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Metformin volume of distribution

654 L for metformin 850 mg administered as a single dose. The volume of distribution following IV administration is 63-276 L, likely due to less binding in the GI tract and/or different methods used to determine volume of distribution.

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What is Metformin

Metformin is a biguanide antihyperglycemic agent used for treating non-insulin-dependent diabetes mellitus (NIDDM). It improves glycemic control by decreasing hepatic glucose production, decreasing glucose absorption and increasing insulin-mediated glucose uptake. Metformin may induce weight loss and is the drug of choice for obese NIDDM patients. Use of metformin is associated with modest weight loss. When used alone, metformin does not cause hypoglycemia; however, it may potentiate the hypoglycemic effects of sulfonylureas and insulin. Its main side effects are dyspepsia, nausea and diarrhea. Dose titration and/or use of smaller divided doses may decrease side effects. Metformin should be avoided in those with severely compromised renal function (creatinine clearance 30 ml/min), acute/decompensated heart failure, severe liver disease and for 48 hours after the use of iodinated contrast dyes due to the risk of lactic acidosis. Lower doses should be used in the elderly and those with decreased renal function. Metformin decreases fasting plasma glucose, postprandial blood glucose and glycosolated hemoglobin (HbA1c) levels, which are reflective of the last 8-10 weeks of glucose control. Metformin may also have a positive effect on lipid levels. In 2012, a combination tablet of linagliptin plus metformin hydrochloride was marketed under the name Jentadueto for use in patients when treatment with both linagliptin and metformin is appropriate.

Metformin mechanism of action

Metformin’s mechanisms of action differ from other classes of oral antihyperglycemic agents. Metformin decreases blood glucose levels by decreasing hepatic glucose production, decreasing intestinal absorption of glucose, and improving insulin sensitivity by increasing peripheral glucose uptake and utilization. These effects are mediated by the initial activation by metformin of AMP-activated protein kinase (AMPK), a liver enzyme that plays an important role in insulin signaling, whole body energy balance, and the metabolism of glucose and fats. Activation of AMPK is required for metformin’s inhibitory effect on the production of glucose by liver cells. Increased peripheral utilization of glucose may be due to improved insulin binding to insulin receptors. Metformin administration also increases AMPK activity in skeletal muscle. AMPK is known to cause GLUT4 deployment to the plasma membrane, resulting in insulin-independent glucose uptake. The rare side effect, lactic acidosis, is thought to be caused by decreased liver uptake of serum lactate, one of the substrates of gluconeogenesis. In those with healthy renal function, the slight excess is simply cleared. However, those with severe renal impairment may accumulate clinically significant serum lactic acid levels. Other conditions that may precipitate lactic acidosis include severe hepatic disease and acute/decompensated heart failure.

Dosage forms of Metformin

DrugDosageQuantityPrice
Metformin500mg100 Tablet$33.00
Glucophage850mg100 Tablet$32.80
Glumetza1000mg90 ER Tablet$146.00
Glucophage XR500mg84 ER Tablet$59.00
Metformin Hydrochloride Er750mg90 ER Tablet$50.00
Kombiglyze XR5/1000mg84 Tablet$198.00
Avandamet4mg/500mg100 Tablet$255.00
Pioglitazone/Metformin15/850mg90 Tablet$89.50
Actoplus Met15/850mg56 Tablet$121.00
Janumet50/500mg112 Tablet$63.45
Galvus Met50/1000mg120 Tablet$181.00
Glyburide/Metformin2.5/500mg90 Tablet$51.00
Janumet XR100/1000mg84 Extended Release Tablet$707.00
Janumet XR100/1000mg84 Extended Release Tablet$707.00
Xigduo XR10/1000mg84 Tablet$380.00
Invokamet50/500mg60 Tablet$600.00

Prescription Generics

false

International Brands

Act Metformin

Synonyms

1,1-Dimethylbiguanide Dimethylbiguanid

Manufacturers

Actavis Pharma Company

CAS number

657-24-9

UNII

9100L32L2N

State

solid

Affected organisms

Humans and other mammals

Indication of Metformin

For use as an adjunct to diet and exercise in adult patients (18 years and older) with NIDDM. May also be used for the management of metabolic and reproductive abnormalities associated with polycystic ovary syndrome (PCOS). Jentadueto is for the treatment of patients when both linagliptin and metformin is appropriate.

Toxicity of Metformin

Acute oral toxicity (LD sub 50 /sub ): 350 mg/kg (Rabbit). It would be expected that adverse reactions of a more intense character including epigastric discomfort, nausea, and vomiting followed by diarrhea, drowsiness, weakness, dizziness, malaise and headache might be seen.

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What is Glucophage?

Glucophage is an oral hypoglycemic drug. The drug contains the active ingredient – metformin – a substance with a pronounced hypoglycemic effect, which develops only under the condition of hyperglycemia. In patients with normal plasma glucose levels, the drug does not have a hypoglycemic effect. In patients with hyperglycemia, the drug reduces the initial level of glucose in the blood plasma, as well as the level of glucose after a meal.

The mechanism of action of the drug is based on its ability to inhibit gluconeogenesis and glycogenolysis, increase insulin sensitivity, as well as reduce the absorption of glucose in the gastrointestinal tract. Thus, the drug helps to reduce glucose production in the liver, stimulates the capture and utilization of glucose by the muscles and reduces plasma glucose concentrations. In addition, metformin, regardless of the hypoglycemic effect, leads to an improvement in lipid metabolism, in particular, reduces the level of triglycerides, cholesterol and low-density lipoproteins.

After oral administration, the drug is well absorbed in the gastrointestinal tract, food intake reduces the absorption of metformin. The peak plasma concentration of metformin is observed 2.5 hours after oral administration of the drug Glucophage and 7 hours after taking the drug Glucophage XR. Absolute bioavailability when ingested reaches 50-60%. The drug is characterized by a low degree of communication with plasma proteins, metformin penetrates into red blood cells, while the plasma concentration of the drug is higher than the concentration in the blood. The drug is not metabolized in the body, excreted mainly by the kidneys, some of it is excreted by the intestines. The half-life is about 6.5 hours. In patients with impaired renal function, there is a decrease in clearance of metformin, which is proportional to the decrease in creatinine clearance.

What is Jentadueto?

Jentadueto contains a combination of linagliptin and metformin. Linagliptin and metformin are oral diabetes medications that help control blood sugar levels. Metformin works by reducing the production of glucose (sugar) in the liver and reducing the absorption of glucose in the intestine. Linagliptin works by regulating the insulin levels that your body produces after a meal.

Jentadueto is used with diet and exercise to improve blood sugar control in adults with type 2 diabetes. Jentadueto is not intended to treat type 1 diabetes.

You should not use Jentadueto if you have severe kidney disease or diabetic ketoacidosis (see your doctor for treatment). Some people develop lactic acidosis by taking metformin. Early symptoms worsen over time, and this condition can be fatal. Stop taking Jentadueto and get emergency medical help if you have even mild symptoms, such as muscle pain or weakness, difficulty breathing, stomach pain, nausea, and a feeling of very weakness or fatigue.

Before taking Jentadueto, tell your doctor if you have liver disease, a serious infection, heart disease, a history of pancreatitis, if you have recently had a heart attack, or if you are over 80 years old and have not recently had your kidney. Function checked. If you need to undergo a surgical procedure or a radiological examination or computed tomography using a dye that is injected into your veins, you need to temporarily stop taking Jentadueto.

What is Xigduo?

Xigduo XR contains a combination of dapagliflozin and metformin. Dapagliflozin and metformin are diabetes medications that help control blood sugar levels. Dapagliflozin works by helping the kidneys get rid of glucose from your bloodstream. Metformin reduces the production of glucose in the liver, and also causes your intestines to absorb less glucose.

Xigduo XR is used along with diet and exercise for the treatment of type 2 diabetes. Dapagliflozin is not intended to treat type 1 diabetes. You should not use Xigduo XR if you have severe kidney disease, or if you are in a state of diabetic ketoacidosis. Xigduo XR is not intended for the treatment of type 1 diabetes.

If you need to have an x-ray or CT scan using a dye that is injected into your veins, you need to temporarily stop taking Xigduo XR. Xigduo XR can cause a serious condition called lactic acidosis. Get emergency medical care if you have even mild symptoms, such as muscle pain or weakness, numbness or coldness in your hands and feet, trouble breathing, stomach pain, nausea with vomiting, slow or uneven heart rate , dizziness or feeling very weak Or tired.