Metformin hydrochloride is a prescription medication used to treat type 2 diabetes and certain types of polycystic ovarian syndrome. It works by helping to control blood sugar levels and decrease insulin resistance. It inhibits glucose production from the liver and encourages fat metabolism to help reduce the amount of circulating glucose. Metformin hydrochloride can also help decrease elevated blood triglyceride levels and help decrease LDL cholesterol.
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Metformin hydrochloride is approved by the FDA to treat type 2 diabetes and certain types of polycystic ovarian syndrome. It is also commonly used as an off-label treatment for PCOS-related conditions such as infertility, obesity and hirsutism.
Mechanism of Action
Metformin hydrochloride works by helping the body use insulin more efficiently and reducing the amount of sugar released from the liver into the bloodstream. It helps reduce the amount of circulating glucose by inhibiting hepatic gluconeogenesis and by increasing insulin sensitivity It can also help reduce elevated triglycerides and LDL cholesterol levels.
How Long Does it Take to Work?
The effects of metformin hydrochloride can be seen within 1 to 2 weeks of starting therapy. Maximum effects can take up to 6 to 8 weeks to be achieved.
Absorption
Metformin hydrochloride is rapidly absorbed, reaching peak plasma concentrations within 2 to 4 hours. The maximum plasma concentration is reached within 4 to 8 hours after a single dose.
Route of Elimination
Metformin hydrochloride is eliminated primarily by the kidneys. Fecal elimination accounts for only a small portion of elimination.
Dosage
The usual starting metformin hydrochloride dose is 500 mg taken orally twice a day. The dose can be increased by 500 mg every week or biweekly until the desired blood glucose control is achieved. The maximum recommended daily dose is 2500 mg.
Administration
Metformin hydrochloride should be taken with meals or within 30 minutes of eating a meal. It should be taken with a full glass of water.
Side Effects
The most common side effects of metformin hydrochloride include loss of appetite, nausea, heartburn, abdominal discomfort, and diarrhea. Other rare but serious side effects include lactic acidosis and hypoglycemia.
Toxicity
No fatal overdoses have been reported with metformin hydrochloride overdose. Mild to moderate side effects have been reported with metformin hydrochloride overdose.
Precautions
Patients should be monitored for signs of lactic acidosis, hypoglycemia, and allergic reactions. Metformin hydrochloride should be avoided in patients with renal impairment or in those with dehydration.
Interactions
Metformin hydrochloride may interact with certain medications, including certain antacids, birth control pills, diuretics, and certain medications for diabetes. It is important to tell your doctor or pharmacist about all medications and supplements that you are taking.
Disease Interactions
Metformin hydrochloride should not be used in patients with conditions that lower the body's ability to remove lactic acid, such as kidney or liver disease. It should also not be used in patients who are at risk for lactic acidosis, such as those with significant alcohol intake or those with cardiac or respiratory failure.
Drug Interactions
Metformin hydrochloride may interact with certain drugs, including certain antidiabetic medications, birth control pills, diuretics, and certain medications for diabetes. It is important to tell your doctor or pharmacist about all medications and supplements that you are taking.
Food Interactions
Food does not affect the absorption of metformin hydrochloride. However, food increases gastrointestinal transit time, which increases the risk of side effects, such as abdominal cramping, nausea, etc.
Pregnancy Use
Metformin hydrochloride is not recommended for use during pregnancy as its safety during pregnancy has not been established.
Lactation Use
Metformin hydrochloride is not recommended for use during lactation as its safety during lactation has not been established.
Acute Overdose
Signs and symptoms of metformin hydrochloride overdose are nausea, vomiting, abdominal discomfort, and diarrhea. Treatment of an acute overdose of metformin hydrochloride is supportive and symptomatic.
Contraindications
Metformin hydrochloride is contraindicated in patients with renal impairment, severe hepatic impairment, critical illness with metabolic acidosis, and in those with an allergy/hypersensitivity to metformin. It should also not be used in patients who are at risk for lactic acidosis, such as those with significant alcohol intake or those with cardiac or respiratory failure.
Use Direction
Metformin hydrochloride should be taken with meals or within 30 minutes of eating a meal. It should be taken with a full glass of water. The usual starting metformin hydrochloride dose is 500 mg taken orally twice a day. The dose can be increased by 500 mg every week or biweekly until the desired blood glucose control is achieved.
Storage Condition
Metformin hydrochloride should be stored at room temperature, away from moisture and light. It should not be frozen or exposed to temperatures higher than the recommended storage temperature.
Volume of Distribution
The volume of distribution of metformin hydrochloride is 0.63 L/kg.
Half-Life
The half-life of metformin hydrochloride is 6.2–14.6 hours.
Clearance
The clearance of metformin hydrochloride is 0.22 L/h/kg.