ertugliflozin (Rx)

Brand and Other Names:Steglatro
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

tablet

  • 5mg
  • 15mg

Type 2 Diabetes Mellitus

Indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus

Recommended starting dose is 5 mg PO qDay in the morning

If starting dose tolerated and additional glycemic control is needed, increase dose to maximum of 15 mg qDay

Dosage Modifications

Concomitant use with insulin and insulin secretagogues may increase the risk of hypoglycemia; lower dose of insulin or insulin secretagogue may be required to minimize the risk of hypoglycemia when used in combination with ertugliflozin

Renal impairment

  • eGFR ≥45 mL/min/1.73 m2: No dosage adjustment necessary
  • eGFR <45 mL/min/1.73 m2: Not recommended
  • Hemodialysis: Contraindicated

Hepatic impairment

  • Mild-to-moderate: No dosage adjustment necessary
  • Severe: Not recommended

Dosing Considerations

Assess renal function before initiating and as clinically indicated

In patients with volume depletion, correct this condition before initiating

Limitations of use

  • Not recommended in patients with type 1 diabetes mellitus; may increase risk of diabetic ketoacidosis in these patients

<18 years: Safety and efficacy not established

≥65 years: No dosage adjustment necessary

Patients aged ≥65 years had a higher incidence of adverse reactions related to volume depletion compared with younger patients

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Interactions

Interaction Checker

and ertugliflozin

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    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

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            Contraindicated (0)

              Serious - Use Alternative (0)

                Monitor Closely (22)

                • chlorpropamide

                  ertugliflozin, chlorpropamide. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Consider a lower dose of insulin or insulin secretagogue to avoid hypoglycemia when coadministered with ertugliflozin.

                • glimepiride

                  ertugliflozin, glimepiride. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Consider a lower dose of insulin or insulin secretagogue to avoid hypoglycemia when coadministered with ertugliflozin.

                • glipizide

                  ertugliflozin, glipizide. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Consider a lower dose of insulin or insulin secretagogue to avoid hypoglycemia when coadministered with ertugliflozin.

                • glyburide

                  ertugliflozin, glyburide. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Consider a lower dose of insulin or insulin secretagogue to avoid hypoglycemia when coadministered with ertugliflozin.

                • ifosfamide

                  ifosfamide, ertugliflozin. Either increases toxicity of the other by nephrotoxicity and/or ototoxicity. Use Caution/Monitor. Monitor renal function in patients with severe renal impairment, severe intestinal inflammation, or prolonged use >2 gm/day.

                • insulin aspart

                  ertugliflozin, insulin aspart. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Consider a lower dose of insulin or insulin secretagogue to avoid hypoglycemia when coadministered with ertugliflozin.

                • insulin aspart protamine/insulin aspart

                  ertugliflozin, insulin aspart protamine/insulin aspart. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Consider a lower dose of insulin or insulin secretagogue to avoid hypoglycemia when coadministered with ertugliflozin.

                • insulin degludec

                  ertugliflozin, insulin degludec. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Consider a lower dose of insulin or insulin secretagogue to avoid hypoglycemia when coadministered with ertugliflozin.

                • insulin detemir

                  ertugliflozin, insulin detemir. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Consider a lower dose of insulin or insulin secretagogue to avoid hypoglycemia when coadministered with ertugliflozin.

                • insulin glargine

                  ertugliflozin, insulin glargine. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Consider a lower dose of insulin or insulin secretagogue to avoid hypoglycemia when coadministered with ertugliflozin.

                • insulin glulisine

                  ertugliflozin, insulin glulisine. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Consider a lower dose of insulin or insulin secretagogue to avoid hypoglycemia when coadministered with ertugliflozin.

                • insulin inhaled

                  ertugliflozin, insulin inhaled. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Consider a lower dose of insulin or insulin secretagogue to avoid hypoglycemia when coadministered with ertugliflozin.

                • insulin isophane human/insulin regular human

                  ertugliflozin, insulin isophane human/insulin regular human. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Consider a lower dose of insulin or insulin secretagogue to avoid hypoglycemia when coadministered with ertugliflozin.

                • insulin lispro

                  ertugliflozin, insulin lispro. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Consider a lower dose of insulin or insulin secretagogue to avoid hypoglycemia when coadministered with ertugliflozin.

                • insulin lispro protamine/insulin lispro

                  ertugliflozin, insulin lispro protamine/insulin lispro. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Consider a lower dose of insulin or insulin secretagogue to avoid hypoglycemia when coadministered with ertugliflozin.

                • insulin NPH

                  ertugliflozin, insulin NPH. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Consider a lower dose of insulin or insulin secretagogue to avoid hypoglycemia when coadministered with ertugliflozin.

                • insulin regular human

                  ertugliflozin, insulin regular human. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Consider a lower dose of insulin or insulin secretagogue to avoid hypoglycemia when coadministered with ertugliflozin.

                • nateglinide

                  ertugliflozin, nateglinide. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Consider a lower dose of insulin or insulin secretagogue to avoid hypoglycemia when coadministered with ertugliflozin.

                • repaglinide

                  ertugliflozin, repaglinide. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Consider a lower dose of insulin or insulin secretagogue to avoid hypoglycemia when coadministered with ertugliflozin.

                • somapacitan

                  somapacitan decreases effects of ertugliflozin by pharmacodynamic antagonism. Modify Therapy/Monitor Closely. Growth hormone products may decrease insulin sensitivity, particularly at higher doses. Antidiabetic agents may require dose adjustment after initiating somapacitan. .

                • tolazamide

                  ertugliflozin, tolazamide. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Consider a lower dose of insulin or insulin secretagogue to avoid hypoglycemia when coadministered with ertugliflozin.

                • tolbutamide

                  ertugliflozin, tolbutamide. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Consider a lower dose of insulin or insulin secretagogue to avoid hypoglycemia when coadministered with ertugliflozin.

                Minor (0)

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                  Adverse Effects

                  >10%

                  Female genital mycotic infections (9.1-12.2%)

                  1-10%

                  Volume depletion adverse effects (1.9-4.4%)

                  Male genital mycotic infections (3.7-4.2%)

                  Urinary tract infections (4-4.1%)

                  Headache (2.9-3.5%)

                  Vaginal pruritus (2.4-2.8%)

                  Increased urination (2.4-2.7%)

                  Nasopharyngitis (2-2.5%)

                  Back pain (1.7-2.5%)

                  Renal adverse effects (1.3-2.5%)

                  Weight decreased (1.2-2.4%)

                  Thirst (1.4-2.7%)

                  Adverse Effects

                  Postmarketing Reports

                  Necrotizing fasciitis of the perineum (Fournier’s Gangrene)

                  Angioedema

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                  Warnings

                  Contraindications

                  Hypersensitivity to ertugliflozin or any excipient; reactions such as angioedema have occurred

                  Patients on dialysis

                  Cautions

                  Causes intravascular volume contraction; symptomatic hypotension may occur after initiating, particularly in patients with renal impairment, with low systolic blood pressure, on diuretics, or who are elderly; before initiating treatment in patients with one or more of risk factors, assess volume status and renal function

                  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 ertugliflozin 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

                  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

                  Increases risk of urinary tract infections (UTIs), including life-threatening urosepsis and pyelonephritis that started as UTIs

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

                  Dose-related increases in LDL-C reported

                  No conclusive evidence of macrovascular risk reduction with empagliflozin or any other antidiabetic agent

                  Lower limb amputations

                  • An increased risk for lower limb amputation (primarily of the toe) has been observed in clinical studies with another SGLT2 inhibitor; before initiating, consider factors that may predispose patient to increased risk of amputations (eg, history of prior amputation, peripheral vascular disease, neuropathy, diabetic foot ulcers)
                  • Counsel patients about importance of routine preventative foot care; monitor patients receiving drug for signs and symptoms of infection (including osteomyelitis), new pain or tenderness, sores or ulcers involving the lower limbs, and discontinue therapy if these complications occur

                  Ketoacidosis

                  • Not indicated for patients with type 1 diabetes mellitus (T1DM); in placebo-controlled trials, risk of ketoacidosis was increased in patients with T1DM who received SGLT2 inhibitors
                  • Risk of ketoacidosis may be greater with higher doses
                  • Before initiating therapy, consider factors in patient history that may predispose to ketoacidosis, including pancreatic insulin deficiency from any cause, caloric restriction, and alcohol abuse
                  • Consider temporarily discontinuing therapy for at least 3 days for patients who undergo scheduled surgery
                  • 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 prior to restarting therapy
                  • Restart once the patient’s oral intake is back to baseline and any other risk factors for ketoacidosis (blood acid buildup) are resolved

                  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

                  • 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

                  Pregnancy

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

                  Data are limited in pregnant women and are not sufficient to determine a drug-associated risk of adverse developmental outcomes; there are risks to the mother and fetus associated with poorly controlled diabetes in pregnancy

                  Animal data

                  • In animal studies, adverse renal changes were observed in rats when ertugliflozin was administered during a period of renal development corresponding to the late second and third trimesters of human pregnancy; doses ~13 times the maximum clinical dose caused renal pelvic and tubule dilatations and renal mineralization that were not fully reversible
                  • There was no evidence of fetal harm in rats or rabbits at exposures of ertugliflozin ~300 times higher than the maximal clinical dose of 15 mg/day when administered during organogenesis

                  Lactation

                  Not recommended while breastfeeding

                  Unknown if distributed in human breast milk

                  Since human kidney maturation occurs in utero and during the first 2 years of life when lactational exposure may occur, there may be risk to the developing human kidney

                  Because of the potential for serious adverse reactions in a breastfed infant, advise women that ertugliflozin 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 inhibition lowers the renal glucose threshold (ie, the plasma glucose concentration, which exceeds the maximum glucose reabsorption capacity of the kidney); lowering the renal glucose threshold results in increased urinary glucose excretion

                  Absorption

                  Peak plasma time: 1 hr (fasting); 2 hr (high-fat, high-caloric meal)

                  Peak plasma concentration, steady-state: 81.3 ng/mL (5 mg qDay); 268 ng/mL (15 mg qDay)

                  AUC, steady-state: 398 ng⋅hr/mL (5 mg qDay); 1,193 ng⋅hr/mL (15 mg qDay)

                  Steady-state is reached after 4-6 days

                  Bioavailability, 15 mg dose: ~100%

                  Distribution

                  Vd, steady-state: 85.5 L

                  Protein binding: 93.6%

                  Blood-to-plasma concentration ratio of ertugliflozin: 0.66

                  Metabolism

                  Major metabolic pathway for ertugliflozin is UGT1A9 and UGT2B7-mediated O-glucuronidation to 2 glucuronides (pharmacologically inactive at clinically relevant concentrations)

                  YP-mediated (oxidative) metabolism of ertugliflozin is minimal (12%)

                  Excretion

                  Half-life: 16.6 hr

                  Clearance: 11.2 L/hr

                  Excretion, oral [14C]-ertugliflozin solution: Feces (40.9%); urine (50.2%)

                  Excretion, unchanged ertugliflozin: Feces (33.8%); urine (1.5%)

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                  Administration

                  Oral administration

                  Take in the morning qDay, with or without food

                  Missed dose

                  • Take it as soon as possible
                  • If it is almost time for next scheduled dose, skip missed dose and take the next regularly scheduled time
                  • Do not take 2 doses of ertugliflozin at the same time

                  Storage

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

                  Keep tablets dry

                  Store blister packs in the original package

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                  Images

                  BRAND FORM. UNIT PRICE PILL IMAGE
                  Steglatro oral
                  -
                  5 mg tablet
                  Steglatro oral
                  -
                  15 mg tablet

                  Copyright © 2010 First DataBank, Inc.

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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.
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                  NC NOT COVERED – Drugs that are not covered by the plan.
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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.