saxagliptin

REMS

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

Acts as a competitive inhibitor of dipeptidyl peptidase-4 (DPP4), which slows inactivation of incretin hormones, thereby increasing their concentrations and reducing fasting and postprandial glucose concentrations.

Therapeutic Effects:

Improved control of blood glucose.

Absorption: Well absorbed following oral administration.

Distribution: Unknown.

Metabolism/Excretion: Metabolized by the liver via the P450 3A4/5 (CYP3A4/5) enzyme system, with conversion to 5–hydroxysaxagliptin, a pharmacologically active metabolite; 24% of saxagliptin is excreted unchanged in urine, 36% of hydroxysaxagliptin is excreted unchanged in urine, 22% is eliminated in feces as unabsorbed drug/metabolites excreted in bile.

Half-life: Saxagliptin — 2.5 hr; 5–hydroxysaxagliptin — 3.1 hr.

Contraindicated in:

Type 1 diabetes
Diabetic ketoacidosis
History of hypersensitivity reaction.

Use Cautiously in:

HF or renal impairment (↑ risk of worsening HF)
Moderate or severe renal impairment (CCr 45 mL/min) (↓ dose required)
OB: Use only if potential maternal benefit justifies potential fetal risk
Lactation: Use while breast feeding only if potential maternal benefit outweighs potential risk to infant
Pedi: Safety and effectiveness not established
Geri: May be more sensitive to effects; consider age-related ↓ in renal function.

CNS: headache.

CV: HF, peripheral edema (↑ with thiazolidinediones).

Derm: bullous pemphigoid.

Endo: hypoglycemia (↑ with sulfonylureas).

GI: PANCREATITIS, abdominal pain, vomiting.

Hemat: ↓lymphocyte count.

MS: RHABDOMYOLYSIS, arthralgia.

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA).

Drug-Drug:

Strong CYP3A4/5 inhibitors, including ketoconazole, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, and saquinavir↑ blood levels; daily dose should not exceed 2.5 mg.
↑risk of hypoglycemia with sulfonylureas or insulin; may need to ↓ dose of sulfonylureas or insulin.

PO (Adults): 2.5–5 mg once daily; Concurrent use of strong CYP3A4/5 inhibitors — 2.5 mg once daily.

Renal Impairment

PO (Adults): CCr 45 mL/min (including patients undergoing hemodialysis) — 2.5 mg once daily; in patients undergoing hemodialysis, administer after hemodialysis.

Do not confuse saxagliptin with sitagliptin.
Patients stabilized on a diabetic regimen who are exposed to stress, fever, trauma, infection, or surgery may require administration of insulin.
PO: May be administered without regard to food. Swallow tablet whole, do not cut or split.

Therapeutic Classification: antidiabetics

Pharmacologic Classification: dipeptidyl peptidase-4 ddp-4 inhibitors

Tablets: 2.5 mg; 5 mg;
In combination with: dapagliflozin (Qtern); dapagliflozin and metformin XR (Qternmet XR); metformin XR (Kombiglyze XR). See Appendix [not included in this PDA edition].

(DDP-4 inhibition)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	2 hr (4 hr for 5–hydroxysaxagliptin)†	24 hr

†Blood levels.

Observe patient for signs and symptoms of hypoglycemic reactions (abdominal pain, sweating, hunger, weakness, dizziness, headache, tremor, tachycardia, anxiety).
Monitor for signs of pancreatitis (nausea, vomiting, anorexia, persistent severe abdominal pain, sometimes radiating to the back) during therapy. If pancreatitis occurs, discontinue saxagliptin and monitor serum and urine amylase, amylase/creatinine clearance ratio, electrolytes, serum calcium, glucose, and lipase.

Lab Test Considerations:

Monitor hemoglobin A1C prior to and periodically during therapy.
- Monitor renal function prior to and periodically during therapy.
- May cause ↓ absolute lymphocyte count.

Imbalanced nutrition: more than body requirements (Indications).
Noncompliance (Patient/Family Teaching).

Instruct patient to take saxagliptin as directed. If a dose is missed, take the next dose as prescribed; do not double doses. Advise patient to read the Patient Package Insert before starting and with each Rx refill; new information may be available.
Explain to patient that saxagliptin 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. These tests should be monitored closely during periods of stress or illness and health care professional notified if significant changes occur.
Advise patient to notify health care professional promptly if swelling of hands, feet, or ankles; rash; hives; or swelling of face, lips, or throat occur.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
Advise patient to notify health care professional if pregnancy is planned or suspected, or if breast feeding.

Improved hemoglobin A1C, fasting plasma glucose, and 2-hr post-prandial glucose levels.

NDC Code^*

0310- AstraZeneca Pharmaceuticals LP
0310-6100- ONGLYZA 0310-6100-30- 30 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (0310-6100-30)

0310- AstraZeneca Pharmaceuticals LP
0310-6100- ONGLYZA 0310-6100-90- 90 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (0310-6100-90)

0310- AstraZeneca Pharmaceuticals LP
0310-6100- ONGLYZA 0310-6100-95- 1 BLISTER PACK in 1 CARTON (0310-6100-95) > 7 TABLET, FILM COATED in 1 BLISTER PACK

0310- AstraZeneca Pharmaceuticals LP
0310-6105- ONGLYZA 0310-6105-30- 30 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (0310-6105-30)

0310- AstraZeneca Pharmaceuticals LP
0310-6105- ONGLYZA 0310-6105-50- 500 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (0310-6105-50)

0310- AstraZeneca Pharmaceuticals LP
0310-6105- ONGLYZA 0310-6105-90- 90 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (0310-6105-90)

0310- AstraZeneca Pharmaceuticals LP
0310-6105- ONGLYZA 0310-6105-95- 1 BLISTER PACK in 1 CARTON (0310-6105-95) > 7 TABLET, FILM COATED in 1 BLISTER PACK

55154- Cardinal Health
55154-6931- ONGLYZA 55154-6931-2- 1080 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (55154-6931-2)

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Pronunciation ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇

Contraind./Precautions ⬆ ⬇

Adv. Reactions/Side Effects ⬆ ⬇

Interactions ⬆ ⬇

Route/Dosage ⬆ ⬇

Implementation ⬆ ⬇

US Brand Names ⬆ ⬇

Classifications ⬆ ⬇

Availability ⬆ ⬇

Time/Action Profile ⬆ ⬇

Assessment ⬆ ⬇

Pot. Nursing Diagnoses ⬆ ⬇

Patient/Family Teaching ⬆ ⬇

Evaluation/Desired Outcomes ⬆ ⬇

Code ⬆