metformin/sitagliptin (Rx)

Brand and Other Names:Janumet, Janumet XR
  • Print

Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

metformin/sitagliptin

tablet

  • 500mg/50mg
  • 1,000mg/50mg

tablet, extended-release

  • 500mg/50mg
  • 1,000mg/50mg
  • 1,000mg/100mg
more...

Diabetes Mellitus, Type 2

Indicated as adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus who are already treated with sitagliptin or metformin and have inadequate glycemic control on sitagliptin or metformin alone

Adjust dose gradually considering effectiveness and tolerability

Inadequately controlled on metformin alone

  • 100 mg/day sitagliptin PO plus current dose of metformin
  • Not to exceed daily PO dose of 2,000 mg of metformin or 100 mg or sitagliptin

Inadequately controlled on sitagliptin alone

  • 1000 mg/day metformin PO plus 100 mg/day PO sitagliptin
  • Not to exceed daily PO dose of 2,000 mg of metformin or 100 mg or sitagliptin

Dosage Modifications

Hepatic impairment: Do not administer

Renal impairment

  • Obtain eGFR before starting metformin
  • eGFR <30 mL/min/1.73 m²: Contraindicated
  • eGFR 30-45 mL/min/1.73 m²: Not recommended to initiate treatment
  • Monitor eGFR at least annually or more often for those at risk for renal impairment (eg, elderly)
  • If eGFR falls below 45mL/min/1.73 m² while taking metformin, risks and benefits of continuing therapy should be evaluated
  • If eGFR falls below 30 mL/min/1.73 m²: while taking metformin, discontinue the drug

<18 years: Safety and efficacy not established

Initial and maintenance dosing should be conservative due to possibility of decreased renal function. Adjust dose gradually and conservatively considering effectiveness and tolerability

Inadequately controlled on metformin alone

100 mg/day sitagliptin PO plus current dose of metformin

Not to exceed daily PO dose of 2,000 mg of metformin or 100 mg or sitagliptin

Do not administer to patients >80 years before assessing renal function and determined to be normal

Inadequately controlled on sitagliptin alone

1000 mg/day metformin PO plus 100 mg/day PO sitagliptin

Not to exceed daily PO dose of 2,000 mg of metformin or 100 mg or sitagliptin

Do not administer to patients >80 years before assessing renal function and determined to be normal

Next:

Interactions

Interaction Checker

and metformin/sitagliptin

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            All Interactions Sort By:
             activity indicator 
            Previous
            Next:

            Adverse Effects

            1-10%

            Abdominal pain (2.2%)

            Diarrhea (2.4%)

            Hypoglycemia (2.1%)

            Nausea (1.3%)

            Vomiting (1.1%)

            Frequency Not Defined

            Exfoliative disorder of skin of scalp

            Stevens-Johnson syndrome

            Lactic acidosis (rare )

            Anaphylaxis/hypersensitivity reaction

            Rhabdomyolysis

            Acute renal failure

            Angioedema

            Postmarketing Reports

            Hypersensitivity reactions including anaphylaxis, angioedema, rash, urticaria, cutaneous vasculitis, and exfoliative skin conditions including Stevens-Johnson syndrome

            Upper respiratory tract infection

            Hepatic enzyme elevations

            Acute pancreatitis including fatal and nonfatal hemorrhagic and necrotizing pancreatitis

            Gastrointestinal: Constipation, vomiting

            Neurologic: Headache

            Worsening renal function, including acute renal failure (sometimes requiring dialysis)

            Myalgia, pain in extremity, and back pain

            Severe disabling arthralgia

            Pruritus

            Previous
            Next:

            Warnings

            Black Box Warnings

            Discontinue metformin at the time of or before an iodinated contrast imaging procedure in patients with an eGFR between 30-60 mL/minute/1.73 m²; in patients with a history of liver disease, alcoholism, or heart failure; or in patients who will be administered intra-arterial iodinate contrast

            Lactic acidosis

            • Characterized by elevated blood lactate levels (>5 mmol/L)
            • Rare but serious complication that can occur because of metformin accumulation; increased risk with sepsis, dehydration, excess alcohol intake, hepatic insufficiency, renal impairment, and acute congestive heart failure
            • Subtle onset with nonspecific symptoms (eg, malaise, myalgias, respiratory distress, somnolence, nonspecific abdominal distress)
            • Monitor lab for decreased serum pH, increased anion gap, and elevated blood lactate If suspected, discontinue drug and hospitalize patient immediately
            • Metformin is highly dialyzable (clearance up to 170 mL/min under good hemodynamic conditions); prompt hemodialysis is recommended to correct the acidosis and to remove accumulated metformin

            Contraindications

            Hypersensitivity, including anaphylaxis or angioedema

            Severe renal disease: eGFR <30 ml/min/1.73 m²

            Acute/chronic metabolic acidosis, including diabetic ketoacidosis; treat with insulin

            Cautions

            Risk of lactic acidosis with metformin accumulation

            Initiate in patients >80 years only if CrCl indicates no reduction in renal function

            Avoid excessive alcohol use

            Withhold in presence of any condition associated with hypoxemia, dehydration, or sepsis

            Discontinue temporarily prior to any intravascular radiocontrast study with iodine containing materials and for any surgical procedure

            Risk of hypoglycemia esp in elderly, debilitated or malnourished, adrenal/pituitary insufficiency, strenuous exercise not compensated by caloric intake, heavy alcohol use, hepatic/renal impairment, beta blockers

            May cause acute pancreatitis, including hemorrhagic and necrotizing pancreatitis

            Unknown if patients with history of pancreatitis are at increased risk

            Angioedema reported with other DPP-4 inhibitors; caution with history of angioedema

            Severe and disabling arthralgia reported in patients taking DPP-4 inhibitors; consider as a possible cause for severe joint pain and discontinue drug if appropriate

            Cases of lactic acidosis reported primarily in diabetic patients with significant renal impairment, including both intrinsic renal disease and renal hypoperfusion, often in the setting of multiple concomitant medical/surgical problems and multiple concomitant medications; monitor renal function of the elderly closely; withhold metformin promptly in presence of any condition associated with hypoxemia, dehydration, or sepsis

            Iodinated contrast imaging procedures

            • Discontinue metformin at the time of or before an iodinated contrast imaging procedure in patients with an eGFR between 30-60 mL/minute/1.73 m²; in patients with a history of liver disease, alcoholism, or heart failure; or in patients who will be administered intra-arterial iodinate contrast
            • Reevaluate eGFR 48 hr after the imaging procedure; restart metformin if renal function is stable
            Previous
            Next:

            Pregnancy & Lactation

            Pregnancy Category: B

            Lactation: not known if crosses into breast milk, use caution

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

            more...
            Previous
            Next:

            Pharmacology

            Mechanism of Action

            Sitagliptin: Dipeptidyl peptidase 4 (DPP-4) inhibitor, thereby increasing and prolonging incretin hormone activity which are inactivated by DPP-4 enzyme. Incretins increase insulin release and synthesis from pancreatic beta cells and reduce glucagon secretion pancreatic alpha cells

            Metformin: Biguanide; acts by decreasing endogenous hepatic glucose production, decreases intestinal absorption of glucose, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization; improves glucose tolerance and lowers both basal and postprandial plasma glucose

            Pharmacokinetics

            Half-Life

            • Sitagliptin: ~12.4 hr
            • Metformin: ~6.2 hr

            Bioavailability

            • Sitagliptin: 87%
            • Metformin: 50-60%

            Excretion

            • Sitagliptin: Urine 79%
            • Metformin: Urine 90%
            Previous
            Next:

            Administration

            Instructions

            Gradually escalate the dose to reduce the gastrointestinal side effects due to metformin

            Immediate-release: Administer q12hr with meals

            Extended-release: Administer once daily, with a meal preferably in the evening

            Maintain the same total daily dose of sitagliptin and metformin when changing between immediate-release and extended-release, without exceeding the maximum recommended daily dose

            Swallow whole; do not split, crush, or chew

            Previous
            Next:

            Images

            Previous
            Next:

            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
            Additional Offers
            Email to Patient

            From:

            To:

            The recipient will receive more details and instructions to access this offer.

            By clicking send, you acknowledge that you have permission to email the recipient with this information.

            Email Forms to Patient

            From:

            To:

            The recipient will receive more details and instructions to access this offer.

            By clicking send, you acknowledge that you have permission to email the recipient with this information.

            Previous