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Empagliflozin


General


Pronunciation

(em pa gli FLOE zin)


Brand Names: U.S.

  • Jardiance

Indications


Use: Labeled Indications

Diabetes mellitus, type 2: Treatment of type 2 diabetes mellitus (noninsulin dependent, NIDDM) as an adjunct to diet and exercise to improve glycemic control

Limitations of use: US labeling: Not recommended for patients with type 1 diabetes or for the treatment of diabetic ketoacidosis


Contraindications


History of serious hypersensitivity to empagliflozin or any component of the formulation; severe renal impairment (eGFR <30 mL/minute/1.73 m2), end-stage renal disease (ESRD), or dialysis

Canadian labeling: Additional contraindications (not in US labeling): eGFR <45 mL/minute/1.73 m2


Dosing and Administration


Dosing: Adult

Note: If present, correct volume depletion prior to initiation

Diabetes mellitus, type 2: Oral: Initial: 10 mg once daily; may increase to 25 mg once daily


Dosing: Geriatric

Refer to adult dosing.


Dosing: Renal Impairment

eGFR ≥45 mL/minute/1.73 m2: No dosage adjustment necessary.

eGFR <45 mL/minute/1.73 m2: Do not initiate therapy; in patients already taking empagliflozin, discontinue therapy when eGFR is persistently <45 mL/minute/1.73 m2

eGFR <30 mL/minute/1.73 m2: Use is contraindicated.

ESRD, dialysis: Use is contraindicated.


Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturers labeling; may be used in patients with hepatic impairment.


Administration

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


Dietary Considerations

Individualized medical nutrition therapy (MNT) based on ADA recommendations is an integral part of therapy


Storage

Store at 25 ‚ °C (77 ‚ °F); excursions are permitted between 15 ‚ °C and 30 ‚ °C (59 ‚ °F and 86 ‚ °F).


Dosage Forms/Strengths


Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Jardiance: 10 mg, 25 mg


Drug Interactions

Alpha-Lipoic Acid: May enhance the hypoglycemic effect of Antidiabetic Agents. Monitor therapy

Androgens: May enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Exceptions: Danazol. Monitor therapy

Hyperglycemia-Associated Agents: May diminish the therapeutic effect of Antidiabetic Agents. Monitor therapy

Hypoglycemia-Associated Agents: Antidiabetic Agents may enhance the hypoglycemic effect of Hypoglycemia-Associated Agents. Monitor therapy

Insulin: SGLT2 Inhibitors may enhance the hypoglycemic effect of Insulin. Management: Consider a decrease in insulin dose when initiating therapy with a sodium-glucose cotransporter 2 inhibitor and monitor patients for hypoglycemia. Consider therapy modification

Loop Diuretics: Empagliflozin may enhance the hypotensive effect of Loop Diuretics. Monitor therapy

MAO Inhibitors: May enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Monitor therapy

Pegvisomant: May enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Monitor therapy

Quinolone Antibiotics: May enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Quinolone Antibiotics may diminish the therapeutic effect of Blood Glucose Lowering Agents. Specifically, if an agent is being used to treat diabetes, loss of blood sugar control may occur with quinolone use. Monitor therapy

Salicylates: May enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Monitor therapy

Selective Serotonin Reuptake Inhibitors: May enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Monitor therapy

Sulfonylureas: SGLT2 Inhibitors may enhance the hypoglycemic effect of Sulfonylureas. Management: Consider a decrease in sulfonylurea dose when initiating therapy with a sodium-glucose cotransporter 2 inhibitor and monitor patients for hypoglycemia. Consider therapy modification

Teriflunomide: May increase the serum concentration of OAT3 Substrates. Monitor therapy

Thiazide and Thiazide-Like Diuretics: May diminish the therapeutic effect of Antidiabetic Agents. Monitor therapy


Monitoring Parameters

Blood glucose, HbA1c (at least twice yearly in patients who have stable glycemic control and are meeting treatment goals; quarterly in patients not meeting treatment goals or with therapy change (ADA 2016b); renal function and volume status (baseline and periodically during treatment); LDL-C; monitor for genital mycotic infections and UTI; blood pressure; ketoacidosis


Lab Test Interferences


Test Interactions

Positive test for glucosuria; may interfere with 1,5-anhydroglucitol (1,5-AG) assay; use alternative methods to monitor glycemic control.


Adverse Reactions


>10%:

Endocrine & metabolic: Hypoglycemia (combination therapy with insulin: 28%, severe hypoglycemia: ≤1%; combination therapy with metformin and a sulfonylurea: 12% to 16%; combination therapy with metformin: 1% to 2%)

Genitourinary: Urinary tract infection (9%; females: 18%; males: 4%), increased urine output (includes polyuria, pollakiuria, nocturia: 3%)

1% to 10%:

Endocrine & metabolic: Increased LDL cholesterol (5% to 7%), dyslipidemia (4%), increased thirst (including polydipsia: 2%)

Gastrointestinal: Nausea (2%)

Hematologic & oncologic: Increased hematocrit (3% to 4%)

Infection: Genitourinary fungal infection (4%; females: 5% to 6% [includes bacterial vaginosis, cervicitis, vulvitis, vulvovaginal candidiasis, vulvovaginal infection, vulvovaginitis]; males: 2% to 3% [includes balanitis, balanoposthitis, genitourinary fungal infection, penile infection, scrotal abscess])

<1% (Limited to important or life-threatening): Decreased estimated GFR (eGFR), hypotension, hypovolemia, increased serum creatinine, ketoacidosis (FDA Safety Communication, December 4, 2015), phimosis, pyelonephritis (FDA Safety Communication, December 4, 2015), urosepsis (FDA Safety Communication, December 4, 2015)


Warnings/Precautions


Special Populations: Renal Function Impairment

AUC was increased and clearance was decreased in patients with impaired renal function


Special Populations: Hepatic Function Impairment

In patients with mild, moderate, and severe hepatic impairment, AUC increased by approximately 23%, 47%, and 75%, and Cmax increased by approximately 4%, 23%, and 48%, respectively.


Warnings/Precautions

Concerns related to adverse effects:

- Bone fractures: Increased incidence of bone fractures may occur. According to the American Diabetes Association guidelines, sodium glucose co-transporter-2 (SGLT2) inhibitors should be avoided in patients with fracture risk factors (ADA 2016a).

- Genital mycotic infections: May increase the risk of genital mycotic infections (eg, vulvovaginal mycotic infection, vulvovaginal candidiasis, vulvovaginitis, candida balanitis, balanoposthitis). Patients with a history of these infections or uncircumcised males are at greater risk.

- Hematologic: Elevated hemoglobin/hematocrit have been observed; use caution in patients with elevated hematocrit at baseline.

- Hypotension: May cause symptomatic hypotension due to intravascular volume depletion especially in patients with renal impairment, the elderly, patients on diuretics, or those with low systolic blood pressure. Assess volume status prior to initiation in patients at risk of hypotension and correct if depleted; monitor signs and symptoms of hypotension after initiation and increase monitoring in clinical situations where volume contraction is expected.

- Ketoacidosis: Cases of ketoacidosis (some fatal) resulting in urgent hospitalization have been reported in patients with type 1 and type 2 diabetes mellitus receiving sodium glucose co-transporter-2 (SGLT2) inhibitors; before initiating treatment consider risk factors that may predispose to ketoacidosis (eg, pancreatic insulin deficiency from any cause, caloric restriction, and alcohol abuse). Patients presenting with nausea/vomiting, abdominal pain, generalized malaise, and/or shortness of breath should be assessed immediately for ketoacidosis; if indicated, consider interruption or discontinuation of therapy.

- Lipid abnormality: May cause low-density lipoprotein cholesterol (LDL-C) elevation; monitor LDL-C and treat as needed.

- Renal effects: Abnormalities in renal function (decreased eGFR, increased serum creatinine) may occur; elderly patients and patients with preexisting renal impairment may be at greater risk.

- Urinary tract infection: Serious urinary infections including urosepsis and pyelonephritis requiring hospitalization have been reported; treatment with SGLT2 inhibitors increases the risk for urinary tract infection (UTI); monitor for signs and symptoms of UTI and treat as needed.

Disease-related concerns:

- Renal impairment: Glycemic efficacy may be decreased and risk of adverse reactions (eg, adverse reaction related to volume depletion, renal impairment, UTI) may be increased with worsening renal function. Assess renal function prior to initiation and periodically during treatment, empagliflozin should not be initiated in patients with eGFR <45 mL/minute/1.73 m2 and should be discontinued when eGFR is persistently <45 mL/minute/1.73 m2. Use is contraindicated in severe renal impairment (eGFR <30 mL/minute/1.73 m2), ESRD, and in dialysis patients.

Concurrent drug therapy issues:

- Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Special populations:

- Elderly: Risk of intravascular volume depletion, renal impairment, and UTI may be increased in elderly patients.

Other warnings/precautions:

- Appropriate use: Not for use in patients with diabetic ketoacidosis (DKA) or patients with type 1 diabetes mellitus (insulin-dependent, IDDM).


Pregnancy Risk Factor

C


Pregnancy Considerations

Adverse events were observed in some animal reproduction studies. The manufacturer recommends the use of alternative therapies in pregnant women, especially during the second and third trimesters.

In women with diabetes, maternal hyperglycemia can be associated with congenital malformations as well as adverse effects in the fetus, neonate, and the mother (ACOG 2005; ADA 2015; Kitzmiller 2008; Metzger 2007). To prevent adverse outcomes, prior to conception and throughout pregnancy maternal blood glucose and HbA1c should be kept as close to target goals as possible but without causing significant hypoglycemia (ACOG 2013; ADA 2015; Blumer 2013; Kitzmiller 2008). Prior to pregnancy, effective contraception should be used until glycemic control is achieved (Kitzmiller 2008). Other agents are currently recommended to treat diabetes in pregnant women (ACOG 2013; Blumer 2013).


Actions


Pharmacology

By inhibiting sodium-glucose cotransporter 2 (SGLT2) in the proximal renal tubules, empagliflozin reduces reabsorption of filtered glucose from the tubular lumen and lowers the renal threshold for glucose (RTG). SGLT2 is the main site of filtered glucose reabsorption; reduction of filtered glucose reabsorption and lowering of RTG result in increased urinary excretion of glucose, thereby reducing plasma glucose concentrations.


Distribution

Vd: 73.8 L


Metabolism

Primarily through glucuronidation by UGT2B7, UGT1A3, UGT1A8, and UGT1A9 to minor metabolites


Excretion

Urine (54.4%; 50% as unchanged drug); feces (41.2%; majority as unchanged drug)


Time to Peak

1.5 hours


Half-Life Elimination

12.4 hours


Protein Binding

86.2%


Patient and Family Education


Patient Education

- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

- Have patient report immediately to prescriber signs of fluid and electrolyte problems (mood changes, confusion, muscle pain or weakness, abnormal heartbeat, very bad dizziness or passing out, fast heartbeat, more thirst, seizures, feeling very tired or weak, not hungry, unable to pass urine or change in the amount of urine produced, dry mouth, dry eyes, or nausea or vomiting), signs of kidney problems (urinary retention, blood in urine, change in amount of urine passed, or weight gain), signs of lactic acidosis (fast breathing, fast heartbeat, abnormal heartbeat, vomiting, drowsiness, shortness of breath, feeling very tired or weak, severe dizziness, feeling cold, or muscle pain or cramps), signs of a urinary tract infection (blood in the urine, burning or pain when passing urine, polyuria, fever, lower abdominal pain, or pelvic pain), signs of low blood sugar (dizziness, headache, fatigue, feeling weak, shaking, a fast heartbeat, confusion, hunger, or sweating), vaginal yeast infection, or penile yeast infection (HCAHPS).

- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

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