exenatide injectable solution (Rx)

Brand and Other Names:Byetta
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Dosing & Uses


Dosage Forms & Strengths

injectable solution, prefilled pen

  • 250mcg/mL (1.2mL vial)
  • 250mcg/mL (2.4mL vial)

Diabetes Mellitus, Type 2

Adjunct to diet and exercise to improve glycemic control

Alternative monotherapy or as adjunct therapy with thiazolidinediones, metformin, or a sulfonylurea; or add-on therapy to insulin glargine (long-acting insulin)

May administer with or without metformin and/or a thiazolidinedione, in patients not achieving adequate glycemic control on insulin glargine alone

Immediate-release (Byetta): 5 mcg SC q12hr within 60 minutes prior to meal initially; after 1 month, may increase to 10 mcg q12hr

Switching from immediate-release to extended-release

  • Initiate weekly extended-release SC injections 1 day after discontinuing immediate-release exenatide (Byetta)
  • May experience increased blood glucose levels for approximately 2 weeks after initiating extended-release (Bydureon) therapy
  • May initiate extended-release exenatide without pretreating with the immediate-release dosage form

Dosage Modifications

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 (CrCl <30 mL/min) or ESRD: Not recommended
  • Renal transplantation: Use with caution

Intracranial Hypertension (Orphan)

Orphan designation for idiopathic intracranial hypertension


  • Alan Boyd Consultants Ltd; Electra House, Crewe Business Park; Crewe, UK

Safety and efficacy not established



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            Adverse Effects


            Injection-site nodule (6-77%)

            Injection-site reactions (2-18%)

            Nausea (8-11%)

            Vomiting (4-11%)

            Diarrhea (2-11%)


            Constipation (6-10%)

            Headache (5-9%)

            Dyspepsia (3-7%)

            Hyperhidrosis (3%)

            Jitteriness (<3%)

            Dizziness (<2%)


            Postmarketing Reports


            Anaphylactic reaction




            Renal impairment

            Upper respiratory infection



            Black Box Warnings

            Risk of thyroid C-cell tumors

            • 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



            ESRD, severe renal impairment (CrCl <30 mL/min)

            History of drug-induced immune-mediated thrombocytopenia from drug or related products

            Family or current history of medullary thyroid carcinoma


            Never share a pen between patients even if the needle is changed

            Not a substitute for insulin

            Not a first-line therapy for patients inadequately controlled on diet and exercise alone

            Evaluate insulin dose when added on to long-acting insulin (ie, insulin glargine); in patients with increased risk of hypoglycemia, consider decreasing insulin dose

            Not recommended for patients experiencing severe gastrointestinal disease, including gastroparesis

            Not recommended for type 1 diabetes

            Do not take with short- and/or rapid-acting insulins

            Animal studies show association of extended-release dosage form with the formation of thyroid tumors (effects in humans unknown)

            Always administer before a meal and never after a meal

            Weight loss resulting from reduced intake reported

            Serious hypersensitivity reactions (e.g., anaphylaxis and angioedema) reported; if a hypersensitivity reaction occurs, discontinue therapy and other suspect medications and promptly seek medical advice; inform and closely monitor patients with a history of anaphylaxis or angioedema with another GLP-1 receptor agonist for allergic reactions; unknown whether such patients will be predisposed to anaphylaxis with drug

            Risk of acute pancreatitis reported, including fatal and nonfatal hemorrhagic or necrotizing pancreatitis; after initiation and after dose increases, observe patients carefully for signs and symptoms of pancreatitis (including persistent severe abdominal pain, sometimes radiating to the back, which may or may not be accompanied by vomiting); if pancreatitis suspected, discontinue drug promptly and initiate appropriate management; if pancreatitis confirmed, do not restart therapy; consider antidiabetic therapies other than exenatide in patients with history of pancreatitis

            When therapy is used in combination with insulin, evaluate dose of insulin; consider reducing dose of insulin in patients at increased risk of hypoglycemia; concurrent use with prandial insulin not studied and cannot be recommended; also possible that use with other glucose-independent insulin secretagogues (eg, meglitinides or sulfonylureas) could increase risk of hypoglycemia

            Serious bleeding, which may be fatal, from drug-induced immune-mediated thrombocytopenia reported in postmarketing setting; drug-induced thrombocytopenia is an immune-mediated reaction, with exenatide-dependent anti-platelet antibodies; in presence of exenatide, these antibodies cause platelet destruction; if drug-induced thrombocytopenia suspected, discontinue therapy immediately and do not re-expose patient to exenatide

            Antibody formation to exenatide is likely; up to 4% of patients may have worsening glycemic control and require alternative antidiabetic therapy

            Acute kidney injury

            • Altered renal function with exenatide, including increased serum creatinine, renal impairment, worsened chronic renal failure, and acute renal failure, sometimes requiring hemodialysis or kidney transplantation reported
            • Some events reported in patients receiving one or more pharmacologic agents known to affect renal function or hydration status
            • Reversibility of altered renal function observed in many cases with supportive treatment and discontinuation of potentially causative agents; drug has not been found to be directly nephrotoxic in preclinical or clinical studies
            • Because drug may induce nausea and vomiting with transient hypovolemia, treatment may worsen renal function; exercise caution when initiating or escalating doses from 5 to 10 mcg in patients with moderate renal impairment (creatinine clearance 30-50 mL/min)

            Pregnancy & Lactation


            Limited data in pregnant women are not sufficient to determine a drug-associated risk for major birth defects or miscarriage; there are risks to mother and fetus associated with poorly controlled diabetes in pregnancy

            Based on animal reproduction studies, there may be risks to fetus from exposure to therapy during pregnancy; drug should be used during pregnancy only if potential benefit justifies potential risk to fetus

            Poorly controlled diabetes in pregnancy increases maternal risk for diabetic ketoacidosis, preeclampsia, spontaneous abortions, preterm delivery, and delivery complications; poorly controlled diabetes increases fetal risk for major birth defects, stillbirth, and macrosomia related morbidity

            Animal data

            • Animal reproduction studies identified increased adverse fetal and neonatal outcomes from exposure to exenatide during pregnancy and lactation in association with maternal effects
            • In mice, exenatide administered during gestation and lactation caused increased neonatal deaths at systemic exposure 3 times human exposure resulting from maximum recommended human dose (MRHD) of 20 mcg/day


            There is no information regarding presence of drug, in human milk, effects on breastfed infant, or on milk production; drug was present in milk of lactating mice; however, due to species-specific differences in lactation physiology, clinical relevance of data is not clear; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed child from drug or from underlying maternal condition

            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.



            Mechanism of Action

            A glucagonlike peptide-1 (GLP-1) that mimics incretin and promotes insulin secretion, suppresses glucagon, and slows gastric emptying


            Peak plasma time: 2.1 hr

            Peak plasma concentration: 211 pg/mL

            AUC: 1036 pg·hr/mL


            Vd: 28.3 L


            Proteolytic degradation following glomerular filtration


            Half-life: 2.4 hr (immediate release); 2 weeks (extended release)

            Renal clearance: 9.1 L/hr

            Excretion: Urine (primarily)



            SC Administration

            Administer within 60 minutes before morning and evening meals, approximately 6 hr or more apart

            Administer SC only; do not administer IM or IV

            Injection sites are thigh, abdomen, or upper arm





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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.