glyburide/metformin (Rx)

Brand and Other Names:Glucovance
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

glyburide/metformin

tablet

  • 1.25mg/250mg
  • 2.5mg/500mg
  • 5mg/500mg
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Type 2 Diabetes Mellitus

1.25/250 mg glyburide/metformin PO qDay or q12hr

May titrate up at 2 week intervals; maximum 20/2000 mg/day

Dosage Modifications

Hepatic impairment: Avoid use; cases of lactic acidosis reported

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

Safety and efficacy not established

1.25/250 mg glyburide/metformin PO qDay or q12hr

Adjust conservatively in patients with advanced age; do not use in patients >80 years unless renal function is assessed (do not titrate to maximum dose)

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Interactions

Interaction Checker

and glyburide/metformin

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            Adverse Effects

            Frequency Not Defined

            Dermatologic reactions

            Heartburn

            Hypoglycemia

            Nausea/vomiting

            Postmarketing Reports

            Gastrointestinal: Cholestatic jaundice and hepatitis may occur rarely which may progress to liver failure; discontinue drug

            Allergic: Angioedema, arthralgia, myalgia, and vasculitis

            Dermatologic: Porphyria cutanea tarda and photosensitivity

            Hematologic: Leukopenia, agranulocytosis, thrombocytopenia, which occasionally may present as purpura, hemolytic anemia, aplastic anemia, and pancytopenia

            Metabolic: Hepatic porphyria reactions reported with sulfonylureas but not with glyburide; disulfiram-like reactions reported very rarely with glyburide; cases of hyponatremia reported most often in patients who are on other medications or have medical conditions known to cause hyponatremia or increase release of antidiuretic hormone

            Liver function abnormalities, including isolated transaminase elevations (glyburide)

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            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 to glyburide or metformin

            Congestive heart failure, metabolic acidosis

            Diabetic ketoacidosis, with or without coma (treat with insulin)

            Coadministration with bosentan (increased risk of hepatotoxicity)

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

            Cautions

            If metformin-associated lactic acidosis suspected, general supportive measures should be instituted promptly in a hospital setting, along with immediate discontinuation of therapy; in patients with a diagnosis or strong suspicion of lactic acidosis, prompt hemodialysis is recommended to correct acidosis and remove accumulated metformin (metformin hydrochloride is dialyzable, with a clearance of up to170 mL/minute under good hemodynamic conditions); hemodialysis has often resulted in reversal of symptoms and recovery

            Allergic skin reactions, eg, pruritus, erythema, urticaria, and morbilliform or maculopapular eruptions, occur in 1.5% of glyburide-treated patients, which may be transient and may disappear despite continued use; if skin reactions persist, drug should be discontinued

            Use with caution in patients with risk of severe hypoglycemia: elderly, debilitated, or malnourished, adrenal or pituitary insufficiency

            Use with caution in patients with stress due to infection, fever, trauma, or surgery

            Before initiating therapy, obtain an estimated glomerular filtration rate

            Pregnancy/lactation

            Withholding of food and fluids during surgical or other procedures may increase risk for volume depletion, hypotension, and renal impairment; therapy should be temporarily discontinued while patients have restricted food and fluid intake

            Several of the postmarketing cases of metformin-associated lactic acidosis occurred in setting of acute congestive heart failure (particularly when accompanied by hypoperfusion and hypoxemia); cardiovascular collapse (shock) acute myocardial infarction, sepsis, and other conditions associated with hypoxemia have been associated with lactic acidosis and may also cause prerenal azotemia; discontinue therapy when such events occur

            Use with caution in patients with dehydration, heavy use of alcohol, hypoxic states, impaired hepatic or renal function

            Hemolytic anemia may occur with glucose 6-phosphate dehydrogenase (G6PD) deficiency when treated with sulfonylurea agents

            Clinical recommendations based upon the patient’s renal function

            • Before initiating therapy, obtain an eGFR.
            • Initiation of therapy is not recommended in patients with eGFR between 30 –45 mL/minute/1.73 m²
            • Obtain an eGFR at least annually in all patients receiving therapy
            • In patients at increased risk for development of renal impairment (e.g., the elderly), renal function should be assessed more frequently
            • If eGFR later falls below 45 mL/minute/1.73 m², assess benefit and risk of continuing therapy

            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
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            Pregnancy & Lactation

            Pregnancy Category: B

            Lactation: Excretion in milk unknown; not recommended

            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.

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            Pharmacology

            Mechanism of Action

            Initial effect is to increase beta-cell insulin secretion

            May also decrease rate of hepatic glucose production, increase insulin receptor sensitivity, and increase number of insulin receptors

            Pharmacokinetics

            Onset: 2-3 hr

            Metabolites: 4-trans-hydroxyglyburide, 3-cis-hydroxyglyburide (active)

            Half-Life

            • Glyburide: Approx. 10 hr
            • Metformin: Approx. 6 hr

            Duration

            • Glyburide: 24 hr
            • Metformin: No data

            Protein Bound

            • Glyburide: 99%
            • Metformin: Minimal

            Vd

            • Glyburide: No studies
            • Metformin: 650 L

            Metabolism

            • Glyburide: Extensively, in liver to less active metabolites
            • Metformin: Not metabolized

            Excretion

            • Glyburide: Urine 50%, bile 50%
            • Metformin: Urine 90%

            Dialyzable

            • Glyburide: No data
            • Metformin: Hemodialysis
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            Formulary

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            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.
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