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Farxiga

Generic Name: Dapagliflozin Propanediol
Class: Sodium-glucose Cotransporter 2 (SGLT2) Inhibitors
Chemical Name: (1S)-1,5-Anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-d-glucitol,
Molecular Formula: C21H25ClO6
CAS Number: 461432-26-8

Medically reviewed by Drugs.com. Last updated on Nov 18, 2019.

Introduction

Antidiabetic agent; sodium-glucose cotransporter 2 (SGLT2) inhibitor.1 53 55

Uses for Farxiga

Type 2 Diabetes Mellitus

Used as monotherapy as an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus.1 2 3 15 32 34

Used in combination with other antidiabetic agents (e.g., metformin and/or a sulfonylurea, a peroxisome proliferator-activated receptorγ [PPARγ] agonist [thiazolidinedione], a dipeptidyl peptidase-4 [DPP-4] inhibitor) and/or insulin or a glucagon-like peptide 1 (GLP-1) receptor agonist (e.g., exenatide) as an adjunct to diet and exercise in patients with type 2 diabetes mellitus who have not achieved adequate glycemic control.1 4 5 6 7 8 9 10 12 13 16 52

Used in fixed combination with extended-release metformin hydrochloride as an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus when treatment with both drugs is appropriate.53

Used in fixed combination with saxagliptin as an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus.55

Current guidelines for the treatment of type 2 diabetes mellitus generally recommend metformin as first-line therapy in addition to lifestyle modifications due to its well-established safety and efficacy (e.g., beneficial effects on glycosylated hemoglobin [hemoglobin A1c; HbA1c], weight, and cardiovascular mortality).598 604 Consider patient's comorbidities when selecting additional antidiabetic agents.598 604

Patients with type 2 diabetes mellitus who have established atherosclerotic cardiovascular disease (ASCVD) should receive a drug with demonstrated cardiovascular disease benefit (e.g., GLP-1 receptor agonist [e.g., liraglutide], SGLT2 inhibitor [e.g., empagliflozin]).604 In patients with ASCVD and heart failure or at an increased risk of heart failure, an SGLT2 inhibitor with demonstrated cardiovascular benefit may be preferred.604

Evidence of macrovascular risk reduction with dapagliflozin, the fixed combination of dapagliflozin and extended-release metformin hydrochloride, or the fixed combination of dapagliflozin and saxagliptin has not been conclusively demonstrated in clinical trials.1 53 55

In patients with type 2 diabetes mellitus and CKD, an SGLT2 inhibitor or GLP-1 receptor agonist with demonstrated ability to reduce the risk of CKD progression, cardiovascular events, or both should be considered.604

In patients without ASCVD, heart failure, or CKD, the decision regarding the addition of other antidiabetic agents (e.g., sulfonylurea, thiazolidinedione, DPP-4 inhibitor, SGLT2 inhibitor, GLP-1 receptor agonist, basal insulin) should be based on drug-specific effects and individual patient factors.604

Some data indicate that in addition to its beneficial glycemic effects, dapagliflozin therapy is associated with a reduction of heart failure-related hospitalizations and reduction in CKD progression.70 86 604 605

Not indicated for type 1 diabetes mellitus or treatment of diabetic ketoacidosis.1 53 55

Farxiga Dosage and Administration

Administration

Oral Administration

Dapagliflozin: Administer once daily in the morning, with or without food.1

Fixed combination of dapagliflozin and extended-release metformin hydrochloride: Administer once daily in the morning with food to reduce the adverse GI effects of the metformin hydrochloride component.53

Fixed combination of dapagliflozin and saxagliptin: Administer once daily in the morning, with or without food.55

Fixed-combination tablets of dapagliflozin and metformin hydrochloride or saxagliptin should be swallowed whole; tablets should not be split or cut.53 55

If a dose of dapagliflozin, the fixed combination of dapagliflozin and metformin hydrochloride, or the fixed combination of dapagliflozin and saxagliptin is missed, take missed dose as soon as it is remembered followed by resumption of regular schedule.1 53 56 If missed dose is not remembered until the time of the next dose, skip missed dose and resume regular schedule.1 53 56 Do not double dose to replace a missed dose.1 53 56

Dosage

Dosage of dapagliflozin propanediol is expressed in terms of dapagliflozin.1

Adults

Type 2 Diabetes Mellitus
Dapagliflozin
Oral

Initially, 5 mg once daily.1

If well tolerated, increase dosage to 10 mg once daily in patients who require additional glycemic control.1

Dapagliflozin/Metformin Hydrochloride Fixed-combination Therapy
Oral

Initial dosage based on patient's current regimen with dapagliflozin and/or metformin hydrochloride.53 May gradually increase dosage based on effectiveness and tolerability.53

In patients currently not receiving dapagliflozin, initial recommended dosage of the dapagliflozin component is 5 mg once daily.53 Titrate gradually based on effectiveness and tolerability, up to a maximum dosage of 10 mg of dapagliflozin and 2 g of extended-release metformin hydrochloride daily.53

Patients who are already receiving extended-release metformin hydrochloride in the evening and are switching to the fixed combination of dapagliflozin and metformin hydrochloride should skip their last dose of metformin hydrochloride before initiating therapy with the fixed combination the following morning.53

Dapagliflozin/Saxagliptin Fixed-combination Therapy
Oral

Recommended initial dosage in patients not already receiving dapagliflozin therapy is 5 mg of dapagliflozin and 5 mg of saxagliptin once daily in the morning.55

In patients requiring additional glycemic control and tolerating initial dosage, may increase dosage of fixed combination to 10 mg of dapagliflozin and 5 mg of saxagliptin once daily.55

Do not use fixed combination in patients receiving concomitant therapy with a potent CYP3A4/5 inhibitor (e.g., atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin).55

Special Populations

Hepatic Impairment

Dapagliflozin Monotherapy
Oral

Mild, moderate, or severe hepatic impairment: No dosage adjustment necessary.1

Dapagliflozin/Metformin Hydrochloride Fixed-combination Therapy
Oral

Use not recommended in patients with hepatic impairment.53

Dapagliflozin/Saxagliptin Fixed-combination Therapy
Oral

Mild, moderate, or severe hepatic impairment: No dosage adjustment necessary.55

Renal Impairment

Dapagliflozin Monotherapy
Oral

Mild renal impairment (eGFR ≥45 mL/minute per 1.73 m2): No dosage adjustment necessary.1

Moderate renal impairment: Do not use if eGFR <45 mL/minute per 1.73 m2.1 (See Renal Impairment under Cautions.)

Severe renal impairment (eGFR <30 mL/minute per 1.73 m2): Contraindicated.1

Dapagliflozin/Metformin Hydrochloride Fixed-combination Therapy
Oral

Mild renal impairment (eGFR ≥45 mL/minute per 1.73 m2): No dosage adjustment necessary.53

Moderate renal impairment: Do not use if eGFR <45 mL/minute per 1.73 m2.53

Severe renal impairment (eGFR <30 mL/minute per 1.73 m2): Contraindicated.53

Dapagliflozin/Saxagliptin Fixed-combination Therapy
Oral

Mild renal impairment (eGFR ≥45 mL/minute per 1.73 m2): No dosage adjustment necessary.55

Moderate or severe renal impairment: Contraindicated in patients with an eGFR <45 mL/minute per 1.73 m2.55

Geriatric Patients

No dosage adjustment of dapagliflozin necessary based solely on age.1

Gender

Dosage adjustment of dapagliflozin based on gender not necessary.1

Race

Dosage adjustment of dapagliflozin based on race not necessary.1

Body Weight

Dosage adjustment of dapagliflozin based on body weight not necessary.1

Cautions for Farxiga

Contraindications

  • History of serious hypersensitivity reaction to dapagliflozin.1

  • Dapagliflozin is contraindicated in patients with severe renal impairment (eGFR <30 mL/minute per 1.73 m2), end-stage renal disease, or on dialysis.1

Warnings/Precautions

Ketoacidosis

Ketoacidosis (e.g., diabetic ketoacidosis, ketoacidosis, ketosis) requiring hospitalization reported with SGLT2 inhibitors; may occur without markedly elevated blood glucose concentrations (e.g., <250 mg/dL).1 39 40 41 42 50

Evaluate for the presence of acidosis, including ketoacidosis, in patients experiencing signs or symptoms of acidosis regardless of the patient's blood glucose concentration; discontinue SGLT2 inhibitor and initiate appropriate treatment to correct acidosis if confirmed.1 39 40 50 (See Advice to Patients.)

Prior to initiating dapagliflozin therapy, consider factors that may predispose patients to ketoacidosis (e.g., pancreatic insulin deficiency, reduced caloric intake, alcohol abuse).1 50

Consider temporarily discontinuing SGLT2 inhibitor in patients with clinical situations known to predispose to ketoacidosis (e.g., prolonged fasting due to acute illness or surgery).1 50

Some clinicians suggest monitoring of urine and/or plasma ketone levels if patients feel unwell, regardless of ambient glucose concentrations.40 42

Hypotension

May cause intravascular volume contraction.1 Symptomatic hypotension can occur, particularly in patients with impaired renal function (eGFR <60 mL/minute per 1.73 m2), geriatric patients, or patients receiving loop diuretics.1 (See Specific Drugs and Laboratory Tests under Interactions.) Assess and correct intravascular volume status prior to initiating dapagliflozin in such patients.1

Monitor patients for signs and symptoms of hypotension after initiating therapy.1

Renal Effects

Causes intravascular volume contraction and can cause renal impairment.1 51

May increase Scr concentration and decrease eGFR; geriatric patients and patients with impaired renal function may be more susceptible to these changes.1 Adverse reactions related to renal function can occur following initiation of the drug.1

Prior to initiating dapagliflozin therapy, consider factors that may predispose patients to acute kidney injury, such as hypovolemia, chronic renal insufficiency, heart failure, and concomitant medications (e.g., diuretics, ACE inhibitors, angiotensin II receptor antagonists, NSAIAs).1 51

Consider temporarily discontinuing dapagliflozin in any setting of reduced oral intake (e.g., acute illness, fasting) or fluid losses (e.g., GI illness, excessive heat exposure).1 51

Evaluate renal function prior to initiation of dapagliflozin and monitor periodically thereafter.1 Discontinue dapagliflozin and initiate appropriate treatment if kidney injury occurs.1 51

Concomitant Therapy with Hypoglycemic Agents

When adding dapagliflozin to therapy with an insulin secretagogue (e.g., a sulfonylurea) or insulin, consider reducing dosage of the concomitant insulin secretagogue or insulin to reduce the risk of hypoglycemia.1 (See Specific Drugs and Laboratory Tests under Interactions)

Fournier Gangrene

Fournier gangrene (necrotizing fasciitis of the perineum), a rare but serious life-threatening bacterial infection requiring urgent surgical intervention, reported during postmarketing surveillance of men and women with type 2 diabetes mellitus receiving an SGLT2 inhibitor.1 59 60 61 62

Assess patient for necrotizing fasciitis if pain or tenderness, erythema, or swelling in the genital or perineal area occurs in addition to fever or malaise.1 60

If Fournier gangrene suspected, discontinue dapagliflozin and initiate treatment immediately with broad-spectrum antibiotics and, if necessary, perform surgical debridement.1 60 Closely monitor blood glucose concentrations and initiate alternative antidiabetic agent to maintain glycemic control.1 60

Genital Mycotic Infections

Possible increased risk of genital mycotic infections in males (e.g., balanitis) and females (e.g., vulvovaginal mycotic infection).1 11 37 Patients with a history of genital mycotic infections were more likely to develop such infections.1 37

Monitor patients for genital mycotic infections and institute appropriate treatment if these infections occur.1

Urosepsis and Pyelonephritis

May increase the risk of serious urinary tract infections (e.g., urosepsis, pyelonephritis requiring hospitalization).1 50

Prior to initiating dapagliflozin therapy, consider patient factors that may predispose to serious urinary tract infections (e.g., history of difficulty urinating; infection of the bladder, kidneys, or urinary tract).50

Monitor patients for urinary tract infections and initiate treatment if indicated.1 50

Risk of Bone Fracture

Increased risk of bone fracture, along with dose-related decreases in bone mineral density in older adults, observed in patients receiving another SGLT2 inhibitor (canagliflozin).43 Bone fractures observed more frequently than with placebo in patients with moderate renal impairment (eGFR 30 to <60 mL/minute per 1.73 m2) receiving dapagliflozin, usually within 52 weeks of initiating therapy.1 FDA continuing to evaluate bone fracture risk with SGLT2 inhibitors.43

Effects on Lipoproteins

Increases in LDL-cholesterol can occur.1 Monitor serum LDL-cholesterol concentrations and treat such lipid elevations according to the standard of care.1

Bladder Cancer

Newly diagnosed cases of bladder cancer reported in clinical studies.1 10 Too few cases to determine whether the emergence of these events is related to dapagliflozin; insufficient data to determine whether dapagliflozin has an effect on pre-existing bladder tumors. 1

Do not use dapagliflozin in patients with active bladder cancer.1 Consider benefits of glycemic control versus unknown risks for cancer recurrence.1

Use of Fixed Combinations

When dapagliflozin is used in fixed combination with metformin hydrochloride, saxagliptin, or other drugs, consider the cautions, precautions, contraindications, and interactions associated with the concomitant agent(s) in addition to those associated with dapagliflozin.1 53 55

Sensitivity Reactions

Hypersensitivity reactions (e.g., angioedema, urticaria, hypersensitivity), some serious, reported.1 53 55 If a hypersensitivity reaction occurs, discontinue dapagliflozin, institute appropriate treatment, and monitor patients until signs and symptoms resolve.1

Specific Populations

Pregnancy

No adequate and well-controlled studies of dapagliflozin in pregnant women.1

Studies in animals indicate that dapagliflozin use during pregnancy may affect renal development and maturation.1

Dapagliflozin therapy not recommended in pregnant women during the second and third trimesters of pregnancy.1

Lactation

Distributed into milk in rats; not known whether distributed into human milk.1 Use of dapagliflozin in women who are breast-feeding not recommended.1

Pediatric Use

Safety and efficacy not established in pediatric patients <18 years of age.1

Geriatric Use

Efficacy similar in patients <65 years of age and those ≥65 years of age after controlling for renal function (eGFR).1 Such patients more likely to experience adverse effects related to volume depletion and renal impairment or failure.1

Hepatic Impairment

No dosage adjustment of dapagliflozin necessary for patients with mild, moderate, or severe hepatic impairment.1 Assess benefits versus risks in patients with severe hepatic impairment; safety and efficacy not established in such patients.1 22

Renal Impairment

Patients with an eGFR of 45 to <60 mL/minute per 1.73 m2 receiving dapagliflozin had substantial improvement in glycemic control and experienced adverse effects similar to those without renal impairment.1 71 Patients receiving dapagliflozin therapy had a greater reduction in eGFR compared with those receiving placebo; however, renal function generally increased back to baseline values after discontinuing treatment with dapagliflozin.1 71 Patients with an eGFR of 30 to <60 mL/minute per 1.73 m2 receiving dapagliflozin had a greater incidence of bone fractures compared with those receiving placebo.1 35

Impact of hemodialysis on dapagliflozin exposure is not known; contraindicated in patients on dialysis.1

Assess renal function prior to initiation of therapy and periodically thereafter.1

Common Adverse Effects

Dapagliflozin monotherapy: Female genital mycotic infection,1 2 3 4 6 7 8 nasopharyngitis,1 2 3 5 6 7 8 urinary tract infection,1 2 3 4 5 6 8 33 back pain,1 5 8 increased urination,1 male genital mycotic infection,1 2 3 4 7 nausea,1 4 dyslipidemia,1 4 8 constipation,1 discomfort with urination,1 pain in extremity.1 8

Dapagliflozin in combination with metformin hydrochloride: Female genital mycotic infection,53 nasopharyngitis,53 urinary tract infection,53 diarrhea,53 headache,53 male genital mycotic infection,53 influenza,53 nausea,53 back pain,53 dizziness,53 cough,53 constipation,53 dyslipidemia,53 pharyngitis,53 increased urination,53 discomfort with urination.53

Dapagliflozin in combination with saxagliptin and metformin hydrochloride: Upper respiratory tract infection,55 urinary tract infection,55 dyslipidemia,55 headache,55 diarrhea,55 back pain,55 genital infection,55 arthralgia.55

Interactions for Farxiga

Metabolism principally mediated by uridine diphosphate-glucuronosyltransferase (UGT) isoenzyme 1A9.1 20

Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes

Did not inhibit CYP-450 isoenzymes 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6 or 3A4 in vitro.1 19 Did not induce CYP isoenzymes 1A2, 2B6, or 3A4 in vitro.1 19

Drugs Affected by Organic Anion Transporter

Dapagliflozin 3-O-glucuronide, inactive metabolite of dapagliflozin, is a substrate of organic anion transport (OAT) 3.1 Dapagliflozin and dapagliflozin 3-O-glucuronide did not meaningfully inhibit OAT1 or OAT3 active transporters; pharmacokinetic interactions unlikely with OAT1 or OAT3 substrates.1

Drugs Affected by Organic Cation Transporter

Did not meaningfully inhibit organic cation transporter (OCT) 2; pharmacokinetic interactions unlikely with substrates of OCT2.1

Drugs Affected by P-glycoprotein Transport

Weak P-glycoprotein substrate; did not meaningfully inhibit P-glycoprotein.1 19 20 Unlikely to affect pharmacokinetics of concurrently administered P-glycoprotein substrates.1

Specific Drugs and Laboratory Tests

Drug or Test

Interaction

Comments

Antidiabetic agents

Risk of hypoglycemia increased when used concomitantly with insulin secretagogue (e.g,, sulfonylurea) or insulin1

Reduced dosage of insulin or insulin secretagogue may be required to reduce the risk of hypoglycemia1

Bumetanide

Increased bumetanide AUC and peak plasma concentration1 (see also Diuretics entry in this table)

No dosage adjustment necessary1

Digoxin

No clinically meaningful effect on digoxin AUC or peak plasma concentration1 20 26

No adjustment of digoxin dosage necessary1

Diuretics

Possible increased incidence of symptomatic hypotension1

Assess and correct intravascular volume prior to dapagliflozin initiation; monitor for signs and symptoms of hypotension after initiating therapy1

Glimepiride

Increased glimepiride AUC1 20

No dosage adjustment necessary1 25

Hydrochlorothiazide

No clinically important effect on pharmacokinetics of either drug1 20 (see also Diuretics entry in this table)

No dosage adjustment necessary1

Mefenamic acid

Increased dapagliflozin peak plasma concentration and AUC1 20 24

No adjustment of dapagliflozin dosage necessary.24

Metformin

No clinically meaningful effect on pharmacokinetics of either drug 1 20 25

No dosage adjustment necessary1 25

Pioglitazone

Decreased pioglitazone peak plasma concentration1 20

No dosage adjustment necessary1 25

Rifampin

Decreased dapagliflozin peak plasma concentration and AUC 1 20 24

No adjustment of dapagliflozin dosage necessary1 24

Simvastatin

Increased simvastatin AUC1 26

No dosage adjustment necessary1

Sitagliptin

No clinically meaningful effect on pharmacokinetics of either drug (single-dose administration)1

No dosage adjustment necessary1 25

Urine glucose tests (e.g., 1,5-anhydroglucitol assay)

SGLT2 inhibitors increase urinary glucose excretion and will result in false-positive urine glucose tests1

Use alternative methods to monitor glycemic control1

Valsartan

Decreased peak plasma concentrations of valsartan and dapagliflozin and increased valsartan AUC1 20 26

No dosage adjustment necessary1

Voglibose (not commercially available in the US)

No clinically meaningful effect on dapagliflozin1

Warfarin

No clinically meaningful effect on warfarin pharmacokinetics or pharmacodynamics1 20 26

No warfarin dosage adjustment necessary1 20

Farxiga Pharmacokinetics

Absorption

Bioavailability

Absolute oral bioavailability: 78%.1 27 Peak plasma concentration usually attained within 2 hours after oral dosing in fasted state.1 18 19 20 23 30

Food

Administration with a high-fat meal decreased peak plasma concentration by up to 50% and prolonged time to peak plasma concentration by approximately 1 hour, but did not alter AUC.1 20 21 These changes are not considered clinically meaningful; administer dapagliflozin with or without food.1 20 21

Special Populations

Mild (Child-Pugh class A) or moderate (Child-Pugh class B) hepatic impairment: No clinically important differences in peak plasma concentration or AUC.1

Severe hepatic impairment (Child-Pugh class C): AUC and peak plasma concentration increased by 67 and 40%, respectively, compared with individuals with normal hepatic function following a single 10-mg dose of dapagliflozin.1 22

Mild renal impairment: Geometric mean systemic exposure of dapagliflozin at steady state increased by 45% compared with individuals with normal renal function.1

Moderate renal impairment: Geometric mean systemic exposure of dapagliflozin at steady state increased 2.04-fold compared with individuals with normal renal function.1

Severe renal impairment: Geometric mean systemic exposure of dapagliflozin at steady state increased 3.03-fold compared with individuals with normal renal function.1

Distribution

Extent

Extensively distributed.20

Plasma Protein Binding

Approximately 91%.1 19

Special Populations

Renal or hepatic impairment does not meaningfully alter plasma protein binding.1

Elimination

Metabolism

Metabolized principally by UGT1A9 to inactive metabolites.1

Elimination Route

75 and 21% of total radioactivity excreted in urine and feces, respectively, with <21 19 and approximately 15% in urine and feces, respectively, as parent drug.1 20

Half-life

Approximately 12.9 hours following a single oral dose of 10 mg.1

Stability

Storage

Oral

Tablets

Dapagliflozin, the fixed combination of dapagliflozin and extended-release metformin hydrochloride, or the fixed combination of dapagliflozin and saxagliptin: 20–25°C (may be exposed to 15–30°C).1 53 55

Actions

  • Inhibits SGLT2, a transporter expressed in proximal renal tubules and responsible for majority of reabsorption of filtered glucose from the tubular lumen.1 20

  • Reduces reabsorption of filtered glucose and lowers the renal threshold for glucose in a dose-dependent manner, leading to increased urinary glucose excretion.1 17 30 31

  • Increases glucose excretion independent of insulin secretion.36

  • Improves muscle insulin sensitivity;28 29 however, glucosuria induction appears to increase endogenous glucose production.28

  • Endogenous glucose production increases, accompanied by an increase in fasting plasma glucagon concentration.28

Advice to Patients

  • When dapagliflozin is used in fixed combination with other drugs, importance of informing patients of important cautionary information about the concomitant agents.1 53 55

  • Importance of patient reading medication guide before initiating therapy and each time the drug is dispensed.1 38 53 54 55 56

  • Importance of informing patients of the potential risks and benefits of dapagliflozin and of alternative therapies.1 38 Importance of not using dapagliflozin in patients with type 1 diabetes mellitus or diabetic ketoacidosis.1 38

  • Importance of informing patients that ketoacidosis, which can be a life-threatening condition, has been reported with dapagliflozin therapy.1 Importance of informing patients and their caregivers of the signs and symptoms of ketoacidosis (e.g., tachypnea or hyperventilation, anorexia, abdominal pain, nausea, vomiting, lethargy, mental status change) and of instructing patients to discontinue dapagliflozin and seek medical attention immediately should they experience any such signs or symptoms.1 39 42 50 Advise patients to use a ketone dipstick to check for ketones in their urine (when possible) if symptoms of ketoacidosis occur, even if blood glucose is not elevated (e.g., <250 mg/dL).1 38 50

  • Importance of informing patients that symptomatic hypotension may occur with dapagliflozin and to report such symptoms to their clinicians.1 38 Inform patients that dapagliflozin-induced dehydration may increase the risk of hypotension and that patients should maintain adequate fluid intake.1 38

  • Importance of informing patients that acute kidney injury has been reported with dapagliflozin therapy.1 38 51 Advise patients to seek medical attention immediately if they experience decreased urine output or swelling of the legs or feet.51 Advise patients to seek medical advice immediately if they have reduced oral intake (such as due to acute illness or fasting) or increased fluid losses (such as due to vomiting, diarrhea, or excessive heat exposure), as it may be appropriate to temporarily discontinue dapagliflozin in those settings.1 51

  • Importance of informing patients that necrotizing infections of the perineum (Fournier gangrene) have occurred with SGLT2 inhibitor therapy.1 60 Advise patients to promptly seek medical attention if they develop pain or tenderness, redness, or swelling of the genitals or the area from the genitals back to the rectum, in addition to fever (>38°C) or malaise.1 60

  • Importance of informing patients that yeast infection may occur (e.g., vulvovaginitis, balanitis, balanoposthitis).1 38 Importance of informing female patients of the signs and symptoms of vaginal yeast infections (e.g., vaginal discharge, odor, itching) and male patients of the signs and symptoms of balanitis or balanoposthitis (e.g., rash or redness of the glans or foreskin of the penis).1 38 53 55 Advise patients of treatment options and when to seek medical advice.1 38

  • Importance of informing patients of the potential for urinary tract infections, which may be serious.1 38 Advise patients of the signs and symptoms of urinary tract infection and the need to contact a clinician promptly if such signs and symptoms occur.1 50

  • Importance of informing patients that due to the mechanism of action of dapagliflozin, patients taking the drug will test positive for glucose in their urine.1 Importance of not using urine glucose tests to monitor glycemic status while taking dapagliflozin.1

  • Risk of serious hypersensitivity reactions, such as urticaria and angioedema.1 38 If signs or symptoms of such a reaction occur, importance of discontinuing dapagliflozin and promptly informing clinician.1 38

    Importance of informing patients to promptly report any signs of macroscopic hematuria or other symptoms potentially indicative of bladder cancer.1 38

  • Importance of informing patients about the importance of adherence to dietary instructions, regular physical activity, periodic blood glucose monitoring and glycosylated hemoglobin (hemoglobin A1c; HbA1c) testing, recognition and management of hypoglycemia and hyperglycemia, and assessment of diabetes complications.1 38

  • Importance of promptly seeking medical advice during periods of stress such as fever, trauma, infection, or surgery as medication requirements may change.1 38

  • Importance of taking dapagliflozin exactly as directed by clinician.1 38 (See Administration under Dosage and Administration.)

  • Importance of women informing their clinicians immediately if they are or plan to become pregnant or plan to breast-feed.1 38

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant illnesses.1 38 53 55

  • Importance of informing patients of other important precautionary information.1 38 (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Dapagliflozin Propanediol

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Tablets, film-coated

5 mg (of dapagliflozin)

Farxiga

AstraZeneca

10 mg (of dapagliflozin)

Farxiga

AstraZeneca

Dapagliflozin Propanediol Combinations

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Tablets, extended-release

2.5 mg (of dapagliflozin) with Extended-release Metformin Hydrochloride 1 g

Xigduo XR

AstraZeneca

5 mg (of dapagliflozin) with Extended-release Metformin Hydrochloride 500 mg

Xigduo XR

AstraZeneca

5 mg (of dapagliflozin) with Extended-release Metformin Hydrochloride 1 g

Xigduo XR

AstraZeneca

10 mg (of dapagliflozin) with Extended-release Metformin Hydrochloride 500 mg

Xigduo XR

AstraZeneca

10 mg (of dapagliflozin) with Extended-release Metformin Hydrochloride 1 g

Xigduo XR

AstraZeneca

Tablets, film-coated

5 mg (of dapagliflozin) with Saxagliptin 5 mg

Qtern

AstraZeneca

10 mg (of dapagliflozin) with Saxagliptin 5 mg

Qtern

AstraZeneca

AHFS DI Essentials™. © Copyright 2020, Selected Revisions November 18, 2019. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

References

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3. Bailey CJ, Iqbal N, T'joen C, List JF. Dapagliflozin monotherapy in drug-naïve patients with diabetes: a randomized-controlled trial of low-dose range. Diabetes Obes Metab. 2012 Oct; 14:951-9.

4. . Henry RR, Murray AV, Marmolejo MH, et al. Dapagliflozin, metformin XR, or both: initial pharmacotherapy for type 2 diabetes, a randomised controlled trial. Int J Clin Pract. 2012 May; 66:446-56.

5. Bailey CJ, Gross JL, Pieters A, Bastien A, List JF. Effect of dapagliflozin in patients with type 2 diabetes who have inadequate glycaemic control with metformin: a randomised, double-blind, placebo-controlled trial. Lancet. 2010 Jun 26; 375:2223-33.

6. Nauck MA, Del Prato S, Meier JJ et al. Dapagliflozin versus glipizide as add-on therapy in patients with type 2 diabetes who have inadequate glycemic control with metformin: a randomized, 52-week, double-blind, active-controlled noninferiority trial. Diabetes Care. 2011 Sep; 34:2015-22.

7. Strojek K, Yoon KH, Hruba V. Effect of dapagliflozin in patients with type 2 diabetes who have inadequate glycaemic control with glimepiride: a randomized, 24-week, double-blind, placebo-controlled trial. Diabetes Obes Metab. 2011 Oct; 13:928-38.

8. Rosenstock J, Vico M, Wei L, Salsali A, List JF. Effects of dapagliflozin, an SGLT2 inhibitor, on HbA(1c), body weight, and hypoglycemia risk in patients with type 2 diabetes inadequately controlled on pioglitazone monotherapy. Diabetes Care. 2012 Jul; 35:1473-8.

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