Category: Antidiabetic
Introduction:
Metformin is an antidiabetic medication approved by the FDA to control high blood sugar in patients with type 2 diabetes. Metformin has been shown to prevent diabetes in high-risk individuals and Reduces most diabetic complications. Diabetes is a group of metabolic disorders in which blood sugar levels are higher than normal because the body does not release enough insulin or cells respond inappropriately to insulin, leading to high blood pressure. Metformin functions by aiding in the restoration of the body's insulin-responsiveness. It reduces blood sugar produced by the liver and absorbed by the intestines or stomach.
Uses:
How To Consume:
Use metformin exactly as prescribed by your doctor. Take metformin with meals unless your doctor tells you otherwise. Some forms of metformin are taken only once daily with dinner. Follow your doctor's instructions.
Do not crush, chew, or break extended-release tablets. Swallow it whole. Carefully measure liquid medication. Shake the oral suspension before measuring a dose. Use the dosing syringe provided or use a medicine container (not a kitchen spoon).
Keep out of the heat, light, and moisture at room temperature.
Duration Between Two Dose:
Metformin comes in 2 different types of tablets: Standard and Delayed-release tablets.
Standard tablets release metformin into your body quickly. You may need to take them several times a day depending on your dosage.
Slow-release tablets work gradually so you don't need to take them often.
The maximum daily dose is 2,000 mg per day. This can be taken as four 500 mg tablets per day.
Liquid metformin should be used in doses of 5ml of 500mg, 850mg or 1000mg.
Packets are available in doses of 500 mg or 1000 mg
Side Effects:
low blood sugar;
Nausea or Upset Stomach
Diarrhea.
Bloating
Gas
Indigestion
Constipation
Unpleasant Metallic Taste In Mouth
Heartburn
Headache
Redness Of The Skin
Nail change
Drug Mechanism:
Pharmacokinetics:
The absolute bioavailability of metformin 500 mg tablets administered on an empty stomach is approximately 50-60%. Food reduces metformin absorption. Metformin is insignificantly bound to plasma proteins. Intravenous studies using single doses of metformin in normal subjects showed that metformin is excreted unchanged in the urine and does not undergo hepatic metabolism or biliary excretion. This drug is largely eliminated through the kidneys. Renal clearance of metformin is approximately 3.5 times higher than creatinine clearance, indicating that renal tubular secretion is the major route of metformin elimination. After oral administration, approximately 90% of absorbed metformin is excreted by the kidneys within 24 hours of administration.
Pharmacodynamics:
Insulin is an important hormone that helps regulate blood sugar levels. Type II diabetes is characterized by decreased insulin sensitivity, leading to high blood sugar levels when the pancreas is no longer able to compensate. In patients diagnosed with type 2 diabetes, insulin cannot exert its full effect on tissues and cells and insulin deficiency can also occur.
Metformin reduces hepatic glucose production, reduces intestinal glucose absorption, and improves insulin sensitivity by increasing both peripheral glucose absorption and utilization. Unlike sulfonylurea drugs that cause hyperinsulinemia, insulin secretion is not altered by metformin use.
Safety Measures:
When to See Doctor:
Unusual Muscle Pain
Feeling Cold
Shortness In Breathing
Feeling Dizzy, Light-Headed, Tired, Or Very Weak
Stomach Pain
Vomiting
Slow Or Irregular Heart Rate.
Chest Pain
Rashes
If conditions from this occur you should see the doctor or it can be hazardous for your health if not cured as soon as possible.
Allergic Reaction:
This drug can cause severe allergic reactions. Symptoms include:
Anaphylaxis (life-threatening allergic reaction)
Skin rashes
Hives
Trouble breathing
Immediately go to the doctor if these symptoms occur.
Available Dosage Form:
Tablet:
Immediate-release
Strengths: 500 mg, 850 mg, 1000 mg
Extended-release tablet
Strengths: 500 mg, 750 mg, 1000 mg
Oral solution
Strength: 500 mg, 750 mg, 1000 mg
Child Dosage:
Pediatric Dosage Forms & Strengths for Diabetes
Immediate-release (10-16 years)
Initial: 500 mg orally every 12 hours
Moderate: Titrate once in week by 500 mg; not more than 2000 mg/day in divided doses
Immediate-release (17 years of age and older)
Initial dose: 500 mg orally every 12 hours or 850 mg orally once daily with meals; increase every two weeks
Moderate doses: 1500-2550 mg/day orally divided once every 8-12hr with meal
No more than 2550 mg/day
Extended-release (under 17 years of age)
Safety and efficacy not established
Extended-release (17 years of age and older)
Glucophage XR: 500 mg orally once/daily with dinner; titrate by 500 mg/day once each week; not to exceed 2000 mg/day
Fortamet: 500-1000 mg orally once/daily; titrate by 500 mg/day once each week; not to exceed 2500 mg/day
Adult Dosage:
Immediate-release tablet or solution
Initial dose: 500 mg orally every 12 hours or 850 mg orally once/day with meals; increase every two weeks
Maintenance doses: 1500-2550 mg/day taken orally divided once every 8-12hr with meal
Not to exceed 2550 mg/day
Extended-release
Glucophage XR: 500 mg orally once/day with dinner; titrate by 500 mg/day each week; not to exceed 2000 mg/day
Fortamet: 500-1000 mg orally once/day; titrate by 500 mg/day each week; not to exceed 2500 mg/day
Glumetza: 1000 mg orally once/day; titrate by 500 mg/day each week; not to exceed 2000 mg/day
Important Note:
Follow the complete treatment prescribed by the physician, do not skip a dose in the treatment.
Completely comply with the treatment course as prescribed by your doctor, do not skip a single dose during treatment.
Make sure to inform the doctor or dentist that you are using this medicine. You may need to stop using this medication several days before surgery or medical tests.
Do not take other medications unless discussed with your doctor. This includes over-the-counter medicines such as aspirin and medicines for appetite control, asthma, colds, coughs, hay fever or sinus problems.
If symptoms of lactic acidosis occur, you should seek emergency medical help immediately.
Keep out of reach of CHILDREN. Get medical attention right away if you overdose, or call a poison control centre.
Use with caution in patients with congestive heart failure, fever, trauma, surgery, the elderly, renal failure, or liver failure.
Various Brands:
Reference:
Indian Pharmacopeia
Book Of Rang & Dale’s Pharmacology (9th Edition)
Book Of Essentials of Medical Pharmacology – K D Tripathi (8th edition)
Metformin: A review of its therapeutic efficacy and adverse effects
https://www.sciencedirect.com/science/article/abs/pii/S2451847620300063
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