ertugliflozin

Absorption: Completely absorbed following oral administration.

Distribution: Extensively distributed to tissues.

Metabolism/Excretion: Mostly metabolized by UDP-glucuronyl transferases (UGT) to inactive metabolites; minimal metabolism by CYP isoenzymes (12%). 41% excreted in feces (33.8% as unchanged drug), 50.2% excreted in urine (1.5% as unchanged drug).

Half-Life: 16.6 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	1 hr	24 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
eGFR <45 mL/min/1.73 m² or on dialysis;
Type 1 diabetes;
Diabetic ketoacidosis;
Severe hepatic impairment;
OB: Avoid use during 2nd and 3rd trimesters ( risk of renal impairment in fetus);
Lactation: Lactation.

Use Cautiously in:

Renal impairment (eGFR <60 mL/min/1.73 m²), age ≥65 yr, low systolic BP, or concurrent use of diuretics (↑ risk of hypotension);
Acute febrile illness, reduced caloric intake due to illness or surgery, history of pancreatitis or pancreatic surgery, or alcohol abuse (↑ risk of ketoacidosis);
Hypovolemia, chronic kidney disease, HF, or concurrent use of diuretics, NSAIDs, ACE inhibitors, or angiotensin receptor blockers (↑ risk of acute kidney injury);
Previous amputation, peripheral vascular disease, neuropathy, or diabetic foot infection (↑ risk of lower limb amputation);
History of genital mycotic infections or uncircumcised (↑ risk of genital mycotic infections);
OB: Use during 1st trimester only if potential maternal benefit justifies potential fetal risk;
Pedi: Safety and effectiveness not established in children;
Geri: Appears on Beers list. Older adults may have risk of urogenital infections (especially women in the 1st mo of treatment) and euglycemic diabetic ketoacidosis. Use with caution in older adults.

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypotension

Endo: hypoglycemia (↑ with other medications)

F and E: dehydration, KETOACIDOSIS, polydipsia

GI: ↓weight

GU: genital mycotic infection, acute kidney injury, NECROTIZING FASCIITIS OF PERINEUM (FOURNIER'S GANGRENE), polyuria, urinary tract infection (including pyelonephritis), UROSEPSIS, vaginal pruritus

Metab: hyperlipidemia

MS: back pain, lower limb amputation (primarily toe and foot)

Neuro: dizziness, headache, syncope

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANGIOEDEMA)

Interactions ⬆ ⬇

Drug-drug:

↑risk of hypoglycemia with insulin or insulin secretagogues; dose adjustments may be required.
Concurrent use with NSAIDs, diuretics, ACE inhibitors, or angiotensin receptor blockers may ↑ risk of acute kidney injury.
May ↓ lithium levels and effectiveness.

Route/Dosage ⬆ ⬇

PO (Adults ): 5 mg once daily initially; may ↑ to 15 mg once daily if needed.

Availability ⬆ ⬇

(Generic available)

Tablets: 5 mg; 15 mg
In combination with: metformin (Segluromet); sitagliptin (Steglujan). See Appendix [not included in this PDA edition]

Assessment ⬆ ⬇

Observe patient for signs and symptoms of hypoglycemic reactions (abdominal pain, sweating, hunger, weakness, dizziness, headache, tremor, tachycardia, anxiety).
Monitor for signs and symptoms of volume depletion (dizziness, feeling faint, weakness, orthostatic hypotension) after initiating therapy.
Monitor for signs and symptoms of ketoacidosis (nausea, vomiting, abdominal pain, generalized malaise, shortness of breath). Treat clinically and discontinue ertugliflozin if ketoacidosis occurs.
Monitor for urinary tract infection, new pain, pain on urination, fever, flank pain, tenderness, sores, or ulcers involving lower limbs; discontinue ertugliflozin if these occur.
Monitor for signs and symptoms of necrotizing fasciitis of the perineum (pain or tenderness, erythema, or swelling in the genital or perineal area, along with fever or malaise). If suspected, discontinue ertugliflozin, monitor blood glucose levels, and provide alternative therapy for glycemic control. Start treatment immediately with broad-spectrum antibiotics. May require surgical debridement.

Lab Test Considerations:

Monitor hemoglobin A1C prior to and periodically during therapy.
- May cause ↑ uric acid levels.
- Assess renal function prior to and periodically during therapy. May ↑ serum creatinine and ↓ eGFR. Monitor renal function, especially in patients with eGFR <60 mL/min/1.73 m².
- May cause ↑ serum phosphate levels.
- May cause ↑ LDL-C. Monitor serum lipid levels periodically during therapy.
- Causes positive test for urine glucose.
- Monitor for ketoacidosis, especially during prolonged fasting for illness or surgery. Consider temporarily discontinuing therapy for at least 4 days prior to surgery.

Implementation ⬆ ⬇

Do not confuse Steglatro with Spravato.
Correct volume depletion before starting ertugliflozin.
Patients stabilized on a diabetic regimen who are exposed to stress, fever, trauma, infection, or surgery may require administration of insulin.
Correct volume depletion prior to beginning therapy with ertugliflozin.
PO: Administer in morning with or without food.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take ertugliflozin as directed. Take missed doses as soon as remembered, unless it is almost time for next dose; do not double doses. Advise patient to read the Medication Guide before starting and with each Rx refill in case of changes.
Explain to patient that ertugliflozin helps control hyperglycemia but does not cure diabetes. Therapy is usually long term.
Instruct patient not to share this medication with others, even if they have the same symptoms; it may harm them.
Encourage patient to follow prescribed diet, medication, and exercise regimen to prevent hyperglycemic or hypoglycemic episodes.
Review signs of hypoglycemia and hyperglycemia with patient. If hypoglycemia occurs, advise patient to take a glass of orange juice or 2–3 tsp of sugar, honey, or corn syrup dissolved in water, and notify health care professional.
Instruct patient in proper testing of blood glucose and urine ketones. Inform patient that ertugliflozin will cause a positive test result when testing for urine glucose. Advise patient to monitor ketones, even if blood glucose is not elevated and blood glucose during periods of stress or illness. Notify health care professional if signs and symptoms of ketoses or significant changes occur.
Inform patient that ertugliflozin may cause yeast infections. Women may have signs and symptoms of a vaginal yeast infection (vaginal odor, white or yellow vaginal discharge [may be lumpy or look like cottage cheese], vaginal itching). Men may have signs and symptoms of a yeast infection of the penis (redness, itching, or swelling of penis; rash on penis; foul smelling discharge from penis; pain in skin around penis). Advise patient to notify health care professional if yeast infection occurs.
Advise patient to notify health care professional promptly if rash; hives; or swelling of face, lips, or throat occur.
Advise patient to notify health care professional if signs and symptoms of urinary tract infections (painful urination, flank pain, fever), hypotension, or perineal necrotizing fasciitis (pain or tenderness, redness, or swelling of genitals or area from genitals back to the rectum, with a fever above 100.4°F; malaise) occur.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications, especially other oral hypoglycemic medications.
Rep: Advise females of reproductive potential to use effective contraception, especially during the 2nd and 3rd trimesters and to avoid breastfeeding during therapy. Advise patient to notify health care professional if pregnancy is planned or suspected.

Evaluation/Desired Outcomes ⬆ ⬇

Improved hemoglobin A1C and glycemic control in adults with type 2 diabetes.

US Brand Names ⬆ ⬇

Code ⬆

NDC Code

0006- Merck Sharp and Dohme Corp.
- 0006-5363- STEGLATRO
  - 0006-5363-03- 30 TABLET, FILM COATED in 1 BOTTLE (0006-5363-03)

0006- Merck Sharp and Dohme Corp.
- 0006-5363- STEGLATRO
  - 0006-5363-06- 90 TABLET, FILM COATED in 1 BOTTLE (0006-5363-06)

0006- Merck Sharp and Dohme Corp.
- 0006-5363- STEGLATRO
  - 0006-5363-07- 500 TABLET, FILM COATED in 1 BOTTLE (0006-5363-07)

0006- Merck Sharp and Dohme Corp.
- 0006-5363- STEGLATRO
  - 0006-5363-09- 2 BOTTLE in 1 CARTON (0006-5363-09) > 7 TABLET, FILM COATED in 1 BOTTLE (0006-5363-08)

0006- Merck Sharp and Dohme Corp.
- 0006-5363- STEGLATRO
  - 0006-5363-10- 30 TABLET, FILM COATED in 1 BOTTLE (0006-5363-10)

0006- Merck Sharp and Dohme Corp.
- 0006-5364- STEGLATRO
  - 0006-5364-03- 30 TABLET, FILM COATED in 1 BOTTLE (0006-5364-03)

0006- Merck Sharp and Dohme Corp.
- 0006-5364- STEGLATRO
  - 0006-5364-06- 90 TABLET, FILM COATED in 1 BOTTLE (0006-5364-06)

0006- Merck Sharp and Dohme Corp.
- 0006-5364- STEGLATRO
  - 0006-5364-07- 500 TABLET, FILM COATED in 1 BOTTLE (0006-5364-07)

0006- Merck Sharp and Dohme Corp.
- 0006-5364- STEGLATRO
  - 0006-5364-09- 2 BOTTLE in 1 CARTON (0006-5364-09) > 7 TABLET, FILM COATED in 1 BOTTLE (0006-5364-08)

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇