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Metformin / Sitagliptin Dosage

Medically reviewed on April 13, 2018.

Applies to the following strengths: 500 mg-50 mg; 1000 mg-50 mg; 1000 mg-100 mg

Usual Adult Dose for Diabetes Type 2

Dose should be individualized based on patient's current regimen, effectiveness, and tolerability.
Initial doses: IMMEDIATE-RELEASE:
-For patients not receiving with metformin: sitagliptin 50 mg/ metformin 500 mg orally twice a day
-For patients receiving metformin 1000 mg/day: sitagliptin 50 mg/ metformin 500 mg orally twice a day
-For patients receiving metformin 1700 or 2000 mg/day: sitagliptin 50 mg/ metformin 1000 mg orally twice a day
Initial Doses: EXTENDED-RELEASE:
-For patients not receiving metformin: sitagliptin 100 mg/ metformin 1000 mg orally once a day
-For patients receiving metformin 1000 mg/day: sitagliptin 100 mg/ metformin 1000 mg orally once a day
-For patients receiving metformin 1700 or 2000 mg/day: sitagliptin 100 mg/ metformin 2000 mg orally once a day
Titrate dose to achieve optimal glycemic control
MAXIMUM daily doses: Sitagliptin 100 mg; Metformin 2000 mg

Comments:
- For patients changing between immediate-release and extended-release: Maintain the same daily dose of metformin-sitagliptin
-When initiating therapy, dose adjustment of insulin secretagogue (e.g., sulfonylurea) or insulin may be necessary to reduce the risk of hypoglycemia.

Use: As an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus when treatment with both sitagliptin and metformin is appropriate.

Renal Dose Adjustments

Mild renal impairment (eGFR greater than 45 mL/min/1.73 m2): No dose adjustments recommended
Moderate renal impairment (eGFR 30 to 45 mL/min/1.73 m2): Initiating therapy is not recommended
Severe renal impairment (eGFR less than 30 mL/min/1.73 m2): Use is contraindicated

If eGFR falls below 30 mL/min/1.73 m2 during therapy: Discontinue therapy
If eGFR that falls below 45 mL/min/1.73 m2 during therapy: Maximum Sitagliptin dose: 50 mg/day; assess risks versus benefit of continued therapy

IODINATED CONTRAST PROCEDURE:
-For patients with eGFR between 30 and 60 mL/min/1.73 m2: Stop this drug at the time of, or before imaging procedure; re-evaluate eGFR 48 hours after procedure; restart therapy only if renal function is stable

Liver Dose Adjustments

Hepatic impairment: Use is not recommended

IODINATED CONTRAST PROCEDURE:
-For patients with a history of hepatic impairment: Stop this drug at the time of, or before imaging procedure; re-evaluate eGFR 48 hours after procedure; restart therapy only if renal function is stable

Dose Adjustments

Elderly: Dose selection should be cautious usually starting at the low end of the dosing range; assess renal function frequently

Radiological Studies with Contrast:
-Stop this drug at time of or prior to an iodinated contrast imaging procedure using intra-arterial iodinated contrast
-Stop this drug at time of or prior to an iodinated contrast imaging procedure in patients with an eGFR between 30 and 60 mL/min/1.73 m2, in patients with a history of hepatic impairment, alcoholism, or heart failure
-Re-evaluate eGFR 48 hours after the procedure and restart only if renal function is stable

If heart failure develops, evaluate and manage according to current standards of care and consider discontinuation of this drug

Precautions

US BOXED WARNINGS: LACTIC ACIDOSIS
Postmarketing case of metformin-associated lactic acidosis have resulted in death, hypothermia, hypotension, and resistant bradyarrhythmias. Onset is often subtle, accompanied by only nonspecific symptoms such as malaise, myalgias, respiratory distress, somnolence, and abdominal pain. Metformin-associated lactic acidosis was characterized by elevated blood lactate levels (greater than 5 mmol/L), anion gap acidosis (without evidence of ketonuria or ketonemia), an increased lactate/pyruvate ratio, and metformin plasma levels generally greater than 5 mcg/mL
-Risk factors for metformin-associated lactic acidosis include renal impairment, concomitant use of certain drugs (e.g. carbonic anhydrase inhibitors such as topiramate), age 65 years old or greater, having a radiological study with contrast, surgery and other procedures, hypoxic states (e.g. acute congestive heart failure), excessive alcohol intake, and hepatic impairment.
-Steps to reduce the risk of and manage metformin-associated lactic acidosis in high risk groups are provided in the full prescribing information.
-If metformin-associated lactic acidosis is suspected, immediately discontinue therapy and institute general supportive measures in a hospital setting. Prompt hemodialysis is recommended.

CONTRAINDICATIONS:
-Severe renal impairment (eGFR below 30 mL/min/1.73 m2)
-Hypersensitivity to metformin
-Acute or chronic metabolic acidosis, including diabetic ketoacidosis
-History of a serious hypersensitivity reaction to this combination drug or sitagliptin, such as anaphylaxis or angioedema

Safety and efficacy have not been established in patients younger than 18 years.

Consult WARNINGS section for additional precautions.

Dialysis

Contraindicated in patients with moderate to severe renal dysfunction
Hemodialysis:
-Metformin is dialyzable with a clearance of up to 170 mL/min
-Sitagliptin is modestly dialyzable
Peritoneal dialysis: Data not available

Other Comments

Administration advice:
-Immediate-release: Take orally twice a day with meals
-Extended-release: Take orally once a day with the evening meal; swallow whole, do not crush, cut, or chew
-If a dose is missed, take with food as soon as remembered, but if it is time for the next dose, skip the missed dose; do not take 2 doses as the same time.

General:
-Occasionally, a mass resembling the extended-release tablet (XR) may be eliminated in the feces. It is not known whether this mass contains active drug, but if a patient repeatedly sees tablets in their feces, glycemic control should be assessed.
-This drug may need to be stopped at the time or prior to radiologic studies utilizing iodinated contrast materials; if hold is needed, hold for 48 hours after procedure and resume only after adequate renal function is confirmed.
-This drug should be held for surgical procedures, or anytime restricted food or fluid intake is expected; may resume once adequate renal function is confirmed.
-This drug is not recommended for patients with type 1 diabetes mellitus or for the treatment of diabetic ketoacidosis as it would not be effective in these settings.

Monitoring:
-Monitor glycemic control
-Renal: Assess renal function at baseline and at least annually, more frequent (e.g. every 3 to 6 months) is recommended in patients with serum creatinine levels at the upper limit of normal, elderly patients, and in patients at risk for developing renal impairment
-Hematologic: Measure hematologic parameters annually
-Monitor for signs and symptoms of pancreatitis
-Monitor for skin disorders such as blistering or ulceration

Patient advice:
-Instruct patient to report signs and symptoms of pancreatitis; if persistent, severe abdominal pain occurs, seek medical advice promptly.
-Hypoglycemia may occur, more commonly when used in combination with insulin or a sulfonylurea.
-Patients should understand the importance of adhering to dietary instructions and regular physical activity; during periods of stress such as fever, trauma, infection, or surgery, management of diabetes may change and patients should be advised to seek medical advice.
-Inform patients about the risk of lactic acidosis, conditions that might predispose them to its occurrence, and symptoms to watch for and report.
-Advise patient that this drug may need to be temporarily stopped if undergoing radiologic studies with intravascular iodinated contrast materials or surgical procedures that will limit food or fluid intake.
-Advise patients on the risks of excessive alcohol intake.
-Instruct patients to contact their health care provider if they develop severe and persistent joint pain or skin blistering or ulceration.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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