strictly follow the physician’s recommendations for continuing or stopping treating.

It is never allowed to experiment with the goal to find out, ‘How does metformin work for me in bigger doses?’ Follow only the doctor’s directions, go through healthful diagnostics, check your blood sugar level on a regular basis, keep a record of the results, and always tell your doctor if they change in one or another direction.

During Pregnancy

The medicine is not recommended to use for pregnant women due to the numerous risks. Even though some sources claim it to be safe to use before and during pregnancy, there is little data about the safety and metformin interactions with the placenta. In addition, the first-line help in diabetes mellitus therapy is insulin. In separate cases, doctors might advise taking metformin along with insulin to take better control over blood sugar. But this is a good decision only if the benefits of metformin intake outweigh the hazards for a mother’s and child’s health.

Best Time to Take Metformin

If you are prescribed metformin, you might be wondering what the best time to take metformin to get good results is. As a rule, taking a tablet with food or after a meal is the most common way to reach the goal. If you are to take a few tablets a day, do it with the according number of meals. However, if you have to take only one pill per day, choose to do it in the morning with breakfast. Taking Glucophage on an empty stomach might be harder for the body to handle and even cause complications.

Metformin Side Effects

Glucophage side effects

Patients prescribed metformin may experience a range of side effects, especially at the start of the therapy or in the case of an overdose. Serious consequences of taking Glucophage might be revealed in anemia, blindness, lactic acidosis, liver or kidney function impairment, or hypoglycemia. These side effects are rare but if you notice the symptoms of any of them, give your doctor an emergency call.

The symptoms of hypoglycemia include:

Symptom Frequency
Weakness Commonly
Vomiting Rarely
Dizziness Rarely
Nausea Commonly
Changes of sight Rarely
Stomachache Commonly
Unusually fast or slow heartbeat Commonly
Headache Commonly

The mechanism of action of metformin can also cause other reactions.

Diarrhea

The uses of metformin are great to manage type 2 diabetes and prediabetes; still, it has a specific feature of working directly on the stomach that often results in diarrhea, nausea, and vomiting, which may come and go. Some individuals experience weight loss, gut discomfort, and a strange ‘metallic’ taste in one’s mouth, along with the described symptoms. This is why patients are recommended to start with low doses to avoid such unpleasant effects in the first few weeks.

Bloating

It was estimated that nearly 25 % of people taking metformin complain of too much gas, bloating, the loss of appetite (which often leads to weight loss), and belly pain. About 5% of them also have trouble with headaches. These might not be the most dangerous side effects, but they still cause much discomfort. If any of them turn in, doctors advise taking Glucophage with meals. Increasing the metformin dosage is allowed only at a very slow tempo under the doctor’s supervision.

Seeking worthy alternatives to metformin is another way to avoid these side effects. After a medical examination, lab appointments, and a talk with a doctor, you might be prescribed tablets such as Prandin, Dapagliflozin, Actos, or herbal medications with fewer aftereffects.

Indigestion

Stomach issues are common for the activity of metformin and other medications of the anti-diabetes drug class. The so-called syndrome of ‘upset stomach’ can be avoided if you take the tablets with the biggest meal of the day, ideally with breakfast or dinner. Here you should also be careful with dietary supplements and changes in the diet.

Heartburn

Through being a rare side effect, heartburn is a result of stomach irritation. Doctors say drinking a full glass of water and avoiding taking Glucophage while hungry can help eliminate the symptom.

Muscle Pain

Muscle pain together with sleepiness, breathing problems, chest discomfort, tummy ache, and fatigue is a set of lactic acidosis symptoms. If muscle pain is intense and goes together with the described effects, immediately contact the doctor.

Possible Glucophage Benefits

A few recent research, including one made at Howard University School of Pharmacy, have proven that Glucophage has a cardioprotective effect even for individuals with severe heart congestive failure. This makes it a good option for elderly people, especially considering the fact that the medication might also be neuroprotective, reducing the risks of getting dementia or stroke. To find out other research, read FDA updates on Glucophage.

Younger patients can also make the most of taking Glucophage. The researched agent can help women get pregnant even with the background of polycystic ovary syndrome. Some endocrinologists claim the medicine is also good at delaying the natural process of aging and old age-related illnesses. Protection from breast, prostate, and pancreatic cancer are also included in the list of possible benefits; however, further research is needed.

Interaction With Other Drugs

The area of studying how metformin behaves if combined with other medicines is still growing as new anti-diabetes agents appear. Among the most studied ones by 2022, here are the following ones.

Fluconazole Blood sugar level can reach lower marks in this case, so never use the two drugs together (until prescribed).
Amlodipine In this combination, the blood sugar level can get too low, causing severe dizziness, sweating, breathing disorders, headaches, and tremor. Always consult a doctor before combining the medicines.
Dexamethasone The use of any medicine that contains dexamethasone has a big chance of decreasing the use of metformin. Make sure your doctor is informed about the prior use of dexamethasone (its effect might stay for some time even after you stop taking it).
Ibuprofen / Diclofenac These types of drugs can also lower the results of taking Glucophage. Don’t take the medicine without consulting the pharmacist.
Digoxin This is a dangerous combination that often leads to lactic acidosis that finds reflection in symptoms like fainting, stomachache, slow heartbeat, breathing problems. Never take the medicines together without seeing a doctor first.

Metformin Warnings

Some other precautions tell patients who use Glucophage regularly to give up alcohol, and there is a solid reason why you should follow the warning. The point is that both alcohol and Glucophage tend to build up lactic acid, which is the reason of causing the medical condition known as lactic acidosis. This condition can be fatal. However, you can exclude it if you avoid overdose, don’t drink alcohol, and ensure your health condition is stable during the medicine intake.

Drugs Similar to Glucophage (Metformin)

All of the following medications are combination therapies containing metformin, which is the primary active ingredient in Glucophage. While each combination drug has a distinct mechanism of action due to the additional active ingredient, they all share the commonality of including metformin, which is a biguanide that primarily works by reducing hepatic glucose production, enhancing peripheral glucose uptake, and inhibiting intestinal glucose absorption.

  1. Metaglip (Glipizide-Metformin): Combines glipizide, a sulfonylurea, with metformin. Glipizide stimulates insulin secretion from pancreatic beta cells, complementing metformin’s actions to improve insulin sensitivity and reduce hepatic glucose output.

  2. Janumet (Sitagliptin-Metformin): Contains sitagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, along with metformin. Sitagliptin enhances insulin secretion and inhibits glucagon release, while metformin addresses insulin resistance and reduces hepatic glucose production.

  3. Kombiglyze XR (Metformin+Saxagliptin): Combines metformin with saxagliptin, another DPP-4 inhibitor. Similar to Janumet, saxagliptin works by increasing insulin secretion and inhibiting glucagon release, synergizing with metformin’s effects on glucose metabolism.

  4. Jentadueto (Linagliptin + Metformin): Includes linagliptin, yet another DPP-4 inhibitor, along with metformin. Linagliptin, like sitagliptin and saxagliptin, enhances insulin secretion and suppresses glucagon release, working in conjunction with metformin to improve glycemic control.

  5. Glucovance (Glyburide + Metformin): Combines glyburide, a sulfonylurea similar to glipizide, with metformin. Glyburide stimulates insulin secretion from pancreatic beta cells, while metformin addresses insulin resistance and hepatic glucose output.

  6. Galvumet (Vildagliptin + Metformin): Contains vildagliptin, another DPP-4 inhibitor, along with metformin. Vildagliptin enhances insulin secretion and inhibits glucagon release, working synergistically with metformin to improve glycemic control.

In summary, while these combination therapies incorporate different secondary agents with metformin, they all share the primary mechanism of action of metformin in improving insulin sensitivity, reducing hepatic glucose production, and enhancing peripheral glucose uptake. However, the additional agents provide supplementary mechanisms to further improve glycemic control, making them effective alternatives or adjuncts to Glucophage in managing type 2 diabetes mellitus.

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