Linagliptin / Metformin Dosage

Medically reviewed by Drugs.com. Last updated on Apr 5, 2024.

Usual Adult Dose for Diabetes Type 2

Immediate release tablets:

• Initial dose for patients currently not receiving metformin: linagliptin 2.5 mg/metformin 500 mg orally twice a day
• Initial dose for patients currently receiving metformin: linagliptin 2.5 mg in combination with one-half of current metformin dose orally twice a day
• Initial dose for patients currently receiving linagliptin and metformin as individual components: switch to combination product containing the same doses of each component orally twice a day

Maintenance dose: Individualize dose based on safety and efficacy
Maximum dose: linagliptin 5 mg/day; metformin 2000 mg/day

Extended-release tablets:

• Initial dose for patients currently not receiving metformin: linagliptin 5 mg/metformin extended-release 1000 mg orally once a day
• Initial dose for patients currently receiving metformin: linagliptin 5 mg in combination with a similar total daily dose of metformin orally once a day
• Initial dose for patients currently receiving linagliptin and metformin as individual components: switch to combination product containing similar doses of each component orally once a day

Maintenance dose: Individualize dose based on safety and efficacy
Maximum dose: linagliptin 5 mg/day; metformin 2000 mg/day

Comments:

• Patients taking two linagliptin 2.5 mg/metformin 1000 mg extended-release tablets should take the 2 tablets together once a day.
• When used in combination with insulin or an insulin secretagogue, a lower dose of insulin or the insulin secretagogue may be necessary to reduce the risk of hypoglycemia.
• Should not be used in patients with type 1 diabetes.

Use: To improve glycemic control in adults with type 2 diabetes mellitus as an adjunct to diet and exercise.

Renal Dose Adjustments

• Severe renal impairment (eGFR below 30 mL/min/1.73 m2): Contraindicated
• Moderate renal impairment (eGFR 30 to 45 mL/min/1.73 m2): Do not initiate therapy

During therapy:

• If eGFR falls below 45 mL/min/1.73 m2: Assess risk vs benefit of continuing therapy
• If eGFR falls below 30 mL/min/1.73 m2: Discontinue therapy

IODINATED CONTRAST PROCEDURE: Stop this drug at time of, or prior to, an iodinated contrast imaging procedure for:

• Patients with an eGFR between 30 and 60 mL/min/1.73 m2
• Patients who will be administered intra-arterial iodinated contrast
• Patients with a history of hepatic impairment, alcoholism, or heart failure
• Reevaluate eGFR 48 hours after the imaging procedure; this drug may be restarted once adequate renal function is confirmed.

Liver Dose Adjustments

Not recommended in hepatic impairment

Dose Adjustments

IODINATED CONTRAST PROCEDURE:

• Stop this drug at time of, or prior to, an iodinated contrast imaging procedure for patients with an eGFR between 30 and 60 mL/min/1.73 m2.
• Stop this drug in any patient who will be administered intra-arterial iodinated contrast.
• Stop this drug in any patient with a history of hepatic impairment, alcoholism, or heart failure.
• Reevaluate eGFR 48 hours after the imaging procedure; this drug may be restarted once adequate renal function is confirmed.

Precautions

US BOXED WARNING: Risk of lactic acidosis

• Postmarketing cases of metformin-associated lactic acidosis have resulted in death, hypothermia, hypotension, and resistant bradyarrhythmias. The onset of metformin-associated lactic acidosis is often subtle, accompanied only by nonspecific symptoms such as malaise, myalgias, respiratory distress, somnolence, and abdominal pain. Metformin-associated lactic acidosis is characterized by elevated blood lactate levels (greater than 5 mmol/L), anion gap, acidosis (without evidence of ketonuria or ketonemia) and 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., cationic drugs such as topiramate), age 65 years or greater, radiological study with contrast, surgery, and other procedures, hypoxic state (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 less than 30 mL/min 1.73 m2)
• Acute or chronic metabolic acidosis, including diabetic ketoacidosis
• Hypersensitivity to active substances or to any product excipients; reactions such as anaphylaxis, angioedema, exfoliative skin conditions, urticaria, or bronchial hyperreactivity have occurred with linagliptin

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

Consult WARNINGS section for additional precautions.

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 a meal

• Swallow whole; do not split, crush, dissolve, or chew before swallowing
• Incompletely dissolved tablets may be eliminated in the feces; if this occurs assess adequacy of glycemic control.

Missed Dose: If a dose is missed, advise patients not to double their next dose

General:

• Should not be used in patients with type 1 diabetes.
• Has not been studied in patients with with a history of pancreatitis; it is unknown whether patients with a history of pancreatitis are at an increased risk for development of pancreatitis with use of this drug.
• When used in combination with insulin or an insulin secretagogue, a lower dose of insulin or insulin secretagogue may be necessary to reduce the risk of hypoglycemia.
• Therapy may need to be temporarily stopped prior to radiologic studies utilizing iodinated contrast materials and for surgical procedures when restricted food or fluid intake is expected; adequate renal function should be confirmed before reinitiating therapy. See dose adjustment section for guidance.

Monitoring:

• Renal: Assess eGFR at baseline, repeat at least annually or more often as clinically indicated
• Hematologic: Measure hematologic parameters annually; monitor B12 levels every 2 to 3 years if warranted
• Monitor for signs and symptoms of pancreatitis; severe and disabling arthralgia; signs and symptoms of lactic acidosis
• Monitor glycemic control

Patient advice:

• Patients should be instructed to read the US FDA-approved patient labeling (Medication Guide).
• 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.
• Patients should be instructed to seek medical attention promptly for severe and persistent abdominal pain and/or any signs or symptoms of serious allergic reactions.
• Inform patients that hypoglycemia may occur, especially if used in combination with insulin or a sulfonylurea; patients should be knowledgeable on treating hypoglycemia and urged to use caution when operating hazardous equipment, including driving a car.
• Patients should be instructed to report symptoms heart failure, unusual muscle pain, blisters or erosions of the skin.

Further information

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

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