dapagliflozin (Rx)

Brand and Other Names:Farxiga
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 5mg
  • 10mg

Type 2 Diabetes Mellitus

Improve glycemic control

  • Indicated as an adjunct to diet and exercise to improve glycemic control with type 2 diabetes mellitus (T2DM)
  • Initial: 5 mg PO qDay in AM
  • May increase to 10 mg qDay in patients tolerating 5 mg/day who require additional glycemic control

Reduce risk of hospitalization for heart failure

  • Indicated to reduce hospitalization risk for heart failure in adults with T2DM and established cardiovascular disease (CVD) or multiple CV risk factors
  • 10 mg PO qDay in AM

Heart Failure

Indicated to reduce the risk of cardiovascular death and hospitalization for heart failure (HF) in adults with HF (NYHA class II-IV) with reduced ejection fraction

10 mg PO qDay

Chronic Kidney Disease

Indicated to reduce risk of sustained eGFR decline, end-stage kidney disease (ESKD), cardiovascular death, and hospitalization for HF in adults with chronic kidney disease (CKD) who are at risk of progression

10 mg PO qDay

Dosage Modifications

Renal impairment

eGFR ≥45mL/min/1.73 m2: No dosage adjustment required

  • eGFR 25 to <45 mL/min/1.73 m2
    • T2DM: Not recommended
    • HF or CKD: No dosage adjustment required
  • eGFR <25 mL/min/1.73 m2
    • Initiation not recommended
    • Patients with HF or CKD may continue 10 mg/day to reduce risk of eGFR decline, ESKD, CV death, and HF hospitalization

​ESRD/dialysis: Contraindicated

Hepatic impairment

  • Mild or moderate: No dosage adjustment required
  • Severe: Not studied

Dosing Considerations

Limitations of use

  • Not for treatment of type 1 diabetes mellitus; may increase risk of diabetic ketoacidosis in these patients
  • Not recommended to improve glycemic control in adults with T2DM with eGFR <45 mL/min/1.73 m2; dapagliflozin likely to be ineffective owing to its mechanism of action
  • Not recommended for CKD in patients with polycystic kidney disease, or those requiring or with recent history of immunosuppressive therapy for kidney disease; dapagliflozin is likely to be ineffective in these populations

Before initiation

  • Assess renal function and periodically thereafter
  • Assess, and if needed, correct volume depletion

Safety and efficacy not established

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Interactions

Interaction Checker

and dapagliflozin

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    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Renal impairment

            • Overall (1.8-6.7%)
            • Age ≥65 yr (3.1-14%)
            • eGFR 30-60 mL/min (8-28.3%)
            • Age ≥65 yr and eGFR 30-60 mL/min (7-35.1%)

            1-10%

            Female genital mycotic infections (6.9-8.4%)

            Nasopharyngitis (6.3-6.6%)

            Urinary tract infection (4.3-5.7%)

            Back pain (3.1-4.2%)

            Increased urination (2.9-3.8%)

            Male genital mycotic infections (2.7-2.8%)

            Nausea (2.5-2.8%)

            Influenza (2.3-2.7%)

            Dyslipidemia (2.1-2.5%)

            Constipation (1.9-2.2%)

            Discomfort with urination (2.1-2.6%)

            Extremity pain (1.7-2%)

            Volume depletion

            • Overall (0.6-1.1%)
            • Patients on loop diuretics (0-9.7%; 1.8-2.5%)
            • Patients with moderate renal impairment, GFR 30-60 mL/min (0.9-1.9%)
            • Age ≥65 yr (0.5-1.7%)

            <1%

            Hypersensitivity (0.3%)

            Postmarketing Reports

            Rash

            Ketoacidosis

            Acute kidney injury and renal impairment

            Urosepsis and pyelonephritis

            Necrotizing fasciitis of the perineum

            Hypoglycemia

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            Warnings

            Contraindications

            Serious hypersensitivity to dapagliflozin (eg, anaphylaxis, angioedema)

            Patients on dialysis

            Cautions

            Genital mycotic infections may occur; patients with history of genital mycotic infections and uncircumcised males are more susceptible

            Serious urinary tract infections, including urosepsis and pyelonephritis, requiring hospitalization reported in patients receiving SGLT2 inhibitors

            Necrotizing fasciitis of the perineum (Fournier gangrene) reported with SGLT2 inhibitors; signs and symptoms include tenderness, redness or swelling of the genitals, or area from the genitals to the rectum, and have a fever >100.4ºF or generally feeling unwell; if suspected, discontinue SGLT2 inhibitor and start treatment immediately with broad-spectrum antibiotics and surgical debridement if necessary

            Intravascular volume contraction

            • Patients with diabetes and renal impairment may be more likely to experience hypotension and may be at higher risk for acute kidney injury secondary to volume depletion
            • Symptomatic hypotension may occur after initiating, particularly in patients with renal impairment (eGFR <60 mL/min/1.73 m2), with low systolic blood pressure, taking loop diuretics, or who are elderly
            • Renal impairment may occur owing to intravascular volume contraction; before initiating, consider factors that may predispose patients to acute kidney injury, including hypovolemia, chronic renal insufficiency, CHF, and concomitant medications (eg, diuretics, ACE inhibitors, ARBs, NSAIDs); consider temporarily discontinuing dapagliflozin in any setting of reduced oral intake or fluid loss; monitor for signs and symptoms of acute kidney injury, and, if evident, discontinue drug promptly and institute treatment

            Ketoacidosis

            • Sodium-glucose cotransporter 2 (SGLT2) inhibitors increase risk of ketoacidosis in patients with type 1 and type 2 diabetes mellitus
            • Before initiating therapy, consider factors that may predispose patients to ketoacidosis, including pancreatic insulin deficiency from any cause, caloric restriction, and alcohol abuse
            • Consider temporarily discontinuing dapagliflozin for at least 3 days before undergoing scheduled surgery to avoid euglycemic ketoacidosis
            • Consider monitoring for ketoacidosis and temporarily discontinuing therapy in other clinical situations known to predispose to ketoacidosis (eg, prolonged fasting due to acute illness or post-surgery); ensure risk factors for ketoacidosis are resolved before resumption

            Drug interactions overview

            • Hypoglycemia risk increased with insulin and insulin secretagogues (eg, sulfonylureas); a lower dose of insulin or insulin secretagogue may be required

            Laboratory testing

            • Increase in LDL-cholesterol compared with placebo
            • Urine glucose tests is not recommended in patients taking SGLT2 inhibitors, as SGLT2 inhibitors, increase urinary glucose excretion and lead to positive urine glucose tests; use alternative methods to monitor glycemic control
            • 1,5-AG assay is not recommended, as measurements of 1,5-AG are unreliable in assessing glycemic control in patients taking SGLT2 inhibitors; use alternative methods to monitor glycemic control

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            Pregnancy & Lactation

            Pregnancy

            Based on animal data showing adverse renal effects drug is not recommended during second and third trimesters of pregnancy

            Limited data in pregnant women are not sufficient to determine drug-associated risk for major birth defects or miscarriage; there are risks to mother and fetus associated with poorly controlled diabetes in pregnancy

            In animal studies, adverse renal pelvic and tubule dilatations, that were not fully reversible, were observed in rats when administered during a period of renal development corresponding to late second and third trimesters of human pregnancy, at all doses tested

            Clinical considerations

            • Poorly controlled diabetes in pregnancy increases maternal risk for diabetic ketoacidosis, preeclampsia, spontaneous abortions, preterm delivery, still birth and delivery complications; poorly controlled diabetes increases fetal risk for major birth defects, stillbirth, and macrosomia related morbidity

            Lactation

            There is no information regarding presence of dapagliflozin in human milk, effects on breastfed infant, or on milk production; drug is present in milk of lactating rats; however, due to species-specific differences in lactation physiology, clinical relevance of these data are not clear

            Since human kidney maturation occurs in utero and during first 2 years of life when lactational exposure may occur, there may be risk to developing human kidney; because of potential for serious adverse reactions in breastfed infants, advise women that therapy is not recommended while breastfeeding

            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

            Selective sodium-glucose transporter-2 (SGLT2) inhibitor

            SGLT-2, expressed in the proximal renal tubules, is responsible for the majority of the reabsorption of filtered glucose from the tubular lumen; SGLT2 inhibitors will reduce glucose reabsorption and lower the renal threshold for glucose, thereby increasing urinary glucose excretion

            Absorption

            Bioavailability: 78%

            Peak plasma time: 2 hr (fasting); ~3 hr (with high fat meal)

            High fat meal decreases peak plasma concentration by up to 50%

            Distribution

            Protein bound: 91%

            Metabolism

            Metabolism primarily mediated by UGT1A9

            CYP-mediated metabolism is a minor clearance pathway in humans

            Extensively metabolized, primarily to yield dapagliflozin 3-O-glucuronide (inactive metabolite)

            Elimination

            Half-life: 12.9 hr

            Excretion: 75% urine; 21% feces

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            Administration

            Oral Administration

            Administer in the morning, with or without food

            Storage

            Store at room temperature at 20-25°C (68-77°F)

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            Formulary

            FormularyPatient Discounts

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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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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.