Steglujan

— THERAPEUTIC CATEGORIES —
  • Diabetes

Steglujan Generic Name & Formulations

General Description

Ertugliflozin, sitagliptin; 5mg/100mg, 15mg/100mg; tabs.

Pharmacological Class

Sodium-glucose co-transporter 2 (SGLT2) inhibitor + dipeptidyl peptidase-4 (DPP-4) inhibitor.

How Supplied

Tabs—30, 90

Manufacturer

Generic Availability

NO

Mechanism of Action

Ertugliflozin inhibits SGLT2 reducing renal reabsorption of filtered glucose and lowers the renal threshold for glucose, and thereby increases urinary glucose excretion. Sitagliptin is believed to exert its actions in patients with type 2 diabetes mellitus by slowing the inactivation of incretin hormones. Concentrations of the active intact hormones are increased by sitagliptin, thereby increasing and prolonging the action of these hormones.

Steglujan Indications

Indications

Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

Limitations of Use

Not for improving glycemic control in patients with type 1 diabetes. Not studied in patients with a history of pancreatitis.

Steglujan Dosage and Administration

Adult

Swallow whole. Take in the AM. Initially 5mg/100mg once daily; if tolerated and need additional glycemic control; may increase to max 15mg/100mg once daily. Renal impairment (eGFR <45mL/min/1.73m2): not recommended.

Children

<18yrs: not established.

Steglujan Contraindications

Contraindications

Severe renal impairment (eGFR <30mL/min/1.73m2), ESRD, or on dialysis.

Steglujan Boxed Warnings

Not Applicable

Steglujan Warnings/Precautions

Warnings/Precautions

Increased risk for volume depletion or hypotension in those with renal impairment (eGFR <60mL/min/1.73m2), elderly, low systolic BP, or on loop diuretics. Assess volume status, renal function before and after initiating therapy. Correct volume depletion before initiating. Assess for ketoacidosis in presence of signs/symptoms of metabolic acidosis, regardless of blood glucose levels; discontinue if suspected; evaluate and treat if confirmed. Monitor for resolution of ketoacidosis before restarting. Withhold (at least 4 days), if possible, prior to major surgery or procedures associated with prolonged fasting. Consider risks/benefits in patients with known risk factors for heart failure; monitor for signs/symptoms; evaluate and consider discontinuing if develops. Monitor for pancreatitis, serious hypersensitivity reactions, severe joint pain, or bullous pemphigoid; discontinue if suspected or occurs. Necrotizing fasciitis of the perineum (Fournier's gangrene); discontinue and treat immediately if suspected; use alternative antidiabetic. Increased risk of genital mycotic infections, UTIs (including urosepsis, pyelonephritis); monitor and treat appropriately. Prior to initiation, consider factors that may predispose the need for amputations (eg, history of prior amputation, peripheral vascular disease, neuropathy, diabetic foot ulcers). Monitor for infection (including osteomyelitis), new pain/tenderness, sores or ulcers of the lower limbs; discontinue if occur. History of angioedema to other DPP-4 inhibitors. Severe hepatic impairment: not recommended. Elderly. Pregnancy (during 2nd & 3rd trimesters), nursing mothers: not recommended.

Steglujan Pharmacokinetics

Absorption

Peak plasma concentration: 1 hour postdose under fasted conditions (ertugliflozin). Absolute bioavailability: ~100% (ertugliflozin); ~87% (sitagliptin).

Distribution

Mean steady-state volume of distribution: 85.5 L (ertugliflozin); 198 L (sitagliptin). Plasma protein bound: 93.6% (ertugliflozin).

Metabolism

Ertugliflozin: UGT1A9, UGT2B7-mediated O-glucuronidation; CYP-mediated metabolism is minimal.

Elimination

Sitagliptin: renal (87%), fecal (13%). Ertugliflozin: renal (50.2%), fecal (40.9%). Half-life: 12.4 hours (sitagliptin), 16.6 hours (ertugliflozin). 

Steglujan Interactions

Interactions

Greater potential for volume depletion or hypotension with concomitant diuretics. May need a lower dose of concomitant insulin or insulin secretagogue (eg, sulfonylurea) to reduce risk of hypoglycemia. Ertugliflozin may antagonize serum lithium concentrations; monitor levels more frequently. Ertugliflozin will lead to false (+) urine glucose tests or unreliable measurements of 1,5-AG assay; use alternative methods to monitor glycemic control.

Steglujan Adverse Reactions

Adverse Reactions

Genital mycotic infections (esp. females), upper RTIs, nasopharyngitis, headache, UTIs, vaginal pruritus, increased urination, back pain, weight decrease, thirst; hypoglycemia, pancreatitis, ketoacidosis, renal impairment, severe and disabling arthralgia, bullous pemphigoid; rare: Fournier's gangrene.

Steglujan Clinical Trials

See Literature

Steglujan Note

Not Applicable

Steglujan Patient Counseling

See Literature