bexagliflozin

Absorption: Well absorbed following oral administration.

Distribution: Extensive tissue distribution.

Protein Binding: 93%.

Metabolism/Excretion: Mostly metabolized by UDP-glucuronyl transferases (UGT) to inactive metabolites, with minimal metabolism by CYP3A. 51% excreted in feces (mostly as parent drug), 40% in urine (mostly as metabolites).

Half-Life: 12 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	2–4 hr	24 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Severe renal impairment (eGFR <30 mL/min/1.73 m²);
Type 1 diabetes;
Severe hepatic impairment;
OB: Use not recommended during 2nd and 3rd trimesters of pregnancy (may cause fetal harm); other agents recommended for glycemic control during pregnancy;
Lactation: Lactation.

Use Cautiously in:

History of pancreatitis, pancreatic surgery, reduced caloric intake due to illness or surgery, surgical procedures, or alcohol abuse (↑ risk of ketoacidosis);
Hypovolemia, chronic kidney disease (eGFR <60 mL/min/1.73 m²), low systolic BP, or concurrent use of loop diuretics (↑ risk of volume depletion or hypotension);
Previous amputation, peripheral vascular disease, neuropathy, or diabetic foot infection (↑ risk of lower limb amputation);
Pedi: Safety and effectiveness not established in children;
Geri: Older adults at risk of volume depletion or hypotension.

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypotension

Derm: rash

Endo: hypoglycemia (↑ with other medications)

F and E: KETOACIDOSIS, dehydration, thirst

GU: genital mycotic infections, acute kidney injury, glucosuria, ↓renal function, ↑urination, NECROTIZING FASCIITIS OF PERINEUM (FOURNIER'S GANGRENE), urinary tract infection (including pyelonephritis), UROSEPSIS, vulvovaginal pruritus

MS: bone fractures, lower limb amputation

Neuro: dizziness

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS OR ANGIOEDEMA)

Interactions ⬆ ⬇

Drug-drug:

UGT inducers, including phenobarbital, phenytoin, rifampin, and ritonavir, may ↓ levels and effectiveness; may need to add another antihyperglycemic medication if additional glycemic control needed.
↑risk of hypoglycemia with insulin or insulin secretagogues; may need to lower dose of insulin or insulin secretagogue.
Concurrent use with loop diuretics may ↑ risk of hypovolemia and hypotension.

Route/Dosage ⬆ ⬇

PO (Adults ): 20 mg once daily in the morning.

Availability ⬆ ⬇

Assessment ⬆ ⬇

Monitor fluid volume status at initiation and throughout therapy; correct volume status prior to therapy initiation, especially in patients with hypotension, renal impairment, or concomitantly receiving diuretics.
BP should be monitored throughout therapy; ↑ risk of symptomatic hypotension in older adults and those concomitantly receiving diuretics.
Monitor for signs and symptoms of hypoglycemia (nausea, tachycardia, sweating, hunger, dizziness, light-headedness, confusion, anxiety), especially if used concomitantly with insulin and insulin secretagogues; dosage adjustment of insulin or insulin secretagogues may be necessary.
Monitor for signs and symptoms of ketoacidosis regardless of blood glucose levels (weakness, fatigue, flushed face, nausea, vomiting, thirst, fruity breath, polyuria). Older adults and women at ↑ risk especially in 1st mo of therapy. Treat promptly and provide supportive care.
Monitor for signs and symptoms of urinary tract infection (fever, dysuria, polyuria, hematuria, flank pain, suprapubic pain or pressure). Genital mycotic infections (genital pruritis and yeasty discharge) may occur, especially in patients with history of genital mycotic infections; females and uncircumcised males at higher risk. Treat infection promptly.
Assess the lower limbs for signs and symptoms of infection, including osteomyelitis, new pain or tenderness, and sores or ulcers especially in patients with a history of prior amputation, peripheral arterial disease, neuropathy, or diabetic foot ulcers.
Assess for signs and symptoms of necrotizing fasciitis of the perineum (Fournier gangrene—tenderness, redness, or swelling of the genitals or perineum; fever; malaise; perineal skin discoloration or gangrenous appearance; drainage; sores; blisters; foul odor).

Lab Test Considerations:

Verify a negative pregnancy test before starting therapy.
- Assess renal function at baseline, regularly during therapy, and as clinically indicated. Can ↑ serum creatinine and ↓ eGFR.
- Check A1c twice yearly in patients who are meeting treatment goals, every 3 mo in patients whose therapy has changed or who are not meeting glycemic goals, and more frequently as clinically warranted.
- Monitor ketones in patients at risk for ketoacidosis.
- May ↑ LDL-C.
- May ↑ hemoglobin and hematocrit.

Implementation ⬆ ⬇

Correct volume depletion prior to initiation, especially older adults or those who are hypotensive, have renal impairment, or are concomitantly receiving diuretics .
PO: Administer one tablet once daily in the morning without regard to food.DNC: Do not crush or chew tablet.

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of bexagliflozin to patient. Instruct them to take medication as directed. If a dose is missed, take the dose as soon as possible. Do not double the next dose. Advise patient to read Patient Information before starting therapy and with each Rx refill in case of changes.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications, especially lithium.
Teach the patient how and when to self-monitor blood glucose and how to treat hypoglycemia. Glucose tablets, glucose gel, cranberry juice, or hard candy should be kept at home for use in hypoglycemia emergency. Symptoms of hypoglycemia include nausea, rapid heartbeat, sweating, hunger, dizziness, light-headedness, confusion, and anxiety.
Tell patient to maintain adequate hydration to prevent hypotension and report symptoms of hypotension (faintness, light-headedness, dizziness, palpitations, heart racing).
Instruct patient to immediately seek treatment for and report symptoms of ketoacidosis (weakness, fatigue, flushed face, nausea, vomiting, thirst, fruity breath, frequent urination).
Tell patient to immediately seek treatment for and report symptoms of necrotizing fasciitis of the perineum (Fournier gangrene—tenderness, redness, or swelling of the genitals or perineum; fever; malaise; perineal skin discoloration; sores; blisters; drainage; foul odor).
Teach about the importance of and how to perform meticulous daily foot and lower leg care. Counsel patient to report new pain or tenderness, sores, ulcers, or infections involving the leg or foot.
Advise patient to report symptoms of urinary tract infection (fever, frequent and painful urination, bloody urine, flank pain, pelvic pain or pressure) or genital mycotic infections (genital itchiness and yeasty discharge).
Rep: Instruct patient to notify health care professional if pregnancy if planned or suspected or if breastfeeding. Avoid use in 2nd and 3rd trimester and weigh risk vs. benefit of use during 1st trimester. Avoid use during breastfeeding.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇