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Metformin

Metformin is an FDA-approved antidiabetic medicine containing the active ingredient Metformin Hydrochloride. It is one of the most commonly prescribed medications for type 2 diabetes. It works by lowering blood sugar levels in the body. Metformin helps the body respond better to insulin, a hormone that regulates blood sugar. It is available in tablet form and is taken orally. You may also experience stomach upset, diarrhea, and, in rare cases, lactic acidosis (an accumulation of lactic acid in your bloodstream). The most effective results can be achieved when Metformin is taken according to instructions and a healthy lifestyle is followed.

Product Overview

Metformin is an oral medication with the active ingredient Metformin Hydrochloride, used to treat type 2 diabetes mellitus. It helps lower blood sugar levels by decreasing glucose production in the liver and improving insulin sensitivity in the body’s cells. It is typically used as a first-line treatment for type 2 diabetes, either alone or in combination with other antidiabetic medications. It is taken orally as tablets or extended-release tablets, usually once or twice daily, with meals to reduce the risk of gastrointestinal side effects. 

The dosage of Metformin varies depending on individual factors such as age, kidney function, and blood sugar levels. It is usually started at a low dose and gradually increased to achieve optimal blood sugar control. The typical starting dose for adults is 500 mg to 1000 mg, taken once or twice daily with meals. Extended-release formulations may be taken once daily. Dosage adjustments may be necessary for elderly patients or those with kidney impairment.

Metformin is generally considered safe and well-tolerated. However, it may cause side effects such as gastrointestinal upset (e.g., diarrhea, nausea, abdominal discomfort), which can often be minimized by taking the medication with meals or using extended-release formulations. Rare but serious side effects may include lactic acidosis. Regular monitoring of blood sugar levels and periodic medical check-ups are recommended to ensure the safe and effective use of Metformin for diabetes management.

Uses of Metformin

  • Metformin is primarily used for the treatment of type 2 diabetes mellitus. 
  • It may also be prescribed off-label for the conditions like Polycystic Ovary Syndrome (PCOS) symptoms, weight loss, and gestational diabetes.

How to Use Metformin?

Dosage

Forms and Strengths

Metformin is available in various forms and strengths:

  • Immediate-release (IR) tablets (available in strengths ranging from 500 mg to 1000 mg)
  • Extended-release (ER) tablets (available in strengths ranging from 500 mg to 1000 mg)
  • Metformin is also available in a liquid solution for those who have difficulty swallowing tablets. The liquid form is typically available in a concentration of 500 mg/5 mL.
  • Metformin is sometimes combined with other diabetes medications, such as sulfonylureas or DPP-4 inhibitors, to enhance its effectiveness. 

The dose of Metformin will vary from patient to patient and these are the average doses for this medicine. Make sure you follow your doctor’s instructions if your dose is different.

Recommended Dosage for Type 2 Diabetes

Standard Adult Dose for Type 2 Diabetes

  • Immediate-Release: The initial dose is 500 mg orally twice a day or 850 mg orally once a day. It can be increased weekly by 500 mg or every 2 weeks by 850 mg as tolerated. A maintenance dose of 2000 mg/day should be taken in divided doses. The maximum daily dose is 2550 mg.
  • Extended-Release: The initial dose should be 500 to 1000 mg taken orally once daily. Gradually increase the dose to 500 mg increments every week as tolerated. The maximum daily dose is 2000 mg.
  • Switching to Extended-Release: When receiving immediate-release, patients may switch to extended-release once a day at the same total daily dose (up to 2000 mg).

Standard Pediatric Dose for Type 2 Diabetes (10 Years or Older)

  • Immediate-Release: The initial dose is 500 mg taken twice daily. During dosage titration, doses should be increased by 500 mg each week as tolerated. Take daily doses with meals two to three times per day in divided doses. The maximum daily dose is 2000 mg.
  • Extended-Release Oral Suspension: The initial dose is 500 mg orally once a day with dinner. The dose should be titrated in 500 mg increments based on glycemic control and tolerability. The maximum daily dose is 2000 mg. Ensure that you titrate slowly to minimize side effects on your gastrointestinal system.

Additional Dosage Information

  • Kidney Disease (Renal Impairment): Metformin dosage based on estimated glomerular filtration rate (eGFR):
    • If eGFR ≥ 60 mL/min/1.73 m², dosage adjustment is not required.
    • If eGFR 45-59 mL/min/1.73 m², use with caution; monitor renal function closely. The maximum daily dose is typically reduced to 1000-1700 mg.
    • If eGFR is 30-44 mL/min/1.73 m², Metformin should be avoided due to the increased risk of lactic acidosis.
    • If eGFR < 30 mL/min/1.73 m², Metformin is contraindicated due to the risk of lactic acidosis. In some cases, Canadian pharmacy Metformin extended-release formulations may be preferred because they may be better tolerated in patients with renal impairment.
  • Liver Disease (Hepatic Impairment): A liver problem can increase the risk of lactic acidosis. The use of Metformin may not be recommended if you have liver problems. However, the use of Metformin in those with liver issues should be decided on an individual basis, weighing the potential benefits against the risks.

How to Take It?

Immediate-Release Formulation 

It should be taken two to three times each day with meals. Titrate slowly to minimize side effects on the gastrointestinal tract. Generally, significant responses do not occur with doses below 1500 mg per day, and doses above 2000 mg are associated with little additional efficacy and poorer tolerability.

Extended-Release Formulation 

Swallow ER tablets whole; do not crush, cut, dissolve, or chew them. Take once a day with dinner; if glycemic control is not achieved with 2000 mg twice a day, divide the dose to 1000 mg twice a day; if it is still not achieved, switch to immediate-release tablets. 

When using ER oral suspension, measure the dose in the provided dose cup and shake well for at least 10 seconds before each use.

How Does Metformin Work?

Metformin works primarily by decreasing glucose production in the liver and improving insulin sensitivity in peripheral tissues. It activates AMP-activated protein kinase (AMPK), a cellular enzyme that regulates energy metabolism, inhibiting hepatic gluconeogenesis and enhancing glucose uptake in skeletal muscles. Additionally, Metformin may also decrease intestinal glucose absorption. These actions reduce blood glucose levels, making Metformin a cornerstone therapy for type 2 diabetes mellitus. Moreover, it has been associated with various pleiotropic effects, such as anti-inflammatory and anti-aging properties, contributing to its potential benefits beyond glycemic control.

Important Safety Information

Side Effects

Common Side Effects:

  • Heartburn
  • Stomach pain
  • Nausea or vomiting
  • Bloating
  • Diarrhea
  • Constipation
  • Weight loss

When people start taking Metformin Canadian pharmacy, they usually experience nausea, vomiting, and diarrhea for a short time.

Mild Side Effects:

  • Nausea
  • Vomiting
  • Diarrhea
  • Gas or bloating
  • Abdominal discomfort or cramping
  • Metallic taste in the mouth

These side effects are usually temporary and tend to improve as your body adjusts to the medication

Adverse/Serious Side Effects:

Lactic Acidosis: Lactic acidosis is Metformin’s most serious side effect, although it is rare. There is a boxed warning on Metformin about this risk. Lactic acidosis is caused by a pH imbalance caused by a buildup of Metformin. This medical emergency needs to be treated in the hospital immediately. The following symptoms may occur:

  • Experiencing extreme fatigue
  • Decreased appetite
  • A fast or slow heart rate
  • Nausea and vomiting
  • Trouble breathing
  • Muscle pain
  • Dizziness and lightheadedness
  • A cold feeling
  • Stomach pain 
  • Flushing or sudden reddening and warmth in your skin combined with any of these other symptoms

In case of symptoms of lactic acidosis, contact a doctor as soon as possible. Call 911 or go to the nearest emergency room if you are having trouble breathing.

Anemia: Metformin can decrease your body’s level of vitamin B12. Rarely, this can result in anemia (low red blood cell count). You may have a higher risk of having very low levels of vitamin B12 if you don’t get enough of it through your diet. Some of the more common symptoms of anemia are:

  • Fatigue
  • Feeling dizzy
  • Feeling lightheaded

Make an appointment with your doctor if you think you may have anemia. Stopping Metformin or taking vitamin B12 supplements may improve your vitamin B12 levels. Make sure to talk with the healthcare provider who prescribed Metformin before you stop taking it.

Hypoglycemia: Metformin rarely causes low blood sugar (hypoglycemia). You should consult your doctor if you have any of these symptoms of hypoglycemia:

  • Weakness and tiredness
  • Nausea and vomiting
  • Stomach pain
  • Dizziness or lightheadedness
  • Unusually fast or slow heartbeat

Warnings

Hypoglycemia: While hypoglycemia is rare with Metformin alone, it may occur in combination with other glucose-lowering agents, especially in elderly, debilitated, or malnourished patients. Caution is advised during concurrent use with sulfonylureas, insulin, or ethanol.

Kidney Problems: It is your kidneys that remove Metformin from your body. You will have higher Metformin levels if your kidneys aren’t working properly. As a result, you are more likely to develop lactic acidosis. Depending on your kidney problems, your doctor may prescribe you a lower dose of Metformin. Metformin may not be right for you if you have severe kidney problems or are 80 years old or older. It is likely that your kidney function will be tested before you begin taking Metformin and then every year afterward.

Liver Issues: If you suffer from severe liver problems, you should not take Metformin canadian pharmacy. If you suffer from severe liver problems, you may develop lactic acidosis due to a buildup of lactic acid. Metformin also raises your risk of liver disease, so taking it can be harmful.

Boxed Warning (Lactic Acidosis)

Metformin treatment can lead to a rare but serious condition called lactic acidosis, which can be fatal in approximately 50% of cases. Lactic acidosis may occur due to Metformin accumulation, particularly in patients with kidney disease, hypoxemia, or significant tissue hypoperfusion. Monitoring of renal function is crucial to minimize the risk, and Metformin should be discontinued in patients with impaired renal function (creatinine clearance levels below normal for age). 

The risk of lactic acidosis increases with factors such as advanced age, congestive heart failure, and the use of multiple medications. Prompt discontinuation of Canadian pharmacy Metformin and supportive measures are essential if lactic acidosis is suspected.

Precautions

  1. Monitoring of Renal Function: Metformin is excreted by the kidneys, so renal function should be assessed before starting treatment and annually after that. Patients with elevated serum creatinine levels should not receive Metformin. Close monitoring is essential in elderly patients, especially those aged 80 years and above.
  2. Concomitant Medications: Caution is advised when using medications that may affect renal function or interfere with Metformin disposition. Cationic drugs eliminated by renal tubular secretion should be used cautiously.
  3. Radiologic Studies: Intravascular contrast studies can lead to acute renal function alteration and have been associated with lactic acidosis in Metformin-treated patients. Therefore, Metformin should be temporarily discontinued before such procedures and reinstituted only after normal renal function is confirmed.
  4. Hypoxic States: Conditions like shock, acute congestive heart failure, or acute myocardial infarction can lead to lactic acidosis and should prompt discontinuation of Metformin.
  5. Surgical Procedures: Metformin should be suspended temporarily for surgical procedures, except for minor ones that do not affect food and fluid intake.
  6. Alcohol Intake: Excessive alcohol consumption can potentiate Metformin’s effects on lactate metabolism, so patients should be cautioned against it.
  7. Impaired Hepatic Function: Metformin should generally be avoided in patients with clinical or laboratory evidence of hepatic disease due to its association with lactic acidosis.
  8. Vitamin B12 Levels: Metformin use may lead to decreased serum vitamin B12 levels, particularly in elderly patients. Regular monitoring of hematologic parameters is advised, and vitamin B12 supplementation may be necessary.
  9. Hypoglycemia: Elderly, debilitated, or malnourished patients are particularly susceptible to hypoglycemic effects, especially when using other glucose-lowering agents concurrently with Metformin.
  10. Loss of Glycemic Control: During periods of stress, such as illness or surgery, temporary loss of glycemic control may occur, necessitating temporary insulin therapy and discontinuation of Metformin until the acute episode resolves.

Metformin Contraindications 

Metformin is contraindicated in those with,

  • Severe renal dysfunction, defined as a GFR >30 mL/min/1.73m²
  • Serum creatinine levels greater than or equal to 1.5 in men and 1.4 in women
  • Abnormal creatinine clearance (CrCl)
  • Hypersensitivity to metformin
  • Lactic acidosis
  • GFR <60 mL/min/1.73m²
  • Risk factors for lactic acidosis
  • Hepatic impairment
  • Unstable heart failure

Missed Dose

When you remember that you missed a Metformin dose, take it right away. If your next dose is almost due, skip the one you missed and get back on schedule. Taking two doses to compensate for a missed one is not a good idea.

[Note: It’s important to follow your prescribed dosing schedule for Metformin. If you have questions or concerns about missed doses, consult your healthcare provider for guidance].

Overdose

Taking too much Metformin can cause diarrhea, nausea, and stomach pain. Metformin alone isn’t as likely to cause hypoglycemia (low blood glucose). You should check your blood glucose if you feel weak, shaky, or sweaty. Follow the instructions to bring it back up to normal if it’s less than 70 mg/dL. Metformin may cause lactic acidosis in some people if they take too much of it. People with kidney or liver problems, as well as older adults, are examples. Symptoms like trouble breathing, muscle aches, and stomach pain require immediate medical attention.

[Note: You can contact Poison Control at 1-800-222-1222 if you believe you have taken too much Metformin. Visit your nearest emergency room if you are experiencing any symptoms that feel life-threatening].

Storage

Keep the medicine in a closed container at room temperature, away from sunlight and heat. Don’t let it freeze. Make sure this product is not accessible to children. The use of outdated or unnecessary medicines should be avoided. Do not discard any medicine you no longer need without consulting your healthcare professional.

[Note: Proper storage of Metformin helps maintain its effectiveness and safety. If you have any questions about storing your medication, ask your pharmacist or healthcare provider for advice].

Metformin Interactions

There are 364 drugs known to interact with Metformin, as well as 5 disease interactions and 1 alcohol/food interaction. A total of 23 drug interactions are major, 332 are moderate, and 9 are minor. 

Some of the drugs include:

  • Amiloride (midamor)
  • Beta-blockers:
    • Tenormin (atenolol)
    • Trandate (labetalol)
    • Lopressor, Toprol XL (metoprolol)
    • Corgard, Corzide (nadolol)
    • Hemangeol, Inderal, InnoPran (propranolol)
  • Angiotensin-converting enzyme (ACE) inhibitors:
    • Zestoretic (lisinopril)
    • Univasc (moexipril)
    • Captopril
    • Vasotec, Vaseretic (enalapril)
    • Fosinopril
    • Altace (ramipril)
    • Mavik (trandolapril)
    • Aceon (perindopril)
    • Accupril (quinapril)
    • Lotensin, Lotrel (benazepril)
  • Cimetidine (tagamet)
  • Digoxin (lanoxin)
  • Diuretics (water pills):
    • Lasix (furosemide)
  • Laniazid, Rifamate, Rifater (isoniazid)
  • Calcium channel blockers:
    • Norvasc (amlodipine)
    • Cardizem, Cartia, Diltzac (diltiazem)
    • Felodipine
    • Isradipine
    • Cardene (nicardipine)
    • Adalat, Afeditab CR, Procardia (nifedipine)
    • Nymalize (nimodipine)
    • Sular (nisoldipine)
    • Calan, Covera, Verelan, Tarka (verapamil)
  • MS Contin (morphine)
  • Niacin
  • Oral contraceptives 
  • Oral steroids:
    • Dexamethasone
    • Medrol (methylprednisolone)
    • Rayos (prednisone)
  • Dilantin, Phenytek (phenytoin)
  • Procainamide
  • Nuedexta (quinidine)
  • Quinine
  • Zantac (ranitidine)
  • Dyrenium, Maxzide (triamterene)
  • Primsol (trimethoprim)
  • Vancocin (vancomycin)

Metformin and Alcohol/Food Interactions

Avoid excessive alcohol intake as it can increase this risk, especially if you have kidney or liver disease, congestive heart failure, or dehydration. Alcohol can also affect blood sugar levels, leading to hypoglycemia or hyperglycemia. Limit alcohol consumption if your diabetes is not well controlled or if you have certain complications. Talk to your doctor or pharmacist for more guidance.

[Note: Discuss with your healthcare provider or pharmacist if you have concerns about how Metformin may interact with other drugs or conditions. They can provide guidance on managing these interactions and adjusting your treatment regimen as needed].

Metformin Alternatives

  1. Amaryl (glimepiride)
  2. Januvia (sitagliptin)
  3. Actos (pioglitazone)
  4. Jardiance (empagliflozin)
  5. Farxiga (dapagliflozin)
  6. Tradjenta (linagliptin)
  7. Diabeta, Glynase (glyburide)
  8. Prandin (repaglinide)
  9. Avandia (rosiglitazone)
  10. Precose (acarbose)
  11. Onglyza (saxagliptin)
  12. Invokana (canagliflozin)

[Note: These alternative medications work through different mechanisms to help control blood sugar levels. It’s important to consult with your healthcare provider to determine the most suitable treatment option for you].

Quick Tips

  1. Can Metformin Help with Gestational Diabetes in Pregnancy
  2. Causes and Treatment of Metformin-Induced Diarrhea
  3. Ozempic vs Metformin Comparison

Frequently Asked Questions

How long can I take Metformin? 

You can take Metformin for a long time if it’s helping you. Your doctor will monitor how well it’s working and if you’re experiencing any side effects. If you’re doing well on it and it’s controlling your blood sugar, you can keep taking it for as long as your doctor recommends. It’s essential to follow their advice and attend regular check-ups to ensure it continues to be safe and effective for you. Always communicate any concerns or changes in your health to your doctor.

Is it safe to use Metformin during pregnancy? 

Metformin is usually not recommended during pregnancy. However, your doctor may prescribe it in certain situations, like if you have gestational diabetes or Polycystic Ovary Syndrome (PCOS). They’ll carefully weigh the risks and benefits for you and your baby. If you’re pregnant or planning to become pregnant, always talk to your doctor before starting or stopping any medications. They’ll help you make the safest choices for you and your baby’s health. Regular prenatal care is crucial for monitoring your condition.

Can Metformin cause weight loss? 

Yes, Metformin can sometimes cause weight loss as a side effect, especially in people with type 2 diabetes who are overweight or obese. It helps lower blood sugar levels and can also reduce appetite in some individuals. However, not everyone will experience weight loss with Metformin, and its effect on weight can vary from person to person. If you’re taking Metformin and notice changes in your weight, it’s essential to discuss them with your doctor to ensure they’re safe and appropriate for you.

Does Metformin interact with alcohol? 

Yes, it’s generally safe to have moderate amounts of alcohol while taking Metformin. However, heavy alcohol consumption can increase the risk of lactic acidosis, a rare but serious side effect of Metformin. Drinking alcohol excessively while on Metformin can also affect your blood sugar levels and increase the risk of hypoglycemia (low blood sugar) or hyperglycemia (high blood sugar). It’s important to drink alcohol in moderation and to monitor your blood sugar levels closely if you choose to drink while taking Metformin.

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