exenatide injectable suspension (Rx)

Brand and Other Names:Bydureon, Bydureon BCise
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

injectable suspension

  • 2mg/vial (Bydureon)
  • 2mg/syringe pen (Bydureon)

injectable suspension, single-dose autoinjector

  • 2mg/0.85mL (Bydureon BCise)
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Diabetes Mellitus Type 2

Indicated as adjunct to diet and exercise to improve glycemic control with DM type 2; not recommended as first-line therapy if inadequately controlled on diet and exercise; use with insulin has not been studied and is not recommended

2 mg SC once weekly

Changing from Byetta to Bydureon

  • Prior treatment with Byetta (short-acting exenatide) is not required when initiating Bydureon or Bydureon BCise therapy
  • If starting Bydureon or Bydureon BCise in a patient already taking Byetta, discontinue Byetta
  • Patients may experience transient (~2-4 weeks) elevations in blood glucose concentrations

Dosage Modifications (Bydureon)

Renal impairment

  • Mild (CrCl 50-80 mL/min): No dosage adjustment required
  • Moderate (CrCl 30-50 mL/min): Caution when initiating or escalating dose
  • Severe (eCrCl <30 mL/min) or end-stage renal disease (ESRD): Not recommended
  • Renal transplantation: Use with caution

Hepatic impairment

  • Has not been studied; cleared primarily by the kidney; hepatic impairment is not expected to affect blood concentrations

Dosage Modifications (Bydureon BCise)

Renal impairment

  • Mild (eCrCl 60-80 mL/min): No dosage adjustment required
  • Moderate (eCrCl 30-59 mL/min): Caution when initiating or escalating dose
  • Severe (eCrCl <30 mL/min) or ESRD: Not recommended
  • Renal transplantation: Use with caution

Dosing Considerations

Limitations of Use

  • Not recommended as first-line therapy for patients inadequately controlled on diet and exercise
  • Should not be used to treat type 1 diabetes or diabetic ketoacidosis
  • Use with insulin has not been studied and is not recommended Bydureon BCise and Bydureon are extended-release formulations of exenatide
  • Do not coadminister with other exenatide containing products Has not been studied in patients with a history of pancreatitis
  • Consider other antidiabetic therapies in patients with a history of pancreatitis

Safety and efficacy not established

Bydureon

In the 5 comparator-controlled trials exenatide injectable suspension was studied in 132 patients (16.6%) who were at least 65 years old and 20 patients who were at least 75 years old

No differences in safety or efficacy were observed between these patients and younger patients

Because elderly patients are more likely to have decreased renal function, use caution

Bydureon BCise

In 2 comparator-controlled 28-week trials, exenatide auto-injector was studied in 74 patients (18%) who were at least 65 years old and 10 patients who were at least 75 years old

No differences in safety or efficacy were observed between these patients and younger patients

Because elderly patients are more likely to have decreased renal function, use caution

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Interactions

Interaction Checker

and exenatide injectable suspension

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    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

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            Adverse Effects

            >10%

            Injection site nodule, Bydureon BCise (10.5%)

            Bydureon

            • Nausea (11-24%)
            • Diarrhea (11-20%)
            • Hypoglycemia (with sulfonylurea) (12.5-20%)
            • Vomiting (11.3%)

            1-10%

            Bydureon

            • Headache (9.4%)
            • Constipation (8.5%)
            • Headache (8.1%)
            • Dyspepsia (7.3%)
            • Constipation (6.3%)
            • Fatigue (5.6%)
            • Dyspepsia (5%)
            • Decreased appetite (5%)
            • Injection site pruritus (5%)
            • Hypoglycemia (without sulfonylurea) (1.3-3.7%)

            Bydureon BCise

            • Nausea (8.2%)
            • Headache (4.4%)
            • Diarrhea (4%)
            • Vomiting (3.4%)
            • njection site pruritus (3.2%)
            • Dizziness (2.5%)
            • Injection site erythema (2.3%)
            • Constipation (2.1%)

            Postmarketing Reports

            Bydureon

            • Acute pancreatitis, including fatal and nonfatal hemorrhagic or necrotizing pancreatitis
            • Allergy and hypersensitivity: Injection-site reactions

            Bydureon BCise

            • Allergy/hypersensitivity: Injection-site reactions, generalized pruritus and/or urticaria, macular or papular rash, angioedema; anaphylactic reaction
            • Drug interactions: Increased INR sometimes associated with bleeding, with concomitant warfarin
            • Gastrointestinal: Nausea, vomiting, and/or diarrhea resulting in dehydration; abdominal distension, abdominal pain, eructation, constipation, flatulence, acute pancreatitis, hemorrhagic and necrotizing pancreatitis sometimes resulting in death
            • Neurologic: Dysgeusia; somnolence
            • Renal and urinary disorders: Altered renal function (eg, increased serum creatinine, renal impairment, worsened chronic renal failure or acute renal failure [sometimes requiring hemodialysis], kidney transplant and kidney transplant dysfunction)
            • Skin and subcutaneous tissue disorders: Alopecia
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            Warnings

            Black Box Warnings

            Risk of thyroid C-cell tumors

            • Exenatide extended-release causes an increased incidence in thyroid C-cell tumors at clinically relevant exposures in rats compared to controls; unknown whether this risk for medullary thyroid carcinoma (MTC) exists in humans, as human relevance could not be determined by clinical or nonclinical studies
            • Contraindicated in patients with a personal or family history of MTC and in patients with multiple endocrine neoplasia syndrome type 2 (MEN 2)
            • Routine serum calcitonin or thyroid ultrasound monitoring is of uncertain value in patients treated with exenatide injectable suspension
            • Patients should be counseled regarding the risk and symptoms of thyroid tumors

            Contraindications

            Hypersensitivity

            Personal or family history of medullary thyroid carcinoma or in patients with multiple endocrine neoplasia syndrome type 2 (see Black Box Warnings)

            Cautions

            Do not administer Byetta and Bydureon concomitantly

            Serious injection-site reactions (eg, abscess, cellulitis, and necrosis) reported, with or without SC nodules; some required surgical intervention

            Thyroid C-cell tumors in animals observed; human relevance unknown (see Black Box Warnings)

            Pancreatitis reported, including fatal and nonfatal hemorrhagic or necrotizing pancreatitis; discontinue promptly if pancreatitis is suspected

            Reports of serious hypersensitivity reactions (eg, anaphylaxis and angioedema); inform and closely monitor patients with a history of anaphylaxis or angioedema with another GLP-1 receptor agonist for allergic reactions; it is unknown whether such patients will be predisposed to anaphylaxis

            Antibodies to exenatide following treatment may develop; anti-exenatide antibodies were measured in controlled studies; patients with higher titer antibodies may have an attenuated HbA1c response; if glycemic control worsens, consider alternative antidiabetic therapy

            Not recommended with severe gastrointestinal disease (eg, gastroparesis)

            Evaluate patient further If serum calcitonin is measured and found to be elevated

            Evaluate further patients with thyroid nodules noted on physical examination or neck imaging

            Acute kidney injury and renal impairment

            • Renal impairment reported, including some instances requiring hemodialysis and kidney transplantation; not recommended if severe renal impairment or ESRD exist
            • Caution in patients with renal transplantation or moderate renal impairment
            • Not recommended for use in patients with severe renal impairment (creatinine clearance <30 mL/min) or end-stage renal disease; should be used with caution in patients with renal transplantation

            Drug interactions overview

            • Use caution when administering oral medications with Bydureon and Bydureon BCise where a slower rate of oral absorption may be clinically meaningful
            • Postmarketing reports for exenatide of increased INR with concomitant use of warfarin, sometimes associated with bleeding; monitor INR
            • Risk of hypoglycemia is increased when exenatide is used in combination with insulin secretagogues (eg, sulfonylureas) or insulin; lower dose of the secretagogue or insulin to reduce risk of hypoglycemia
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            Pregnancy & Lactation

            Pregnancy

            Limited data with exenatide in pregnant women are not sufficient to determine a drug-associated risk for major birth defects or miscarriage

            Based on animal reproduction studies, there may be risks to the fetus from exposure to exenatide injection during pregnancy

            Exenatide extended-release injection should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus

            Animal reproduction studies identified increased adverse fetal and neonatal outcomes from exposure to exenatide extended-release during pregnancy or from exposure to exenatide during pregnancy and lactation, in association with maternal effects

            Lactation

            There is no information on the presence of exenatide, in human milk, the effects of exenatide on the breastfed infant, or the effects of exenatide on milk production

            Exenatide was present in the milk of lactating mice; exenatide concentration in milk was up to 2.5% of the concentration in maternal plasma after administering SC injection twice a day

            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

            Glucagon-like peptide-1 (GLP-1) agonist

            Incretins, such as GLP-1, enhance glucose-dependent insulin secretion by pancreatic beta-cells, suppresses inappropriately elevated glucagon secretion, and slows gastric emptying

            Absorption

            Bydureon

            • Peak Plasma Time: Gradual increase observed over 6-7 weeks after initiating
            • Peak Plasma Concentration: 300 pg/mL (after 6-7 weeks)

            Bydureon BCise

            • Peak plasma concentration, steady-state: 208 pg/mL

            Distribution

            Vd: 28.3 L

            Elimination

            Renal clearance: 9.1 L/hr

            Excretion: Predominantly urine

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            Administration

            SC Preparation

            Bydureon

            • Examine diluent provided to be sure that it is clear and free of particulate matter
            • Suspend powder in vial with diluent provided and transfer to syringe
            • Final concentration of suspension is 2 mg/0.65 mL
            • The suspension should be white to off-white and cloudy

            Bydureon BCise

            • Remove autoinjector from the refrigerator 15 minutes prior to resuspending the suspension
            • Shake vigorously for at least 15 seconds
            • Drug should appear as an opaque, white to off-white suspension (autoinjector contains microspheres which appear as white to off-white particles)
            • Visually inspect for particulate matter and discoloration prior to administration
            • Do not use if foreign particulate matter is present or if discoloration is observed

            SC Administration

            Subcutaneous use only

            Use immediately after autoinjector is prepared or following reconstitution (vial)

            Administer as SC injection in abdomen, thigh or upper arm region

            Rotate injection sites each week when injecting in the same region

            Do not administer IV or IM

            Missed dose and next dose is due at least 3 days later: Administer dose as soon as possible; resume usual dosing schedule of qWeek thereafter

            Missed dose and next dose is due 1 or 2 days later: Do not administer missed dose; resume next regularly scheduled dose

            Storage

            Unopened vials should be stored in the refrigerator at 36-46°F (2-8°C) and protected from light

            Do not freeze; do not use if suspension has been frozen

            If needed, each single-dose tray can be kept at room temperature (not to exceed 77°F [25°C]) for no more than a total of 4 weeks

            Reconstituted vial: Use immediately, do not store

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            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.
            Code Definition
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